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. |