GSK2830371

Catalog No.S7573 Batch:S757305

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Technical Data

Formula

C23H29ClN4O2S
Molecular Weight 461.02 CAS No. 1404456-53-6
Solubility (25°C)* In vitro DMSO 92 mg/mL (199.55 mM)
Ethanol 46 mg/mL (99.77 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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). This compound 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 this chemical results in a synergistic antiproliferative effect in DOHH2 and MX-1 tumor cells.

In vivo

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

Protocol (from reference)

Kinase Assay:

[1]
  • In vitro phosphatase assays

    50 μM FDP substrate with this 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 Assay:

[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 this 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 Study:

[1]
  • Animal Models

    Female SCID mice bearing DOHH2 tumor xenografts

  • Dosages

    150 mg/kg BID

  • Administration

    p.o.

References

  • https://pubmed.ncbi.nlm.nih.gov/24390428/

Selleck's GSK2830371 Has Been Cited by 15 Publications

PPM1D is directly degraded by proteasomes in a ubiquitination-independent manner through its carboxyl-terminal region [ J Biomed Sci, 2025, 32(1):88] PubMed: 40931354
PPM1D is directly degraded by proteasomes in a ubiquitination-independent manner through its carboxyl-terminal region [ Journal of Biomedical Science, 2025, 88]
AMPK phosphorylates WIP1 to promote DNA repair and radioresistance in cancer cells [ Cell Death & Disease, 2025, 864] PubMed: 41315219
NR2F1 is a barrier to dissemination of early stage breast cancer cells [ Cancer Res, 2022, canres.4145.2021] PubMed: 35471456
NR2F1 is a barrier to dissemination of early-stage breast cancer cells [ Cancer Res, 2022, 82 (12): 2313–2326.] PubMed: None
NR2F1 Is a Barrier to Dissemination of Early-Stage Breast Cancer Cells [ Cancer Research, 2022, 2313-2326] PubMed: 35471456
Substrate spectrum of PPM1D in the cellular response to DNA double-strand breaks [ iScience, 2022, 25(9):104892] PubMed: 36060052
CDK5RAP2 loss-of-function causes premature cell senescence via the GSK3β/β-catenin-WIP1 pathway [ Cell Death Dis, 2021, 13(1):9] PubMed: 34930892
WIP1 promotes cancer stem cell properties by inhibiting p38 MAPK in NSCLC [ Signal Transduction and Targeted Therapy, 2020, 36] PubMed: 32296033
WIP1 Promotes Cancer Stem Cell Properties by Inhibiting p38 MAPK in NSCLC [ Signal Transduct Target Ther, 2020, 15;5(1):36] PubMed: 32296033

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.