Compound 919278

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

化合物919278是淋巴毒素β受体的特异性抑制剂（LTβR，IC50=0.169 uM）。

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, does not inhibit the TNF-α-mediated nuclear translocation of p65 (RelA); prevents the accumulation of NIK, selectively inhibits the noncanonical NF-kB pathway; 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; 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; phenocopies the effect of CDK12 knockdown on DEGs.

Western Blot Analysis Cell Line:U-2 OS cells Concentration:1 μM, 3 μM, and 10 μM Incubation Time:30 min Result:Reduced the phosphorylating of Ser2 in cells stimulated by 20 ng/mL TWEAK for 4 hr.Note: CDK12 activated RNA Pol II–mediated transcription by phosphorylating Ser2 within the 52 heptad (Y1S2P3T4S5P6S7) repeats in the C-terminal domain (CTD) of RNA Pol II. Ser2 phosphorylation aids in the release of paused RNA Pol II from promoters, resulting in transcriptional elongation, which is particularly important for the transcription of some long, complex genes.

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Angiogenesis

CDK

CDK

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2189366-77-4

320.352

C18H16N4O2

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (390.20 mM)

CC(C(=O)NC1=NC2=CC=CC=C2N1)N3CC4=CC=CC=C4C3=O

(R)-N-(1H-benzo[d]imidazol-2-yl)-2-(1-oxoisoindolin-2-yl)propanamide

(-20℃)

With Ice Pack

≥ 2 years