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  3. Uprosertib hydrochloride

Uprosertib hydrochloride (Synonyms: GSK2141795 (hydrochloride))

Cat. No.: HY-15965A
Handling Instructions

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.

For research use only. We do not sell to patients.

Uprosertib hydrochloride Chemical Structure

Uprosertib hydrochloride Chemical Structure

CAS No. : 1047635-80-2

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Top Publications Citing Use of Products

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

    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).

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

    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: Oncotarget. 2018 Jul 31;9(59):31549-31558.

    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.

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    Description

    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]

    Akt3

    38 nM (IC50)

    Akt1

    180 nM (IC50)

    Akt2

    328 nM (IC50)

    ROCK1

    1570 nM (IC50)

    ROCK2

    1850 nM (IC50)

    CDK7

    2100 nM (IC50)

    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.

    Clinical Trial
    Molecular Weight

    465.71

    Formula

    C₁₈H₁₇Cl₃F₂N₄O₂

    CAS No.

    1047635-80-2

    SMILES

    O=C(C1=CC(C2=C(Cl)C=NN2C)=C(Cl)O1)N[[email protected]@H](CC3=CC=C(F)C(F)=C3)CN.Cl

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    References
    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.

    References
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    Keywords:

    UprosertibGSK2141795GSK 2141795GSK-2141795AktPKBProtein kinase BInhibitorinhibitorinhibit

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    Uprosertib hydrochloride
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