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 is a potent and selective cell-permeable, ATP-competitive GSK3α inhibitor with an IC50 and a Ki of 78 and 31 nM, respectively. SB 415286 competes with ATP. SB 415286 has minimal activity against 24 other protein kinases (IC50 > 10 μ M). SB 415286 stimulates glycogen synthesis, gene transcription and is neuroprotective. As a result of GSK3 inhibition, SB 415286 stimulates glycogen synthesis in the Chang human liver cell line with an EC50 value of 2.9 µM. SB 415286 also protects primary neurons from death induced by the PI3-kinase pathway. In L6 myotubes, SB 415286 induced a much greater activation of GS (6.8-fold) . In adipocytes, SB 415286 caused a comparable activation of GS despite a substantial differentiation-linked reduction in GSK3 expression ( approximately 85%) indicating that GSK3 remains an important determinant of GS activation in fat cells. SB 415286 induced expression of a beta-catenin-LEF/TCF regulated reporter gene in HEK293 cells.
体外实验* | |
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细胞系 | OPM-2, RPMI-8226, U-266, and INA-6 |
方法 | Exposing cells to different concentrations of SB 415286 for 48 or 72 hours in 96-flat well plates. 48 or 72 hours later, [3H]thymidine is added to the cultures (10 μCi/well) for the last 12 hours. Using a top count β-counter to evaluate the [3H]thymidine incorporation by scintillation counting .Assessing apoptosis by annexin V/Propidium Iodide staining or by detection of mitochondrial membrane potential. Evaluating cell death by the analysis of Forward/Side scatter fluorescence changes. Fluorescence Activated Cell Sorting (FACS) analysis is performed . |
浓度 | Dissolved in DMSO, final concentrations ~10 μM |
处理时间 | 48, or 72 hours |
*上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。
体内实验* | |
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动物模型 | Male Wistar rats with acute colitis provoked by trinitrobenzene sulphonic acid (TNBS) |
配制 | Dissolved in DMSO |
剂量 | ~1 mg/kg mg/kg |
给药处理 | Administered subcutaneously twice daily |
*上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。
分子量 | 359.72 |
分子式 | C16H10ClN3O5 |
CAS号 | 264218-23-7 |
溶解性(25°C) | DMSO 70 mg/mL |
储存条件 |
粉末型式 -20°C 3年;4°C 2年 溶于溶剂 -80°C 6个月;-20°C 1个月 |
运输方式 | 冰袋运输,根据产品的不同,可能会有相应调整。 |
*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前,需考虑其在不同溶剂中的溶解度限制。
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
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1 mM | 2.7799 mL | 13.8997 mL | 27.7994 mL |
5 mM | 0.556 mL | 2.7799 mL | 5.5599 mL |
10 mM | 0.278 mL | 1.39 mL | 2.7799 mL |
小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 | |
重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km 系数 | 3 | 6 | 12 | 8 | 5 | 20 |
动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
动物 A的Km系数 |
例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。
[2] Yaling Yang, et al. GSK3β regulates ameloblast differentiation via Wnt and TGF-β pathways
[4] Xiaoyu Jiang, et al. A GSK-3β inhibitor protects against radiation necrosis in mouse brain
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