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BDK inhibitor BT2

Chemical Structure : BDK inhibitor BT2

CAS No.: 34576-94-8

BDK inhibitor BT2

Catalog No.: PC-49378Not For Human Use, Lab Use Only.

BDK inhibitor BT2 is a small molecule allosteric inhibitor of BCKDC kinase (BDK) with IC50 of 3.19 uM.

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Biological Activity

BDK inhibitor BT2 is a small molecule allosteric inhibitor of BCKDC kinase (BDK) with IC50 of 3.19 uM.
BDK inhibitor BT2 significantly increases BCKDC activity in wild-type and MSUD cells the mitochondrial branched-chain α-ketoacid dehydrogenase complex (BCKDC).
BDK inhibitor BT2 binds to the same site in BDK as other known allosteric BDK inhibitors, including (S)-α-cholorophenylproprionate ((S)-CPP).
Administration of BT2 at 20 mg/kg/day to wild-type mice for 1 week leads to nearly complete dephosphorylation and maximal activation of BCKDC in heart, muscle, kidneys, and liver with reduction in plasma BCAA concentrations.
BT2 treatment reduced steatosis and/or inflammation, improved sulin sensitivity in HFD-fed and lean mice.

Physicochemical Properties

M.Wt 247.089
Formula C9H4Cl2O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3,6- dichlorobenzo[b]thiophene-2-carboxylic acid

References

1. Shih-Chia Tso, et al. J Biol Chem. 2014 Jul 25;289(30):20583-93.

2. Bollinger E, et al. Mol Metab. 2022 Oct 8:101611.

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