IHMT-IDH1-053

MedChem Express

IHMT-IDH1-053 [3049485-80-2]

14

Research Use Only

C25H33FN6O4S

532.63

IHMT-IDH1-053 (compound 16) is a highly selectivity and irreversible IDH1-mutant inhibitor with an IC50 of 4.7 nM for IDH1 R132H. IHMT-IDH1-053 displays high selectivity against IDH1 mutants over IDH1 wt and IDH2 wt/mutants. IHMT-IDH1-053 inhibits 2-hydroxyglutarate (2-HG) production in IDH1 R132H mutant transfected 293T cells (IC50=28 nM). IHMT-IDH1-053 binds to the IDH1 R132H protein in the allosteric pocket adjacent to the NAPDH binding pocket through a covalent bond with residue Cys269. IHMT-IDH1-053 inhibits the proliferation of HT1080 cell line and primary AML cells which both bear IDH1 R132 mutants[1].

C[C@H](NC1=NC=C(F)C(N2C(OC[C@@H]2C(C)C)=O)=N1)C3=CC=C(N4CCC(NS(C=C)(=O)=O)CC4)C=C3

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