PeptideDB

cRIPGBM chloride

CAS: 2361988-77-2 F: C26H20ClFN2O2 W: 446.90

cRIPGBM chloride, an orally active, proapoptotic derivative. cRIPGBM can be generated from glioblastoma multiforme (GBM)
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This product is for research use only, not for human use. We do not sell to patients.

Bioactivity 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].
Invitro cRIPGBM(chloride) (0.25 μM;0-24 小时) 时间依赖性地激活半胱天冬酶 1、半胱天冬酶 9 和半胱天冬酶 7,以及 PARP 裂解[1]。cRIPGBM(chloride) (0.125 μM, 0.25 μM;24 小时) 在 CBM-1 GBM CSCs[1] 中诱导 caspase 1 介导的细胞凋亡[1]。 Western Blot Analysis[1] Cell Line:
In Vivo cRIPGBM chloride (50 mg/kg;口服;每天两次,持续 5 周) 在携带患者来源的 GBM CSC 颅内异种移植的小鼠模型再,抑制肿瘤生长[1]。 Animal Model:
Name cRIPGBM chloride
CAS 2361988-77-2
Formula C26H20ClFN2O2
Molar Mass 446.90
Appearance Solid
Transport Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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.