MedChemExpress - Model cRIPGBM chloride - 2361988-77-2
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].MCE products for research use only. We do not sell to patients.
cRIPGBM chloride
MCE China:cRIPGBM chloride
Brand:MedChemExpress (MCE)
Cat. No.HY-115630
CAS:2361988-77-2
Purity:99.73%
Storage:4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Shipping:Room temperature in continental US; may vary elsewhere.
Description: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.
In Vitro: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].
In Vivo: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].
IC50 & Target:Caspase-1 RIPK2
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References:
[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. [Content Brief]
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