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Senexin A

MCE China：Senexin A

Brand：MedChemExpress (MCE)

Cat. No.HY-15681

CAS：1366002-50-7

Purity：99.79%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Senexin A is an inhibitor of CDK8/19 (IC50: 280 nM, CDK8) and an inhibitor downstream of p21 transcription. It only inhibits p21-induced transcription but does not inhibit other biological effects of p21. Senexin A inhibits CMV-GFP induction as well as the p21 stimulatory activity of the consensus NF-κB-dependent promoters.

In Vitro：Senexin A inhibits CDK8 and CDK19 ATP site binding with Kd50 of 0.83 μM and 0.31 μM, respectively[1].Senexin A inhibits β-catenin-dependent transcription in HCT116 colon cancer cells[1].In HT1080 cells, Senexin A strongly inhibits the induction of the transcription factor EGR1 upon serum starvation[1].Senexin A also reduces the expression of many secreted tumor-promoting factors in doxorubicin-treated wild-type HCT116 cells[1].

In Vivo：Five daily treatment of Senexin A fully reverses tumor-promoting effect of chemotherapy. Senexin A shows no detectable toxicity and 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[1].

Animal Administration：Mice: Senexin A toxicity study is conducted by Taconic in C57BL/6 mice, using five mice per group treated with 20 mg/kg Senexin A or carrier (80% propylene glycol), with five daily i.p. injections. Mice are weighed on days 3 and 6, and killed on day 6. Organ weights are determined for brain, kidney, thymus, spleen, lung, and liver. Terminal blood samples are analyzed to determine the numbers of total white blood cells, neutrophils, lymphocytes, monocytes, eosinophils, and basophils[1].

IC50 & Target：CDK19 0.31 μM (Kd) CDK8 0.83 μM (Kd) CDK8 280 nM (IC50)

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References：

[1]. Porter DC, et al. Cyclin-dependent kinase 8 mediates chemotherapy-induced tumor-promoting paracrine activities. Proc Natl Acad Sci U S A. 2012 Aug 21;109(34):13799-804.  [Content Brief]

[2]. Ho TY, et al. The study of a novel CDK8 inhibitor E966-0530-45418 that inhibits prostate cancer metastasis in vitro and in vivo. Biomed Pharmacother. 2023 Jun;162:114667.  [Content Brief]