cRIPGBM chloride

• CAT Number: I041822
• CAS Number: 2361988-77-2
• Molecular Formula: C26H20ClFN2O2
• Molecular Weight: 446.90
• Purity: ≥95%
• Synonyms: 3-benzyl-1-[(4-fluorophenyl)methyl]-2-methylbenzo[f]benzimidazol-3-ium-4,9-dione;chloride
• InChI: InChI=1S/C26H20FN2O2.ClH/c1-17-28(15-18-7-3-2-4-8-18)23-24(29(17)16-19-11-13-20(27)14-12-19)26(31)22-10-6-5-9-21(22)25(23)30;/h2-14H,15-16H2,1H3;1H/q+1;/p-1
• InChIKey: IHNGETPFBJHWFE-UHFFFAOYSA-M
• SMILES: CC1=[N+](C2=C(N1CC3=CC=C(C=C3)F)C(=O)C4=CC=CC=C4C2=O)CC5=CC=CC=C5.[Cl-]

cRIPGBM chloride, an orally active, proapoptotic derivative. cRIPGBM can be generated from glioblastoma multiforme (GBM) cancer stem cells (CSCs). cRIPGBM(chloride) targets to receptor-interacting protein kinase 2 (RIPK2) to induce caspase 1-dependent apoptosis. cRIPGBM(chloride) suppresses the formation of RIPK2/TAK1 (prosurvival complex), and increases the formation of RIPK2/caspase 1 (proapoptotic complex). cRIPGBM(chloride) exerts potent anti-tumor activity in vivo in animal models[1].
cRIPGBM chloride (0.25 μM; 0-24 h) time-dependently activates caspase 1, caspase 9, and caspase 7, as well as PARP cleavage, in CBM-1 GBM CSCs[1].
cRIPGBM chloride (0.125 μM, 0.25 μM; 24 h) induces cell apoptosis mediated by caspase 1 in CBM-1 GBM CSCs[1].
cRIPGBM chloride (50 mg/kg; p.o.; twice daily for 5 weeks) inhibits tumor growth in patient-derived GBM CSC intracranial xenograft mouse models[1].

Reference

[1]. Lucki NC, et al. A cell type-selective apoptosis-inducing small molecule for the treatment of brain cancer. Proc Natl Acad Sci U S A. 2019 Mar 26;116(13):6435-6440.
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