カゼインキナーゼ

阻害剤の選択性比較

カタログ番号	製品カタログ	溶解度(25°C)
カタログ番号	製品カタログ	水	DMSO	アルコール
S1105	LY294002	<1 mg/mL	36 mg/mL	'21 mg/mL
S2248	Silmitasertib (CX-4945)	<1 mg/mL	16 mg/mL	<1 mg/mL
S2805	LY364947	<1 mg/mL	1 mg/mL	<1 mg/mL
S7085	IWP-2	<1 mg/mL	4 mg/mL	<1 mg/mL
S0707	Silmitasertib (CX-4945) sodium salt	74 mg/mL	74 mg/mL	'''<1 mg/mL
E2826	Hematein	<1 mg/mL	60 mg/mL	2 mg/mL
S9850	(E/Z)-GO289	<1 mg/mL	21 mg/mL	<1 mg/mL
S6544	SR-3029	<1 mg/mL	47 mg/mL	<1 mg/mL
S5265	TBB	-1 mg/mL	86 mg/mL	-1 mg/mL
S6536	TTP 22	<1 mg/mL	66 mg/mL	8 mg/mL
S6578	Longdaysin	<1 mg/mL	67 mg/mL	67 mg/mL
S2249	PF 4800567	<1 mg/mL	72 mg/mL	<1 mg/mL
S0350	CK1-IN-1	<1 mg/mL	77 mg/mL	'''<1 mg/mL
S0995	BioE-1115	<1 mg/mL	68 mg/mL	'''<1 mg/mL
S6734	PF-670462	82 mg/mL	82 mg/mL	28 mg/mL
S7642	D 4476	<1 mg/mL	79 mg/mL	<1 mg/mL
S8237	IC261	<1 mg/mL	62 mg/mL	'<1 mg/mL
S0186	TA-01	<1 mg/mL	20 mg/mL	'''5 mg/mL
S5516	Ellagic Acid hydrate	-1 mg/mL	2 mg/mL	-1 mg/mL
S3143	Pyruvic acid			' mg/mL

亜型選択性的な製品

Casein Kinase製品

All (20) Casein Kinase阻害剤(19) Casein Kinase活性剤(1)

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S1105	LY294002 LY294002 (SF 1101, NSC 697286) is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation. It not only binds to class I PI3Ks and other PI3K-related kinases, but also to novel targets seemingly unrelated to the PI3K family. LY294002 also inhibits CK2 with IC50 of 98 nM. LY294002 is a non-specific DNA-PKcs inhibitor and activates autophagy and apoptosis.	Immunity, 2022, 55(1):159-173.e9 Adv Sci (Weinh), 2022, 10.1002/advs.202104055 Cancer Res, 2022, canres.2292.2021	Inhibition of PI3K, ERK and mTOR prevents the activation of S6K1 and S6 induced by suppression of PKD1 activity. A549 cells were incubated in the absence (-) or presence of either 5 uM Kb or 5 uM Kb and 20 uM LY294002 or 5 uM Kb and 10 uM BKM120 (as indicated) for 1 h prior to stimulation of cells with 50 nM PMA for 30 min and 1 h.
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.	Mol Cell, 2022, S1097-2765(22)00394-X EMBO Rep, 2022, e54801 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.	Cell Rep, 2022, 38(5):110329 Front Immunol, 2022, 13:853894 Aging Dis, 2022, 13(1):313-328	The cytoplasmic and nuclear proteins were separated and the protein expression levels were determined by performing western blotting. LY364947 (1 uM), which is a potent ATP-competitive inhibitor of TGF-βRI, was used as the positive control. GAPDH and PARP were used as cytosolic and nuclear markers, respectively.
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, 2022, 29(4):545-558.e13 Adv Sci (Weinh), 2022, e2104299 Nat Commun, 2022, 13(1):2387	KIF3A knockdown promotes both ligand secretion and intracellular signalling of the Wnt/β-catenin pathway in NSCLC cell lines. (c,d) SuperTOPFlash reporter assay to examine the effect of KIF3A knockdown on signalling pathway activation by autocrine or exogenous WNTs in A549 and SW900 cell lines. A549 and SW900 cells were incubated with DMSO or IWP-2 (30 μ M) for 48 h, and then treated with BSA or WNT3A (100 ng/ml) for additional 24 h. Luciferase reporter activity was calculated by dividing TOP/RL ratio by FOP/RL ratio (n = 3; error bars indicate SEM; p-value was determined by one-way ANOVA). P < 0.05; *P < 0.01.
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'.	Proc Natl Acad Sci U S A, 2022, 119(12):e2114336119 Cell Mol Gastroenterol Hepatol, 2022, S2352-345X(22)00003-0 Int J Mol Sci, 2022, 23(8)4409
E2826^新	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.
S9850^新	(E/Z)-GO289 (E/Z)-GO289 potently and selectively inhibits casein kinase 2 (CK2) at an IC50 of 7 nM in vitro kinase assay.
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.
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.	J Proteome Res, 2022, 21(4):1073-1082 bioRxiv, 2021, 10.1101/2021.03.17.435124 Commun Biol, 2021, 4(1):336
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.
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
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.
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.
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.	Nat Commun, 2022, 13(1):3034 J Cell Biol, 2022, 221(1)e202103033 Adv Sci (Weinh), 2021, e2004846	Western blot of signaling effects. 48 hrs after transfection cells were serum‐starved for 12 h before stimulation with Wnt5a for 30 min or 120 min (200 ng/ml) in the presence or absence of casein kinase inhibitor D4476 (100 μM).
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 Metab, 2022, S1550-4131(21)00542-8 Sci Rep, 2022, 12(1):7 EMBO Rep, 2021, e51503
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.
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.
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.

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S1105	LY294002 LY294002 (SF 1101, NSC 697286) is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation. It not only binds to class I PI3Ks and other PI3K-related kinases, but also to novel targets seemingly unrelated to the PI3K family. LY294002 also inhibits CK2 with IC50 of 98 nM. LY294002 is a non-specific DNA-PKcs inhibitor and activates autophagy and apoptosis.	Immunity, 2022, 55(1):159-173.e9 Adv Sci (Weinh), 2022, 10.1002/advs.202104055 Cancer Res, 2022, canres.2292.2021	Inhibition of PI3K, ERK and mTOR prevents the activation of S6K1 and S6 induced by suppression of PKD1 activity. A549 cells were incubated in the absence (-) or presence of either 5 uM Kb or 5 uM Kb and 20 uM LY294002 or 5 uM Kb and 10 uM BKM120 (as indicated) for 1 h prior to stimulation of cells with 50 nM PMA for 30 min and 1 h.
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.	Mol Cell, 2022, S1097-2765(22)00394-X EMBO Rep, 2022, e54801 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.	Cell Rep, 2022, 38(5):110329 Front Immunol, 2022, 13:853894 Aging Dis, 2022, 13(1):313-328	The cytoplasmic and nuclear proteins were separated and the protein expression levels were determined by performing western blotting. LY364947 (1 uM), which is a potent ATP-competitive inhibitor of TGF-βRI, was used as the positive control. GAPDH and PARP were used as cytosolic and nuclear markers, respectively.
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, 2022, 29(4):545-558.e13 Adv Sci (Weinh), 2022, e2104299 Nat Commun, 2022, 13(1):2387	KIF3A knockdown promotes both ligand secretion and intracellular signalling of the Wnt/β-catenin pathway in NSCLC cell lines. (c,d) SuperTOPFlash reporter assay to examine the effect of KIF3A knockdown on signalling pathway activation by autocrine or exogenous WNTs in A549 and SW900 cell lines. A549 and SW900 cells were incubated with DMSO or IWP-2 (30 μ M) for 48 h, and then treated with BSA or WNT3A (100 ng/ml) for additional 24 h. Luciferase reporter activity was calculated by dividing TOP/RL ratio by FOP/RL ratio (n = 3; error bars indicate SEM; p-value was determined by one-way ANOVA). P < 0.05; *P < 0.01.
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'.	Proc Natl Acad Sci U S A, 2022, 119(12):e2114336119 Cell Mol Gastroenterol Hepatol, 2022, S2352-345X(22)00003-0 Int J Mol Sci, 2022, 23(8)4409
E2826^新	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.
S9850^新	(E/Z)-GO289 (E/Z)-GO289 potently and selectively inhibits casein kinase 2 (CK2) at an IC50 of 7 nM in vitro kinase assay.
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.
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.	J Proteome Res, 2022, 21(4):1073-1082 bioRxiv, 2021, 10.1101/2021.03.17.435124 Commun Biol, 2021, 4(1):336
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.
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
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.
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.
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.	Nat Commun, 2022, 13(1):3034 J Cell Biol, 2022, 221(1)e202103033 Adv Sci (Weinh), 2021, e2004846	Western blot of signaling effects. 48 hrs after transfection cells were serum‐starved for 12 h before stimulation with Wnt5a for 30 min or 120 min (200 ng/ml) in the presence or absence of casein kinase inhibitor D4476 (100 μM).
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 Metab, 2022, S1550-4131(21)00542-8 Sci Rep, 2022, 12(1):7 EMBO Rep, 2021, e51503
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.
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.

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
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.

製品コード

製品説明

文献中Selleckの製品使用例

お客様のフィードバック

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.

研究分野別

製品類型

カゼインキナーゼ

阻害剤の選択性比較

亜型選択性的な製品

Casein Kinase製品