Borussertib |
| Catalog No.GC65367 |
Borussertib은 Akt에 대해 IC50이 0.8nM이고 Ki가 2.2nM인 단백질 키나제 Akt의 공유 알로스테릭 및 동급 최초의 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1800070-77-2
Sample solution is provided at 25 µL, 10mM.
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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.
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