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Products Details
Product Description
– 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].
Web ID
– HY-149359
Shipping
– Room temperature
Molecular Formula
– C25H33FN6O4S
References
– [1]Qianmao Liang, et al. Structure-based discovery of IHMT-IDH1-053 as a potent irreversible IDH1 mutant selective inhibitor. Eur J Med Chem. 2023 Aug 5;256:115411.
Molecular Weight
– 532.63
SMILES
– 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
Clinical Information
– No Development Reported
Research Area
– Cancer
Solubility
– 10 mM in DMSO
Target
– Isocitrate Dehydrogenase (IDH)
Isoform
– IDH1;IDH2
Pathway
– Metabolic Enzyme/Protease
Product type
– Reference compound
Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.
