抗体薬物複合体(ADC)

抗体薬物複合体(ADC)

製品コード 製品名 製品説明
D4001 Trastuzumab deruxtecan (DS-8201a, T-DXd) Trastuzumab deruxtecan (DS-8201a, T-DXd) is an antibody-drug conjugate (ADC) composed of an anti-HER2 (human epidermal growth factor receptor 2) antibody and a cytotoxic topoisomerase I inhibitor. Trastuzumab deruxtecan shows durable antitumor activity. Trastuzumab deruxtecan has a molecular weight of 153KDa.
D4002 Sacituzumab govitecan Sacituzumab govitecan (IMMU-132) is an antibody-drug conjugate (ADC) targeting Trop-2 for delivery of SN-38, showing anticancer activity. Sacituzumab govitecan has a molecular weight of 160KDa. This product is supplied as 10mg/ml PBS solution.
D4003 Trastuzumab Emtansine(T-DM1) Trastuzumab Emtansine(T-DM1,Ado-Trastuzumab emtansine) is an antibody-drug conjugate (ADC) that incorporates the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of the microtubule-inhibitory agent DM1.Trastuzumab emtansine has a molecular weight of 145kDa.This product is supplied as 10mg/ml PBS solution.
D4004 Patritumab deruxtecan Patritumab deruxtecan (HER3-DXd) is an antibody-drug conjugate (ADC) composed of a fully human anti-HER3 IgG1 monoclonal antibody and a cytotixic topoisomerase I inhibitor. Patritumab deruxtecan shows anticancer activity.
D4005 Vorsetuzumab mafodotin Vorsetuzumab mafodotin (SGN-75) is an antibody-drug conjugate (ADC) composed of a humanized monoclonal antibody directed against the extracellular domain of the human CD70 molecule, and a cytotoxic tubulin polymerization inhibitor. It is used in the treatment of renal cell carcinoma.
D4006 Anetumab-MMAE Anetumab-MMAE is an antibody-drug conjugate (ADC) composed of a human anti-mesothelin (MSLN) antibody and the anti-mitotic cytotoxic agent monomethyl auristatin (MMAE).
D4007 Clivatuzumab-MMAE Clivatuzumab-MMAE is an antibody-drug conjugate (ADC) composed of a humanized anti-mucin (MUC1) monoclonal antibody and a anti-mitotic cytotoxic agent monomethyl auristatin (MMAE).
D4009 Indusatumab vedotin Indusatumab vedotin (MLN-0264) is an antibody-drug conjugate (ADC) composed of an anti-human GUCY2C (Guanylate cyclase 2C) monoclonal antibody and a anti-mitotic cytotoxic agent, monomethyl auristatin E (MMAE).
D4010 Lifastuzumab vedotin Lifastuzumab vedotin (LIFA, DNIB0600A, RG-7599) is an antibody-drug conjugate (ADC) composed of a humanized anti-NaPi2b monoclonal antibody and an anti-mitotic cytotoxic agent, monomethyl auristatin E (MMAE) . Lifastuzumab vedotin is used in the treatment of platinum-resistant ovarian cancer.
D4011 Anetumab ravtansine Anetumab ravtansine (BAY 94-9343) is an antibody-drug conjugate (ADC) composed of a human anti-mesothelin antibody and a cytotoxic maytansinoid tubulin inhibitor DM4. Anetumab ravtansine has the potential to treat advanced solid tumors.
D4012 Polatuzumab vedotin-piiq Polatuzumab vedotin-piiq (polatuzumab vedotin, DCDS4501A, RG7596) is an antibody-drug conjugate (ADC) composed of a monoclonal antibody against CD79b (a B cell receptor component) and the anti-mitotic cytotoxic agent monomethyl auristatin (MMAE). It is used for the treatment of relapsed/refractory diffuse large B-cell lymphoma (DLBCL).
D4013 Zilovertamab vedotin Zilovertamab vedotin (VLS-101, MK-2140) is an antibody-drug conjugate (ADC) composed of a humanised monoclonal antibody targeting ROR1 and the anti-mitotic cytotoxic agent monomethyl auristatin E (MMAE). It has potential for the treatment of lymphoid malignancies.
D4015 Farletuzumab-MMAE Farletuzumab-MMAE is an antibody-drug conjugate (ADC) composed of humanized anti-human folate receptor-alpha (FRα) and the cytotoxic agent monomethyl auristatin (MMAE) via a MC-Vc linker. It has a potent antitumor activity.
D4016 Iladatuzumab vedotin Iladatuzumab vedotin (DCDS0780A;RO7032005 ), is an antibody-drug conjugate (ADC) composed of CD79B (immunoglobulin-associated CD79 beta) antibody and cytotoxic agent monomethyl auristatin E (MMAE) conjugated through maleimidocaproyl-valyl-citrullinyl-p-aminobenzyloxycarbonyl (mc-val-cit-PABC) type linker. Iladatuzumab vedotin has the potential for B-cell non-Hodgkin lymphoma (B-NHL) research.
D4017 Pinatuzumab vedotin Pinatuzumab Vedotin (RG-7593, DCDT2980S, DCDT-2989S), is an antibody-drug conjugate (ADC) composed of CD22 (Sialic acid binding Ig-like lectin 2, SIGLEC2, SIGLEC-2, B-lymphocyte cell adhesion molecule, BL-CAM, Leu-14) antibody and cytotoxic agent monomethyl auristatin E (MMAE) conjugated through maleimidocaproyl-valyl-citrullinyl-p-aminobenzyloxycarbonyl (mc-val-cit-PABC) type linker.
D4019 Sirtratumab vedotin Sirtratumab Vedotin (ASG-15ME), is an antibody-drug conjugate (ADC) composed of SLTRK6 (SLIT and NTRK like family member 6, "SLIT and NTRK-like family, member 6") and cytotoxic agent monomethyl auristatin E (MMAE). It delivers a small molecule microtubule-disrupting agent, monomethyl auristatin E (MMAE), to tumor cells expressing SLITRK6. SIRTRATUMAB VEDOTIN has the potential for Bladder Cancer, Metastatic urothelial cancer research.
D4021 Codrituzumab-MMAE Codrituzumab-MMAE, is an antibody-drug conjugate composed of a anti-GPC3 monoclonal antibody and a cytotoxic tubulin polymerase inhibitor conjugated through MC-Vc-PAB (maleimidocaproyl-valine-citrulline-p-aminobenzoyloxycarbonyl) type linker.
D4022 Cetuximab-MMAE Cetuximab-MMAE is an antibody-drug conjugate composed of a anti-EGFR monoclonal antibody and a cytotoxic tubulin polymerase inhibitor conjugated through MC-Vc-PAB (maleimidocaproyl-valine-citrulline-p-aminobenzoyloxycarbonyl) type linker.
D4026 Tusamitamab ravtansine Tusamitamab Ravtansine (SAR-408701), is an antibody-drug conjugate (ADC) composed of CEACAM5 (carcinoembryonic antigen-related cell adhesion molecule ) targeting antibody and a cytotoxic maytansinoid tubulin inhibitor DM4. TUSAMITAMAB RAVTANSINE has the potential for use in research of several solid tumors.
D4027 Serclutamab talirine Serclutamab Talirine (ABBV-321), is an antibody-drug conjugate (ADC) composed of an humanized immunoglobulin G1 anti-EGFR monoclonal antibody conjugated to a pyrrolobenzodiazepine (PBD) dimer via a maleimidocaproyl-valine-alanine linker. Serclutamab Talirine has the potential for use in advanced solid tumors associated with overexpression of the epidermal growth factor receptor (EGFR) or its ligands.
D4031 Cantuzumab mertansine Cantuzumab mertansine (HUC242-DM1, SB-408075) is an anti-MUC1 sialylated carbohydrate, tumour-associated (CA242, cancer antigen 242), humanized monoclonal antibody conjugated to maytansinoid DM1 ([N2’-deacetyl-N2’-(3-mercapto-1-oxopropyl)-maytansine]) via a reductible SPP linker [N-succinimidyl 4-(2-pyridyldithio)pentanoate].
D4032 Cantuzumab ravtansine Cantuzumab ravtansine (IMGN242, HUC242-DM4) is an ADC. It is a humanized monoclonal antibody, huC242, covalently linked via a disulfide bond to DM4. Cantuzumab ravtansine has broad antitumor efficacy against a range of CanAg-positive human tumor xenografts.
D4033 Ozuriftamab vedotin Ozuriftamab vedotin (BA 3021) is an antibody-drug conjugate (ADC) composed of ozuriftamab, a conditionally active biologic (CAB) antibody against receptor tyrosine kinase-like orphan receptor 2 (ROR2) conjugated to monomethyl auristatin E, with potential antineoplastic activity.
D4034 Lorvotuzumab mertansine Lorvotuzumab mertansine (IMGN901, LM) is an antibody-drug conjugate, linking an anti-mitotic agent (DM1) to an anti-CD56 antibody (lorvotuzumab).
D4036 Sofituzumab vedotin Sofituzumab Vedotin (DMUC5754A, RG-7458) is an antibody-drug conjugate (ADC) that contains the humanized IgG1 anti-MUC16 monoclonal antibody (mAb) and a potent anti-mitotic agent, monomethyl auristatin E (MMAE), linked through a protease-labile linker. DMUC5754A binds to the MUC16 extracellular domain with high affinity.
D4037 Laprituximab emtansine Laprituximab emtansine (IMGN-289) is an anti-EGFR (epidermal growth factor receptor, receptor tyrosine-protein kinase erbB-1, ERBB1, HER1, HER-1, ERBB), chimeric monoclonal antibody conjugated to maytansinoid DM1 via a succinimidyl-4-(N-maleimidomethyl) cyclohexane-1-carboxylate (SMCC) linker, forming a nonreducible thioether bond.
D4038 Enapotamab vedotin Enapotamab vedotin (EnaV, HuMAX-AXL-ADC) is an AXL-specific human IgG1 antibody conjugated to the microtubule disrupting agent monomethyl auristatin E (MMAE) through a protease cleavable valine-citrulline (vc) linker.
D4039 Praluzatamab ravtansine Praluzatamab ravtansine (CX-2009) is a conditionally activated Probody drug conjugate (PDC) comprising an anti-CD166 mAb conjugated to DM4, with a protease-cleavable linker and a peptide mask that limits target engagement in normal tissue and circulation.
D4042 Depatuxizumab mafodotin Depatuxizumab Mafodotin (Depatux-M, ABT-414) is an antibody-drug conjugate consisting of an EGFR IGg1 monoclonal antibody conjugated to the tubulin inhibitor monomethyl auristatin F via a stable maleimidocaproyl link. Depatuxizumab Mafodotin is used in the treatment of recurrent EGFR-amplified Glioblastoma (GBM).
D4045 Brentuximab vedotin Brentuximab vedotin (SGN-35; Adcetris,cAC10-vcMMAE) is an anti-CD30 antibody conjugated via a protease-cleavable linker to the potent anti-microtubule agent monomethyl auristatin E (MMAE). Brentuximab vedotin can be used for the research of relapsed and refractory Hodgkin lymphoma.
D4046 Telisotuzumab vedotin Telisotuzumab vedotin (Teliso-V, ABBV-399) is an antibody-drug conjugate (ADC) composed of the anti–c-Met humanized monoclonal antibody coupled to the cytotoxic monomethyl auristatin E (MMAE) through a mc-val-cit-PABC type linker. Telisotuzumab vedotin can be used for research on advanced solid tumours.
D4048 Labetuzumab govitecan Labetuzumab govitecan (IMMU-135) is a humanised anti-CEACAM5 (carcinoembryonic antigen-related cell adhesion molecule 5) antibody linked site-specifically to the active metabolite of irinotecan SN-38 via a proprietary linker. Labetuzumab govitecan can be used for research on colorectal cancer.
D4049 Disitamab vedotin Disitamab Vedotin (RC-48 ,RC 480-ADC) is an antibody-drug conjugate(ADC) composed of anti-[ERBB2 (epidermal growth factor receptor 2, receptor tyrosine-protein kinase erbB-2, EGFR2, HER2, HER-2, p185c-erbB2, NEU, CD340)] humanized monoclonal antibody, conjugated to monomethylauristatin E (MMAE), via a cleavable maleimidocaproyl-valyl-citrullinyl-p-aminobenzyloxycarbonyl (mc-val-cit-PABC) type linker. Disitamab Vedotin has the potential for use in solid tumors mainly in advanced breast cancer.
D4050 Datopotamab deruxtecan Datopotamab deruxtecan (DS-1062, DS-1062A, Anti-TRP2/dxd) is an antibody-drug conjugate (ADC) composed of a humanized anti-TROP2 monoclonal antibody, conjugated to topoisomerase I inhibitor, via a tetrapeptide-based linker. Datopotamab deruxtecan has the potential for use in solid tumors mainly in advanced unresectable advanced NSCLC.
D4051 Tisotumab vedotin Tisotumab vedotin (TF-011-MMAE, HuMax-TF-ADC) is an antibody-drug conjugate (ADC) composed of a fully human monoclonal antibody to tissue factor III (thromboplastin) also known as CD142, conjugated to Monomethyl Auristatin E (MMAE), via a cleavable maleimidocaproyl-valyl-citrullinylp-aminobenzyloxycarbonyl (mc-val-cit-PABC) type linker. Tisotumab vedotin has the potential for use in research of solid tumors mainly in cervical cancer.
D4052 Trastuzumab MMAE Trastuzumab MMAE is an antibody-drug conjugate (ADC). It is composed of monomethyl auristatin E (MMAE) and trastuzumab conjugated via a Vc (Valine‐citrulline) linker. Trastuzumab MMAE has high affinity, specificity and anti-tumor activity in vitro.
D4053 Enfortumab vedotin-ejfv Enfortumab vedotin-ejfv (Padcev) is an antibody-drug conjugate (ADC) composed of an fully human anti-Nectin-4 IgG1 kappa monoclonal antibody (AGS-22C3), conjugated to Monomethyl Auristatin E (MMAE), via a protease-cleavable maleimidocaproyl-valyl-citrullinyl-p-aminobenzyloxycarbonyl. Enfortumab vedotin-ejfv has the potential for use in research of urothelial carcinoma.
D4054 Glembatumumab vedotin Glembatumumab vedotin (CDX-011 (DOX), CR011,CR011-vcMMAE) is an antibody-drug conjugate (ADC) composed of an fully human IgG2 monoclonal antibody (CR011) directed against glycoprotein NMB (GPNMB), conjugated to Monomethyl Auristatin E (MMAE), via a cleavable maleimidocaproyl-valyl-citrullinyl-p-aminobenzyloxycarbonyl (mc-val-cit-PABC) type linker. Glembatumumab vedotin has the potential for use in research of Breast cancer (TNBC) and advanced or metastatic melanoma.
D4057 Ladiratuzumab vedotin Ladiratuzumab vedotin (SGN-LIV1A, Anti-LIV-1 ADC) is an antibody-drug conjugate (ADC) composed of humanized anti-LIV-1 antibody, conjugated to Monomethyl auristatin E (MMAE), via a proteolytically cleavable type linker. Ladiratuzumab vedotin has the potential for use in multiple carcinomas.
D4058 IMGN779 IMGN779 is an antibody-drug conjugate (ADC) targeting CD33. It exhibits promising therapeutic approaches in acute myeloid leukemia (AML). MW :146.48 KD.
D4060 Mirvetuximab-MMAE Mirvetuximab-MMAE is an ADC targeting FOLR1 (folate receptor 1). It can be used in ovarian and other FRα-positive cancer research. MW :145.96 KD.
D4061 Anti-GPC3 / Glypican-3 (Codrituzumab-MMAE) Anti-GPC3 / Glypican-3 (Codrituzumab-MMAE) is an ADC targeting GPC3 (glypican-3). It induces antibody-dependent cellular cytotoxicity (ADCC) and inhibits tumor growth and can be used in the research of hepatocellular carcinoma (HCC). MW :145.58 KD.
D4062 Anti-KAAG1 (ADCT-901-MMAE) Anti-KAAG1 (ADCT-901-MMAE) is an ADC composed of a humanized monoclonal antibody (3A4) targeting human KAAG1. It is used for the treatment of advanced solid tumors including platinum resistant ovarian cancer and triple negative breast cancer. MW :145.28 KD.
E0200 Trastuzumab-deruxtecan (DS-8201a, T-DXd) Trastuzumab deruxtecan (DS-8201a, T-DXd) is an antibody-drug conjugate (ADC) composed of an anti-HER2 (human epidermal growth factor receptor 2) antibody and a cytotoxic topoisomerase I inhibitor. Trastuzumab deruxtecan shows durable antitumor activity. Trastuzumab deruxtecan has a molecular weight of 153KDa. This product is supplied as 10mg/ml PBS solution.This product is discontinued. We recommend the replacement products: D4001.
E2841 Sacituzumab-govitecan Sacituzumab govitecan (IMMU-132) is an antibody-drug conjugate (ADC) targeting Trop-2 for delivery of SN-38, showing anticancer activity. Sacituzumab govitecan has a molecular weight of 160KDa. This product is supplied as 10mg/ml PBS solution.This product is discontinued. We recommend the replacement products: D4002.
E2851 Trastuzumab-Emtansine(T-DM1) Trastuzumab Emtansine(T-DM1,Ado-Trastuzumab emtansine) is an antibody-drug conjugate (ADC) that incorporates the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of the microtubule-inhibitory agent DM1.Trastuzumab emtansine has a molecular weight of 145kDa.This product is supplied as 10mg/ml PBS solution. This product is discontinued. We recommend the replacement products: D4003
S0564 SPDP SPDP is a short-chain crosslinker for amine-to-sulfhydryl conjugation via NHS-ester and pyridyldithiol reactive groups that form cleavable disulfide bonds with cysteine sulfhydryls. SPDP is a glutathione cleavable ADC linker used for the antibody-drug conjugates (ADCs).
S0566 Sulfo-SMCC sodium Sulfo-SMCC sodium is a hetero-bifunctional, noncleavable ADC crosslinker which consists of N-hydroxysuccinimide (NHS) ester and maleimide groups to react with primary amines and sulfhydryl groups.
S0572 SMCC SMCC (Succinimidyl-4-(N-maleimidomethyl cyclohexane)-1-carboxylate) is a hetero-bifunctional crosslinker that contain N-hydroxysuccinimide (NHS) ester and maleimide groups that allow covalent conjugation of amine- and sulfhydryl-containing molecules. SMCC-conjugated antigen couples spleen cells to induce antigen-specific immune responses.
S0577 6-Maleimidohexanoic acid N-hydroxysuccinimide ester 6-Maleimidohexanoic acid N-hydroxysuccinimide ester (EMCS) is a heterobifunctional cross-linking reagent. EMCS is used as a unique and useful reagent for preparation of hapten conjugate and enzyme immunoconjugates.
S0586 Succinic anhydride Succinic anhydride (SA, Succinyl Oxide, Butanedioic Anhydride) is a cyclic anhydride that can be used in the homogeneous chemical modification of cellulose and as a noncleavable ADC linker that reacts with other compound to link the prodrug to an amine or hydroxy 1 group of a targeting polypeptide.
S0603 m-PEG12-amine m-PEG12-amine is a PEG-based PROTAC linker that can be applied into the synthesis of PROTACs. m-PEG12-amine is also a non-cleavable 12-unit PEG ADC linker applied into the synthesis of antibody-drug conjugates (ADCs).
S0623 Bis-PEG1-NHS ester Bis-PEG1-NHS ester is a noncleavable 1-unit PEG linker for antibody-drug-conjugation (ADC).
S0626 DSP Crosslinker DSP Crosslinker is a cleavable ADC linker applied into the synthesis of antibody-drug conjugates (ADCs).
S0627 PDEC-NB PDEC-NB is a disulfide cleavable linker that can be applied into the synthesis of antibody-drug conjugates (ADCs).
S0630 Mal-PEG6-NHS ester Mal-PEG6-NHS ester is a non-cleavable ADC linker containing a Maleimide group, 6-unit PEG and a NHS ester.
S0651 N-Butanoyl-L-homoserine lactone N-Butyryl-L-homoserine lactone (N-Butanoyl-L-homoserine lactone, N-Butyrylhomoserine lactone, C4-HSL) is a cleavable ADC linker applied into the synthesis of antibody-drug conjugates (ADCs). N-Butyryl-L-homoserine lactone is a small diffusible signaling molecule involved in quorum sensing, controlling gene expression, and cellular metabolism.
S0654 Mal-​PEG4-​NHS ester Mal-PEG4-NHS ester is a non-cleavable ADC linker containing a Maleimide group, 4-unit PEG and an NHS ester.
S0655 Propargyl-PEG4-NHS ester Propargyl-PEG4-NHS ester is a 4-unit amine reactive PEG linker for antibody-drug-conjugation (ADC) which is noncleavable.
S0657 DSS Crosslinker DSS Crosslinker (Disuccinimidyl suberate) is a membrane permeable homobifunctional crosslinking agent and a non-cleavable ADC linker applied into the synthesis of antibody-drug conjugates (ADCs).
S0675 Azide-PEG5-Tos Azide-PEG5-Tos (Azido-PEG5-OTs) is a cleavable 5-unit PEG ADC linker applied into the synthesis of antibody-drug conjugates (ADCs).
S6669 MC-Val-Cit-PAB MC-Val-Cit-PAB,also known as MC-Val-Cit-PAB-OH,is a cathepsin cleavable ADC peptide linker and is used for making ADC conjugate (antibody-drug conjugate).
S6688 Fmoc-Val-Cit-PAB Fmoc-Val-Cit-PAB (Fmoc-Val-Cit-PAB-OH) is a cleavable linker for antibody-drug conjugates (ADC).
S8670 Vipivotide tetraxetan (PSMA-617) Vipivotide tetraxetan (PSMA-617) is a chemically modified PSMA(prostate-specific membrane antigen) inhibitor with a Ki of 0.37 nM.
S0328 MMAF MMAF (Monomethylauristatin F) is a synthetic antineoplastic agent and a potent inhibitor of tubulin polymerization. MMAF (Monomethylauristatin F) is applied as a cytotoxic component of antibody-drug conjugates (ADCs) such as vorsetuzumab mafodotin, ABT-414 and SGN-CD19A.
S0346 NAcM-OPT NAcM-OPT is a specific, reversible and orally bioavailable inhibitor of cullin neddylation 1 (DCN1) that targets N-Acetyl-UBE2M (E2 conjugating enzyme, UBC12) interaction with DCN1 with IC50 of 79 nM.
S0563 10-Deacetyl-7-xylosyl paclitaxel 10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol, 7-xylosyl-10-deacetylpaclitaxel), a derivative of paclitaxel and naturally occurring xyloside isolated from Taxus chinensis, causes significant mitotic arrest in PC-3 cells followed by up-regulating expression of pro-apoptotic Bax and Bad protein, as well as down-regulating expression of anti-apoptotic Bcl-2 and Bcl-XL , which leads to a disturbance of the mitochondrial membrane permeability and to the activation of caspase-9.
S0564 SPDP SPDP is a short-chain crosslinker for amine-to-sulfhydryl conjugation via NHS-ester and pyridyldithiol reactive groups that form cleavable disulfide bonds with cysteine sulfhydryls. SPDP is a glutathione cleavable ADC linker used for the antibody-drug conjugates (ADCs).
S0566 Sulfo-SMCC sodium Sulfo-SMCC sodium is a hetero-bifunctional, noncleavable ADC crosslinker which consists of N-hydroxysuccinimide (NHS) ester and maleimide groups to react with primary amines and sulfhydryl groups.
S0702 α-Conotoxin GI α-Conotoxin GI, a 13-residue peptide originally isolated from the venom of the fish-hunting cone snail Conus geographus, acts as a competitive antagonist for the muscle-type nicotinic acetylcholine receptor (nAChR) with excellent selectivity for α/δ receptor subunit binding over α/γ.
S1150 Paclitaxel Paclitaxel is a microtubule polymer stabilizer with IC50 of 0.1 pM in human endothelial cells.Paclitaxel can cause both mitotic arrest and apoptotic cell death. Paclitaxel also induces autophagy.
S1208 Doxorubicin (DOX) HCl Doxorubicin (DOX) HCl is an antibiotic agent that inhibits human DNA topoisomerase I and topoisomerase II with IC50s of 0.8 μM and 2.67 μM, respectively. Doxorubicin reduces basal phosphorylation of AMPK. Doxorubicin is used in the concomitant treatment of HIV-infected patients but is found to be at high risk of HBV reactivation.This product may precipitate when dissolved in PBS solution. It is recommended to prepare the stock solution in pure water and dilute with either pure water or saline to obtain the working solution.
S1210 Methotrexate Methotrexate, analog of folic acid, is a nonspecific inhibitor of the dihydrofolate reductase(DHFR) of bacteria and cancerous cells as well as normal cells. It forms an inactive ternary complex with DHFR and NADPH. Methotrexate (MTX) induces apoptosis.
S1282 Artemisinin Artemisinin is a sesquiterpene endoperoxide which is a potent antimalarial agent.
S1288 Camptothecin (CPT) Camptothecin (CPT) is a specific inhibitor of DNA topoisomerase I (Topo I) with IC50 of 0.68 μM in a cell-free assay. Camptothecin induces apoptosis in cancer cells via microRNA-125b-mediated mitochondrial pathways. Phase 2.
S1339 Galanthamine HBr Galanthamine is an AChE inhibitor with IC50 of 0.35 μM, exhibits 50-fold selectivity against butyryl-cholinesterase.
S1421 Staurosporine (STS) Staurosporine (STS) is a potent PKC inhibitor for PKCα, PKCγ and PKCη with IC50 of 2 nM, 5 nM and 4 nM, less potent to PKCδ (20 nM), PKCε (73 nM) and little active to PKCζ (1086 nM) in cell-free assays. Also shows inhibitory activities on other kinases, such as PKA, PKG, S6K, CaMKII, etc. Phase 3.
S1640 Albendazole Albendazole is a member of the benzimidazole compounds used as a drug indicated for the treatment of a variety of worm infestations.
S2130 Atropine sulfate monohydrate Atropine sulfate monohydrate is a competitive antagonist for the muscarinic acetylcholine receptor, used to decrease the production of saliva and secretions of the airway prior to surgery.
S2264 Artemether Artemether (SM-224, CGP 56696) is an antimalarial for the treatment of resistant strains of falciparum malaria.
S2265 Artesunate Artesunate is a part of the artemisinin group of agents with an IC50 of < 5 μM for small cell lung carcinoma cell line H69. It is a potential inhibitor of STAT-3 and exhibits selective cytotoxicity of cancer cells over normal cells in vitro; A potent inhibitor of EXP1.
S2304 Gramine Gramine (Donaxine) is a natural indole alkaloid isolated from giant reed, acts as an active adiponectin receptor (AdipoR) agonist, with IC50 of 3.2 µM and 4.2 µM for AdipoR2 and AdipoR1, respectively. Gramine is also a human and mouse β2-Adrenergic receptor (β2-AR) agonist.
S2320 Luteolin Luteolin (Luteoline, Luteolol, Digitoflavone) is a flavonoid found in Terminalia chebula, which is a non-selective phisphodiesterase PDE inhibitor for PDE1-5 with Ki of 15.0 μM, 6.4 μM, 13.9 μM, 11.1 μM and 9.5 μM, respectively.
S2350 Rutin Rutin (Rutoside), a flavonol glycoside found in many plants including buckwheat; tobacco; forsythia; hydrangea; viola, etc., which possesses healthy effects for human.
S2372 Xanthone Xanthone (Genicide) is an organic compound, which can be prepared by the heating of phenyl salicylate.
S2387 Lappaconite HBr Lappaconite Hydrobromide is a kind of alkaloid extracted from Aconitum sinomontanum Nakai and has anti-inflammatory effects.
S2417 20-Hydroxyecdysone 20-Hydroxyecdysone (Ecdysterone, 20E, B-ecdysone, Commisterone, Crustecdysone) is a naturally occurring ecdysteroid hormone which controls the ecdysis (moulting) and metamorphosis of arthropods.20-Hydroxyecdysone (Ecdysterone, 20E) inhibits caspase activity and induces autophagy via the 20E nuclear receptor complex, EcR-USP.
S2447 Ansamitocin p-3 (Maytansinol isobutyrate, NSC292222) Ansamitocin p-3 (Maytansinol isobutyrate, NSC292222, Antibiotic C 15003P3) is a potent inhibitor of tubulin polymerization with IC50 of 3.4 μM.
S3035 Daunorubicin HCl Daunorubicin HCl inhibits both DNA and RNA synthesis and inhibits DNA synthesis with Ki of 0.02 μM in a cell-free assay. Daunorubicin is a topoisomerase II inhibitor that induces apoptosis.
S3604 Triptolide Triptolide is a diterpene triepoxide, immunosuppresive agent extracted from the Chinese herb Tripterygium wilfordii. It functions as a NF-κB inhibitor with dual actions by disruption of p65/CBP interaction and by reduction of p65 protein. Triptolide (PG490) abrogates the transactivation function of heat shock transcription factor 1 (HSF1). Triptolide inhibits MDM2 and induces apoptosis through a p53-independent pathway.
S3628 BHQ BHQ (2,5-di-t-butyl-1,4-benzohydroquinone) is a potent and selective inhibitor of the sarco-endoplasmic reticulum Ca2+-ATPase (SERCA).
S3800 Lycorine hydrochloride Lycorine (Galanthidine, Amarylline, Narcissine, Licorine), a natural alkaloid extracted from the Amaryllidaceae plant family, has been reported to exhibit a wide range of physiological effects, including the potential effect against cancer. It is an HCV inhibitor with strong activity.
S3817 Harmine hydrochloride Harmine (Telepathine), a fluorescent harmala alkaloid belonging to the beta-carboline family of compounds, is a highly cell-permeant and competitive inhibitor of ATP binding to the kinase pocket of DYRK1A, with about 60-fold higher IC50 value for DYRK2. Harmine also inhibits monoamine oxidases (MAOs), PPARγ and cdc-like kinases (CLKs). Harmine inhibits 5-HT2A serotonin receptor with Ki of 397 nM.
S3854 Tetrahydropalmatine hydrochloride Tetrahydropalmatine (THP, Gindarine, 1-Tetrahydropalmitine) is an isoquinoline alkaloid found in several different plant species, mainly in the Corydalis genus (Yan Hu Suo), but also in other plants such as Stephania rotunda. It is a potent muscle relaxant. Tetrahydropalmatine hydrochloride acts through inhibition of amygdaloid release of dopamine to inhibit an epileptic attack in rats.
S3883 Protopine Protopine (Corydinine, Fumarine, Biflorine, Macleyine), an alkaloid present in different plants, has been shown to exhibit a number of activities, such as inhibition of calcium influx through both voltage and receptor-operated channels and inhibition of rabbit blood platelet aggregation. It also possesses anti-cholinergic and anti-histaminic as well as anti-bacterial activities.
S3892 Isopsoralen Isopsoralen (Angelicin), also known as angelicin, is a constituent of roots and leaves of angelica with anti-inflammatory activity and regulates LPS-induced inflammation via inhibiting MAPK/NF-κB pathways. It also shows antiviral activity against gammaherpesviruses.
S3941 Pinocembrin Pinocembrin (Dihydrochrysin, Galangin flavanone, 5,7-Dihydroxyflavanone) is a major flavonoid molecule incorporated as multifunctional in the pharmaceutical industry. Its vast range of pharmacological activities has been well researched including antimicrobial, anti-inflammatory, antioxidant, and anticancer activities.
S4181 Nicardipine HCl Nicardipine HCl (RS-69216,YC-93) is a dihydropyridine calcium-channel blocking agent used for the treatment of vascular disorders.
S4630 Diazoxide Diazoxide is a well-known small molecule that activates KATP channels in the smooth muscle of blood vessels and pancreatic beta-cells by increasing membrane permeability to potassium ions.
S4737 Psoralen Psoralen (Psoralene, Ficusin, Furocoumarin) is a naturally occurring furocoumarin that intercalates with DNA, inhibiting DNA synthesis and cell division.
S4859 TriacetonaMine TriacetonaMine (Tempidon, Tmpone, Odoratine, Vincubine), a member of the class of compounds known as piperidinones, is an extremely weak acidic compound found in green vegetables and tea.
S4908 SN-38 SN-38 (NK012) is an active metabolite of CPT-11, inhibits DNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks. SN-38 induces autophagy.
S5018 Mebhydrolin napadisylate Mebhydrolin Napadisylate (Diazoline, Diazolin, Incidal, Omeril) is classified as an antihistamine drug classes used to treat allergies.
S5153 Tetrahydroberberine Tetrahydroberberine (Canadine) is an isoquinoline alkaloid with micromolar affinity for dopamine D2 (antagonist, pKi = 6.08) and 5-HT1A (agonist, pKi = 5.38) receptors but moderate to no affinity for other relevant serotonin receptors.
S5478 Dantrolene sodium Dantrolene sodium(F 440) acts as a postsynaptic muscle relaxant by inhibiting Ca2+ ions release from sarcoplasmic reticulum stores by antagonizing ryanodine receptors.
S6773 DM1 (Mertansine) DM1 (Mertansine), an antibody-conjugatable maytansinoid, is a selective microtubule inhibitor that is developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery. Mertansine can be attached to a monoclonal antibody with a linker to create an antibody-drug conjugate (ADC).Solutions are unstable and should be fresh-prepared.
S7071 (+)-Bicuculline (+)-Bicuculline (d-Bicuculline) is a competitive antagonist of GABAA receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels.
S7721 MMAE (Monomethyl auristatin E) MMAE (Monomethyl auristatin E) is a synthetic antineoplastic agent. It is also a microtubule-disrupting agent .
S8146 Mitomycin C Mitomycin C (Ametycine) is an antineoplastic antibiotic by inhibiting DNA synthesis, used to treat different cancers. Mitomycin C induces apoptosis in a caspases-dependent and Fas/CD95-independent manner.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing.
S9018 Luteoloside Luteoloside (Cynaroside, Luteolin 7-β-D-Glucopyranoside) is a member of the flavonoids family that exhibits several bioactivities including anti-microbial and anti-cancer activities. It is an inhibitor of 3C Protease of Enterovirus 71 with an IC50 value of 0.36 mM.
S9065 Songorine Songorine, a ubiquitous alkaloid in the genus Aconitum, is a novel antagonist of the GABAA receptor in rat brain and has antiarrhythmic, antinociceptive, anti-inflammatory, regenerative and CNS-modulating properties.
S9223 Talatisamine Talatisamine, a delphinine type alkaloid extracted from Aconitum talassicum, is a newly identified K+ channel blocker with hypotensive and antiarrhythmic activities.
S9233 Imperialine Imperialine (Sipeimine, Kashmirine) is an alkaloid found in the bulbs of species of the genus Fritillaria.