Home Others phosphatase inhibitor GSK2830371 For research use only.

GSK2830371

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

GSK2830371 Chemical Structure

GSK2830371 Chemical Structure

CAS No. 1404456-53-6

Purity & Quality Control

GSK2830371 Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF7 cells Function assay 24 h Inhibition of cell proliferation of human MCF7 cells incubated for 24 hrs, IC50=9.5 μM 26358280
Escherichia coli BL21 (DE3) pLysS cells Function assay Inhibition of His-tagged PPM1D (1 to 420 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) pLysS cells using Ac-VEPPLS(P)QETFSDLW-NH2 substrate, IC50=0.0863 μM 26358280
SF9 Function assay 5 mins Inhibition of human Wip1 (2 to 420 residues) expressed in baculovirus-infected insect SF9 cells assessed as diphosphate hydrolysis after 5 mins by assay, IC50=0.006μM 26914744
Click to View More Cell Line Experimental Data

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 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]
Kinase Assay In vitro phosphatase assays
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 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.
Experimental Result Images Methods Biomarkers Images PMID
Growth inhibition assay Cell viability 27991505
Western blot p-Chk2 / Chk2 / p-p53 / p53 / p-p38 / p38 / p21 Wip1 / γH2AX / Mdm2 27991505
In Vivo
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]
Animal Research Animal Models Female SCID mice bearing DOHH2 tumor xenografts
Dosages 150 mg/kg BID
Administration p.o.

Chemical Information & Solubility

Molecular Weight 461.02 Formula

C23H29ClN4O2S
CAS No. 1404456-53-6 SDF Download GSK2830371 SDF
Smiles CC1=C(C=C(C=N1)Cl)NCC2=CC=C(S2)C(=O)NC(CC3CCCC3)C(=O)NC4CC4
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 92 mg/mL ( (199.55 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 92 mg/mL

Water : Insoluble


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In vivo
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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.

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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.

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