Uprosertib hydrochloride (Synonyms: GSK2141795 (hydrochloride)) |
| رقم الكتالوجGC37859 |
هيدروكلوريد Uprosertib (GSK2141795 hydrochloride) هو مثبط قوي وانتقائي pan-Akt بقيم IC50 180/328/38 نانومتر لـ Akt1 / Akt2 / Akt3 ، على التوالي
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Cas No.: 1047635-80-2
Sample solution is provided at 25 µL, 10mM.
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Uprosertib hydrochloride (GSK2141795 hydrochloride) is a potent and selective pan-Akt inhibitor with IC50 values of 180/328/38 nM for Akt1/Akt2/Akt3, respectively. Akt1|180 nM (IC50)|Akt2|328 nM (IC50)|Akt3|38 nM (IC50)|CDK7|2100 nM (IC50)|ROCK1|1570 nM (IC50)|ROCK2|1850 nM (IC50)
Uprosertib inhibits Akt1/2/3 with the Kd values of 16/49/5 nM, respectively. Uprosertib potently inhibits only the PKC family members PRKACA and PRKACB as well as the cGMP-dependent protein kinase PRKG1 aqpart from the Akts. Protein targets that bind Uprosertib in the lysate show a dose-dependent reduction in binding to the kinobeads, while proteins unaffected by the drug show no reduction in binding[1].
[1]. Pachl F, et al. Characterization of a chemical affinity probe targeting Akt kinases. J Proteome Res. 2013 Aug 2;12(8):3792-800.
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