TG2-179-1

Description: TG2-179-1 is a BRCA1-associated protein 1 (BAP1) inhibitor that effectively hampers BAP1's deubiquitinase activity in cell-free assays at concentrations between 25 µM and 1.5 mM. This compound exhibits cytotoxicity towards a range of eight colon cancer cell lines, with half-maximal inhibitory concentrations (IC50s) spanning from 4.48 to 7.52 µM. Additionally, in an HCT116 colon cancer mouse xenograft model, TG2-179-1 administration at doses of 10 and 30 mg/kg significantly reduces tumor volume, demonstrating its potential in vivo efficacy against colon cancer. Target: Others. Smiles: N#CC1=C(NC(CSC2=NN=C(C(C=C3)=CC=C3Cl)O2)=O)SC(C)=C1C(C=C4)=CC=C4F