| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| S408839-1ml |
1ml |
现货  |
|
| 英文别名 | 3-(2,4-dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | SB216763 |
| 生化机理 | SB216763 是一种强效的 GSK-3 选择性抑制剂，对 GSK-3α 的 IC50 值为 34.3 nM，对人类 GSK-3β 的抑制作用也同样有效。SB216763 可激活自噬。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 糖原合酶激酶 3 alpha 抑制剂；糖原合酶激酶 3 beta 抑制剂 |
| 产品介绍 |
SB 216763 SB 216763是有效，选择性和ATP竞争性的 GSK-3 抑制剂，抑制GSK-3α和GSK-3β的 IC50 为34.3 nM。 Information SB216763 is a potent and selectiveGSK-3inhibitor withIC50of 34.3 nM for GSK-3α and equally effective at inhibiting human GSK-3β. SB216763 activatesautophagy. SB 216763 displays similar potency for GSK-3β with 96% inhibition at 10 μM while exhibiting minimal activity against 24 other protein kinases including PKBα and PDK1 with IC50 of >10 μM. SB 216763 stimulates glycogen synthesis in human liver cells with EC50 of 3.6 μM, and induces dose-dependent transcription of a β-catenin-LEF/TCF regulated reporter gene in HEK293 cells with a maximum 2.5-fold induction at 5 μM. SB 216763 protects the cerebellar granule neurones from apoptotic cell death induced by LY-294002 or potassium-deprivation in a concentration-dependent manner, with a maximal neuroprotection at 3 μM in contrast with the effect of lithium chloride at which 10 mM is required. SB 216763 at 3 μM also completely prevents death of chicken dorsal root ganglion sensory neurones induced by LY-294002 regardless of NGF. SB 216763 treatment at 5 μM markedly inhibits the GSK-3-dependent phosphorylation of neuronal-specific microtubule-associated protein tau in cerebellar granule neurones or recombinant tau in HEK293 cells, and induces increased levels of cytoplasmic β-catenin in both cells mimicking the effect of Wnt-mediated inhibition of GSK-3. In pancreatic cancer cell lines including BXPC-3, MIA-PaCa2, PANC1, ASPC1, and CFPAC, SB 216763 treatment at 25-50 μM reduces cell viability in a dose-dependent manner, and leads to significant increase in apoptosis by 50% at 72 hours due to the specific down regulation of GSK-3β, while has no effect in HMEC or WI38 cell lines. In vivo Administration of SB 216763 at 20 mg/kg significantly prevents lung inflammation and the subsequent fibrosis in bleomycin (BLM)-induced pulmonary inflammation and fibrosis model in mice by significantly blocking the production of inflammatory cytokines MCP-1 and TNF-α by macrophages, and significantly improves the survival of BLM-treated mice. SB 216763 treatment causes a significant reduction in BLM-induced alveolitis by inhibiting alveolar epithelial cell damage. cell lines：Breast cancer cells, including MCF-7, HCC1954, MDA-MB-468, and KPL4 Concentrations：Dissolved in DMSO, final concentrations ~50 μM Incubation Time：24, 48, and 72 hours Powder Purity:≥95% |
| IC50 | GSK-3β, IC50: ~34.3 nM |
|---|
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | C[N]1C=C(C2=C1C=CC=C2)C3=C(C(=O)NC3=O)C4=CC=C(Cl)C=C4Cl |
| 分子量 | 371.22 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 46 mg/mL (199.09 mM); Ethanol: 12 mg/mL (51.93 mM); Water: Insoluble; |
|---|
| Concentration | 9-11（mmol/L） |
|---|---|
| NMR Spectrum 1H | Conforms to Structure |
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