CH091138

CH091138 is a potent and selective KRASG12D PROTAC degrader with DC50s of 148.3 nM in HeLa cells and 469.8 nM in AsPC-1 cells. CH091138 selectively degrades exogenous and endogenous KRASG12D but not KRASWT or other KRAS mutants (G12C/G12S/G12V), depending on the VHL-mediated ubiquitin-proteasome system. CH091138 exhibits potent anti-tumor activity and induces cancer cell apoptosis. CH091138 can be used for the studies of pancreatic cancer and colon cancer. (Pink: KRASG12D ligand (HY-175144) ; Blue: VHL E3 ligase ligand (HY-138678) ; Black: Linker; VHL E3 ligase ligand + Linker (HY-136006B) ) [1].

Product Specifications

UNSPSC

12352005

Target

Apoptosis; PROTACs; Ras

Related Pathways

Apoptosis; GPCR/G Protein; MAPK/ERK Pathway; PROTAC

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Smiles

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