ML309

ML309 is a highly selective and potent inhibitor of the R132H mutant isocitrate dehydrogenase 1 (IDH1 R132H), with an IC50 of 96 nM. ML309 is a competitive inhibitor of α-KG, with a Ki value of 156 nM, and its inhibitory activity against the wild-type IDH1 is greater than 35 μM. ML309 effectively reduces the production of the tumor metabolite 2-HG in U87MG cells. ML309 can be used as a chemical probe to study the role of the mutant IDH1 in cancer[1].

Product Specifications

CAS Number

[1355446-05-7]

UNSPSC

12352005

Target

Isocitrate Dehydrogenase (IDH)

Related Pathways

Metabolic Enzyme/Protease

Field of Research

Cancer

Smiles

O=C(N(C(C1=CC=CC=C1C)C(NC2CCCC2)=O)C3=CC=CC(F)=C3)CN4C5=CC=CC=C5N=C4

Molecular Formula

C29H29FN4O2

Molecular Weight

484.56

References & Citations

[1]Davis M, et al. ML309: A potent inhibitor of R132H mutant IDH1 capable of reducing 2-hydroxyglutarate production in U87 MG glioblastoma cells. 2012 Apr 16 [updated 2013 May 8]. In: Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD) : National Center for Biotechnology Information (US) ; 2010–.