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Uprosertib hydrochloride
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。
Uprosertib hydrochloride图片
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议

产品介绍
Uprosertib hydrochloride (GSK2141795 hydrochloride) 是一种有效的,选择性的 Akt 广谱抑制剂,抑制 Akt1/Akt2/Akt3 的活性,IC50 值分别为 180/328/38 nM。

Kinase experiment:

For selectivity profiling experiments, the lysates (5 mg of total protein each) are preincubated with 0 (DMSO control), 2.5 nM, 25 nM, 250 nM, 2.5 μM or 25 μM free compound (GSK690693 or Uprosertib) on an end-over-end shaker for 45 min at 4℃. Subsequently, lysates are incubated with beads (coupled Akt probe or kinobeads) for 1 h at 4℃, for both qualitative and quantitative experiments. The beads are washed with 1×CP buffer and collected by centrifugation. Bound proteins are eluted with 2×NuPAGE LDS sample buffer, and eluates are reduced and alkylated by 50 mM dithiothreitol and 55 mM iodoacetamide.

产品描述

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.