GSK2830371

Catalog No.S7573

For research use only.

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

GSK2830371 Chemical Structure

CAS No. 1404456-53-6

Selleck's GSK2830371 has been cited by 7 Publications

Purity & Quality Control

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 NYH0TYNlTnWwY4Tpc44h[XO|YYm= NGXzW4xKdmirYnn0bY9vKG:oIFjpd{11[WepZXSgVHBOOURiKEGgeI8hPDJyIILld4llfWW|KTCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBGe2OqZYLpZ4hq[SClb3zpJGJNOjFiKFTFN{kheEy7c2OgZ4VtdHNidYPpcochSWNvVlXQVGxUMFBrUVXUSnNFVFdvTliyJJN2[nO2cnH0[UwhUUN3ME2wMlA5PjNizszN MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN3OEK4NEc,OjZ|NUiyPFA9N2F-
MCF7 cells NFzZN2tHfW6ldHnvckBie3OjeR?= MYiyOEBp M3TZT2lvcGmkaYTpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:wIH;mJIh2dWGwIF3DSlch[2WubIOgbY5kfWKjdHXkJIZweiB{NDDodpMtKEmFNUC9PU42KM7:TR?= NUXGfFJSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[zOVgzQDBpPkK2N|U5OjhyPD;hQi=>
SF9 M4CzfGZ2dmO2aX;uJIF{e2G7 MnrsOUBucW6| M17FW2lvcGmkaYTpc44hd2ZiaIXtZY4hX2myMTCoNkB1dyB2MkCgdoV{cWS3ZYOpJIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3cz3pcoZm[3SnZDDpcpNm[3RiU1[5JINmdGy|IHHzd4V{e2WmIHHzJIZtfW:{ZYPj[YlvKGSrcHjvd5Bp[XSnIHj5[JJwdHm|aYOgZYZ1\XJiNTDtbY5{KGK7IH\seY9z\XOlZX7j[UBie3OjeTygTWM2OD1yLkCwOu69VQ>? MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjlzNEe0OEc,OjZ7MUS3OFQ9N2F-
Assay
Methods Test Index PMID
Western blot Wip1 / γH2AX / Mdm2 ; p-Chk2 / Chk2 / p-p53 / p53 / p-p38 / p38 / p21 26883108 27991505
Growth inhibition assay Cell viability 27991505
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 (from reference)

Kinase Assay:[1]
  • 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]
  • 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.
Animal Research:[1]
  • Animal Models: Female SCID mice bearing DOHH2 tumor xenografts
  • Dosages: 150 mg/kg BID
  • Administration: p.o.

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

Chemical Information

Molecular Weight 461.02
Formula

C23H29ClN4O2S

CAS No. 1404456-53-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C=C(C=N1)Cl)NCC2=CC=C(S2)C(=O)NC(CC3CCCC3)C(=O)NC4CC4

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

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.

Handling Instructions

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