CAS: 1428569-85-0

GDC-0339 is a potent inhibitor of the enzyme farnesyltransferase, which is required for the post-translational modification of proteins. It has been shown to inhibit murine leukemia cells and human cytochrome P450. GDC-0339 is a potent inhibitor of the enzyme farnesyltransferase, which is required for the post-translational modification of proteins. It has been shown to inhibit murine leukemia cells and human cytochrome P450. GDC-0339 inhibits farnesylation by binding to the nicotinamide ring of FTS, preventing its interaction with the protein substrate. The inhibition of this reaction leads to increased levels of cellular prenyl groups and an accumulation of newly synthesized proteins that are not modified by FTS. This drug also has high affinity binding properties and displays constant amplitudes in magnetic resonance analysis (MRA).

GDC-0339: oral Pim kinase inhibitor for multiple myeloma (Kis: Pim1 - 0.03 nM, Pim2 - 0.1 nM, Pim3 - 0.02 nM), well-tolerated.