Senexin A是一种有效且选择性的 CDK8 抑制剂，它还抑制 CDK19，Kd值分别为0.83μM和0.31μM。

Senexin A is an effective and selective CDK8 inhibitor that also inhibits CDK19 with Kd values of 0.83 microns and 0.31 microns, respectively.

Senexin A inhibited CDK8 and CDK19 ATP site binding with Kd50 of 0.83 μM and 0.31 μM, respectively and CDK8 kinase activity with IC50 of 0.28 μM.CDK8 stimulates Wnt/β-catenin, and Senexin A inhibits β-catenin–dependent transcription in HCT116 colon carcinoma cells.

Five daily treatment of Senexin A fully reverses tumor-promoting effect of chemotherapy. Senexin A shows no detectable toxicity as well as no significant effects on body weight, organ weights, or blood cell counts in C57BL/6 mice during the treatment. This effect of doxorubicin treatment is completely abolished, however, when doxorubicin injection is followed by administration of Senexin A. Senexin A treatment strongly improves the response of A549/MEF tumors to doxorubicin.

Tumor-free C57BL/6-derived SCID mice were injected with a single dose of doxorubicin or carrier control.?Five days later, mice received. injection of 2 × 10^6 human A549 lung carcinoma cells, and tumor take was measured over 4 wk.

1366002-50-7

C17H14N4

274.32

Senexin A

DMSO:100 mg/mL (364.54 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years