新製品

製品コード	製品名称	製品説明	添加時期
E1815	STX-478	STX-478 is a highly potent, mutant-selective, allosteric inhibitor of PI3Kα, that selectively targets prevalent mutant forms of PI3Kα. It demonstrates strong efficacy against common PI3Kα helical- and kinase-domain mutations, including the H1047R variant, with an IC50 value of 9.4 nmol/L. STX-478 exhibits 14-fold greater selectivity for mutant PI3Kα over the wild-type form. It spares metabolic dysfunction and improves therapeutic response in PI3Kα-Mutant Xenografts.	Nov 14 2024
E1834	iMDK	iMDK is a potent inhibitor of PI3K. It also inhibits the growth factor MDK (also known as midkine or MK). iMDK use along with a MEK inhibitor suppresses tumor growth of non-small cell lung cancer (NSCLC), including KRAS-mutant NSCLC and squamous NSCLC.	Sep 18 2024
E4674	Cu(II)GTSM	Cu(II)GTSM is a potent cell-permeable inhibitor of GSK3β that also inhibits Aβ oligomers and reduces tau phosphorylation. It shows potential as an anticancer and antimicrobial agent and may restore cognitive function by inhibiting neurotoxic Aβ trimers and phosphorylated tau.	Aug 28 2024
E1710	LY2780301	LY2780301 is a highly selective adenosine triphosphate (ATP)-competitive dual inhibitor of p70S6K and Akt. LY2780301 binds to Akt, inhibiting its activity, which consequently blocks the PI3K/Akt signaling pathway which leads to reduced cell proliferation and the initiation of apoptosis in tumor cells.	Apr 08 2024
S8267	RapaLink-1	RapaLink-1, a third-generation bivalent inhibitor of mTOR, combines Rapamycin with MLN0128 using an inert chemical linker. It demonstrates efficacy against resistant mutants of malignant brain tumors and inhibits cancer cell progression by binding to mesenchymal markers.	Apr 06 2024
E1604	Vevorisertib trihydrochloride	Vevorisertib trihydrochloride(ARQ 751 trihydrochloride) is a selective, allosteric inhibitor of pan-AKT and AKT1-E17K mutant with Kd values of 1.2 nM and 8.6 nM, respectively. It also has IC50 values of 0.55, 0.81, and 1.3 nM for AKT1, AKT2, and AKT3, respectively and can be used for the research of cancer.	Jan 16 2024
E1579	UCL-TRO-1938	UCL-TRO-1938 is a potent allosteric activator of PI3Kα. UCL-TRO-1938 can induce cell proliferation and has cardioprotective and neural regeneration effects.	Nov 22 2023
E2981	PI4KIIIbeta-IN-10	PI4KIIIbeta-IN-10 is a potent inhibitor of PI4KIIIβ with an IC50 of 3.6 nM. It also exhibits weak inhibition of PI3KC2γ, PI3Kα, and PI4KIIIα, and <20% inhibition at concentrations up to 20 µM for PI4K2α, PI4K2β, and PI3Kβ.	Oct 27 2023
E4345	L-Norvaline	L-Norvaline is a non-proteinogenic amino acid, an isomer of valine, and an inhibitor of arginase and p70 ribosomal S6 kinase 1 (p70S6K1) kinase. L-norvaline enhances NO production from activated macrophages.	Oct 11 2023
E1388	ISA-2011B	ISA-2011B is an inhibitor of phosphatidylinositol-4-phosphate 5-kinase-α (PIP5Kα). ISA-2011B exhibits anti-proliferative activity and induces apoptosis in prostate cancer cells.	Aug 28 2023

製品コード	製品名称	製品説明	添加時期
E4598	MEN1703(SEL24,SEL24-B489)	MEN1703(SEL24-B489,SEL24, Pim/flt3 kinase inhibitor SEL24) is a potent, type I, orally active, dual inhibitor of PIM and FLT3-ITD, that exhibits Kd values of 2 nM for PIM1, 2 nM for PIM2 and 3 nM for PIM3, respectively. MEN1703 exhibits its broad therapeutic potential in treatment of acute myeloid leukemia.	Nov 04 2024
E4971	Oclacitinib	Oclacitinib(PF-03394197), an inhibitor of JAK is highly potent at inhibiting JAK1 with an IC50 value of 10 nM, respectively. Oclacitinib is highly potent against the JAK1 enzyme, displaying a 1.8-fold selectivity for JAK1 vs. JAK2 and a 9.9-fold selectivity toward JAK1 vs. JAK3.	Oct 22 2024
E4630	Ilginatinib hydrochloride	Ilginatinib hydrochloride (NS-018 hydrochloride) is a potent small-molecule inhibitor of JAK2 that is competitive with adenosine triphosphate (ATP) which exhibits 30–50-fold greater selectivity for JAK2 over other Jak-family kinases such as JAK1, JAK3, and TYK2.It inhibits JAK2, JAK1, JAK3, and TYK2 with IC50 of 0.72 nM, 33 nM, 39 nM, and 22 nM, respectively. It also showed potent inhibition of Src-family kinases, SRC and FYN. It can be used in research of myeloproliferative neoplasms.	Jul 18 2024
E1526	Zasocitinib	Zasocitinib( NDI-034858, TAK-279) is a TYK2 inhibitor, which is currently being investigated in a phase IIb trial for moderate-to-severe plaque psoriasis.	Oct 11 2023
S8802	Delgocitinib (JTE-052)	Delgocitinib (JTE-052) is a specific  JAK inhibitor with IC50s of 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.	Mar 29 2023
S0456	inS3-54-A18	inS3-54A18 is a potent inhibitor of STAT3 with anti-cancer properties.	Oct 28 2022
S1349	SC99	SC99 is an orally active, selective STAT3 inhibitor targeting JAK2-STAT3 pathway by docking into the ATP-binding pocket of JAK2, also inhibits phosphorylation of JAK2and STAT3 with no effects on the other kinases associated with STAT3 signaling.	Jul 28 2022
E0793	G5-7	G5-7 is an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr1068) and STAT3 by binding to JAK2.	Jul 21 2022
E2644	Tetramethylcurcumin	Tetramethylcurcumin (FLLL31), a small-molecule signal transducer and activator of transcription 3 (STAT3) inhibitor derived from curcumin, binds selectively to Janus kinase 2 and the STAT3 Src homology-2 domain, which serve crucial roles in STAT3 dimerization and signal transduction.	Jul 15 2022
S0986	SC-1	SC-1 (1-(4-Chloro-3-(trifluoromethyl)phenyl)-3-(4-(4-cyanophenoxy)phenyl)urea, STAT3-IN-7), a Sorafenib analogue and potently inhibits the phosphorylation of STAT3, induces cell apoptosis through SHP-1 dependent STAT3 inactivation.	Jun 30 2022

製品コード	製品名称	製品説明	添加時期
E6025	Palbociclib 2HCL	Palbociclib 2HCL (PD-0332991 dihydrochloride), the dihydrochloride salt of Palbociclib, is a highly specific inhibitor of Cdk4 and Cdk6, with IC50 values of 11 nM and 16 nM, respectively. It is a potent antiproliferative agent against retinoblastoma (Rb)-positive tumor cells in vitro, inducing a selective G1 cell cycle arrest and reducing phosphorylation at Ser780 and Ser795 on the Rb protein.	Dec 22 2024
E4717	CP681301	CP681301 is a highly specific, brain-permeable inhibitor of Cdk5. It exhibits antiproliferative and anti-tumor activity by reducing stem cell marker expression, and cell proliferation in mouse xenografts ex vivo.	Dec 22 2024
E4737	Potrasertib	Potrasertib (IMP7068, WEE1-IN-10) is a potent and selective inhibitor of WEE1 Kinase. It displays antitumor activity and is well-tolerated in patients with advanced solid tumors.	Dec 18 2024
E1863	Inixaciclib	Inixaciclib (NUV-422) is a potent inhibitor of CDK2, CDK4, and CDK6. It inhibits the growth of glioma cell lines in vitro and exhibits antitumor activity in GB xenograft models, PDX models of HR+ HER2- metastatic breast cancer resistant to CDK4/6 inhibitors and prostate cancer resistant to anti-androgens.	Dec 12 2024
E1921	NRL-1049	NRL-1049(BA 1049) is a small molecule selective inhibitor of ROCK2 with an IC50 of 0.59 µM. It exhibits potent efficacy in preserving the blood-brain barrier (BBB) and suppresses seizures after brain injury, and inhibits hemorrhagic transformation after ischemic stroke in mice.	Dec 12 2024
E4702	SRX3177	SRX3177 is a potent triple inhibitor targeting CDK4/6, PI3K, and BRD4, with IC50 values of 33 nM for BRD4 BD1, 89 nM for BRD4 BD2, 79 nM for PI3Kα, 83 nM for PI3Kδ, 3.18 μM for PI3Kγ, <2.5 nM for CDK4, and 3.3 nM for CDK6. By simultaneously inhibiting these key pathways, SRX3177 disrupts cancer cell signalling and exhibits significant cytotoxic effects in tumors.	Dec 05 2024
E1856	ARS-1323	ARS-1323 is the racemic mixture, containing ARS-1620, and a potent inhibitor of mutant KRAS G12C. It can be used in research for biochemical binding screens as companion imaging drugs (CID) for KRAS G12C.	Nov 17 2024
E4697	RGT-018	RGT-018, is a potent and selective inhibitor of SOS1. It blocks the interaction of KRAS:SOS1 with an IC50 of 8 nM and inhibited KRAS signaling and the proliferation of KRAS-driven cancer cells. It may exhibit potent anticancer activity against NSCLC, colorectal cancer, and pancreatic cancer.	Oct 23 2024
E4703	Culmerciclib	Culmerciclib (TQB3616) is a potent inhibitor of cyclin dependent kinase (CDK)4/6 and exhibits highly effective antineoplastic activity. TQB3616 exhibits significant synergistic antitumor activity in estrogen receptor (ER)-positive/HER2-negative or HER2-positive breast cancer when combined with endocrine therapy or Human Epidermal Growth Factor Receptor 2 (HER2) targeted therapy.	Oct 15 2024
E1972	AZD8421	AZD8421 is a potent and highly selective inhibitor of Cyclin-dependent Kinase 2 (CDK2), with an IC50 against CDK2 of 9nM with selectivity over CDK1, CDK4 and CDK6. It also exhibits an anti-proliferative effect, effectively inhibits Rb phosphorylation, and shows strong activity both as a monotherapy and in combination with CDK4/6 inhibitors in breast and ovarian cancer models.	Sep 18 2024

製品コード	製品名称	製品説明	添加時期
E4754	Semustine	Semustine is a member of the chloroethyl nitrosourea (CENU) family that induces DNA alkylation at the major groove, forming interstrand cross-links between guanine and cytosine bases (dG-dC). It exerts antitumor activity by inducing these DNA cross-links and is used as an antineoplastic alkylating agent for treating Lewis lung carcinoma, leukemia, and metastatic brain tumors.	Dec 20 2024
S8593	VX-984	VX-984 (M9831) is an orally active, potent, selective, and ATP-competitive inhibitor of DNA-PK. VX-984 effectively suppresses non-homologous end joining (NHEJ) and increases DNA double-strand breaks (DSBs). It enhances the cytotoxic effects of ionizing radiation (IR) in various cancer cell lines, including non-small cell lung cancer (NSCLC) cell lines, in vitro. Additionally, VX-984 reduces DNA-PKcs autophosphorylation.	Dec 18 2024
E5775	Exatecan	Exatecan (DX-8951), is a water-soluble derivative of camptothecin. It acts as an inhibitor of DNA topoisomerase I with an IC50 value of 1.906 μM. It demonstrates potent antitumor effects and triggers apoptotic cell death after treatment in human pancreatic cancer cells.	Dec 11 2024
E1939	ART899	ART899, a derivative of ART558 is a potent, specific allosteric inhibitor of DNA polymerase theta (Polθ), specifically inhibits Polθ MMEJ activity with IC50 of 180 nM. It specifically radiosensitizes tumor cells and have a potent stand-alone antitumor effect in cancer cells.	Dec 05 2024
E4925	Amsacrine	Amsacrine(m-AMSA, acridinyl anisidide) is an inhibitor of topoisomerase II. Amsacrine acts as an antineoplastic agent which intercalates into the DNA of tumor cells, it is also used in the treatment of acute myelogenous leukemia.	Sep 23 2024
E1302	Braco-19 trihydrochloride	Braco-19 trihydrochloride(BRAC-O19, BRACO19 3HCl) is a G-quadruplex-stabilizing agent and an inhibitor of telomere/telomerase. It establishes antiviral activity against HIV-1 and anticancer effects by inhibiting telomerase capping and catalytic functions.	Sep 13 2024
E4660	TAC(TERT activator compound)	TAC(TERT activator compound) is an activator of TERT, that upregulates TERT transcription via the MEK/ERK/AP-1 cascade. It enhances telomere synthesis, reduces aging markers, inflammation, and senescence, and preserves brain function, highlighting TERT's potential in combating aging and related diseases.	Sep 03 2024
E4620	L-778123 hydrochloride	L-778123 hydrochloride is a potent dual inhibitor of farnesyl protein transferase (FPTase) with an IC50 of 2 nM and geranylgeranyl protein transferase I (GGPTase-I) with an IC50 of 98 nM. It also displays promising anti-leukemia activity.	Aug 28 2024
E1989	ART0380	ART0380 (IACS-030380) is a potent and selective, orally bioavailable inhibitor of ATR kinase, with an IC50 of 51.7 nM effectively inhibiting the enzyme activity of the ATR-ATRIP complex. It functions as an ATP-competitive inhibitor, binding to the ATP pocket of ATR, where ATP would typically bind. It interacts with the hinge through its morpholine oxygen and occupies the ribose pocket with a sulfoximine group. It also exhibits antitumor activity.	Aug 28 2024
E4869	Niraparib hydrochloride	Niraparib hydrochloride (MK-4827 hydrochloride) is a potent poly(ADP-ribose)polymerase (PARP) inhibitor with IC50s of 3.8 and 2.1 nM against both the PARP-1 and PARP-2 enzymes, respectively.It inhibits the repair of radiation-induced DNA double-strand breaks, activates apoptosis, and exhibits anti-tumor activity.	Aug 26 2024

製品コード	製品名称	製品説明	添加時期
E1785	PF-06952229	PF-06952229(UNII-1KKS7U3X86) is a selective, orally available inhibitor of the serine/threonine kinase TGF-β receptor 1 (TGF-β-R1). It inhibits pSMAD2 in both tumor and immune cells, reducing TGF-β signalling and reversing EMT in vitro. It modulates the tumor immune microenvironment and shows antitumor activity in mouse models.	Sep 19 2024
A3071	Anti-TGFb1 (NIS793)	Anti-TGFb1 (NIS793) is a monoclonal antibody targeting TGF-β. It can be used in metastatic melanoma and non-small cell-lung cancer. MW :143.78 KD	Oct 11 2023
A2694	Anti-TGFb1 (SRK181)	Anti-TGFb1 (SRK181) is a monoclonal antibody directed against latent human transforming growth factor (TGF)-beta 1 with potential antineoplastic activity. MW : 150 kD.	Oct 11 2023
A2695	Anti-TGFb1 (M7824)	Anti-TGFb1 (M7824) is a bifunctional monoclonal antibody targeting programmed death ligand 1 (PD-L1) and transforming growth factor beta 1 (TGFb1). It exhibits anti-tumor efficacy against breast and colon carcinomas.	Oct 11 2023
A2422	Garetosmab (Anti-INHBA / Activin A)	Garetosmab (Anti-INHBA / Activin A) is a fully human IgG4 monoclonal antibody that specifically inhibits activin A. Garetosmab can be used for fibrodysplasia ossificans progressiva (FOP) research. MW: 145.5 kD.	Aug 10 2023
A2336	Fresolimumab (Anti-TGFb1)	Fresolimumab (Anti-TGFb1) is a pan-specific, recombinant, fully human monoclonal antibody directed against human transforming growth factor (TGF) beta 1, 2, and 3 with potential antineoplastic activity. MW : 145.5 KD.	Aug 10 2023
A2595	Bimagrumab (Anti-ACVR2B)	Bimagrumab (Anti-ACVR2B) is a human monoclonal antibody targeting activin type II receptor (ActRII). It can be used for the treatment of pathological muscle loss and weakness. MW : 150 KD.	Aug 10 2023
E2394	TGFβRI-IN-3	TGFβRI-IN-3 represents a highly selective TGFβR1 inhibitor that has potential applications in immuno-oncology, inhibits TGFβR1 at an IC50 of 0.79 nM with 2000-fold selectivity against MAP4K4.	Jul 08 2022
E2368	N-Desmethyltamoxifen hydrochloride	N-Desmethyltamoxifen hydrochloride (N-Desmethyl tamoxifen HCl), the primary metabolite of tamoxifen, is an estrogen response modifer and protein kinase C inhibitor with IC50 of 25 µM.	Jul 08 2022
E2839	Bisindolylmaleimide VIII (acetate)	Bisindolylmaleimide VIII (acetate) (Ro 31-7549 acetate) is a potent and selective protein kinase C (PKC) inhibitor with an IC50 of 158 nM for rat brain PKC, also exerting IC50s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, PKC-ε, respectively.	Jun 30 2022

製品コード	製品名称	製品説明	添加時期
E4771	Aprocitentan	Aprocitentan (ACT-132577) is a pharmacologically active metabolite of Macitentan. Aprocitentan is an orally active dual antagonist of ETA/ETB with IC50 values of 3.4 nM and 987 nM, and pA2 values of 6.7 and 5.5, respectively.	Dec 16 2024
E1941	ACT-1016-0707	ACT-1016-0707 (LPA1 receptor antagonist 2) is an orally active and selective antagonist of LPA1 Receptor, with IC50 of 3.1 nM for hLPAR1 in tango assay. It has the potential to treat fibrotic diseases.	Dec 12 2024
E4880	Labetalol	Labetalol (AH5158, Sch-15719W free base) is an orally active and selective competitive antagonist of α1-adrenergic receptors and non-selective β-adrenergic receptors. Labetalol, an anti-hypertensive agent is used in the research of cardiovascular diseases.	Dec 02 2024
E4793	Bucladesine calcium	Bucladesine calcium (Dibutyryl-cAMP Calcium Salt, DBcAMP calcium salt) is a cell-permeable analog of cyclic AMP. It serves as a potent activator of protein kinase A (PKA) and mimics the effects of endogenous cAMP. It also inhibits phosphodiesterase (PDE) activity, with the potential to treat congestive heart failure, wound healing, and inflammation.	Nov 25 2024
E4740	TAK-861	TAK-861 is a potent, orally bioavailable agonist of orexin receptor 2 (OX2R), with an EC50 of 2.5 nM in calcium mobilization assays. It induces dose-dependent membrane depolarization in histaminergic neurons within the mouse tuberomammillary nucleus (TMN) with an EC50 of 31.7 nM.	Nov 14 2024
E4976	Tegaserod	Tegaserod is an orally active agonist of serotonin receptor 4 (5-HT4R) and also acts as an antagonist of 5-HT2B receptor with pKi values of 7.5, 8.4, and 7.0 for human recombinant 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Tegaserod has anti-tumor activity and is used in the research of irritable bowel syndrome (IBS).	Nov 12 2024
E4975	Angiotensin II human TFA	Angiotensin II human TFA(DRVYIHPF TFA, Ang II TFA) is a vasoconstrictor and a major bioactive peptide of the renin/angiotensin system that regulates blood pressure by activating AT1Rand AT2R, stimulating sympathetic activity, aldosterone production, and renal actions. It also promotes vascular cell growth, collagen synthesis, fibrosis, and induces apoptosis and capillary formation via a redox-sensitive pathway.	Oct 30 2024
E4628	BMS-986235	BMS-986235 (LAR-1219) is a selective, orally active and potent agonist of formyl peptide receptor 2 (FPR2), with EC50 values of 0.41 nM and 3.4 nM for hFPR2 and mFPR2, respectively. BMS-986235 therapy shows promising improvements in cardiac structure and function in a mouse model of heart failure, highlighting its potential for preventing the progression of heart failure.	Oct 15 2024
E4956	Ozanimod hydrochloride	Ozanimod hydrochloride(Zeposia, RPC-1063 HCL) is a potent sphingosine 1-phosphate (S1P)receptor modulator and a selective agonist of S1P receptor subtypes 1 (S1P1) and 5 (S1P5) with EC50's of 1.03 nM and 8.6 nM, respectively. It can be used in the trearment of relapsing multiple sclerosis (MS).	Sep 25 2024
E4923	AnaMorelin hydrochloride	Anamorelin hydrochloride(RC-1291 HCL, ONO-7643) is a potent and selective agonist of ghrelin receptor with EC50 of 0.74 nM FLIPR assay. It has a significant appetite-enhancing activity and has the potential to treat cancer anorexia-cachexia syndrome.	Sep 25 2024

製品コード	製品名称	製品説明	添加時期
E6007	Pexidartinib Hydrochloride	Pexidartinib Hydrochloride (PLX-3397 hydrochloride) is an oral tyrosine kinase inhibitor of colony-stimulating factor 1 receptor (CSF1R). It significantly reduces macrophage levels in adipose tissue without altering overall myeloid cell counts in mice. It also induces developmental and immunotoxic effects in zebrafish embryos by hyperactivating Wnt signaling.	Dec 20 2024
E4997	BAY 2927088（Sevabertinib）	BAY 2927088（Sevabertinib) is the first non-covalent, potent, oral, selective, and reversible inhibitor of tyrosine kinase that potently inhibits mutant HER2 and mutant EGFR in preclinical models. It targets Exon 20 insertions in non-small-cell lung carcinoma (NSCLC) patients.	Dec 11 2024
E4884	Icotinib Hydrochloride	Icotinib hydrochloride (BPI-2009H) is a highly potent and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) with an IC50 of 5 nM, utilized in the treatment of non-small cell lung cancer (NSCLC).	Nov 29 2024
E1814	Resigratinib	Resigratinib (KIN-3248) is a potent, kinome selective, irreversible, orally bioavailable, small-molecule inhibitor of pan-FGFR. It exhibits dose-dependent tumor inhibition in FGFR driven cholangiocarcinoma, gastric, and bladder cancer xenograft models.	Nov 27 2024
E1979	Irpagratinib	Irpagratinib (ABSK011) is a potent inhibitor of FGFR4 with an IC50 of < 10 nM in biochemical assays. It effectively suppresses FGFR4 auto-phosphorylation and disrupts downstream signal transduction. It also strongly inhibits tumor growth and induces regression in subcutaneous xenograft models.	Nov 14 2024
S9881	M4205（IDRX-42）	M4205 (IDRX-42) is an oral, selective inhibitor of KIT with broad activity against mutations in KIT exons 11, 13, and 17. It exhibits significant and dose-dependent antitumor activity in the xenograft model of GIST.	Oct 30 2024
E4643	BIIB129	BIIB129, is a unique brain-penetrant covalent inhibitor of Bruton’s tyrosine kinase (BTK), with high kinome selectivity. It exhibits efficacy in targeting B-cell proliferation in the central nervous system (CNS), making it a promising immunomodulatory therapy for multiple sclerosis (MS).	Oct 23 2024
E4886	HS-10296 hydrochloride	HS-10296 hydrochloride(Almonertinib (hydrochloride), HS-10296 HCl) is an irreversible, third-generation inhibitor of EGFR tyrosine kinase that demonstrates high selectivity for EGFR-sensitizing mutations, T790M resistance mutation. It exhibits inhibitory activity against T790M, T790M/L858R, and T790M/Del19, with IC50 of 0.37 nM, 0.29 nM, and 0.21 nM, respectively. It also exhibits anti-tumor activity.	Sep 28 2024
E4680	MTX-531	MTX-531(NSC827271) is a first-in-class, potent and selective inhibitor of EGFR and PI3Kα with an IC50 of 14.7 nM and 6.4 nM, respectively. It may play a role in treating Head and Neck Squamous Cell Carcinoma (HSNCC), squamous lung cancers, and certain EGFR/PI3K-driven triple-negative breast cancers.	Sep 25 2024
E4675	Rezivertinib	Rezivertinib(BPI-7711) is a potent third-generation inhibitor of EGFR tyrosine kinase, targeting both EGFR-sensitizing mutations and the EGFR T790M mutation. Additionally, it has excellent CNS penetration and has antitumor activity.	Sep 25 2024

製品コード	製品名称	製品説明	添加時期
S7615	MS417	MS417 (GTPL7512) is a selective inhibitor of BET-specific BRD4. MS417 binds to BRD4-BD1 and BRD4-BD2 with IC50 values of 30 nM and 46 nM and Kd values of 36.1 nM, and 25.4 nM, respectively. MS417 effectively blocks BRD4 binding to the acetylated NF-κB and attenuates NF-κB transcriptional activation of proinflammatory genes in kidney cells treated with TNFα.	Dec 20 2024
E4995	Cl-amidine hydrochloride	Cl-amidine hydrochloride is an inhibitor of pan-peptidylarginine deiminase (PAD), with an IC50 of 0.8 µM, 6.2 µM, and 5.9 µM for PAD1, PAD3, and PAD4, respectively.	Dec 20 2024
E5782	Remodelin	Remodelin is a potential inhibitor of the acetyltransferase NAT10. It enhances nuclear shape and cellular fitness in both progeric cells and cells depleted of Lamin A/C by inhibiting NAT10. Remodelin exhibits anti-proliferation activity and significantly inhibits tumour growth and tumour cell proliferation in the PDX model of HNSCC.	Dec 19 2024
E1974	MS8709	MS8709 (EX-A11295) is a first-in-class G9a/GLP proteolysis targeting chimera (PROTAC) degrader, that induces G9a/GLP degradation in a concentration, time, and ubiquitin-proteasome system (UPS)-dependent manner, and does not alter the mRNA expression of G9a/GLP over other methyltransferases. It displays superior cell growth inhibition in prostate, leukemia, and lung cancer cells over parent G9a/GLP inhibitors.	Dec 16 2024
E1664	GNE-987	GNE-987 is a BRD4-degradating PROTAC consisting of BRD4B1 and BRD4B2 (BRD4 bromodomains 1 and 2) and the VHL E3-ubiquitin ligase. It exhibits BRD4 degradation activity with DC50 of 0.03 nM for the EOL-1 AML cell line. GNE-987 inhibits cell proliferation and induces apoptosis by promoting the rapid and sustained degradation of BRD4 and inhibiting its downstream targets. It also demonstrates potent antitumor activity in AML cell lines.	Dec 02 2024
E4994	JNJ-75276617	JNJ-75276617 (Bleximenib, Menin-MLL inhibitor 24) is an orally bioavailable, potent inhibitor of menin targeting the menin-KMT2A selective protein-protein interaction. It also acts as an inhibitor of menin-mixed-lineage leukemia 1 (menin-MLL). JNJ-75276617 displays highly potent antiproliferative activity across several acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL) cell lines and patient samples.	Nov 25 2024
E4719	XYL-1	XYL-1 is a highly potent inhibitor of PARP7 with and IC50 of 0.6 nM. It could enhance the type-Ⅰinterferon signaling in vitro, and can be a potential candidate for developing cancer immunotherapy agents.	Nov 25 2024
E1819	Zavondemstat	Zavondemstat(QC8222, TACH 101) is a small-molecule pan-inhibitor of histone lysine demethylase 4D (KDM4D) that selectively targets KDM4A-D with no effect on other KDM families. It exhibits potent antiproliferative activity in various cancer cell lines and organoid models. It displays antineoplastic activity and acts as a potential anticancer agent.	Oct 27 2024
E1782	DSP5336	DSP5336 is an oral small molecule inhibitor of menin and MLL protein interaction. DSP5336 is undergoing clinical evaluation for its use in the treatment of patients with Relapsed or Refractory Acute Leukemia.	Oct 27 2024
S7475	NU9056	NU9056 is a potent and selective inhibitor of Tip60 (KAT5) histone acetyltransferase with an IC50 value of 2 µM. NU9056 demonstrates over 16-fold selectivity for Tip60 compared to PCAF, p300, and GCN5 and effectively induces apoptosis in prostate cancer cells.	Oct 24 2024

製品コード	製品名称	製品説明	添加時期
E1973	R16	R16(NSC29869, Nrf2-IN-3) is an inhibitor of NRF2 (nuclear factor erythroid 2-related factor 2) that selectively binds KEAP1 mutants and restores their NRF2-inhibitory function by repairing the disrupted KEAP1/NRF2 interactions. It significantly enhances the sensitivity of KEAP1-mutated tumor cells to cisplatin and gefitinib.	Sep 28 2024
P1238	SN 52	SN52, a cell-permeable peptide containing the p50 NLS, is a selective inhibitor of NF-κB pathway. It selectively and completely blocks the ionizing radiation (IR)-induced nuclear import of p52 and RelB. It also enhances the radiosensitivity of prostate cancer cells.	Jun 24 2024
E1714	B022	B022 is a potent and selective NF-κB-inducing kinase (NIK) inhibitor with a Ki of 4.2 nM. B022 protects liver from toxin-induced inflammation, oxidative stress, and injury.	Dec 26 2023
E1575	EN450	EN450 is a cysteine-reactive covalent molecular glue degrader targeting NF-κB. It interacts with allosteric C111 in the E2 ubiquitin ligase UBE2D that induces the ternary complex formation between UBE2D and NFKB1. It exhibits anti-proliferative effects through a Cullin E3 ligase and proteasome-dependent mechanism.	Oct 17 2023
E1351	NF-κΒ activator 1	NF-κΒ activator 1(Compound 32) is a potent NF-κΒ activator, with an EC50 of 0.9 μM.	Apr 20 2023
E2661	Chitosan oligosaccharide	Chitosan oligosaccharide (COS) is an oligomer of β-(1➔4)-linked d-glucosamine, of which actions involve the modulation of several important pathways including the suppression of nuclear factor kappa B (NF-κB) and mitogen-activated protein kinases (MAPK) and the activation of AMP-activated protein kinase (AMPK).	Aug 10 2022
E0944	IMD-0560	IMD-0560 is an Inhibitor of nuclear factor kappa-B kinase (IKK) which can suppress the production of inflammatory cytokines and chemokines.	Jul 27 2022
E0812	CXD101	CXD101 (HDAC-IN-4) is a potent, selective and orally active class I histone deacetylase (HDAC) inhibitor with IC50s of 63 nM, 570 nM and 550 nM for HDAC1, HDAC2 and HDAC3, respectively.	Jul 21 2022
E0796	NF-κB-IN-1	NF-κB-IN-1 is a potent NF-κB signaling pathway inhibitor, which acts by directly inhibiting inhibitory κB kinase (IKK).	Jul 21 2022
S0844	NDMC101	NDMC101 inhibits osteoclastogenesis which also ameliorates paw swelling and inflammatory bone destruction, associating with the inhibition of such transcription factors as NF-κB and NFATc1 as well as multiple protein kinases, including p38, ERK, and JNK.	Jul 06 2022

製品コード	製品名称	製品説明	添加時期
E6031	Tipiracil	Tipiracil [TPI (freebase)] is a potent inhibitor of thymidine phosphorylase. It increases exposure to its co-administered drug by inhibiting its metabolism through thymidine phosphorylase, enhancing its therapeutic effects and is used as adjunct therapy for certain gastric and colorectal cancers.	Dec 20 2024
E1896	BMS-502	BMS-502 is a potent dual inhibitor of diacylglycerol kinase (DGK) α and ζ with IC50 values of 4.6 nM and 2.1 nM, respectively. BMS-502 also exhibits an EC50 value of 340 nM in the mouse cytotoxic T cell IFN-γ assay (mCTC). BMS-502 can be used in tumor immunity-related research.	Dec 02 2024
E6005	Saxagliptin hydrochloride	Saxagliptin hydrochloride (BMS-477118 hydrochloride) is a potent, selective, reversible, competitive, and orally active inhibitor of dipeptidyl peptidase-4 (DPP-4). It exhibits 400-950 fold selective inhibition of DPP-4 than DPP-8. Saxagliptin hydrochloride is used in the research of type 2 diabetes mellitus research.	Dec 02 2024
E5768	Indolelactic acid	Indolelactic acid (Indole-3-lactic acid), a metabolite of tryptophan (Trp), plays a role in immune cell differentiation and cytokine production by activating aryl hydrocarbon receptors (AhR). This regulation supports immune responses and aids in anti-inflammatory and anti-allergic activities. It also plays an important role in the balance of Th17/Treg cells by reprogramming CD4+ Th cells into CD4+CD8+ Treg cells and inhibiting the polarization of Th17 cells.	Nov 29 2024
E4792	Atorvastatin calcium hydrate	Atorvastatin calcium hydrate (Totalip) is a potent inhibitor of the HMG-CoA reductase . It is used as a potent hypolipidemic agent to reduce the elevated total-cholesterol, low-density lipoprotein (LDL), apolipoprotein B (apo B), and triglyceride (TG) levels, and to increase the high-density lipoprotein cholesterol (HDL-C) level in patients with primary hypercholesterolemia and mixed dyslipidemia.	Nov 27 2024
E4637	PK 11195	PK 11195 (RP 52028) is a translocator protein (TSPO) ligand, a potent and selective antagonist of peripheral benzodiazepine receptorwith high affinity Ki of 3.1 nM in cerebellum and 4.1 nM in spinal cord. It is also an antagonist of human constitutive androstane receptor (hCAR), and human pregnane X receptor (PXR). It displaces [3H] RO5-4864 from its binding sites across organs and also targets Leishmania in chemotherapy.	Nov 25 2024
E4977	Zileuton sodium	Zileuton sodium (A 64077 sodium) is a potent, selective, and specific inhibitor of 5-lipoxygenase, exhibiting inflammatory activities. Zileuton sodium prevents polyp formation efficiently by reducing tumor-associated and systemic inflammation in in vivo models. Zileuton sodium also acts as a potential chemo-preventive agent in patients that are at high risk of developing colon cancer.	Nov 20 2024
E4922	Allopurinol riboside	Allopurinol riboside, a metabolite of allopurinol, competitively inhibits the action of purine nucleoside phosphorylase on inosine in vitro with a Ki value of 277 μM. It displays potent activities against parasites.	Nov 14 2024
F0765	UCP1 Rabbit mAb		Nov 14 2024
E4924	Anagrelide	Anagrelide(BL416201), an imidazoquinazoline derivative, is an inhibitor of phosphodiesterase type III (PDEIII) with IC50 of 36 nM, which acts as an antithrombotic and platelet-reducing agent.	Oct 30 2024

製品コード	製品名称	製品説明	添加時期
E6002	Ledipasvir D-tartrate	Ledipasvir D-tartrate (GS-5885 D-tartrate), the D-tartrate salt form of ledipasvir, is an inhibitor of the HCV NS5A, which is essential for the replication of the virus. It exhibits EC50 of 31 pM against GT1a and 4 pM against GT1b replicons.	Dec 22 2024
E6013	Sivelestat sodium	Sivelestat sodium (ONO-5046, Sodium sivelestat, LY544349 sodium) is a potent, specific, and intravenously active inhibitor of neutrophil elastase with an IC50 value of 44 nm. It is a useful agent for studying the roles of neutrophil elastase in animal disease models such as emphysema, adult respiratory distress syndrome, septic shock and disseminated intravascular coagulation in COVID-19.	Nov 21 2024
E4814	Teneligliptin Hydrobromide Hydrate	Teneligliptin Hydrobromide Hydrate(MP-513 hydrobromide hydrate) is a potent, competitive, and long-lasting inhibitor of DPP-4. It competitively inhibited rhDPP-4, human plasma, and rat plasma with IC50 values of 0.889, 1.75, and 1.35 nM respectively. It suppresses high glucose-mediated mitochondrial dysfunction and can be used for treatment of type 2 diabetes.	Oct 17 2024
P1242	Proteinase K	Proteinase K is a serine endoprotease, is used for isolating amyloid cores and is effective over a wide pH range (4–12), including in the presence of SDS or urea. It is commonly used as a preparative reagent for destruction of proteins, including DNAses and RNAses, in DNA and RNA preparations.	Jul 29 2024
E1188	Brensocatib	Brensocatib (AZD7986, INS1007) is an oral, selective, reversible inhibitor of dipeptidyl peptidase-1 (DPP-1). It reduces the activity of all major neutrophil serine proteases (NSPs) including, neutrophil elastase (NE), proteinase 3 (PR3), and cathepsin G (CatG) in patients with bronchiectasis.	Jun 24 2024
E1740	Mepazine hydrochloride	Mepazine hydrochloride (Pecazine hydrochloride) is a potent and selective inhibitor of MALT1 protease, with IC50 values of 0.83 μM for GSTMALT1 full length and 0.42 μM for GSTMALT1 aa 325-760. It effectively suppresses the activation of the NF-kB pathway specifically in activated B cell subtype of diffuse large B cell lymphoma (ABC-DLBCL) cells and makes it a promising candidate for the treatment of ABC-DLBCL.	Apr 25 2024
E4453	Cathepsin G Inhibitor I	Cathepsin G Inhibitor I exhibits reversible, competitive cathepsin G inhibition with IC50 and Ki values of 53 nM and 63 nM respectively. It can be used in antigen-processing studies and for modulation of T cell response in situ and in vivo.	Jan 22 2024
E1203	Sirpiglenastat	Sirpiglenastat (DRP-104) is a broad acting glutamine antagonist. It has anticancer effects by directly targeting tumor metabolism and simultaneously inducing a potent antitumor immune response with immunomodulatory and antineoplastic activities.	Dec 13 2023
E4466	Saquinavir Mesylate	Saquinavir mesylate (Ro 31-8959/003) is a potent inhibitor of HIV Protease used in antiretroviral therapy. It blocks proteolysis of polyproteins containing either wild-type or single-chain dimer retroviral proteinase (PR).	Nov 22 2023
E4454	DL-Thiorphan	Thiorphan (DL-3-Mercapto-2-benzylpropanoylglycine) is a selective NEP (neprilysin) inhibitor with an IC50 of 6.9 nM. It is also a potent inhibitor of enkephalinase, with antinociceptive activity.	Nov 19 2023

製品コード	製品名称	製品説明	添加時期
E6014	Primaquine	Primaquine, an 8-aminoquinoline, is an antimalarial agent and a potent gametocytocidal in falciparum malaria. It also prevents relapse in vivax and ovale malaria.	Dec 20 2024
E6017	Ornidazole (Levo-)	Ornidazole (Levo-) (Levornidazole, (S)-Ornidazole), the levo-isomer of ornidazole, is a third-generation nitroimidazole derivative. It exhibits antiprotozoal and antibacterial properties against anaerobic bacteria.	Nov 14 2024
E4983	Omadacycline hydrochloride	Omadacycline hydrochloride (PTK0796 hydrochloride) is a first-in-class orally active member of the tetracycline class of antibiotics. Omadacycline inhibits bacterial protein synthesis by binding to the 30S ribosomal subunit. Omadacycline hydrochloride exhibits broad-spectrum antibacterial activity against aerobic and anaerobic Gram-positive and Gram-negative bacteria, as well as atypical bacteria.	Nov 12 2024
E1758	Bersacapavir	Bersacapavir(JNJ-6379, JNJ-56136379) is a potent capsid assembly modulator (CAM) that accelerates capsid assembly and induces the formation of morphologically intact viral capsids devoid of genomic material. It inhibits HBV replication with an EC50 of 54 nM in HepG2.117 cells.	Nov 07 2024
E4984	Avibactam free acid	Avibactam free acid(NXL-104 free acid) is a potent, covalent, reversible, non–β-lactam Inhibitor of β-lactamase, inhibiting β-lactamase TEM-1 and CTX-M-15 with an IC50 of 8 nM and 5 nM, respectively. It is useful in research on Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus faecium, Gram-negative infections.	Oct 30 2024
E4985	Avibactam sodium hydrate	Avibactam sodium hydrate(NXL-104 hydrate) is a covalent and reversible non-β-lactam inhibitor of β-lactamase which inhibits β-lactamase activity with IC50 values of 8 nM for TEM-1 and 5 nM for CTX-M-15, respectively.	Oct 27 2024
E4954	Demeclocycline	Demeclocycline(Demethylchlortetracycline (DMCT), Ledermycin) is a bacteriostatic antibiotic from the tetracycline class, that induces diuresis and can cause nephrogenic diabetes insipidus. It also manages the syndrome of inappropriate antidiuretic hormone secretion (SIADH) by restoring normal plasma sodium levels and permitting unrestricted water intake.	Sep 26 2024
E4946	Tafenoquine Succinate	Tafenoquine Succinate(WR 238605 Succinate, Etaquine, Krintafel) is an 8-aminoquinoline (8AQ) anti-malarial drug that kills both the liver and blood stages of the parasite, broadening its applicability for chemoprophylaxis to all species of malaria. It is specifically used for the prevention of Plasmodium vivax relapse.	Sep 25 2024
E4939	Sulfisoxazole acetyl	Sulfisoxazole acetyl(N1-Acetylsulfisoxazole, Acetyl sulfafurazole), a sulfisoxazole derivative, is an orally active inhibitor of dihydropteroate synthase. Sulfisoxazole acetyl can be biotransformed primarily to sulfisoxazole, and partly to N(4)-acetyl sulfisoxazole (N4AS). Sulfisoxazole acetyl exhibits antibacterial action.	Sep 23 2024
E4891	Fostemsavir Tris	Fostemsavir Tris(BMS-663068 Tris) is a phosphonooxymethyl prodrug of BMS-626529, formulated as a tris(hydroxymethyl)aminomethane salt. It inhibits human immunodeficiency virus type 1 (HIV-1) by binding to the gp120 protein, preventing the virus from attaching to CD4+ T-cells.	Sep 12 2024

製品コード	製品名称	製品説明	添加時期
E1510	Sonrotoclax	Sonrotoclax(BGB-11417) is a highly potent, orally active and selective inhibitor of Bcl2. Sonrotoclax demonstrates increased potency along with in vitro and in vivo inhibitory activity against both WT Bcl-2 and the G101V mutant. Bcl-xL Sonrotoclax has effective cell killing effect against a variety of lymphoma and leukemia cell lines.	Nov 05 2024
E1491	Brigimadlin	Brigimadlin(BI 907828) is a potent, orally active inhibitor of E3 ubiquitin-protein ligase MDM-2. Brigimadlin inhibits MDM-2's suppression of the tumor suppressor p53. It promotes apoptosis and enhances the transcription of p53 targets such as p21 and PUMA in BT48, BT67, and BT73 cells.	Sep 23 2024
E1971	Rezatapopt	Rezatapopt(PC14586) is a first-in-class p53 reactivator. It selectively binds to the mutated p53 Y220C protein and restores its wild-type activity. It can also be used to inhibit solid tumor with p53 mutation.	Sep 05 2024
E1560	Raptinal	Raptinal is a pro-apoptotic compound that induces apoptosis by promoting the release of cytochrome c from the mitochondria, thereby activating the intrinsic apoptotic pathway. It also inhibits the activity of caspase-activated Pannexin 1 (PANX1), a ubiquitously expressed transmembrane channel involved in regulating various cell death-associated processes.	Aug 15 2024
E4831	L-Arginine (L-glutamate)	L-Arginine (L-glutamate) (Arginine glutamate) is a mixture of amino acids that induces apoptosis via hypertonic stress. It also promotes gastric relaxation by providing L-arginine for nitric oxide production, thereby benefiting gastrointestinal motility and conditions associated with vagus nerve dysfunction.	Jul 19 2024
E1867	NPD4928	NPD4928 is an inhibitor of Ferroptosis Suppressor Protein 1 (FSP1) that enhances ferroptosis. It enhances the cytotoxic effects on various cell types when combined with GPX4 antagonists.	Jul 11 2024
E1761	AMG PERK 44	AMG PERK 44 is a highly selective and orally active inhibitor of PERK with an IC50 of 6 nM. AMG PERK 44 exhibits 1000-fold and 160-fold selectivity over GCN2 and B-Raf, respectively.	Jun 02 2024
E1962	RMC-9805	RMC-9805(KRAS G12D ON inhibitor) is an orally active inhibitor of KRAS G12D. RMC-9805 inhibits RAS signaling, leading to apoptosis in cancer cells with the KRAS G12D mutation.	May 15 2024
E1925	Butylhydroxyanisole	Butylhydroxyanisole (Butylated hydroxyanisole, BHA, E320) is an inhibitor of ferroptosis, a food preservative and antioxidant that prevents the formation of harmful compounds, extending shelf life. However, it's associated with liver toxicity, reproductive organ development issues, learning delays, and sleep problems.	Apr 25 2024
S8546	Alrizomadlin	Alrizomadlin(APG-115, AA-115) is a highly potent and efficacious inhibitor of MDM2 and binds to MDM2 with IC50 of 3.8 nM. It exhibits potent antiproliferative and apoptogenic activities and also significantly reduces tumor burden and prolonged survival in AML xenograft models.	Apr 21 2024

製品コード	製品名称	製品説明	添加時期
E6024	Selumetinib sulfate	Selumetinib sulfate (AZD6244 sulfate, ARRY-142886 sulfate) is an oral, non-ATP-competitive inhibitor of MEK1/2, with an IC50 of 14 nmol/L against purified MEK1. It exhibits an anti-tumor effect in the HT-29 xenograft model and is used to treat cancer and inflammation.	Dec 18 2024
S9740	U0126	U0126 is a highly potent and selective inhibitor of the dual-specificity kinases MEK1 and MEK2, with IC50 values of 72 nM and 58 nM, respectively. It also acts as a strong antioxidant, protecting cells from oxidative stress-induced cell death.	Dec 05 2024
E4681	PF-07799933	PF-07799933 (Claturafenib, ARRY-440) is a brain-penetrant, selective, pan-mutant inhibitor of BRAF. It exhibits broad inhibition of pERK levels in HT29 cells with an IC50 value of 1.6 nM. PF-07799933 treatment displays antitumor activity against BRAFV600- and non-V600-mutant cancers preclinically and in treatment-refractory patients.	Nov 24 2024
E4791	Adezmapimod hydrochloride	Adezmapimod hydrochloride (RWJ 64809 hydrochloride, SB 203580 hydrochloride) is an inhibitor of the MAPK family member termed as stress-activated protein kinase 2a(SAPK2a; also known as p38). It exhibits IC50 of SAPK2a/p38 and SAPK2b/p38β2 with IC50 values of 50 nM and 500 nM respectively and can be used in research of chronic inflammatory diseases, such as rheumatoid arthritis.	Nov 17 2024
E1271	Zunsemetinib	Zunsemetinib(ATI-450, CDD-450) is a selective inhibitor of p38α mitogen-activated protein kinase-activated protein kinase 2 (MK2) that mediates inflammatory responses. It reduces inflammation in cryopyrinopathy, alleviates arthritis, and potentially prevents tachyphylaxis.	Sep 25 2024
E4599	BGB-3245(Brimarafenib)	BGB-3245(Brimarafenib, Brimarafenibum) is an inhibitor of Raf kinase. BGB-3245 displays potent effects against different RAF isoforms, including BRAF Class I/II/III mutations, BRAF fusions, and heterodimerization with CRAF in preclinical models. It also exhibits antineoplastic effects.	Sep 23 2024
E1969	ADT-007	ADT-007 is a potent and orally active pan-RAS inhibitor. ADT-007 effectively targets and suppresses the proliferation of cancer cells harboring mutated or hyper-activated wild-type RAS isozymes. ADT-007 exhibits potent anti-cancer effects.	Sep 09 2024
E4651	HRS-4642	HRS-4642 is a selective inhibitor of KRAS G12D with a Kd value of 0.083 nM. It exhibits robust anti-cancer activity against KRAS G12D-mutant cancers both in vitro and in vivo.	Sep 09 2024
E1965	NST-628	NST-628 is a potent and well-tolerated single-agent inhibitor of both RAF and MEK. It acts as a pan-RAF–MEK molecular glue that blocks the phosphorylation and activation of MEK by RAF.	Aug 28 2024
E1902	Nedometinib	Nedometinib (NFX-179) is a highly specific and potent inhibitor of MEK1 with an IC50 of 135 nM. It also results in suppression of p-ERK levels and can be used in research and treatment of cutaneous neurofibromas (cNFs) associated with neurofibromatosis type 1 (NF1).	Aug 12 2024

製品コード	製品名称	製品説明	添加時期
E1625	Elsubrutinib	Elsubrutinib(ABBV-105) is a covalent, irreversible, potent, and highly selective inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 0.18 μM for BTK catalytic domain. It specifically inhibits BTK dependent cellular functions, including both BCR and FcγR mediated signaling. It also exhibits significant efficacy in pre-clinical mechanistic models of antibody production, as well as in models of rheumatoid arthritis and lupus.	Jun 03 2024
E1783	Conteltinib(CT-707)	Conteltinib(CT-707) is a potent multikinase inhibitor of ALK, FAK,Pyk2, showing promising anti-tumor activities. Conteltinib exhibits significant inhibitory effects on FAK with an IC50 value of 1.6 nM in vitro kinase assay.	Mar 26 2024
E1114	Ifebemtinib	Ifebemtinib(IN10018, BI853520) is a highly selective, potent inhibitor of focal adhesion kinase (FAK), with an IC50 of 1 nM for inhibiting FAK autophosphorylation. It also inhibits FER Kinase and FES Kinase with IC50s of 900 nM and 1040 nM, respectively, inhibiting spheroid formation and orthotopic tumor growth in malignant pleural mesothelioma. IN10018 exhibits anti-tumor activity in vitro and in vivo.	Mar 25 2024
E1735	PK11007	PK11007 is a thiol-reactive anticancer agent that stabilizes p53 via selective alkylation of two surface cysteines without compromising its DNA binding. It induces mutant p53 cancer cell death by increasing reactive oxygen species (ROS) levels.	Dec 07 2023
S8617	Acriflavine	Acriflavine is a HIF-1 dimerization inhibitor and have potent inhibitory effects on tumor growth and vascularization. It is used as fluorescent dye for labeling high molecular weight RNA.	Nov 14 2023
E1712	FM19G11	FM19G11 is a hypoxia-inducible factor-1-alpha (HIF-1α) inhibitor, and it inhibits hypoxia-induced luciferase activity with an IC50 of 80 nM in HeLa cells.	Nov 08 2023
E1661	Adaptaquin	Adaptaquin is an inhibitor of hypoxia-inducible factor prolyl hydroxylase 2 (HIF-PHD2), with an IC50 of 2 μM. Adaptaquin also inhibits lipid peroxidation and maintains mitochondrial function.	Nov 05 2023
E4474	Infigratinib Phosphate	Infigratinib Phosphate (NVP-BGJ398 phosphate) is the phosphate salt form of infigratinib, an orally bioavailable pan-inhibitor of human fibroblast growth factor receptors (FGFRs) with IC50 of 0.9 nM, 1.4 nM, 1 nM, and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4 respectively. It also has potential antiangiogenic, antineoplastic and antitumor activities.	Oct 24 2023
A2126	Anti-mouse VEGFR-2-InVivo	Anti-mouse VEGFR-2-InVivo (Clone: DC101) monoclonal antibody reacts with mouse VEGFR-2 (vascular endothelial growth factor receptor 2) also known as CD309, KDR, and Flk-1 and inhibit VEGFR-2 signaling in vivo. VEGFR-2 plays a key role in vascular development and permeability.	Oct 17 2023
A2606	Disitamab (Anti-ERBB2 / HER2 / CD340)	Disitamab (Anti-ERBB2 / HER2 / CD340) is a humanized monoclonal antibody targeting HER2. It can be used in the synthesis of antibody-drug conjugates (ADCs), Disitamab vedotin. It has antitumor and antineoplastic activities. MW :144.16 KD	Oct 11 2023

製品コード	製品名称	製品説明	添加時期
E4800	BML-284	BML-284 (Wnt Agonist) is a potent and cell-permeable activator of Wnt signaling that induces TCF-dependent transcriptional activity with an EC50 value of 0.7 µM. BML-284 also acts as an agonist of β-catenin that effectively activates direct Wnt-β-catenin signaling to induce adipocyte dedifferentiation while circumventing the apoptotic effect in the hypertonic treatment.	Nov 25 2024
E1731	JW74	JW74 is a specific inhibitor of the canonical Wnt signaling with IC50 790 nM in the ST-Luc assay. It inhibit the growth of tumor cells in both mouse xenograft model of colorectal cancer and in ApcMin mice.	Nov 26 2023
E1486	Zamaporvint (RXC004)	Zamaporvint (RXC004) is an orally active and selective inhibitor of Wnt. It targets membrane-bound o-acyltransferase Porcupine and inhibits Wnt ligand palmitoylation, secretion, and pathway activation. RXC004 exhibits potent antiproliferative effects in Wnt ligand-dependent colorectal and pancreatic cell lines and possesses multiple antitumor mechanisms.	Oct 11 2023
A2621	Anti-ACVR1 / ALK-2 (DS-6016a)	Anti-ACVR1 / ALK-2 (DS-6016a) monoclonal antibody targeting ALK-2. It can be used in the treatment of fibrodysplasia ossificans progressiva (FOP). MW :145.56.	Oct 11 2023
A2681	Brontictuzumab (Anti-NOTCH1)	Brontictuzumab (Anti-NOTCH1) is a monoclonal antibody that targets Notch1 signal. It inhibits tumor cell proliferation and can be used in the research of leukemia and lymphoma. MW :150 KD.	Oct 11 2023
A2370	Elezanumab (Anti-RGMA)	Elezanumab (Anti-RGMA) is a human monoclonal antibody that selectively targets repulsive guidance molecule A (RGMa). Elezanumab potently inhibited RGMa mediated BMP signalling via the SMAD1/5/8 pathway with IC50 of 97 pM. MW: 146.44 kD.	Aug 10 2023
A2489	Vantictumab (Anti-FZD)	Vantictumab (Anti-FZD) is a monoclonal antibody targeting the Wnt signaling pathway with potential antineoplastic activity. Vantictumab binds to certain receptors in the Wnt signaling pathway thereby preventing the activation of the Wnt signaling pathway. This results in an inhibition of cancer stem cell (CSC) activity and a subsequent inhibition of cancer cell proliferation. MW: 145.5 KD.	Aug 10 2023
E0787	ALLO-2	ALLO-2 is a potent antagonist of both wild-type mouse Smo and drug-resistant D473H mutant human Smo that inhibits Smo agonist inhibited Gli-Luc activity in TM3-Gli-Luc cells with IC50 of 6 nM.	Jul 28 2022
S9965	M435-1279	M435-1279 is a UBE2T inhibitor, inhibiting the Wnt/β-catenin signaling pathway hyperactivation through blocking UBE2T-mediated degradation of RACK1.	Jul 06 2022
E0480	MRT-81	MRT-81 is a potent antagonist of human and rodent smoothened (Smo) receptors, with an IC50 value of 41 nM in the Shh-light2 cells, exerting potent hedgehog (Hh) signaling pathway inhibiting activity.	Jul 01 2022

製品コード	製品名称	製品説明	添加時期
E1633	BAY-805	BAY-805 is a potent, selective, and cell-active inhibitor that non-covalently targets the catalytic activity of USP21, a member of the ubiquitin-specific protease (USP) subfamily of deubiquitinating enzymes (DUBs).	Oct 15 2024
E1847	GBD-9	GBD-9 is a double-mechanism efficient degrader of BTK and GSPT1 by recruiting the E3 ligase cereblon (CRBN). GBD-9 acts both as a PROTAC molecule to induce the degradation of BTK and as a molecular glue to degrade GSPT1.It exhibits anti-proliferative effects, inhibiting cancer cell survival.	Aug 15 2024
E1957	NX-1607	NX-1607 (Cbl-b-IN-3) is an oral inhibitor of Casitas B-lineage lymphoma proto-oncogene B (CBL-B), which is an E3 ubiquitin ligase and a key regulator of T, NK, and dendritic cell activation and suppresses their anti-tumor functions. NX-1607 enhances antigen recall, reduces T cell exhaustion, and increases cytokine production in response to T cell receptor stimulation, thereby counteracting suppressive signals from the tumor microenvironment.	Jul 23 2024
E1937	PT-179	PT-179, an orthogonal Thalidomide derivative targets cereblon without causing off-target degradation effects. PT-179 specifically binds CRBN, forms a ternary complex with a target protein fused to a zinc finger (ZF) degron, and mediates the degradation of the tagged protein.	May 09 2024
E1798	HOIPIN-8	HOIPIN-8, is a potent inhibitor of linear ubiquitin chain assembly complex (LUBAC) and NF-κB signaling with an IC50 value of 11 nM. It serves as a powerful tool for investigating the physiological and cellular functions of LUBAC.	Apr 23 2024
E1678	SPOP-i-6lc	SPOP-i-6lc is a selective speckle-type POZ protein (SPOP) E3 ubiquitin ligase inhibitor with IC50 of 2.1 μM and 3.5 μM, in A498 and OS-RC-2 cell lines, respectively. In vitro, It suppresses viability and proliferation of A498 and OS-RC-2 kidney cancer cell lines.	Dec 17 2023
E1479	I-138	I-138 is an orally active, potent reversible inhibitor of USP1-UAF1 with IC50 0f 4.1 nM. I-138 is structurally related to ML323 and induces the monoubiquitination of FANCD2 and PCNA in MDA-MB-436 cells and increases PCNA and FANCD2 monoubiquitination in HAP-1 USP1 WT cells.	Oct 11 2023
A2727	Anti-Polyubiquitin	Anti-Polyubiquitin is a monoclonal anti-Polyubiquitin antibody used for isolating polyubiquitin chain-tagged proteins. MW: 144.98 KD.	Oct 11 2023
E1214	KSQ-4279	KSQ-4279 (USP1-IN-1) is an orally bioavailable selective inhibitor of the ubiquitin specific protease 1 (USP1) with anti-proliferative activity. KSQ-4279 also exhibits synergistic activity in combination with PARP inhibitors.	Aug 29 2023
E1389	Eeyarestatin I	Eeyarestatin I is a potent inhibitor of endoplasmic reticulum-associated protein degradation (ERAD). Eeyarestatin I also inhibits Sec61 translocon.	Jul 27 2023

製品コード	製品名称	製品説明	添加時期
E6035	(R)-Propranolol hydrochloride	(R)-Propranolol (hydrochloride) (Dexpropranolol hydrochloride) is a nonselective antagonist of beta-adrenergic receptor (β-adrenergic receptor (βAR) ) that competitively blocks the action of epinephrine (EPI) and norepinephrine (NE) on β1- and β2-adrenoreceptors (AR). It exhibits anti-neuroblastoma activity and is effective in combination therapies for relapsed and refractory neuroblastoma patients.	Dec 22 2024
E4963	Clonidine	Clonidine(Clonidin) is a direct-acting α2-adrenergic agonist. It is potentially used in the treatment of attention-deficit hyperactivity disorder (ADHD) in children and adolescents.	Dec 20 2024
E6011	Agomelatine hydrochloride	Agomelatine hydrochloride (S-20098 hydrochloride) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. It is also a selective antagonist of 5-HT2C receptors with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively. Blockade of these receptors enhances adrenergic and dopaminergic transmission in the frontocortical regions.	Dec 12 2024
E4774	4-DAMP	4-DAMP (4-diphenyl-acetoxy-N-methyl-piperidine) (4-DAMP methiodide) is a selective antagonist of M3 type muscarinic acetylcholine receptors (M3-mAChR) with a pKi of 9.3. It also has a high affinity for the closely-related M5 receptor with a pKi of 8.9. It is routinely used to study the regulation and functions of the M3 receptor.	Dec 05 2024
E1841	Monlunabant	Monlunabant(INV-202, (S)-MRI-1891) is a peripherally acting inverse agonist of the cannabinoid type-1 receptor (CB1R), with the potential to treat respiratory and renal complications associated with metabolic disorders. It improves lung compliance in a mouse model of asthma and reduces renal fibrosis in a streptozotocin-induced diabetic nephropathy mouse model.	Oct 30 2024
E4940	Chlorphenesin carbamate	Chlorphenesin carbamate(Maolate, Rinlaxer, U 19646) is a centrally-acting muscle relaxant that inhibits motoneuron excitability. It is also used to treat pain and discomfort related to skeletal muscle trauma and inflammation.	Oct 30 2024
E4955	Pitolisant	Pitolisant(BF2.649, Tiprolisant) is a potent, selective antagonist of the non-imidazole histamine H3 receptor, with a Ki value of 0.16 nM and an EC50 of 1.5 nM as an inverse agonist. It enhances the activity of histaminergic neurons, promoting vigilance and cognitive function. It is useful in research on wakefulness, memory deficits, and cognitive disorders.	Oct 30 2024
E4714	Xanomeline	Xanomeline(LY-246708) is a selective agonist of muscarinic type 1(M(1) receptor and muscarinic type 4 receptor(M(4). It increases neuronal excitability and inhibits behaviors induced by D-amphetamine and (-)-apomorphine.	Oct 23 2024
E4881	Ifenprodil	Ifenprodil(Dilvax, RC 61-91) is a potent antagonist of N-methyl-D-aspartate (NMDA) receptor that selectively inhibits receptors containing the NR2B subunit. It exhibits potential for its use in the treatment of various neurological diseases.	Oct 22 2024
E4938	Diphenylpyraline	Diphenylpyraline(Allergen, Difenilpiralina; 4-Diphenylmethoxy-1-methylpiperidine), also known as 4-Diphenylmethoxy-1-methylpiperidine, is a first-generation antihistamine that acts as an antagonist of the histamine H1 receptor. It provides therapeutic antiallergic effects and has the potential to treat cocaine addiction.	Oct 17 2024

製品コード	製品名称	製品説明	添加時期
E1913	MZ-101	MZ-101 (GYS1-IN-2) is a potent small molecule inhibitor of Glycogen synthase 1(GYS1) with an IC50 value of 0.041 µM. By depleting muscle glycogen, MZ-101 treatment normalizes glycogen levels and corrects transcriptional and metabolic abnormalities in Pompe mice.	Dec 22 2024
E1890	A-967079	A-967079 is a selective antagonist of TRPA1 receptor with IC50 values of 67 nM and 289 nM at human and rat TRPA1 receptors, respectively. A-967079 decreases the responses of wide dynamic range (WDR), and nociceptive specific (NS) neurons following noxious pinch stimulation and high-intensity mechanical stimulation in rats. It demonstrates strong penetration into the central nervous system (CNS).	Dec 20 2024
E4734	MeAIB	MeAIB (α-(Methylamino)isobutyric acid) is a specific substrate for amino acid transport system A, especially System A (ATA1). It also inhibits SNAT2, which reduces intracellular levels of essential amino acids and impairs cell proliferation in porcine enterocytes by disrupting the mTOR signalling pathway.	Dec 20 2024
E4754	Semustine	Semustine is a member of the chloroethyl nitrosourea (CENU) family that induces DNA alkylation at the major groove, forming interstrand cross-links between guanine and cytosine bases (dG-dC). It exerts antitumor activity by inducing these DNA cross-links and is used as an antineoplastic alkylating agent for treating Lewis lung carcinoma, leukemia, and metastatic brain tumors.	Dec 20 2024
E5773	Gypenoside L	Gypenoside L, is a saponin from Gynostemma pentaphyllum, increases SA-β-galactosidase activity, enhances senescence-associated cytokine production, inhibits proliferation and LPS-induced nitric oxide (NO) production, induces S-phase arrest, and activates p21, p27, p38, ERK MAPK, and NF-κB pathways to promote senescence.	Dec 20 2024
S8593	VX-984	VX-984 (M9831) is an orally active, potent, selective, and ATP-competitive inhibitor of DNA-PK. VX-984 effectively suppresses non-homologous end joining (NHEJ) and increases DNA double-strand breaks (DSBs). It enhances the cytotoxic effects of ionizing radiation (IR) in various cancer cell lines, including non-small cell lung cancer (NSCLC) cell lines, in vitro. Additionally, VX-984 reduces DNA-PKcs autophosphorylation.	Dec 18 2024
E4782	17-OH PREG (17a-Hydroxypregnenolone)	17-OH PREG (17a-Hydroxypregnenolone) is a pregnenolone metabolite and DHEA precursor. It is formed through CYP17A1 hydroxylase and 17,20-lyase activities. It is the most relevant steroid for the study of elevated plasma levels linked to type II 3β-hydroxysteroid dehydrogenase deficiency.	Dec 12 2024
E5775	Exatecan	Exatecan (DX-8951), is a water-soluble derivative of camptothecin. It acts as an inhibitor of DNA topoisomerase I with an IC50 value of 1.906 μM. It demonstrates potent antitumor effects and triggers apoptotic cell death after treatment in human pancreatic cancer cells.	Dec 11 2024
E5777	Tris(benzyltriazolylmethyl)amine	Tris(benzyltriazolylmethyl)amine (TBTA) is a ligand used as a biochemical tool for labeling proteins and enzymes. It dramatically enhances the Copper(II) acetate (Cu(OAc)2)-accelerated azide-alkyne cycloaddition (AAC) reactions involving nonchelating azides.	Dec 11 2024
E4621	BHPI	BHPI is a potent noncompetitive inhibitor of estrogen receptor α (ERα), which disrupts the protective estrogen–ERα-mediated activation of the unfolded protein response (UPR), leading to sustained UPR activation. It specifically inhibits the growth of drug-resistant ERα-positive breast and ovarian cancer cells and induces significant tumor regression in a mouse xenograft model of breast cancer.	Dec 05 2024