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GSK 2830371

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Purity:99.3%

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COA HNMR HPLC

GSK 2830371

Catalog No. T6521Cas No. 1404456-53-6

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

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Pack Size	Price	Availability
5 mg	$48	In Stock
10 mg	$82	In Stock
25 mg	$153	In Stock
50 mg	$267	In Stock
100 mg	$447	In Stock
1 mL x 10 mM (in DMSO)	$48	In Stock

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Product Introduction

Bioactivity

Description	GSK 2830371 is an orally active, allosteric Wip1 phosphatase inhibitor with IC50 of 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)
Alias	GSK2830371

Chemical Properties

Molecular Weight	461.02
Formula	C23H29ClN4O2S
Cas No.	1404456-53-6

Storage & Solubility Information

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)

Solution Preparation Table

DMSO/Ethanol

	1mg	5mg	10mg	50mg
1 mM	2.1691 mL	10.8455 mL	21.6910 mL	108.4552 mL
5 mM	0.4338 mL	2.1691 mL	4.3382 mL	21.6910 mL
10 mM	0.2169 mL	1.0846 mL	2.1691 mL	10.8455 mL
20 mM	0.1085 mL	0.5423 mL	1.0846 mL	5.4228 mL

DMSO

	1mg	5mg	10mg	50mg
50 mM	0.0434 mL	0.2169 mL	0.4338 mL	2.1691 mL
100 mM	0.0217 mL	0.1085 mL	0.2169 mL	1.0846 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc