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CCT251545
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CCT251545图片
CAS NO:1661839-45-7
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
500 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
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。

产品描述

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

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].

体内活性

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

Cas No.

1661839-45-7

分子式

C23H24ClN5O

分子量

421.92

储存和溶解度

DMSO:45mg/ml (106.66 Mm)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years