IHMT-IDH1-053
Product Specifications
UNSPSC 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].
Target Antigen
Isocitrate Dehydrogenase (IDH)
Type
Reference compound
Related Pathways
Metabolic Enzyme/Protease
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/ihmt-idh1-053.html
Solubility
10 mM in DMSO
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
Molecular Weight
532.63
References & Citations
[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.
Shipping Conditions
Room temperature
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-149359/IHMT-IDH1-053-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-149359/
Clinical Information
No Development Reported
CAS Number
3049485-80-2
Curated Selection
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