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.
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Chemical Information
| Name | HQ461 |
|---|---|
| Iupac Chemical Name | 2-(2-((6-methylpyridin-2-yl)amino)thiazol-4-yl)-N-(5-methylthiazol-2-yl)acetamide |
| Synonyms | HQ461; HQ-461; HQ 461; |
| Molecular Formula | C15H15N5OS2 |
| Molecular Weight | 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 Number | 1226443-41-9 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Off-white solid |
|---|---|
| Purity | 98% Min. |
| Storage | Dry, dark and at 0 - 4℃ for short term (days to weeks) or -20℃ for long term (months to years). |
| Solubility | Soluble in DMSO |
| Handling | |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
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| Mechanism | |
| Cell study | |
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| 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.
Chemical Structure
