IHMT-IDH1-053

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.


Cat. No.: EX-A13489	Purity: >98%

	Chemical structure of IHMT-IDH1-053

For research only, Do not use for Human!

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CAS No.	3049485-80-2
Purity	>98%
Formula	C25H33FN6O4S
Mol Weight	532.631
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Shipping	Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Reference:	[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.
CoA	CoA of IHMT-IDH1-053

Smiles:	[C@@H](C)(C)[C@@H]1N(C(=O)OC1)C2=NC(N[C@@H](C)C3=CC=C(C=C3)N4CCC(NS(C=C)(=O)=O)CC4)=NC=C2F


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