Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SB 415286 是一种GSK-3α抑制剂,IC50值为 77.5 nM,Ki 值为 30.75 nM。它对人GSK-3α和GSK-3β的抑制效果相同。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 153 | 现货 | ||
2 mg | ¥ 208 | 现货 | ||
5 mg | ¥ 328 | 现货 | ||
10 mg | ¥ 529 | 现货 | ||
25 mg | ¥ 1,060 | 现货 | ||
50 mg | ¥ 1,720 | 现货 | ||
100 mg | ¥ 2,780 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 363 | 现货 |
产品描述 | SB 415286 is a potent GSK3α inhibitor with IC50/Ki of 78 nM/31 nM with equally effective inhibition of GSK-3β. |
靶点活性 | GSK-3α:78 nM, GSK-3β:31 nM(ki) |
体外活性 | SB 415286以Ki为31nM的方式与ATP竞争性抑制GSK3α,并对GSK3β显示出类似的效力。SB 415286对其他24种蛋白激酶几乎没有活性,其IC50 > 10 μM。SB 415286在Chang人肝细胞系中刺激糖原合成,EC50为2.9 μM,并在HEK293细胞中诱导β-连环蛋白-LEF/TCF受控的报告基因表达。[1] SB 415286通过与抑制GSK-3活性和调节GSK-3底物tau和β-连环蛋白相关的方式,浓度依赖性地保护培养中的中枢和周围神经系统神经元免遭因PI3激酶通路活性降低而引起的死亡。[2] 在L6肌管中,SB 415286诱导的GS激活水平(6.8倍)远大于胰岛素(4.2倍)或Li(4倍)引起的激活。[3] SB 415286 (10 μM)抑制雷帕霉素诱导的cyclin D1下调,并阻断了雷帕霉素和紫杉醇诱导的细胞凋亡,提示GSK3β在雷帕霉素介导的紫杉醇增敏中扮演关键角色。[4] SB 415286通过稳定β-连环蛋白的方式,呈剂量依赖性地防止柯萨奇病毒引起的细胞死亡。[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,而锂并不减轻过氧化氢的毒性作用。[7] SB 415286处理增强了TRAIL和CH-11在HepG2细胞中诱导的细胞凋亡。[8] 通过激活内源性途径,SB 415286的GSK-3抑制作用导致多发性骨髓瘤(MM)细胞生长停滞和凋亡。[9] SB 415286降低Neuro-2A细胞的存活率,并诱导细胞在细胞周期的G2/M期积累及随后的凋亡。[10] |
体内活性 | Administration of SB 415286 (~10 mg/kg twice daily) reduces the extent and degree of the trinitrobenzene sulphonic acid (TNBS)-provoked colonic inflammation in the rat, and reduces the fall in body weight, which is related to downregulation of NF-κB activity, involved in the generation of proinflammatory mediators. [6] SB 415286 treatment at 1 mg/kg significantly delays the growth of Neuro-2A cells in vivo in nude mice. [10] |
激酶实验 | GSK-3 activity assay: GSK-3 kinase activity is measured, in the presence of various concentrations of SB 415286, in a reaction mixture containing final concentrations of: 1 nM human GSK3α or rabbit GSK3α; 50 mM MOPS pH 7.0; 0.2 mM EDTA; 10 mM Mg-acetate; 7.5 mM L-mercaptoethanol; 5% (w/v) glycerol; 0.01% (w/v) Tween-20; 10% (v/v) DMSO; 28 μM GS-2 peptide substrate. The GS-2 peptide sequence corresponds to a region of glycogen synthase that is phosphorylated by GSK-3. The assay is initiated by the addition of 0.34 μCi [33P]γ-ATP (IC50 determinations) or 2.7 μCi [33P]γ-ATP (Ki determinations). The total ATP concentration is 10 μM (IC50 determinations) or ranged from 0 to 45 μM (Ki determinations). Following 30 minutes incubation at room temperature the assay is stopped by the addition of one third assay volume of 2.5% (v/v) H3PO4 containing 21 mM ATP. Samples are spotted onto P30 phosphocellulose mats and these are washed six times in 0.5% (v/v) H3PO4. The filter mats are sealed into sample bags containing Wallac betaplate scintillation fluid. 33P incorporation into the substrate peptide is determined by counting the mats in a Wallac microbeta scintillation counter. |
细胞实验 | Cells are exposed to different concentrations of SB 415286 for 48 or 72 hours in 96-flat well plates. After 48 or 72 hours, [3H]thymidine is added to the cultures (10 μCi/well) for the last 12 hours. The [3H]thymidine incorporation is evaluated by scintillation counting by using a top count β-counter. Apoptosis is assessed by annexin V/Propidium Iodide staining or by detection of mitochondrial membrane potential. Cell death is evaluated by the analysis of Forward/Side scatter fluorescence changes. Fluorescence Activated Cell Sorting (FACS) analysis is performed using a FACS-Calibur Cell Cytometer. (Only for Reference) |
别名 | 3-[(3-氯-4-羟苯基)氨基]-4-(2-硝苯基)-1H-吡咯-2,5-二酮, SB415286 |
分子量 | 359.72 |
分子式 | C16H10ClN3O5 |
CAS No. | 264218-23-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 18 mg/mL (50 mM)
Ethanol: 9 mg/mL (25 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.7799 mL | 13.8997 mL | 27.7994 mL | 69.4985 mL |
5 mM | 0.556 mL | 2.7799 mL | 5.5599 mL | 13.8997 mL | |
10 mM | 0.278 mL | 1.39 mL | 2.7799 mL | 6.9498 mL | |
20 mM | 0.139 mL | 0.695 mL | 1.39 mL | 3.4749 mL | |
DMSO | 50 mM | 0.0556 mL | 0.278 mL | 0.556 mL | 1.39 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
SB 415286 264218-23-7 Apoptosis PI3K/Akt/mTOR signaling Stem Cells GSK-3 inhibit 3-[(3-氯-4-羟苯基)氨基]-4-(2-硝苯基)-1H-吡咯-2,5-二酮 Inhibitor Glycogen synthase kinase 3 Glycogen synthase kinase-3 SB415286 SB-415286 inhibitor