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GSK2141795
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GSK2141795图片
CAS NO:1047634-65-0
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
50mg电议
100mg电议
200mg电议

产品介绍
GSK2141795 (GSK2141795) 是一种有效的选择性泛 Akt 抑制剂,对 Akt1/Akt2/Akt3 的 IC50 值分别为 180/328/38 nM。
Cas No.1047634-65-0
别名GSK2141795
化学名N-((S)-1-amino-3-(3,4-difluorophenyl)propan-2-yl)-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)furan-2-carboxamide
Canonical SMILESCN1C(C(C=C(O2)C(N[C@@](CN)([H])CC3=CC(F)=C(F)C=C3)=O)=C2Cl)=C(Cl)C=N1
分子式C18H16Cl2F2N4O2
分子量429.25
溶解度DMF: 1 mg/ml,DMSO: 1 mg/ml
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.