MAT2A inhibitor 28 (AZ-28) is a potent and selective inhibitor of methionine adenosyltransferase MAT2A with IC50 of 22 nM.
MAT2A inhibitor 28 showed inhibition of PRMT5-mediated symmetric dimethylation of arginine (SDMA) with IC50 of 25 nM, inhibited proliferation of HCT116 MTAP knockout cells with an IC50 of 250 nM.
MAT2A inhibitor 28 is a promising in vivo tool that exhibited reduction in tumor SAM levels and antitumor response in an MTAP knockout HCT116 xenograft model.
