GSK2830371

Catalog No.S7573

GSK2830371 Chemical Structure

Molecular Weight(MW): 461.02

GSK2830371 is an orally active, allosteric Wip1 phosphatase inhibitor with IC50 of 6 nM.

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Choose Selective phosphatase Inhibitors

Biological Activity

Description GSK2830371 is an orally active, allosteric Wip1 phosphatase inhibitor with IC50 of 6 nM.
Targets
Wip1 phosphatase [1]
(Cell-free assay)
6 nM
In vitro

In the PPM1D-amplified MCF7 breast carcinoma cells, GSK2830371 increases the phosphorylation of multiple Wip1 substrates, including p53 (S15), Chk2 (T68), H2AX (S139) and ATM (S1981). GSK2830371 shows selective antiproliferative activity in a subset of lymphoid cell lines, all of which carry a wild-type TP53 allele. Furthermore, co-treatment of doxorubicin and GSK2830371 results in a synergistic antiproliferative effect in DOHH2 and MX-1 tumor cells. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Escherichia coli BL21 (DE3) pLysS cells M2HnS2Z2dmO2aX;uJIF{e2G7 MlvZTY5pcWKrdHnvckBw\iCKaYOteIFo\2WmIGDQUVFFKChzIITvJFQzOCC{ZYPp[JVmeyliKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gSZNkcGW{aXPobYEh[2:uaTDCUFIyKCiGRUOpJJBNgXOVIHPlcIx{KHW|aX7nJGFkNV[HUGDMV{hRMVGHVF\TSGxYNU6KMjDzeYJ{fHKjdHWsJGlEPTB;MD6wPFY{KM7:TR?= NX;TeG1xOjZ|NUiyPFA>
MCF7 cells MYLGeY5kfGmxbjDhd5NigQ>? M4LKZlI1KGh? MnzaTY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25ib3[gbJVu[W5iTVPGO{Bk\WyuczDpcoN2[mG2ZXSg[o9zKDJ2IHjyd{whUUN3ME25MlUh|ryP M1H1XFI3OzV6Mkiw

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Growth inhibition assay
Cell viability; 

PubMed: 27991505     


(a) Seven NB cell lines including the established chemoresistant NB cell line LA-N-6, were treated with the indicated concentrations of GSK2830371 for 72 hrs. Cell viability was then assessed by a CCK-8 assay. Each experiment was repeated for six times and data were represented as % vehicle ± S.D. P < 0.05 (*), P < 0.01 (**), or P < 0.001 (***) (Student’s t-test, two-tailed) were indicated. (b) The IC50 values of GSK2830371 on each NB cell line were listed.

27991505
Western blot
p-Chk2 / Chk2 / p-p53 / p53 / p-p38 / p38 / p21 ; 

PubMed: 27991505     


IMR-32, SH-SY5Y and SK-N-AS cells were treated with 50 μM of GSK2830371 for various time points (0–8 hrs), then the cell lysates were subjected to SDS-PAGE, and immunoblotted with the indicated antibodies.

Wip1 / γH2AX / Mdm2 ; 

PubMed: 26883108     


B. MCF7 cells were incubated as in A and analysed by immunoblotting. Staining for TFIIH was used as loading control. Asterisk indicates an unspecific reactivity band. Short exposure (SE) or long exposure (LE) is shown. D. MCF7 cells were incubated with indicated doses of nutlin-3 and GSK2830371 for 1 day and analysed by immunoblotting. Staining for TFIIH was used as loading control. Asterisk indicates an unspecific reactivity band. Short exposure (SE) or long exposure (LE) is shown.

27991505 26883108
In vivo In vivo, GSK2830371 increases phosphorylation of Chk2 (T68) and p53 (S15) and decreases Wip1 protein concentrations in DOHH2 tumors. GSK2830371 (150 mg/kg p.o.) also inhibits the growth of DOHH2 tumor xenografts via inhibition of Wip1. [1]

Protocol

Kinase Assay:[1]
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In vitro phosphatase assays:

The primary in vitro Wip1 enzymatic assay measures fluorescence generated by Wip-1 (2–420) hydrolysis of fluorescein diphosphate (FDP). 50 μM FDP substrate with compound or DMSO is added 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).
Cell Research:[1]
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  • Cell lines: 36 TP53 wild-type cells and 25 TP53 mutant cells
  • Concentrations: ~10 μM
  • Incubation Time: 7 days
  • Method: Cells are seeded into 96 well plates at 200–400 cells per well and treated with a compound dilution series on day 1. After 7 d, The CellTiter-Glo cell viability assay is used to determine effects on cell growth. Luminescent signal is detected on an EnVision 2104.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Female SCID mice bearing DOHH2 tumor xenografts
  • Formulation: 2% DMSO and 40% Captisol, pH 4.0
  • Dosages: 150 mg/kg BID
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 92 mg/mL (199.55 mM)
Ethanol 92 mg/mL warmed (199.55 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+dd H2O
For best results, use promptly after mixing.
10mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 461.02
Formula

C23H29ClN4O2S

CAS No. 1404456-53-6
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID