| CAS: | 264218-23-7 | ||
| 分子式: | C16H10ClN3O5 | ||
| 分子量: | 359.72 | ||
| 英文名称: |
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| 用途: | SB415286是一种有效的GSK3α抑制剂，IC50/Ki为78 nM/31 nM，也等效抑制GSK-3β。SB 415286以ATP竞争的方式抑制GSK3α，Ki为31 nM，并且对GSK3β表现出相似的效能。SB 415286对24种其他蛋白激酶几乎没有活性，IC50>10 μ M。SB 415286刺激Chang人肝细胞系中糖原合成，EC50为2.9 μM，并诱导HEK293细胞中β-连环蛋白-LEF/TCF调节的报告基因表达。[1] SB 415286剂量依赖性保护培养基中中枢和外周神经系统的神经元免于PI3激酶通路活性降低诱导的死亡，这与GSK-3活性的抑制和GSK-3底物tau与β-连环蛋白的调节相关。[2]在L6肌小管中，与insulin (4.2-倍)或Li (4-倍)相比，SB 415286能够诱导更强的GS (6.8-倍)活化。[3] SB 415286 (10 μM)抑制rapamycin诱导的细胞周期蛋白D1的下调，并阻断rapamycin和paclitaxel诱导的细胞凋亡，表明GSK3β在rapamycin介导的paclitaxel敏化作用中具有重要作用。[4] SB 415286通过稳定β-连环蛋白，以剂量依赖的方式防止柯萨基病毒诱导的细胞死亡。[5] SB 415286对B65大鼠神经母细胞瘤细胞和神经元中过氧化氢诱导的细胞死亡具有保护作用， 而锂不会减弱过氧化氢的毒性作用。[7] SB 415286治疗增强HepG2细胞中TRAIL- 和CH-11诱导的细胞凋亡。[8] SB 415286对GSK-3的抑制通过内源性途径的激活，引起多发性骨髓瘤(MM)细胞生长抑制和细胞凋亡。[9] SB 415286降低Neuro-2A细胞的活性，并诱导细胞累积在细胞周期的G2/M期，随后细胞凋亡。[10] |
| 货号 | 品牌 | 产品名称 | 规格 | 包装、参考价格 | 详情 | ||||||||||||||||||||||||||||||||||||||||
| S873244 | MACKLIN | SB415286 | 99% | 554元/10mg; 2888元/100mg; 4621元/250mg; 10165元/1g; | 展开 | ||||||||||||||||||||||||||||||||||||||||
储存：-20℃ 状态：粉末 | |||||||||||||||||||||||||||||||||||||||||||||
| S797480 | MACKLIN | SB415286 | 10mM in DMSO | 783元/1ml; | 展开 | ||||||||||||||||||||||||||||||||||||||||
储存：-20°C | |||||||||||||||||||||||||||||||||||||||||||||
| S3567 | Sigma-Aldrich | SB 415286 | ≥98% (HPLC) | 2085.96元/5 MG; 6684.85元/25 MG; | 展开 | ||||||||||||||||||||||||||||||||||||||||
产品说明 应用 SB 415286 was used to treat neuroblastoma cells and study the effect of GSK-3 inhibition on cell proliferation. 包装 5, 25 mg in glass bottle 生化/生理作用 SB 415286 is a small molecule inhibitor of GSK-3 in muscle and fat cells. SB 415286 induces activation of glycogen synthase and regulates the transport glucose. SB 415286 reduces the systemic inflammation induced by endotoxic shock in rat model of acute colitis. It increases the axonal growth and promotes the recovery of injured adult CNS neurons. SB 415289 is implicated in inducing chromosome instability when used as therapeutic agents. 特点和优势 This compound is featured on the GSK-3 and PKB/Akt pages of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here. 法律信息 Sold for research purposes under agreement from GlaxoSmithKline. 基本信息
产品性质
安全信息
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