HQ461 New
Data Sheet
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| CAS No. | 1226443-41-9 | Cat. No. | BCP47151 |
| Name | HQ461 | ||
| Synonyms | HQ-461; HQ 461; | ||
| SMILES | CC1=NC(=CC=C1)NC2=NC(=CS2)CC(=O)NC3=NC=C(S3)C | ||
| Chemical Name | |||
| Formula | C15H15N5OS2 | M. Wt | 345.44 |
| Purity | 98% | Storage | Store at 4-8°C |
| Description | 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. | ||
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