BT2,34576-94-8

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BT2

CAS No. : 34576-94-8

MCE 国际站：BT2

产品活性：BT2 是 BCKDC 激酶 (BDK) 抑制剂，IC₅₀ 值为 3.19 μM。BT2 与 BDK 的结合会触发支链 α-酮酸脱氢酶复合物 (BCKDC) 的 N 末端结构域的螺旋运动，从而导致 BDK 与 BCKDC 分离。BT2 (compound 4) 也是一种有效的选择性的 Mcl-1 抑制剂，K_i 值为 59 μM。

研究领域：Apoptosis

作用靶点：Bcl-2 Family

In Vivo: BT2 (20 mg/kg/day; intraperitoneal injection; 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. 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 treatment reduces the protein levels of BDK in kidneys and heart.

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