cRIPGBM chloride

SKU: orb1744761

Description

cRIPGBM chloride is a small molecule that promotes apoptosis in glioblastoma stem cells by targeting RIPK2. It functions as a molecular switch, shifting RIPK2 binding from pro-survival TAK1 complexes to pro-apoptotic caspase-1 complexes. This compound is a useful research tool for studying cell death mechanisms in brain tumor models, both in vitro and in vivo.

Research Area

Cell Biology, Protein Biochemistry, Signal Transduction

Key Properties

• CAS Number: 2361988-77-2
• MW: 446.9
• Purity: 99.75% (May vary between batches)
• Formula: C₂₆H₂₀ClFN₂O₂
• SMILES: [Cl-].O=C1C=2C=CC=CC2C(=O)C3=C1N(C(=[N+]3CC4=CC=C(F)C=C4)C)CC=5C=CC=CC5
• Target: Caspase,RIP kinase,Apoptosis
• Solubility: DMSO:16 mg/mL (35.8 mM)

Bioactivity

• Target IC50:
  GBM CSC cells:68 nM (EC50)
• In Vivo:
  In a mouse model of intracranial GBM CSC tumor xenotransplantation in situ, cRIPGBM chloride (20 mg/kg oral) was found to significantly inhibit tumor formation in vivo.
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• In Vitro:
  cRIPGBM chloride induces Caspase-1 dependent apoptosis by binding to receptor interacting protein kinase 2 (RIPK2) and acting as a molecular switch, EC50 = 68 nM. Thus, the formation of pro-survival RIPK2/TAK1 complex was decreased and the formation of pro-apoptotic RIPK2/caspase 1 complex was increased.
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Storage & Handling

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

Compound Identifiers

PubChem CID

156024495