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Home > Phosphatase Inhibitors/Modulators > Wip1 Phosphatase Inhibitor > GSK2830371

GSK2830371

The serine/threonine phosphatase Wip1 plays an important role in tumor development. Despite its aberrant activity characterizing different forms of cancer, selective inhibitors are still lacking. GSK2830371 is an orally active, allosteric Wip1 phosphatase inhibitor with an IC50 of 6 nM. It binds to a flap subdomain that regulates Wip1's enzymatic activity and substrate recognition. Due to lack of this domain in other phosphatases, its binding to GSK2830371 results in a selective and potent inhibition of Wip1. When tested in animal models suffering from a blood cancer (lymphoma), GSK2830371effectively blocked the tumoral growth.

Catalog NO:	CT-GSK283
Synonym:
CAS NO:	1404456-53-6
Mol. Formula:	C₂₃H₂₉ClN₄O₂S
MW:	461.02

** in vivo Quality Material. >99% Pure by Achiral and Chiral HPLCs (attached). Anhydrous, validated by a spot-on quantitative elemental analysis. Bulk stock, prompt.

Pricing and OrderingTechnical Data

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NO	Size	Price	In Stock	Quantity
1	10 mg	$140.00	YES
2	50 mg	$270.00	YES
3	100 mg	$450.00	YES
4	200 mg	$800.00	YES

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Solubility : Soluble in DMSO

Storage : Store at 0°C (short term), -20°C (long term), desiccated

Purity : >99% by Achiral and Chiral HPLCs

Original QC Data : Achiral and Chiral HPLCs, MS, ¹H-NMR, and Quantitative Elemental Analysis Report

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GSK2830371, Current Lot, Certificate of Analysis
C_K, GSK2830371, Lot 01, Achiral HPLC.pdf
C_K, GSK2830371, Lot 01, Chiral HPLC.pdf
C_K, GSK2830371, Lot 01, NMR.pdf

A.G.Gilmartin, et al, Allosteric Wip1 phosphatase inhibition through flap-subdomain interaction, Nature Chemical Biology 10, 181–187 (2014)

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