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HQ461

Chemical Structure : HQ461

CAS No.: 1226443-41-9

HQ461 (HQ-461)

Catalog No.: PC-21053Not For Human Use, Lab Use Only.

HQ461 is a molecular glue promoting CDK12-DDB1 interaction to trigger cyclin K degradation, exhibits potent cytotoxicity to NSCLC cell line A549 with with IC50 of 1.3 uM.

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Biological Activity

HQ461 is a molecular glue promoting CDK12-DDB1 interaction to trigger cyclin K degradation, exhibits potent cytotoxicity to NSCLC cell line A549 with with IC50 of 1.3 uM.
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).
HQ461 is a new molecular glue that recruits its target protein directly to DDB1 to bypass the requirement of a substrate-specific receptor, presenting a new strategy for targeted protein degradation.

Physicochemical Properties

M.Wt 345.44
Formula C15H15N5OS2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-(2-((6-methylpyridin-2-yl)amino)thiazol-4-yl)-N-(5-methylthiazol-2-yl)acetamide

References

1. Lu Lv, et al. Elife. 2020 Aug 17;9:e59994. doi: 10.7554/eLife.59994.

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