SB 216763

SKU: orb1225442

Description

SB 216763 is a potent, selective, ATP competitive and cell permeable inhibitor GSK-3 with Ki of 9 nM (GSK-3α), equally potent for GSK-3β; displays no significant activity against a panel of 24 other protein kinases; stimulates glycogen synthesis in human liver cells and induces expression of a beta-catenin-LEF/TCF regulated reporter gene in HEK293 cells, protects both central and peripheral nervous system neurones in culture from death, activates beta-catenin-mediated transcription, and enhances the survival of CLL lymphocytes; displays therapeutic properties in a mouse model of pulmonary inflammation and fibrosis.

Key Properties

• CAS Number: 280744-09-4
• MW: 371.2168
• Purity: >98% (HPLC)
• Formula: C₁₉H₁₂Cl₂N₂O₂
• SMILES: O=C(C(C1=CC=C(Cl)C=C1Cl)=C2C3=CN(C)C4=C3C=CC=C4)NC2=O
• Target: GSK-3
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  SB216763 (20 mg/kg, i. v.) significantly improves the survival of BLM-treated mice. Mice randomized to receive BLM plus SB216763 shows a noteworthy reduction, compared with BLM-treated mice. SB216763 (20 mg/kg, i. v.) reduces the magnitude of BLM-induced alveolitis. SB 216763 (0.2 mg/kg, i. v.) with either 17β-E100 or Geni100 significantly reduce infarct size when the rabbits' hearts are submitted to 30-min CAO.
• In Vitro:
  SB-216763 (10-20 μM) induces β-catenin mediated-transcription in a dose-dependent manner in HEK293 cells. SB-216763 (10, 15 and 20 μM) can maintain mESCs with a pluripotent-like morphology in long-term culture. SB-216763 (10 μM) can maintain J1 mESCs in a pluripotent state for more than a month. SB-216763 inhibits GSK-3 with IC50 of 34 nM. SB-216763 is equally effective at inhibiting human GSK-3α and GSK-3β.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SB-216763 | SB216763

Quick Database Links

Gene Symbol

GSK-3