Casein Kinase

亜型選択性的な製品

CK1 CK2

Casein Kinase製品

All (24)
Casein Kinase阻害剤 (22)
Casein Kinase活性剤(1)
Casein Kinase拮抗剤(1)
新製品

製品コード	製品名称	製品説明	文献中Selleckの製品使用例
S1105	LY294002	LY294002 (SF 1101, NSC 697286) は人工的に合成した分子としては初めての PI3Kα/δ/β 阻害剤であり、IC50 はそれぞれ 0.5 μM/ 0.57 μM/ 0.97 μM です。溶液中でウォルトマンニン (wortmannin) よりも安定しています。クラス I PI3K および PI3K 関連キナーゼだけでなく、一見 PI3K ファミリーには無関係にある新規のターゲットにも結合します。LY294002 は CK2 阻害剤でもあり、IC50 は 98 nM です。また LY294002 はオートファゴソーム (autophagosome) の形成をブロックする一方で、DNA-PKｃｓを非特異的に阻害することによりオートファジー (autophagy) を活性化し、アポトーシス (apoptosis) を誘導します。	Signal Transduct Target Ther, 2024, 9(1):109 Signal Transduct Target Ther, 2024, 9(1):109 Nat Genet, 2024, 10.1038/s41588-024-01891-8
S2248	Silmitasertib (CX-4945)	Silmitasertib (CX-4945) is a potent and selective inhibitor of CK2 (casein kinase 2) with IC50 of 1 nM in a cell-free assay, less potent to Flt3, Pim1 and CDK1 (inactive in cell-based assay). Silmitasertib induces autophagy and promotes apoptosis. Phase 1/2.	Diabetologia, 2024, 10.1007/s00125-024-06128-1 Biomed Pharmacother, 2024, 180:117499 Front Immunol, 2024, 15:1393485
S7085	IWP-2	IWP-2 is an inhibitor of Wnt processing and secretion with IC50 of 27 nM in a cell-free assay, selective blockage of Porcn-mediated Wnt palmitoylation, does not affect Wnt/β-catenin in general and displays no effect against Wnt-stimulated cellular responses. IWP-2 specifically inhibits CK1δ.	Cell Stem Cell, 2024, S1934-5909(24)00256-X Nat Commun, 2024, 15(1):1351 Nat Commun, 2024, 15(1):167
S0707	Silmitasertib (CX-4945) sodium salt	Silmitasertib (CX-4945) sodium salt is a potent, orally bioavailable and selective inhibitor of casein kinase 2 (CK2) with IC50 of 1 nM against CK2α and CK2α'.	Diabetologia, 2024, 10.1007/s00125-024-06128-1 J Diabetes Investig, 2024, 15(6):684-692 Proc Natl Acad Sci U S A, 2022, 119(12):e2114336119
S2805	LY364947	LY364947 (HTS 466284) is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM in a cell-free assay, shows 7-fold selectivity over TGFβR-II.	Adv Sci (Weinh), 2024, 11(4):e2304987 Cell Rep Med, 2024, 5(2):101416 Cell Commun Signal, 2024, 22(1):242
S7642	D 4476	D 4476 is a potent, selective, and cell-permeant CK1 (casein kinase 1) inhibitor with IC50 of 200 nM and 300 nM in a cell-free assay for CK1 from Schizosaccharomyces pombe and CK1δ, respectively. Also acts as an ALK5 inhibitor with IC50 of 500 nM.	Cell Rep Med, 2023, 4(4):101015 Cell Rep, 2023, 42(9):113035 Nat Commun, 2022, 13(1):3034
S5265	TBB	TBB (4,5,6,7-tetrabromobenzotriazole) is a selective cell-permeable CK2 inhibitor with IC50 values of 0.9 and 1.6 μM for rat liver and human recombinant CK2 respectively.	Cell Rep, 2024, 43(2):113779 Mol Cell, 2023, 83(15):2792-2809.e9 Cancers (Basel), 2022, 15(1)200
S8237	IC261	IC261 (SU-5607) is a novel inhibitor of CK1. The IC50 of IC261 for CK1 was 16 μM and for Cdk5 is 4.5 mM.	Cell Rep, 2023, 42(7):112812 Cell Metab, 2022, S1550-4131(21)00542-8 Sci Rep, 2022, 12(1):7
S9850	(E/Z)-GO289	(E/Z)-GO289 potently and selectively inhibits casein kinase 2 (CK2) at an IC50 of 7 nM in vitro kinase assay.	Autophagy, 2023, 10.1080/15548627.2023.2281128
S6536	TTP 22	TTP22 is a casein kinase 2 (CK2) inhibitor with an IC50 value of 100 nM. It displays selectivity for CK2 over JNK3, ROCK1, and MET with no inhibitory effects towards these kinases at 10 μM.	J Cell Biol, 2022, 221-11e202202100
S6578	Longdaysin	Longdaysin is a Casein Kinase inhibitor with IC50 values of 8.8 μM, 5.6 μM, 52 μM and 29 μM for CKIδ, CKIα, ERK2 and CDK7.	Nat Commun, 2021, 12(1):7003
S2249	PF 4800567	PF 4800567 is a novel and potent inhibitor of casein kinase 1 epsilon (IC50=32 nM) with greater than 20-fold selectivity over casein kinase 1 delta(IC50=711 nM).	Blood Adv, 2020, 4(13):3072-3084
S5516	Ellagic Acid hydrate	Ellagic acid is a potent inhibitor of protein kinase CK2 with IC50s of 0.04, 2.9 and 3.5 μM for CK2, Lyn and PKA respectively. It shows potent antioxidant, anti-mutagenic and antidepressant properties.	J Cell Biol, 2022, 221-11e202202100
S9331	7-Hydroxy-4-methyl-8-nitrocoumarin	7-Hydroxy-4-methyl-8-nitrocoumarin is a chemical.
S6544	SR-3029	SR-3029 is a potent and selective casein kinase 1δ/1ε (CK1δ/ε) inhibitor with IC50 values of 44 and 260 nM for CK1δ and CK1ε, respectively.
S3143	Pyruvic acid	Pyruvic acid (Acetylformic acid) is an important organic chemical intermediate that plays a role in cardiomyocyte pathophysiology and therapy. Pyruvic acid markedly increases the level of lactate dehydrogenase (LDH) and creatine kinase (CK) and reduces the level of Ca²⁺Mg²⁺-ATPase and Na⁺K⁺-ATPase.
S0350	CK1-IN-1	CK1-IN-1 (PUN51207, Compound 1C) is an inhibitor of casein kinase 1 (CK1) with IC50 of 15 nM, 16 nM and 73 nM for CK1δ, CK1ε and p38α MAPK, respectively.
S0995	BioE-1115	BioE-1115 is a highly selective and potent dual inhibitor of PAS kinase (PASK) and casein kinase 2α (CK2α) with IC50 of ~4 nM and ~10 μM, respectively.
E2914	5,6-Dichlorobenzimidazole 1-beta-D-ribofuranoside	5,6-Dichlorobenzimidazole riboside(DRB) is a nucleoside analog that inhibits several carboxyl-terminal domain (CTD) kinases including casein kinase II and CDKs. It trigger p53-dependent apoptosis of human colon adenocarcinoma cells without inducing genotoxic stress to healthy cells.
S6734	PF-670462	PF-670462 is a potent and selective inhibitor of CK1ε and CK1δ with IC50 value of 90 nM and 13 nM, respectively.	J Biomed Sci, 2024, 31(1):72
E2659	DMAT	DMAT is a high affinity and selective casein kinase-2 (CK2) inhibitor with IC50 of ~0.14 μM and Ki of ~40 nM.
E2506	A-3 hydrochloride	A-3 hydrochloride, a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases, againsts cAMP-dependent protein kinase (PKA) (Ki=4.3 µM), casein kinase II (CK2) (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM), also inhibits Protein Kinase C (PKC) and casein kinase I (CK1) with Ki values of 47 µM and 80 µM, respectively.
E2826	Hematein	Hematein inhibits casein kinase II activity in a selective, dose-dependent and ATP non-competitive manner in vitro, with IC50 of 0.55 μM in the presence of 10 μM ATP.
S0186	TA-01	TA-01 is a potent inhibitor of CK1δ/ε and p38 MAPK with IC50 of 6.4 nM, 6.8 nM and 6.7 nM for CK1ε, CK1δ and p38 MAPK, respectively.
S1105	LY294002	LY294002 (SF 1101, NSC 697286) は人工的に合成した分子としては初めての PI3Kα/δ/β 阻害剤であり、IC50 はそれぞれ 0.5 μM/ 0.57 μM/ 0.97 μM です。溶液中でウォルトマンニン (wortmannin) よりも安定しています。クラス I PI3K および PI3K 関連キナーゼだけでなく、一見 PI3K ファミリーには無関係にある新規のターゲットにも結合します。LY294002 は CK2 阻害剤でもあり、IC50 は 98 nM です。また LY294002 はオートファゴソーム (autophagosome) の形成をブロックする一方で、DNA-PKｃｓを非特異的に阻害することによりオートファジー (autophagy) を活性化し、アポトーシス (apoptosis) を誘導します。	Signal Transduct Target Ther, 2024, 9(1):109 Signal Transduct Target Ther, 2024, 9(1):109 Nat Genet, 2024, 10.1038/s41588-024-01891-8
S2248	Silmitasertib (CX-4945)	Silmitasertib (CX-4945) is a potent and selective inhibitor of CK2 (casein kinase 2) with IC50 of 1 nM in a cell-free assay, less potent to Flt3, Pim1 and CDK1 (inactive in cell-based assay). Silmitasertib induces autophagy and promotes apoptosis. Phase 1/2.	Diabetologia, 2024, 10.1007/s00125-024-06128-1 Biomed Pharmacother, 2024, 180:117499 Front Immunol, 2024, 15:1393485
S7085	IWP-2	IWP-2 is an inhibitor of Wnt processing and secretion with IC50 of 27 nM in a cell-free assay, selective blockage of Porcn-mediated Wnt palmitoylation, does not affect Wnt/β-catenin in general and displays no effect against Wnt-stimulated cellular responses. IWP-2 specifically inhibits CK1δ.	Cell Stem Cell, 2024, S1934-5909(24)00256-X Nat Commun, 2024, 15(1):1351 Nat Commun, 2024, 15(1):167
S0707	Silmitasertib (CX-4945) sodium salt	Silmitasertib (CX-4945) sodium salt is a potent, orally bioavailable and selective inhibitor of casein kinase 2 (CK2) with IC50 of 1 nM against CK2α and CK2α'.	Diabetologia, 2024, 10.1007/s00125-024-06128-1 J Diabetes Investig, 2024, 15(6):684-692 Proc Natl Acad Sci U S A, 2022, 119(12):e2114336119
S2805	LY364947	LY364947 (HTS 466284) is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM in a cell-free assay, shows 7-fold selectivity over TGFβR-II.	Adv Sci (Weinh), 2024, 11(4):e2304987 Cell Rep Med, 2024, 5(2):101416 Cell Commun Signal, 2024, 22(1):242
S7642	D 4476	D 4476 is a potent, selective, and cell-permeant CK1 (casein kinase 1) inhibitor with IC50 of 200 nM and 300 nM in a cell-free assay for CK1 from Schizosaccharomyces pombe and CK1δ, respectively. Also acts as an ALK5 inhibitor with IC50 of 500 nM.	Cell Rep Med, 2023, 4(4):101015 Cell Rep, 2023, 42(9):113035 Nat Commun, 2022, 13(1):3034
S5265	TBB	TBB (4,5,6,7-tetrabromobenzotriazole) is a selective cell-permeable CK2 inhibitor with IC50 values of 0.9 and 1.6 μM for rat liver and human recombinant CK2 respectively.	Cell Rep, 2024, 43(2):113779 Mol Cell, 2023, 83(15):2792-2809.e9 Cancers (Basel), 2022, 15(1)200
S8237	IC261	IC261 (SU-5607) is a novel inhibitor of CK1. The IC50 of IC261 for CK1 was 16 μM and for Cdk5 is 4.5 mM.	Cell Rep, 2023, 42(7):112812 Cell Metab, 2022, S1550-4131(21)00542-8 Sci Rep, 2022, 12(1):7
S9850	(E/Z)-GO289	(E/Z)-GO289 potently and selectively inhibits casein kinase 2 (CK2) at an IC50 of 7 nM in vitro kinase assay.	Autophagy, 2023, 10.1080/15548627.2023.2281128
S6536	TTP 22	TTP22 is a casein kinase 2 (CK2) inhibitor with an IC50 value of 100 nM. It displays selectivity for CK2 over JNK3, ROCK1, and MET with no inhibitory effects towards these kinases at 10 μM.	J Cell Biol, 2022, 221-11e202202100
S6578	Longdaysin	Longdaysin is a Casein Kinase inhibitor with IC50 values of 8.8 μM, 5.6 μM, 52 μM and 29 μM for CKIδ, CKIα, ERK2 and CDK7.	Nat Commun, 2021, 12(1):7003
S2249	PF 4800567	PF 4800567 is a novel and potent inhibitor of casein kinase 1 epsilon (IC50=32 nM) with greater than 20-fold selectivity over casein kinase 1 delta(IC50=711 nM).	Blood Adv, 2020, 4(13):3072-3084
S5516	Ellagic Acid hydrate	Ellagic acid is a potent inhibitor of protein kinase CK2 with IC50s of 0.04, 2.9 and 3.5 μM for CK2, Lyn and PKA respectively. It shows potent antioxidant, anti-mutagenic and antidepressant properties.	J Cell Biol, 2022, 221-11e202202100
S9331	7-Hydroxy-4-methyl-8-nitrocoumarin	7-Hydroxy-4-methyl-8-nitrocoumarin is a chemical.
S6544	SR-3029	SR-3029 is a potent and selective casein kinase 1δ/1ε (CK1δ/ε) inhibitor with IC50 values of 44 and 260 nM for CK1δ and CK1ε, respectively.
S0350	CK1-IN-1	CK1-IN-1 (PUN51207, Compound 1C) is an inhibitor of casein kinase 1 (CK1) with IC50 of 15 nM, 16 nM and 73 nM for CK1δ, CK1ε and p38α MAPK, respectively.
S0995	BioE-1115	BioE-1115 is a highly selective and potent dual inhibitor of PAS kinase (PASK) and casein kinase 2α (CK2α) with IC50 of ~4 nM and ~10 μM, respectively.
E2914	5,6-Dichlorobenzimidazole 1-beta-D-ribofuranoside	5,6-Dichlorobenzimidazole riboside(DRB) is a nucleoside analog that inhibits several carboxyl-terminal domain (CTD) kinases including casein kinase II and CDKs. It trigger p53-dependent apoptosis of human colon adenocarcinoma cells without inducing genotoxic stress to healthy cells.
S6734	PF-670462	PF-670462 is a potent and selective inhibitor of CK1ε and CK1δ with IC50 value of 90 nM and 13 nM, respectively.	J Biomed Sci, 2024, 31(1):72
E2659	DMAT	DMAT is a high affinity and selective casein kinase-2 (CK2) inhibitor with IC50 of ~0.14 μM and Ki of ~40 nM.
E2826	Hematein	Hematein inhibits casein kinase II activity in a selective, dose-dependent and ATP non-competitive manner in vitro, with IC50 of 0.55 μM in the presence of 10 μM ATP.
S0186	TA-01	TA-01 is a potent inhibitor of CK1δ/ε and p38 MAPK with IC50 of 6.4 nM, 6.8 nM and 6.7 nM for CK1ε, CK1δ and p38 MAPK, respectively.
S3143	Pyruvic acid	Pyruvic acid (Acetylformic acid) is an important organic chemical intermediate that plays a role in cardiomyocyte pathophysiology and therapy. Pyruvic acid markedly increases the level of lactate dehydrogenase (LDH) and creatine kinase (CK) and reduces the level of Ca²⁺Mg²⁺-ATPase and Na⁺K⁺-ATPase.
E2506	A-3 hydrochloride	A-3 hydrochloride, a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases, againsts cAMP-dependent protein kinase (PKA) (Ki=4.3 µM), casein kinase II (CK2) (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM), also inhibits Protein Kinase C (PKC) and casein kinase I (CK1) with Ki values of 47 µM and 80 µM, respectively.

Casein Kinase阻害剤の選択性比較