Casein Kinase

Inhibitory Selectivity

Catalog No.	Inhibitor Name	CK1	CK2	Other
A11060	Silmitasertib		***
A13949	D 4476	**		ALK5
A16235	SR-3029	**
A15764	IC 261	*
A15257	TBB		*
A15069	DMAT		**
A16236	TA-01	***		p38α
A14101	TTP-22		**	JNK3, ROCK1, and MET
A13574	LH 846	**
A11781	PF 670462	***
A13977	TMCB		**	ERK8

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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CX-4945 (Silmitasertib)

Catalog No. A11060
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CK2 抑制剂

CX-4945 (Silmitasertib)是有效的，选择性CK2(casein kinase 2)抑制剂，可抑制人脐静脉内皮细胞迁移，管形成，并阻止癌细胞中CK2依赖性缺氧诱导的因子1α（HIF-1α）转录。了解更多

Product Citations (13)

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- Xixi Zhao, .et al. Phosphorylation and Stabilization of PD-L1 by CK2 Suppresses Dendritic Cell Function, Cancer Res, 2022, Jun 6;82(11):2185-2195 PMID: 35385574
- Janeen H. Trembley, .et al. CX-4945 and siRNA-Mediated Knockdown of CK2 Improves Cisplatin Response in HPV(+) and HPV(-) HNSCC Cell Lines, Biomedicines, 2021, May; 9(5): 571 PMID: 34070147
- Tianzhi Huang, .et al. PRMT6 methylation of RCC1 regulates mitosis, tumorigenicity, and radiation response of glioblastoma stem cells, Mol Cell, 2021, Mar 18;81(6):1276-1291 PMID: 33539787
- M Afzal, .et al. Protein kinase CK2 impact on intracellular calcium homeostasis in prostate cancer, Molecular and Cellular Biochemistry, 2020, 470, pages131-143
- Zaman MS, .et al. Protein kinase CK2 is involved in zinc homeostasis in breast and prostate cancer cells, Biometals, 2019, Oct 3 PMID: 31583500
- Fukumoto Y, .et al. Human Rad17?C-terminal tail is phosphorylated by concerted action of CK1δ/ε and CK2 to promote interaction with the 9-1-1 complex, Biochem Biophys Res Commun, 2019, Sep 17;517(2):310-316 PMID: 31353086
- Fukumoto Y, .et al. Casein kinase 2 promotes interaction between Rad17 and the 9-1-1 complex through constitutive phosphorylation of the C-terminal tail of human Rad17, Biochem Biophys Res Commun, 2018, Oct 2;504(2):380-386 PMID: 29902452
- ST Ribeiro, .et al. Casein kinase 2 controls the survival of normal thymic and leukemic γδ T cells via promotion of AKT signaling, Leukemia, 2017, Jul; 31(7): 1603-1610 PMID: 27899804
- Valentina Gandin, .et al. mTORC1 and CK2 coordinate ternary and eIF4F complex assembly, Nat Commun, 2016, 7: 11127 PMID: 27040916
- Ampofo E, .et al. Protein Kinase CK2 Regulates Leukocyte-Endothelial Cell Interactions during Ischemia and Reperfusion in Striated Skin Muscle, Eur Surg Res, 2016, 57(1-2):111-24 PMID: 27287005
- Emmanuel Ampofo, .et al. Role of protein kinase CK2 in the dynamic interaction of platelets, leukocytes and endothelial cells during thrombus formation., Thromb Res., 2015, Nov;136(5):996-1006 PMID: 26381437
- Emmanuel Ampofo, .et al. Inhibition of protein kinase CK2 suppresses tumor necrosis factor (TNF)-α-induced leukocyte-endothelial cell interaction., Biochim Biophys Acta., 2015, Oct;1852(10 Pt A):2123-36 PMID: 26189586
- A. Margarida Gomes, .et al. Adult B-cell acute lymphoblastic leukemia cells display decreased PTEN activity and constitutive hyperactivation of PI3K/Akt pathway despite high PTEN protein levels, Haematologica, 2014, 99(6): 1062-1068 PMID: 24561792
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LH 846

Catalog No. A13574
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CK1 抑制剂

LH 846是酪蛋白激酶（CK）1δ的选择性抑制剂（CK1δ，ε和α的IC50值为290 nM，1.3μM和2.5μM）。了解更多

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D4476

Catalog No. A13949
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CK1 抑制剂

D4476是酪蛋白激酶1的细胞渗透抑制剂。了解更多

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TTP-22

Catalog No. A14101
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CK2 抑制剂

TTP 22是一种高亲和力的酪蛋白激酶2（CK2）抑制剂（IC50 = 0.1uM，Ki = 40nM）。另外，TTP 22显示出对CK2的选择性超过JNK3，ROCK1和MET（显示出的抑制作用大于10 uM）。TTP 22是高度保守的丝氨酸/苏氨酸蛋白激酶，也参与细胞增殖，细胞分化和凋亡。了解更多

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DMAT

Catalog No. A15069
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CK2 抑制剂

DMAT是一种有效的特异性CK2抑制剂，IC50为0.13 uM。了解更多

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TBB

Catalog No. A15257
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CK2 抑制剂

TBB是酪蛋白激酶2（CK2）的高选择性，ATP/GTP竞争性抑制剂，对大鼠肝脏和人重组CK2的IC50分别为0.9和1.6 uM。了解更多

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IC 261

Catalog No. A15764
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CK1δ and CK1ε 抑制剂

IC 261是CK1δ和CK1ε抑制剂。IC261对CK1的IC50为16 μM，对Cdk5的IC50为4.5 mM。了解更多

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CX-4945 sodium salt

Catalog No. A16234
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CK2 抑制剂

CX-4945 sodium salt是一种有效的选择性ATP竞争性小分子蛋白激酶CK2抑制剂，对重组人CK2α的Ki和IC50分别为0.38和1 nM。了解更多

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SR-3029

Catalog No. A16235
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CK1δ/CK1ε 抑制剂

SR-3029是一种有效且高度特异性的CK1δ/CK1ε抑制剂，IC50为97 nM。了解更多

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TA-01

Catalog No. A16236
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CK 抑制剂

TA-01有效抑制CK1ε，CK1δ和p38α（IC50值分别为6.4、6.8和6.7 nM）。了解更多

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PF 670462

Catalog No. A11781
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Casein kinase 抑制剂

PF-670462是有效的、选择性CK1ε和CK1δ抑制剂，IC50分别为7.7和14 nM，其选择性是其他42种常见激酶的30倍以上。了解更多

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A-3 Hydrochloride

Catalog No. A13584
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PKA, PKG, Casein Kinase I and II 抑制剂

A-3 Hydrochloride是PKA（cAMP依赖性蛋白激酶，Ki =4.3μM）和cGMP依赖性蛋白激酶，Ki =3.8μM，PKC（蛋白激酶C，Ki =47μM），酪蛋白激酶I和II的抑制剂，和MLCK（肌球蛋白轻链激酶）（Ki =7.4μM）。了解更多

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TMCB

Catalog No. A13977
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CK2/ERK8 抑制剂

MCB抑制酪蛋白激酶2（CK2）和细胞外信号调节激酶8（ERK8/MAPK15）（CK2和ERK8的IC50 = 0.50 uM）。了解更多

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