HQ461
| CAS号 | 1226443-41-9 | 货号 | BCP47151 |
| 中文名 | HQ461 | ||
| 英文名 | HQ461 | ||
| 中文别名 | |||
| 英文别名 | HQ-461; HQ 461; | ||
| 分子式 | C15H15N5OS2 | 分子量 | 345.44 |
| 生物活性 | HQ461 is a Molecular-glue degrader. HQ461 acts by promoting an interaction between CDK12 and DDB1-CUL4-RBX1 E3 ubiquitin ligase, leading to polyubiquitination and degradation of CDK12-interacting protein Cyclin K (CCNK). Degradation of CCNK mediated by HQ461 compromised CDK12 function, leading to reduced phosphorylation of a CDK12 substrate, downregulation of DNA damage response genes, and cell death. Structure-activity relationship analysis of HQ461 revealed the importance of a 5-methylthiazol-2-amine pharmacophore and resulted in an HQ461 derivate with improved potency. | ||
| 信号通路 | Cell Cycle/DNA Damage | ||
| 靶 点 | CDK | ||
结构式
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