MIDH1-IN-2

MIDH1-IN-2 is a brain-penetrant isocitrate dehydrogenase 1 (IDH1) inhibitor. mIDH1-IN-2 shows subnanomolar potency against IDH1 R132H and R132C (IC50 = 80.0 and 58.0 nM) and minimal activity against wt-IDH1/2. mIDH1-IN-2 also inhibits PDK1 (IC50 = 0.61 μM) and reduces PDH phosphorylation dose-dependently. mIDH1-IN-2 can inhibit cells proliferation, induces S phase arrest and promotes apoptosis. mIDH1-IN-2 can be used for the research of cancer, such as glioma[1].

Product Specifications

UNSPSC

12352100

Target

Apoptosis; Isocitrate Dehydrogenase (IDH) ; PDK-1

Related Pathways

Apoptosis; Metabolic Enzyme/Protease; PI3K/Akt/mTOR

Field of Research

Cancer

Smiles

O=C(C1=CC=C(SC2=CC=CC(OC3CCC3)=C2)C([N+]([O-])=O)=C1)C(Br)Br

Molecular Formula

C18H15Br2NO4S

Molecular Weight

501.19

References & Citations

[1]Li C, et al. Identification and structure-activity relationship optimization of dibromoacetophenones as novel mIDH1 inhibitors. Eur J Med Chem. 2025 Dec 5;299:118050.