同义名 :	-
	CAS号 :	34576-94-8
	货号 :	A760956
	分子式 :	C9H4Cl2O2S
	纯度 :	97%
	分子量 :	247.1
	MDL号 :	MFCD00781745
	存储条件：	Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性
描述	Impaired branched-chain amino acids (BCAA) catabolism plays a pivotal role in the pathogenesis of metabolic and neurological diseases. The mitochondrial branched-chain α-ketoacid dehydrogenase complex (BCKDC) kinase (BDK) inhibitors that augment BCKDC flux have been shown to reduce BCAA concentrations in vivo. BT2 is a novel BDK inhibitor with an IC50 value of 3.19 μM. In wild-type MEF cells, BT2 robustly stimulated BCKDC activity at concentration of 40 μM for 48 h. Administration of BT2 at 20 mg/kg/day to wild-type mice for 1 week led to nearly complete dephosphorylation and maximal activation of BCKDC in heart, muscle, kidneys, and liver with reduction in plasma BCAA concentrations[3].
作用机制	Mechanism: BT2 binds to an allosteric site in the N-terminal domain of each monomer in homodimeric BDK[3].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	4.05mL 0.81mL 0.40mL	20.23mL 4.05mL 2.02mL	40.47mL 8.09mL 4.05mL

参考文献

[1]Tso SC, et al. Benzothiophene carboxylate derivatives as novel allosteric inhibitors of branched-chain α-ketoacid dehydrogenase kinase. J Biol Chem. 2014 Jul 25;289(30):20583-93. [2]Friberg A, et al. Discovery of potent myeloid cell leukemia 1 (Mcl-1) inhibitors using fragment-based methods and structure-based design. J Med Chem. 2013 Jan 10;56(1):15-30. [3]Tso SC, Gui WJ, Wu CY, et al. Benzothiophene carboxylate derivatives as novel allosteric inhibitors of branched-chain α-ketoacid dehydrogenase kinase. J Biol Chem. 2014 Jul 25;289(30):20583-93.