2. PI3K/Akt/mTOR
  3. Akt
  4. Uprosertib hydrochloride

Uprosertib hydrochloride  (Synonyms: GSK2141795 (hydrochloride))

目录号: HY-15965A
产品使用指南

摩尔计算器

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。

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Uprosertib hydrochloride Chemical Structure

Uprosertib hydrochloride Chemical Structure

CAS No. : 1047635-80-2

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Uprosertib hydrochloride 的其他形式现货产品:

Other Forms of Uprosertib hydrochloride:

Uprosertib hydrochloride 相关抗体

Top Publications Citing Use of Products

    Uprosertib hydrochloride purchased from MCE. Usage Cited in: Oncotarget. 2018 Jul 31;9(59):31549-31558.  [Abstract]

    Western blots of the indicated proteins in the DMS114-P and DMS114-R cells treated with (+) and without (-) the AKT inhibitor, Uprosertib (200 nM) for 6 h (left panel) or 24 h (right panel). In the case of DMS114-P, extracts with (+) and without (-) treatment with PD173074 (1 µM) are also shown.

    Uprosertib hydrochloride purchased from MCE. Usage Cited in: Nat Commun. 2017 Sep 4;8(1):410.  [Abstract]

    Effect of EGFR TKIs and Akt inhibitors on key signal transduction proteins in parental and resistant PC9 cells. Western blot analysis of PC9 and PC9-ER treated for 4 h with Erlotinib (30 µM), GSK2141795 (2.5 µM) or the combination.

    Uprosertib hydrochloride purchased from MCE. Usage Cited in: Mol Cancer Ther. 2017 Apr;16(4):614-624.  [Abstract]

    Western blot analysis is performed with lysates from resistant cell lines treated either with vehicle (DMSO) or GSK2141795 (1 μM) for 24 hours to assess inhibition of Akt (pAKT) and downstream (pGSK3) signaling (three experimental replicates).

    查看 Akt 亚型特异性产品:

    查看所有亚型
    Akt Akt1 Akt2 Akt3

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    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.

    IC50 & Target[1]

    Akt1

    180 nM (IC50)

    Akt2

    328 nM (IC50)

    Akt3

    38 nM (IC50)

    CDK7

    2100 nM (IC50)

    ROCK1

    1570 nM (IC50)

    ROCK2

    1850 nM (IC50)

    体外研究
    (In Vitro)

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Uprosertib hydrochloride 相关抗体:
    Clinical Trial
    分子量

    465.71

    Formula

    C18H17Cl3F2N4O2
    CAS 号
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.
    纯度 & 产品资料
    参考文献
    Kinase Assay
    [1]

    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°C. Subsequently, lysates are incubated with beads (coupled Akt probe or kinobeads) for 1 h at 4°C, 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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    参考文献

    Uprosertib hydrochloride 相关分类

    • 摩尔计算器

    • 稀释计算器

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量   浓度   体积   分子量 *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
    × = ×
    C1   V1   C2   V2
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Uprosertib1047635-80-2GSK2141795GSK 2141795GSK-2141795AktPKBProtein kinase BInhibitorinhibitorinhibit

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