Casein Kinase

抑制剂选择性比较

特异性亚型抑制剂

CK1 Selective

Casein Kinase产品

所有产品 Casein Kinase抑制剂(12)

目录号	产品描述	文献引用	实验数据
S1105	LY294002 LY294002 是首个合成的已知抑制PI3Kα/δ/β的小分子，在无细胞测定中IC50分别为 0.5 μM/0.57 μM/0.97 μM；在溶液中比在Wortmannin中稳定，也能够阻断自噬体的形成。它不仅能够结合class I PI3Ks和其他PI3K相关的激酶，还能够结合一些与PI3K家族无关的新型靶点。LY294002 可以抑制CK2，对应的IC50值为98 nM。LY294002 是一种非特异的 DNA-PKcs 抑制剂，并可激活自噬和凋亡。	Nat Commun, 2020, 27;11(1):2042 Autophagy, 2020, 16(6):1061-1076 EMBO Mol Med, 2020, 12(4):e11177	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)是有效的，选择性CK2(casein kinase 2)抑制剂，无细胞试验中IC50为1 nM,对 Flt3, Pim1 和 CDK1作用效果稍弱(细胞试验中没有活性)。Silmitasertib可诱导自噬并促进细胞凋亡。Phase 1/2。	Nat Commun, 2020, 8;11(1):2289 Fertil Steril, 2020, 113(5):1067-1079 e5 J Anim Sci Biotechnol, 2020, 8;11:31
S7085	IWP-2 IWP-2是一种Wnt信号和分泌抑制剂，无细胞试验中IC50为27 nM，选择性阻断Porcn介导的Wnt棕榈酰化，一般不影响Wnt/β-catenin，且对Wnt刺激的细胞反应没有影响。IWP-2可特定低抑制 CK1δ。	Biomaterials, 2020, 249:120015 Cell Stem Cell, 2019, 24(3):447-461.e8. Nat Neurosci, 2019, 22(3):484-491	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.
S6544^New	SR-3029 SR-3029是有效的、选择性casein kinase 1δ/1ε (CK1δ/ε)抑制剂，对CK1δ和CK1ε的IC50值分别为44 nM和260 nM。
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.	Nucleic Acids Res, 2019, 47(21):10977-10993 Toxicology, 2017, 389:74-84 J Neurochem, 2015, 133(6):828-43
S2249^New	PF 4800567 PF 4800567是casein kinase 1 epsilon (IC50=32 nM) 的新型有效抑制剂，其选择性是casein kinase 1 delta(IC50=711 nM)的20倍以上。
S6734^New	PF-670462 PF-670462是有效的、选择性CK1ε和CK1δ抑制剂，IC50分别为90 nM和13 nM。
S6578^New	Longdaysin Longdaysin是Casein Kinase抑制剂，对CKIδ, CKIα, ERK2和CDK7的IC50值分别为8.8 μM, 5.6 μM, 52 μM和29 μM。
S6536^New	TTP 22 TTP22是casein kinase 2 (CK2)抑制剂，IC50值为100 nM。它对CK2具有选择性，在浓度为10 μM时，对JNK3, ROCK1和MET没有抑制活性。
S7642	D 4476 D 4476 是一种有效的，选择性的，细胞渗透性 CK1 (casein kinase 1) 抑制剂，无细胞测定中对来自粟酒裂殖酵母的 CK1 和 CK1δ，IC50 分别为 200 nM 和 300 nM 。也是一种 ALK5 抑制剂，IC50 为 500 nM。	Nature, 2019, 10.1038/s41586-019-1607-3 Nature, 2019, 574(7777):268-272 Reprod Domest Anim, 2019, 54(8):1104-1112	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是一种新型的CK1抑制剂，IC261对CK1的IC50为16 μM，对Cdk5的IC50为4.5 mM。	Antiviral Res, 2019, 170:104572
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.

目录号	产品描述	文献引用	实验数据
S1105	LY294002 LY294002 是首个合成的已知抑制PI3Kα/δ/β的小分子，在无细胞测定中IC50分别为 0.5 μM/0.57 μM/0.97 μM；在溶液中比在Wortmannin中稳定，也能够阻断自噬体的形成。它不仅能够结合class I PI3Ks和其他PI3K相关的激酶，还能够结合一些与PI3K家族无关的新型靶点。LY294002 可以抑制CK2，对应的IC50值为98 nM。LY294002 是一种非特异的 DNA-PKcs 抑制剂，并可激活自噬和凋亡。	Nat Commun,2020, 27;11(1):2042 Autophagy,2020, 16(6):1061-1076 EMBO Mol Med,2020, 12(4):e11177	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)是有效的，选择性CK2(casein kinase 2)抑制剂，无细胞试验中IC50为1 nM,对 Flt3, Pim1 和 CDK1作用效果稍弱(细胞试验中没有活性)。Silmitasertib可诱导自噬并促进细胞凋亡。Phase 1/2。	Nat Commun,2020, 8;11(1):2289 Fertil Steril,2020, 113(5):1067-1079 e5 J Anim Sci Biotechnol,2020, 8;11:31
S7085	IWP-2 IWP-2是一种Wnt信号和分泌抑制剂，无细胞试验中IC50为27 nM，选择性阻断Porcn介导的Wnt棕榈酰化，一般不影响Wnt/β-catenin，且对Wnt刺激的细胞反应没有影响。IWP-2可特定低抑制 CK1δ。	Biomaterials,2020, 249:120015 Cell Stem Cell,2019, 24(3):447-461.e8. Nat Neurosci,2019, 22(3):484-491	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.
S6544^New	SR-3029 SR-3029是有效的、选择性casein kinase 1δ/1ε (CK1δ/ε)抑制剂，对CK1δ和CK1ε的IC50值分别为44 nM和260 nM。
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.	Nucleic Acids Res,2019, 47(21):10977-10993 Toxicology,2017, 389:74-84 J Neurochem,2015, 133(6):828-43
S2249^New	PF 4800567 PF 4800567是casein kinase 1 epsilon (IC50=32 nM) 的新型有效抑制剂，其选择性是casein kinase 1 delta(IC50=711 nM)的20倍以上。
S6734^New	PF-670462 PF-670462是有效的、选择性CK1ε和CK1δ抑制剂，IC50分别为90 nM和13 nM。
S6578^New	Longdaysin Longdaysin是Casein Kinase抑制剂，对CKIδ, CKIα, ERK2和CDK7的IC50值分别为8.8 μM, 5.6 μM, 52 μM和29 μM。
S6536^New	TTP 22 TTP22是casein kinase 2 (CK2)抑制剂，IC50值为100 nM。它对CK2具有选择性，在浓度为10 μM时，对JNK3, ROCK1和MET没有抑制活性。
S7642	D 4476 D 4476 是一种有效的，选择性的，细胞渗透性 CK1 (casein kinase 1) 抑制剂，无细胞测定中对来自粟酒裂殖酵母的 CK1 和 CK1δ，IC50 分别为 200 nM 和 300 nM 。也是一种 ALK5 抑制剂，IC50 为 500 nM。	Nature,2019, 10.1038/s41586-019-1607-3 Nature,2019, 574(7777):268-272 Reprod Domest Anim,2019, 54(8):1104-1112	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是一种新型的CK1抑制剂，IC261对CK1的IC50为16 μM，对Cdk5的IC50为4.5 mM。	Antiviral Res,2019, 170:104572
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.