GSK 2830371

SKU: orb1300696

Description

GSK 2830371

Research Area

Metabolism Research

Key Properties

• CAS Number: 1404456-53-6
• MW: 461.02
• Purity: 99.85%
• Formula: C₂₃H₂₉ClN₄O₂S
• SMILES: Cc1ncc(Cl)cc1NCc1ccc(s1)C(=O)N[C@@H](CC1CCCC1)C(=O)NC1CC1
• Target: Phosphatase
• Solubility: Ethanol:23.1 mg/mL (50.11 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.34 mM);DMSO:46.1 mg/mL (100 mM)

Bioactivity

• Target IC50:
  Wip1 phosphatase:6 nM
• In Vivo:
  in vivo GSK2830371 increases phosphorylation of Chk2 (T68) and p53 (S15) and decreases Wip1 protein concentration in DOHH2 tumors. GSK2830371 (150 mg/kg p.o.) also inhibit the growth of DOHH2 tumor xenografts via Inhibition of Wip1.
• In Vitro:
  I the PPM1D-amplified MCF7 breast carcinoma cells, GSK2830371 increase the phosphorylation of multiple Wip1 substratees, including p53 (S15), Chk2 (T68), H2AX (S139) and ATM (S1981). GSK2830371 shows Selective ant Proliferative 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 ant Proliferative 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: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

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

Compound Identifiers

PubChem CID

70983932