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IDH-C227 is a potent and selective IDH1 R132H inhibitor first reported in patent WO2012009678. It can inhibit the enzymatic activity of IDH1 R132H in vitro with an IC₅₀ < 0.1 µM, and 2-HG production in HT1080 and U87MG cells with IC₅₀ < 0.25 µM. Because the mutated form of IDH1 produces the metabolite, 2-hydroxyglutarate (2HG), which may contribute to the formation and malignant progression of gliomas as well as other forms of cancer, IDH-C227 serves as a very useful chemical probe to study this novel target.

How to Use:

• In vitro:  IDH-C227 was used at 1-5 µM final concentration in vitro.
• In vivo:  n/a. You can try the new generation IDH1 inhibitor IDH-C35 for in vivo use.

Reference:

• 1. Popovicimuller Janeta, et al. THERAPEUTICALLY ACTIVE COMPOSITIONS AND THEIR METHOD OF USE. (2012) PCT WO 2012009678.
• 2. Dang L, et al.  Cancer-associated IDH1 mutations produce 2-hydroxyglutarate. (2009) Nature 462, 739-744.
• 3. Turcan S, et al. IDH1 mutation is sufficient to establish the glioma hypermethylator phenotype. (2012) Nature. 483(7390):479-83.

Products are for research use only. Not for human use.