CAS: 1648909-73-2

Mutant IDH1-IN-3 (Compound 1) is a selective allosteric inhibitor targeting the mutant isocitrate dehydrogenase 1 (IDH1), with an IC50 of 13 nM for R132HIDH1. It effectively suppresses the production of D-2-hydroxyglutarate (2HG) in cells and is applicable for research in oncology.

Bis-imidazole phenol IDH1 inhibitor is a small-molecule therapeutic, which is a novel compound synthesized to specifically target mutant forms of isocitrate dehydrogenase 1 (IDH1). It operates by binding to the mutant IDH1 enzyme and inhibiting its aberrant function, which involves converting alpha-ketoglutarate to an oncometabolite, 2-hydroxyglutarate (2-HG). This conversion leads to epigenetic changes that drive the tumorigenesis process. The utility of Bis-imidazole phenol IDH1 inhibitors lies in their potential applications within oncology, specifically for treating cancers harboring IDH1 mutations, such as certain gliomas and acute myeloid leukemia. By reducing the production of 2-HG, these inhibitors aim to reverse the epigenetic reprogramming of cancer cells, thereby inhibiting tumor growth and progression. This targeted approach offers a promising direction for personalized cancer therapy, helping to improve outcomes for patients with mutant IDH1-associated malignancies. Researchers continue to explore the pharmacokinetic properties, efficacy, and safety profiles of these compounds in pre-clinical and clinical settings to fully understand their therapeutic potential.