Borussertib 是蛋白激酶 Akt 的首创的、共价变构抑制剂，其对 Aktwt 的IC50 值为 0.8 nM，Ki 值为 2.2 nM。
货号:ajcx39444
CAS:1800070-77-2
分子式:C36H32N6O3
分子量：596.68
溶解度:DMSO : 25 mg/mL (41.90 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Borussertib is a covalent-allosteric and first-in-class inhibitor of protein kinase Akt, with an IC50 of 0.8 nM and a Ki of 2.2 nM for Aktwt[1].

Borussertib exhibits excellent cellular activity in the nanomolar range with superior profile against clinical candidate Akt inhibitors as well as the cytostatic drug doxorubicin. The EC50 values are 191±90 nM, 48±15 nM, 5±1 nM, 277±90 nM, 373±54 nM, 7770±641 nM in AN3CA (endometrium), T47D (breast), ZR-75-1 (breast), MCF-7 (breast), BT-474 (breast) and KU-19-19 (bladder) cell lines, respectively[1].

[1]. Niklas Uhlenbrock, et al. Structural and chemical insights into the covalentallosteric inhibition of the protein kinase Akt. Chem Sci., 2019, 10, 3573.

Protocol:

Aktwt 0.8nM(IC50)

Aktwt 2.2nM(Ki)