CR-1-31-B T38753

Product Introduction
Bioactivity


英文名: CR-1-31-B

描述: CR-1-31-B, a synthetic rocaglate, acts as a highly potent inhibitor of eIF4A. By disrupting the interaction between eIF4A and RNA, it effectively obstructs the initiation phase of protein synthesis. Specifically, CR-1-31-B interferes with the association between Plasmodium falciparum eIF4A (PfeIF4A) and RNA. Additionally, CR-1-31-B induces apoptosis in neuroblastoma and gallbladder cancer cells [4].

体外活性: CR-1-31-B (100 nM; 24 hours) inhibits MUC1-C translation in MCF-10A cells (EGF-stimulated)[1]. CR-1-31-B (10 and 100 nM) decreases MUC1-C abundance in MDA-MB-468 breast cancer cells[1]. CR-1-31B sensitizes gallbladder cancer cells to TRAIL-mediated apoptosis through the translational downregulation of c-FLIP[2]. Neuroblastoma (NB) cell lines exhibit decreased viability, increased apoptosis rates as well as changes in cell cycle distribution when treated with the synthetic rocaglate CR-1-31-B (24-72 hours), which clamps eIF4A and eIF4F onto mRNA, resulting in a translational block[4]. CR-1-31-B (100 nM; 5 hours) treatment increases reverse glutamine metabolism in pancreatic cancer cells[5]. Western Blot Analysis[1]Cell Line: MCF-10A cells (EGF-stimulated) Concentration: 100 nM Incubation Time: 24 hours Result: Blocked increases in MUC1-C abundance. Cell Viability Assay[4]Cell Line: SH-SY5Y cells and Kelly cells Concentration: 0.1-100 nM Incubation Time: 24-72 hours Result: A significant decrease in SH-SY5Y viability was observed at 10 nM for all time points. Significantly decreased the viability of Kelly cells at 5 nM. The calculated IC 50 at 48 h was 20 nM for SH-SY5Y and 4 nM for Kelly cells. Apoptosis Analysis[4]Cell Line: SH-SY5Y and Kelly cells Concentration: SH-SY5Y cells were treated with 10, 20, and 50 nM and Kelly cells with 1, 5, and 10 nM Incubation Time: 24-72 hours Result: Triggered apoptosis.

体内活性: CR-1-31-B (2 mg/kg in 60 μL olive oil; IP; once every 2 days for 28 days) reduces the growth and initiates TRAIL-induced apoptosis in a BALB/c nude mice model of gallbladder cancer cells (GBC)[2]. CR-1-31-B (0.2?mg/kg; IP; daily for 7 days; murine orthotopic transplant model of pancreatic ductal adenocarcinoma) effectively inhibits protein synthesis and growth of pancreatic tumours[5].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: CR-1-31-B | CR 1 31 B | CR131B

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途