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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-Compound 919278
Compound 919278

Chemical Structure : Compound 919278

CAS No.: 2189366-77-4

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Compound 919278 (CDK12 inhibitor Compound 919278)

货号: PC-35532Not For Human Use, Lab Use Only.

Compound 919278 is a specific inhibitor of lymphotoxin β receptor (LTβR, IC50=0.169 uM), and TNF receptor superfamily member 12A (FN14)-dependent nuclear translocation of p52 (IC50=0.167 uM) via inhibiting CDK12/CCNK.

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10 mg ￥1980 In stock
25 mg ￥2980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Compound 919278 is a specific inhibitor of lymphotoxin β receptor (LTβR, IC50=0.169 uM), and TNF receptor superfamily member 12A (FN14)-dependent nuclear translocation of p52 (IC50=0.167 uM) via inhibiting CDK12/CCNK.
Compound 919278 does not inhibit the TNF-α-mediated nuclear translocation of p65 (RelA).
Compound 919278 prevents the accumulation of NIK, selectively inhibits the noncanonical NF-kB pathway.
Compound 919278 prevents the LTβR- and FN14-dependent expression of MAP3K14 (which encodes NIK) as well as NIK accumulation by reducing phosphorylation of the carboxyl-terminal domain of RNA polymerase II.
Compound 919278 reduces the binding of both CDK12 and its associated protein CCNK with IC50 of 30-60 nM, inhibits CDK12 cellular activity and reduces the phosphorylation of Ser2 on the RNA Pol II CTD.
Compound 919278 phenocopies the effect of CDK12 knockdown on DEGs.

物理化学性质&存储条件

分子量 320.352
分子式 C18H16N4O2
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)-N-(1H-benzo[d]imidazol-2-yl)-2-(1-oxoisoindolin-2-yl)propanamide

参考文献

1. Henry KL, et al. Sci Signal. 2018 Jul 31;11(541). pii: eaam8216.

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