BCKDC kinase inhibitor / BT2 is an inhibitor of the mitochondrial branched-chain α-ketoacid dehydrogenase complex kinase (BCKDC) - IC50 = 3.19 µM.1 Inhibition of this kinase has been shown to reduce levels of branched-chain amino acid concentrations in vivo. BT2 has also been shown to be a moderate inhibitor (Ki = 59 µM) of myeloid cell leukemia 1(Mcl 1), a Bcl-2 family protein.2
Biochemicals & reagents
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1) Tso et al. (2014), Benzothiophene carboxylate derivatives as novel allosteric inhibitors of branched-chain α-ketoacid dehydrogenase kinase; J.Biol.Chem. 289 20583 2) Friberg et al. (2013), Discovery of potent myeloid cell leukemia (Mcl 1) inhibitors using fragment based methods and structure based design; J.Med.Chem. 56 15
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TARGET: Kinase -- PATHWAY: Mitochondrial function; Bcl -- DISEASE AREA: Cancer