HQ461

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Catalog Number
ACM1226443419
Product Name
HQ461
CAS
1226443-41-9
Category
Inhibitors
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.
Synonyms
HQ461; HQ-461; HQ 461
IUPAC Name
2-(2-((6-methylpyridin-2-yl)amino)thiazol-4-yl)-N-(5-methylthiazol-2-yl)acetamide
Molecular Weight
345.44
Molecular Formula
C15H15N5OS2
Canonical SMILES
CC1C=CC=C(NC2=NC(CC(=O)NC3=NC=C(C)S3)=CS2)N=1
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)
InChI Key
QMRBCNQCRMTXBE-UHFFFAOYSA-N
Solubility
To be determined
Appearance
Solid powder
Shelf Life
>2 years if stored properly
Storage
Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
Drug Formulation
To be determined
Elemental Analysis
C, 52.16; H, 4.38; N, 20.27; O, 4.63; S, 18.56
Exact Mass
345.0718
HS Tariff Code
2934.99.9001
Shipping
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.
Stock Solution Storage
0-4 °C for short term (days to weeks), or -20 °C for long term (months).
Please kindly note that our products are for research use only.

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