BT2 是 BCKDC 激酶(BDK)抑制剂，IC50值为 3.19 μM。它也是一种选择性的Mcl-1抑制剂，Ki值为 59 μM。BT2 与 BDK 结合触发 N 端结构域的螺旋运动，导致 BDK 从支链 α-酮酸脱氢酶复合物 (BCKDC) 中解离。

BT2 is a BCKDC kinase (BDK) inhibitor with an IC50 of 3.19 μM. BT2 (compound 4) is also a potent and selective Mcl-1 inhibitor with a Ki value of 59 μM. BT2 binding to BDK triggers helix movements in the N-terminal domain, resulting in the dissociation of BDK from the branched-chain α-ketoacid dehydrogenase complex (BCKDC).

BT2 treatment reduces the protein levels of BDK in kidneys and heart. The -fold activation of BCKDC activity in the above tissues correlates with decreased phosphorylation in heart, muscle, and kidney after the long term BT2 treatment. BT2 (20 mg/kg/day; i.p.; daily; for 7 days; C57BL/6J male mice) treatment robustly enhances BCKDC activity in the heart (12.3-fold) compared with the vehicle-treated animals. Less activation is obtained in muscle and kidney at 3.6- and 3.8-fold, respectively [1].

34576-94-8

C9H4Cl2O2S

247.1

3,6-二氯-2-苯并噻吩羧酸

DMSO:83.33 mg/mL (337.23 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years