SB-216763

SKU: orb1304564

Description

SB 216763

Research Area

Cell Biology, Neuroscience, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 280744-09-4
• MW: 371.23
• Purity: >98%
• Formula: C₁₉H₁₂Cl₂N₂O₂
• SMILES: O=C1C(C=2C=3C(N(C)C2)=CC=CC3)=C(C(=O)N1)C4=C(Cl)C=C(Cl)C=C4
• Target: Kinase
• Solubility: Soluble in DMSO (up to 25 mg/ml).

Bioactivity

• Target IC50:
  GSK-3α:34.3 nM|GSK-3β:34.3 nM
• In Vivo:
  In human liver cells, SB-216763 stimulates glycogen synthesis with an EC50 of 3.6 μM. In HEK293 cells, it dose-dependently induces the transcription of β-catenin-LEF/TCF-associated reporter genes, with a 2.5-fold increase at 5 μM. In cerebellar granule neurons, SB-216763 protects against cell apoptosis induced by LY-294002 or potassium deprivation, showing a concentration-dependent effect with maximum neuronal protection at 3 μM. Additionally, SB-216763 at 3 μM completely inhibits the LY-294002-induced apoptosis of chick dorsal root ganglion sensory neurons. At 10 μM, SB-216763 effectively inhibits both GSK-3α and glycogen synthase kinase-3 (96%), with minimal activity against 24 other protein kinases, including PKBα and PDK1 (IC50 > 10 μM). In prostate cancer cell lines, including MIA-PaCa2, BXPC-3, PANC1, ASPC1, and CFPAC, SB-216763 (25-50 μM) reduces cell viability in a dose-dependent manner and significantly promotes apoptosis, reaching 50% after 72 hours of treatment, without affecting HMEC or WI38 cell lines.
• In Vitro:
  SB-216763 significantly reduces bleomycin-induced alveolar damage by inhibiting injury to alveolar epithelial cells. In mice with bleomycin-induced pulmonary inflammation and fibrosis, SB-216763 (20 mg/kg) notably suppresses lung inflammation and fibrosis and significantly increases the lifespan of mice treated with bleomycin. This effect is achieved through the substantial inhibition of the inflammatory cytokines MCP-1 and TNF-α.
• Cell Research:
  Cells are exposed to various concentrations of SB 216763 for 24, 48 and 72 hours. Relative cell viability is measured using the MTS assay. Apoptotic cells are determined by staining with Hoechst.(Only for Reference)

Storage & Handling

• Storage: RT
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SB216763, SB-216763, SB 216763, Autophagy, Inhibitor, GSK3, GSK-3, GSK-3β, GSK-3α, Glycogen synthase kinase-3, Glycogen synthase kinase 3, inhibit

Compound Identifiers

PubChem CID

176158