HQ461
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.
仅供研究使用。 我们不向患者出售。
化学信息
| 名称 | HQ461 |
|---|---|
| Iupac 化学名称 | 2-(2-((6-methylpyridin-2-yl)amino)thiazol-4-yl)-N-(5-methylthiazol-2-yl)acetamide |
| 同义词 | HQ461; HQ-461; HQ 461; |
| 英文同义词 | HQ461; HQ-461; HQ 461; |
| 分子式 | C15H15N5OS2 |
| 分子量 | 345.44 |
| Smile | CC1C=CC=C(NC2=NC(CC(=O)NC3=NC=C(C)S3)=CS2)N=1 |
| InChiKey | QMRBCNQCRMTXBE-UHFFFAOYSA-N |
| InChi | InChI=1S/C15H15N5OS2/c1-9-4-3-5-12(17-9)19-15-18-11(8-22-15)6-13(21)20-14-16-7-10(2)23-14/h3-5,7-8H,6H2,1-2H3,(H,16,20,21)(H,17,18,19) |
| Cas号 | 1226443-41-9 |
| 相关CAS号 |
订购信息
| 包装 | 价格 | 库存 | 纯度 | 备货期 |
|---|---|---|---|---|
| 大货 | 询价 | 询价 | 询价 |
| 外观性状 | 类白色固体 |
|---|---|
| 纯度 | 98% Min. |
| 存储 | 0-4℃，可保存几天到几周；-20℃，可保存 几个月。 |
| 可溶性 | 溶于DMSO等有机溶剂 |
| 处理方式 | |
| 运输条件 | 可以在室温下进行运输。 |
| 海关编码 |
| Targets | |
|---|---|
| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
Lv L, Chen P, Cao L, Li Y, Zeng Z, Cui Y, Wu Q, Li J, Wang JH, Dong MQ, Qi X, Han T. Discovery of a molecular glue promoting CDK12-DDB1 interaction to trigger cyclin K degradation. Elife. 2020 Aug 17;9:e59994. doi: 10.7554/eLife.59994. PMID: 32804079; PMCID: PMC7462607.
