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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 3049485-80-2
- Formule: C25H33FN6O4S
- Masse moléculaire:532.63
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
- Pureté et documentation
- Références
-
Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
R132H IDH1 4.7 μM (IC50) |
IDH1 wt |
IDH2 wt |
Chemical Information
-
CAS No. 3049485-80-2
-
Masse moléculaire 532.63
-
Formule C25H33FN6O4S
-
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
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
IHMT-IDH1-053 Related Classifications
HY-149359 Related Classifications
Powered by Bioz