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GSK 2830371

Catalog No. T6521 CAS 1404456-53-6

Synonyms: GSK2830371

GSK 2830371 is an orally active, allosteric Wip1 phosphatase inhibitor with IC50 of 6 nM.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

GSK 2830371, CAS 1404456-53-6

Pack Size	Availability	Price/USD
5 mg	In stock	$ 48.00
10 mg	In stock	$ 82.00
25 mg	In stock	$ 153.00
50 mg	In stock	$ 267.00
100 mg	In stock	$ 447.00
1 mL * 10 mM (in DMSO)	In stock	$ 48.00

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Purity: 99.3%

Biological Description

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Description	GSK 2830371 is an orally active, allosteric Wip1 phosphatase inhibitor with IC50 of 6 nM.
Targets&IC50	Wip1 phosphatase: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]
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]
Kinase Assay	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	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)

Synonyms	GSK2830371
Molecular Weight	461.02
Formula	C23H29ClN4O2S
CAS No.	1404456-53-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 46.1 mg/mL (100 mM)

Ethanol: 23.1 mg/mL (50 mM)

References and Literature

1. Gilmartin AG, et al. Nat Chem Biol. 2014, 10(3), 181-187

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Metabolism Compound Library NO PAINS Compound Library Bioactive Compounds Library Max Glycometabolism Compound Library Bioactive Compound Library Phosphatase Inhibitor Library

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Keywords

GSK 2830371 1404456-53-6 Metabolism Phosphatase Inhibitor GSK-2830371 GSK2830371 inhibit inhibitor

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