HQ461

  • 化学数据
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
  • 用途
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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