TFMB-R-2-HG is a cell-permeable form of (R)-2-hydroxyglutarate ((R)-2-HG).1 (R)-2-HG is structurally similar to α-ketoglutarate and competitively inhibits α-ketoglutarate-dependent dioxygenases, including lysine demethylases and DNA hydroxylases.2,3,4 TFMB-R-2-HG has been used to assess the role of (R)-2-HG in leukemogenesis.1
1.Losman, J.A., Looper, R.E., and Koivunen, P.(R)-2-hydroxyglutarate is sufficient to promote leukemogenesis and its effects are reversibleScience339(6127)1621-1625(2013) 2.Yang, H., Ye, D., Guan, K.L., et al.IDH1 and IDH2 mutations in tumorigenesis: Mechanistic insights and clinical perspectivesClin. Cancer Res.18(20)5562-5571(2012) 3.Xu, W., Yang, H., Liu, Y., et al.Oncometabolite 2-hydroxyglutarate is a competitive inhibitor of α-ketoglutarate-dependent dioxygenasesCancer Cell19(1)17-30(2011) 4.Chowdhury, R., Yeoh, K.K., Tian, Y.M., et al.The oncometabolite 2-hydroxyglutarate inhibits histone lysine demethylasesEMBO Rep.12(5)463-469(2011)