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BT2

Development stage
Preclinical
Lead developer
University of California
Modality
Small Molecules
01

Overview

BT2 is a small molecule allosteric inhibitor of branched-chain ketoacid dehydrogenase kinase (BDK or BCKDK), with an IC50 of approximately 3.19 μM[1][2][3][4]. By inhibiting BDK, BT2 activates the mitochondrial branched-chain α-ketoacid dehydrogenase complex (BCKDC), thereby enhancing the catabolism of branched-chain amino acids (BCAAs). In preclinical studies, administration of BT2 led to increased BCKDC activity and reduced plasma BCAA concentrations in animal models. This mechanism has shown potential benefits in metabolic disorders such as insulin resistance and steatosis in mice[3][4]. The compound is primarily used as a research tool for studying metabolic pathways involving BCAAs and has not been approved for human therapeutic use.

Other names
3,6-dichlorobenzo[b]thiophene-2-carboxylic acid3,6-dichloro-1-benzothiophene-2-carboxylic acid3,6-dichlorobenzothiophene-2-carboxylic acid
02

Targets

BCKDK (Branched-chain ketoacid dehydrogenase kinase)

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