GSK 215 New
Chemical Name: (2S,4R)-4-Hydroxy-1-((S)-2-(2-(4-(3-methoxy-4-((4-((2-(methylcarbamoyl)phenyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)phenyl)piperazin-1-yl)acetamido)-3,3-dimethylbutanoyl)-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide
Biological ActivityGSK 215 is a potent and selective focal adhesion kinase (FAK) Degrader (PROTAC®; pDC50 = 8.4, last for 96 h). Comprises the FAK inhibitor, PND 1186 (Cat. No. 6891), joined by a linker to a VHL E3 ligase ligand. Kinome binding (KinoBead profiling) shows GSK 215 (at 10 nM) has high selectivity for the FAK kinase domain. GSK 215 inhibits cell proliferation in MCF-7 and A549 cells and suppresses A549 cell motility in a wound scratch model system. In CD1 mice, GSK 215 injection induces rapid and profound degradation of FAK in liver (Dmax = 85% at 18h).
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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