GSK2830371, WIP1 phosphatase inhibitor

Product Details

Formal Name: 5-[[(5-Chloro-2-methylpyridin-3-yl)amino]methyl]-N-[(2S)-3-cyclopentyl-1-(cyclopropylamino)-1-oxopropan-2-yl]thiophene-2-carboxamide

Molecular Formula: C₂₃H₂₉ClN₄O₂S

Formula Weight: 461.00

CAS Number: 1404456-53-6

Purity: >97%

Formulation: powder

Solubility: Soluble in DMSO (up to at least 25 mg/ml)

Storage: -20°C

Stability: ≥ 2 years.

Applications

WIP1 phosphatase inhibitor

Functions

Potent allosteric inhibitor of WIP1 phosphatase (IC50 = 6 nM), a negative regulator of the DNA damage response. It displayed no inhibition of 21 other phosphatases. Active in xenograft model DoHH2 B-cell lymphoma.  GSK2830371 in combination with MDM2 inhibitors has been shown to be efficacious in the treatment of various cancers including liver adenocarcinoma, acute myeloid leukemia, and breast. It enhances phosphorylation of the tumor suppressor p53 leading to activation.

Application Procedures

First dissolved in DMSO (up to at least 25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.

Research use only.

Documents

• Datasheet (PDF)
• MSDS (PDF)