(R)-2-HG ---a-KG-dependent dioxygenases inhibitor
| Overview | |
| Catalog # | bs-60104C |
| Product Name | (R)-2-HG ---a-KG-dependent dioxygenases inhibitor |
| Specifications | |
| Storage Buffer | Powder |
| Storage Condition | Powder: 4C for 1 year, -20C for 3 years. DMSO: 4C for 3 month. |
| Target | |
| Product Information | Molecular Weight: 192.08 Formula: C5 H6 Na2 O5 CAS Number: 103404-90-6 InChi Key: DZHFTEDSQFPDPP-HWYNEVGZSA-L InChi: InChI=1S/C5H8O5.2Na/c6-3(5(9)10)1-2-4(7)8;;/h3,6H,1-2H2,(H,7,8)(H,9,10);;/q;2*+1/p-2/t3-;;/m1../s1 Smiles: [Na+].[Na+].[O-]C(=O)CC[C@@H](O)C([O-])=O Purity: 98.0 Solubility: Water up to 100 mM Appearance: Solid powder Shelf Life: 3.0 years |
| Description | 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). |
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