Mutant IDH1-IN-7

Mutant IDH1-IN-7 is a highly selective Isocitrate Dehydrogenase 1 (IDH1) R132H (IC50 = 0.26 μM, Kd = 2.1 μM) /R132C (IC50 = 1.1 μM) inhibitor. Mutant IDH1-IN-7 has no inhibitory effect on wild-type IDH1, IDH2-wt, and IDH2 R140Q. Mutant IDH1-IN-7 inhibits 2-Hydroxyglutarate (2-HG) production in U87-MG R132H cells (EC50 = 0.55 μM) . Mutant IDH1-IN-7 exhibits moderate antiproliferative effects on U87-MG R132H and HT-1080 cells[1].

Product Specifications

UNSPSC

12352005

Target

Isocitrate Dehydrogenase (IDH)

Related Pathways

Metabolic Enzyme/Protease

Field of Research

Cancer

Smiles

CC1=CC=C(C=C1)NC(CN2C(N/C(C2=O)=C\C3=CC=CN3C4=CC(CC(C)C)=CC=C4)=O)=O

Molecular Formula

C27H28N4O3

Molecular Weight

456.54

References & Citations

[1]Luo D, et al. Discovery and structure-activity relationship study of novel hydantoin-based inhibitors targeting mutant isocitrate dehydrogenase 1 (mIDH1) . Eur J Med Chem. 2025 Jul 5;297:117945.