For research use only. Not for therapeutic Use.
HQ461 is a molecular glue that promotes CDK12-DDB1 interaction to trigger cyclin K degradation. HQ461-mediated degradation of cyclin K impairs CDK12 function, resulting in decreased CDK12 substrate phosphorylation, downregulation of DNA damage response genes, and cell death[1].
HQ461 inhibits A549 viabilbity with an IC50 of 1.3 µM[1].
HQ461 (10 μM, 8 h) reduces CDK12 protein level in A549 cells[1].
HQ461 (0-10 μM) mediates recruitment of CDK12/CCNK to DDB1 in A549 cells[1].
| Catalog Number | I043869 |
| CAS Number | 1226443-41-9 |
| Synonyms | 2-[2-[(6-methylpyridin-2-yl)amino]-1,3-thiazol-4-yl]-N-(5-methyl-1,3-thiazol-2-yl)acetamide |
| Molecular Formula | C15H15N5OS2 |
| Purity | ≥95% |
| 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) |
| InChIKey | QMRBCNQCRMTXBE-UHFFFAOYSA-N |
| SMILES | CC1=NC(=CC=C1)NC2=NC(=CS2)CC(=O)NC3=NC=C(S3)C |
| Reference | [1]. Lv L, et al. Discovery of a molecular glue promoting CDK12-DDB1 interaction to trigger cyclin K degradation. Elife. 2020 Aug 17;9:e59994. |
