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CCT251545

CCT251545 是一种有效的、具有口服活性的WNT 抑制剂，在 7dF3 细胞中对 WNT 抑制作用的IC50值为 5 nM。它是选择性化学探针，用于探索 CDK8 和 CDK19 在人类疾病中的作用。

CAS号

1661839-45-7

分子式

C23H24ClN5O

主要靶点

Wnt/beta-catenin

仅限科研使用

Cat No : CM06891

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Synonyms

验证数据展示

  • CAS No.: 1661839-45-7

    CCT251545
    CAS#: 1661839-45-7

产品信息

CCT251545 is an potent and oral-bioavailable WNT signaling inhibitor(IC50 of 5 nM in 7dF3 cells).

CAS号 1661839-45-7
分子式 C23H24ClN5O
主要靶点 Wnt/beta-catenin
主要通路 细胞骨架|干细胞
分子量 421.92
纯度 99.73%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

靶点活性

WNT(7dF3 cells):5 nM

体内活性

In vivo, CCT251545 with WNT-dependent tumors activity[1].

体外活性

CCT251545, a small-molecule inhibitor of the WNT pathway discovered through cell-based screening, is a potent and selective chemical probe for the human Mediator complex-associated protein kinases CDK8 and CDK19 with >100-fold selectivity over 291 other kinases.?X-ray crystallography demonstrates a type 1 binding mode involving insertion of the CDK8 C terminus into the ligand binding site.?In contrast to type II inhibitors of CDK8 and CDK19, CCT251545 displays potent cell-based activity.?We show that CCT251545 and close analogs alter WNT pathway-regulated gene expression and other on-target effects of modulating CDK8 and CDK19, including expression of genes regulated by STAT1.?Consistent with this, we find that phosphorylation of STAT1(SER727) is a biomarker of CDK8 kinase activity in vitro and in vivo[1].

溶解度

DMSO:45mg/ml (106.66 Mm)

参考文献

1.Dale T, et al. A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease. Nat Chem Biol. 2015 Dec;11(12):973-980.
2.Mallinger A, et al. Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. J Med Chem. 2015 Feb 26;58(4):1717-35.

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