GSK2141795 (Synonyms: GSK795, GSK2141795) |
رقم الكتالوجGC12305 |
GSK2141795 (GSK2141795) هو مثبط قوي وانتقائي من نوع pan-Akt بقيم IC50 تبلغ 180/328/38 نانومتر لـ Akt1 / Akt2 / Akt3 ، على التوالي.
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Cas No.: 1047634-65-0
Sample solution is provided at 25 µL, 10mM.
Uprosertib (GSK2141795) is a potent and selective pan-Akt inhibitor with IC50 values of 180/328/38 nM for Akt1/Akt2/Akt3, respectively.
Uprosertib (GSK2141795) 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 (GSK2141795) 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].
References:
[1]. Pachl F, et al. Characterization of a chemical affinity probe targeting Akt kinases. J Proteome Res. 2013 Aug 2;12(8):3792-800.
[2]. Jacobsen K, et al. Convergent Akt activation drives acquired EGFR inhibitor resistance in lung cancer. Nat Commun. 2017 Sep 4;8(1):410.
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