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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-THZ531
THZ531

Chemical Structure : THZ531

CAS No.: 1702809-17-3

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THZ531 (THZ-531)

货号: PC-62302Not For Human Use, Lab Use Only.

THZ531 (THZ-531) is a first-in-class, selective CDK12 and CDK13 covalent inhibitor with IC50 of 158 nM and 69 nM, respectively.

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5 mg ￥880 In stock
10 mg ￥1380 In stock
25 mg ￥2280 In stock
50 mg ￥3780 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

THZ531 (THZ-531) is a first-in-class, selective CDK12 and CDK13 covalent inhibitor with IC50 of 158 nM and 69 nM, respectively.
THZ531) dispalys 50-fold selectivity over CDK7 and CDK9 (IC50 of 8.5 and 10.5 uM, respectively), and shows no appreciable inhibitory effect on ERK1.
THZ531) irreversiblely inhibits Jurkat cell proliferation with an IC50 of 50 nM, induces apoptosis in a dose- and time-dependent manner with low doses (<350 nM).
THZ531) selectively reduced Ser2 phosphorylation levels without appreciable effect on CTD pSer5/pSer7 levels, causes a loss of gene expression with concurrent loss of elongating and hyperphosphorylated RNA polymerase II, inhibits DDR and transcription factor gene expression.

物理化学性质&存储条件

分子量 558.083
分子式 C30H32ClN7O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(R,E)-N-(4-(3-((5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl)amino)piperidine-1-carbonyl)phenyl)-4-(dimethylamino)but-2-enamide

参考文献

1. Zhang T, et al. Nat Chem Biol. 2016 Oct;12(10):876-84.

2. Paculová H, et al. Cell Div. 2017 Oct 27;12:7. doi: 10.1186/s13008-017-0033-x.

3. Iniguez AB, et al. Cancer Cell. 2018 Jan 17. pii: S1535-6108(17)30561-5.

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