Bioactivity | Senexin A hydrochloride 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 hydrochloride inhibits CMV-GFP induction as well as the p21 stimulatory activity of the consensus NF-κB-dependent promoters[1][2]. |
Invitro | Senexin A hydrochloride 抑制 CDK8 和 CDK19 ATP 位点结合,Kd50 分别为 0.83 μM 和 0.31 μM[1]。Senexin A hydrochloride 抑制 HCT116 结肠癌细胞中 β-连环蛋白依赖性转录[1]。在 HT1080 细胞中,Senexin A hydrochloride 强烈抑制血清饥饿时转录因子 EGR1 的诱导[1]。Senexin A hydrochloride 还可降低阿霉素处理的野生型 HCT116 细胞中许多分泌型肿瘤促进因子的表达[1]。 0 --> Senexin A hydrochloride 相关抗体: |
In Vivo | Senexin A hydrochloride (每天 5 次) 可完全逆转化疗的肿瘤促进作用。在治疗期间,Senexin A hydrochloride 对 C57BL/6 小鼠的体重、器官重量或血细胞计数无显著毒性。Senexin A hydrochloride 可显着改善 A549/MEF 肿瘤对 Doxorubicin (HY-15142A) 的反应[1]。 |
Name | Senexin A hydrochloride |
CAS | 1780390-76-2 |
Formula | C17H15ClN4 |
Molar Mass | 310.78 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. [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. |