|Solubility:||Water up to 100 mM|
|Storage:||Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.|
|Chemical Name:||sodium (R)-2-hydroxypentanedioate|
Mutations in IDH1 and IDH2, the genes coding for isocitrate dehydrogenases 1 and 2, are common in several human cancers, such as leukemia and glioma, and result in overproduction of the (R)-enantiomer of 2-hydroxyglutarate [(R)-2-HG]. Elucidation of the role of IDH mutations and (R)-2-HG in leukemogenesis has been hampered by a lack of appropriate cell-based models. It has been recently reported that a canonical IDH1 mutant, IDH1 R132H, promoted cytokine independence and blocks differentiation in hematopoietic cells. These effects can be recapitulated by (R)-2-HG, but not (S)-2-HG, despite the fact that (S)-2-HG more potently inhibits enzymes previously linked to the pathogenesis of IDH mutant tumors, such as the 5'-methylcytosine hydroxylase TET2. This paradox is perhaps due to the ability of (S)-2-HG, but not (R)-2-HG, to inhibit the EglN prolyl hydroxylases. 2-HG has also been shown to inhibit the activity of multiple other a-KG-dependent dioxygenases, including the JmjC domain-containing histone demethylases (KDMs).
How to Use:
In vitro:(R)-2-HG was used at 100-250 µM final concentration in vitro and in cellular assays.
- Losman JA, et al. (R)-2-Hydroxyglutarate Is Sufficient to Promote Leukemogenesis and Its Effects Are Reversible. (2013) Science. 339(6127):1621-5.
- Ye D, et al. R-2-Hydroxyglutarate as the Key Effector of IDH Mutations Promoting Oncogenesis. (2013) Cancer Cell. 23(3):274-6.
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