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MIDH1-IN-1

MIDH1-IN-1 (compound 43) is a potent and selective mIDH1 (mutant isocitrate dehydrogenases 1) inhibitor, with an IC50 of 961.5 nM. mIDH1-IN-1 potently inhibits intracellular 2-HG (2-hydroxyglutarate) production in HT1080 cells, with an EC50 of 208.6 ± 8.0 nM. mIDH1-IN-1 shows a significant anti-proliferation activity on IDH1 mutant-U-87 cells, with an IC50 of 41.8 nM. mIDH1-IN-1 is an antitumor agent, and can be used for IDH1 mutated solid tumors research[1]. mIDH1-IN-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Product Specifications

CAS Number

[2757155-96-5]

UNSPSC

12352005

Target

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/midh1-in-1.html

Solubility

10 mM in DMSO

Smiles

C#CC(N(C(C1=C(C=C(C=C1)OC)C)C(NC2CCCCC2)=O)C3=CC=C(C=C3)[N+]([O-])=O)=O

Molecular Formula

C25H27N3O5

Molecular Weight

449.50

References & Citations

[1]Zhou X, et al. Discovery of linear unnatural peptides as potent mutant isocitrate dehydrogenase 1 inhibitors by Ugi reaction. Bioorg Chem. 2022 Feb;119:105569.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

IDH1

Curated Selection

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