GSK2830371

SKU: orb1300696

Description

GSK 2830371 is a potent, cell-permeable allosteric inhibitor of the Wip1 phosphatase, exhibiting an IC50 of 6 nM. It is utilized in cancer research to study p53-dependent pathways and has demonstrated antitumor activity in preclinical in vivo models of various cancers.

Research Area

Metabolism Research

Key Properties

• CAS Number: 1404456-53-6
• MW: 461.0
• Purity: >97%
• Formula: C₂₃H₂₉ClN₄O₂S
• SMILES: Cc1ncc(Cl)cc1NCc1ccc(s1)C(=O)N[C@@H](CC1CCCC1)C(=O)NC1CC1
• Target: Phosphatase
• Solubility: Soluble in DMSO (up to at least 25 mg/ml)

Bioactivity

• Target IC50:
  Wip1 phosphatase:6 nM
• 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.
• 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.
• 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)

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GSK2830371, GSK-2830371, GSK 2830371, inhibit, Inhibitor, Wip1 phosphatase, Phosphatase

Compound Identifiers

PubChem CID

70983932