1. Metabolic Enzyme/Protease
  2. Phosphatase
  3. GSK 2830371

GSK 2830371 

Cat. No.: HY-15832 Purity: 98.94%
Handling Instructions

GSK 2830371 is a highly selective Wip1 phosphatase inhibitor with IC50 of 6 nM.

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

GSK 2830371 Chemical Structure

GSK 2830371 Chemical Structure

CAS No. : 1404456-53-6

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 79 In-stock
Estimated Time of Arrival: December 31
5 mg USD 72 In-stock
Estimated Time of Arrival: December 31
10 mg USD 102 In-stock
Estimated Time of Arrival: December 31
50 mg USD 324 In-stock
Estimated Time of Arrival: December 31
100 mg USD 540 In-stock
Estimated Time of Arrival: December 31
200 mg USD 792 In-stock
Estimated Time of Arrival: December 31
500 mg   Get quote  
1 g   Get quote  

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Customer Review

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products

    GSK 2830371 purchased from MCE. Usage Cited in: Oncotarget. 2016 Mar 22;7(12):14458-75.

    Immunoblot analysis of MCF7 cells reveals that addition of GSK2830371 results in a rapid phosphorylation of p53 at Ser15. Two days after addition of GSK2830371, MCF7 cells show increased levels of p21 which indicates a strong activation of the p53 pathway.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    GSK 2830371 is a highly selective Wip1 phosphatase inhibitor with IC50 of 6 nM.

    IC50 & Target

    IC50: 6 nM (Wip1 phosphatase)[1]

    In Vitro

    GSK 2830371 potently inhibits Wip1 (2-420) dephosphorylation of FDP and the endogenous substrates phospho-p38 MAPK (T180) with IC50 values of 6 nM and 13 nM, respectively. In the PPM1D-amplified MCF7 breast carcinoma cells, treatment with GSK 2830371 (0.04, 0.11, 0.33, 1, 3, and 9 μM) increased phosphorylation of substrates in a concentration-dependent manner. Treatment of MX-1 and MCF7 cells (Wip1amplified, p53 wild type) with GSK 2830371 (0.001, 0.01, 0.1, 1, and 10 μM) causes concentration-dependent effects in cell growth assays[1]. GSK2830371 has a 50% growth inhibitory concentration (GI50) of 2.65 μM±0.54 (SEM) in MCF-7 cells. Treatment of MCF-7 cells with 2.5μM GSK2830371 results in marked time-dependent degradation of both isoforms of WIP1 over 8 hours which correlated with p53 stabilisation and phospho-p53Ser15 (pp53Ser15)[2].

    In Vivo

    In a pharmacodynamic assay, orally administered GSK 2830371 increases phosphorylation of Chk2 (T68) and p53 (S15) and decreased Wip1protein concentrations in DOHH2 tumors. Following 14 d of oral dosing at 150 mg per kg body weight, BID (twice daily) and TID (thrice daily), GSK 2830371 inhibits the growth of DOHH2 tumor xenografts by 41% and 68%, respectively. Comparable tumor growth inhibition is observed in mice treated BID with either 75 or 150 mg per kg body weight. Greater tumor growth inhibition with the TID schedule is consistent with a short half-life of GSK 2830371 in mice and suggests that sustained inhibition of Wip1 may be required for maximal antitumor effect[1].

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 51 mg/mL (110.62 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1691 mL 10.8455 mL 21.6910 mL
    5 mM 0.4338 mL 2.1691 mL 4.3382 mL
    10 mM 0.2169 mL 1.0846 mL 2.1691 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Kinase Assay
    [1]

    The primary in vitro Wip1 enzymatic assay measured fluorescence generated by Wip-1 (2-420) hydrolysis of fluorescein diphosphate (FDP). 50 μM FDP substrate is added with GSK 2830371 or DMSO at room temperature before addition of 10 nM Wip1 in assay buffer (50 mM TRIS, pH 7.5, 30 mM MgCl2, 0.8 mM CHAPS, 0.05 mg/mL BSA). Fluorescent signal is detected on a Spectramax microplate reader (485/530 nm)[1].

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

    Cell Assay
    [1]

    Cells are seeded into 96 well plates at 200-400 cells per well and treated with GSK 2830371 dilution series on day 1. After 7 d, we used the CellTiter-Glo cell viability assay to determine effects on cell growth. Luminescent signal is detected on an EnVision 2104. For clonogenic assays, cells are seeded in 12-well tissue culture plates at 2,000 cells per well. Cells are treated with a compound dilution series on day 1 and again on day 7. After 14 d, cells are washed with 1× PBS, stained with 1 mL of Coomassie Brilliant Blue R-250, and colonies are quantitated with the Optomax Sorcerer colony counter[1].

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

    Animal Administration
    [1]

    Mice[1]
    Female SCID mice are subcutaneously inoculated with 1×107 DOHH2 cells and tumor growth is monitored with electronic calipers. When tumors reached 100-200 mm3, animals are treated orally twice (BID) or thrice (TID) daily with vehicle (2% DMSO and 40% Captisol, pH 4.0) or GSK 2830371. For efficacy studies, eight mice per group are administered with GSK 2830371 at 75 or 150 mg per kg body weight BID or 150 mg per kg body weight TID. Tumor growth inhibition (% difference in tumor growth compared to control) is calculated when tumors for vehicle-control mice exceeded 1,000 mm3 (day 11). For pharmacodynamic biomarker analysis, DOHH2 tumors from three mice are harvested 2 or 4 h after final dose following 14 d of treatment with either vehicle or GSK 2830371 at 75 or 150 mg per kg body weight, BID; tumors are frozen in liquid nitrogen for subsequent lysis and western blot analysis.

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

    References
    Molecular Weight

    461.02

    Formula

    C₂₃H₂₉ClN₄O₂S

    CAS No.

    1404456-53-6

    SMILES

    ClC1=CN=C(C)C(NCC2=CC=C(C(N[[email protected]@H](CC3CCCC3)C(NC4CC4)=O)=O)S2)=C1

    Shipping

    Room temperature in continental US; may vary elsewhere

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    Product Name:
    GSK 2830371
    Cat. No.:
    HY-15832
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    GSK 2830371

    Cat. No.: HY-15832