| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| T408478-1ml |
1ml |
现货  |
|
| 英文别名 | 6,7-Bis(3-hydroxyphenyl)pteridine-2,4-diamine |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | TG100-115 |
| 生化机理 | TG100-115 是一种 PI3Kγ/δ 抑制剂，IC50 为 83 nM/235 nM，对 PI3Kα/β 几乎没有影响。1/2阶段。 |
| 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 | PI3 激酶 p110-delta 亚基抑制剂 |
| 产品介绍 |
TG100-115是PI3K γ和δ抑制剂，IC50分别为83和235 nM。A PI3K and FRAP inhibitor with some action against Akt Information TG100-115 is aPI3Kγ/δinhibitor withIC50of 83 nM/235 nM, with little effect on PI3Kα/β. Phase 1/2. TG100-115 inhibits PI3Kγ and -δ, with IC50 of 83 and 235 nM, respectively. TG100-115 is not active for PI3Kα and -β, with IC50 of 1.2 and 1.3 mM. In human umbilical vein endothelial cells (HUVECs), TG100-115 (up to 10 μM) has no effects on cell proliferation and VEGF-stimulated ERK phosphorylation. However, TG100-115 (10 μM) interrupts other VEGF signaling pathways, such as those that culminate in VE-cadherin phosphorylation. In HUVECs, TG100-115 (10 μM) inhibits the VEGF-induced increase of total level of VE-cadherin. TG100-115 inhibits VEGF mediated phosphorylation of mTOR and p70S6 kinase, both of which are downstream of PI3K. TG100-115 (125 nM to 10 μM) also inhibits FGF-stimulated phosphorylation of Akt. In vivo In Miles assay models, TG100-115 (1-5 mg/kg) reduces edema formation and inflammation in rats. In rigorous rodent and porcine models of myocardial ischemia (MI), TG100-115 (0.5-5 mg/kg) provides potent cardioprotection, limits infarct development, and preserves myocardial function. In mice, TG100-115 (5 mg/kg) markedly diminishes vascular permeability (VP) in response to either Sema3A or VEGF, indicating that both factors may depend on PI3Kγ/δ to induce VP. In a mouse asthma model, aerosolized TG100-115 markedly reduces the pulmonary eosinophilia, inhibits interleukin-13 and mucin accumulation. cell lines： Concentrations：10 μM, dissolved in DMSO as stock solution Incubation Time：24, 48, and 72 hours Powder Purity:≥99% |
| IC50 | PI3Kδ, IC50: 235 nM |
|---|
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | NC1=NC2=NC(=C(N=C2C(=N1)N)C3=CC(=CC=C3)O)C4=CC=CC(=C4)O |
| 分子量 | 346.34 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 92 mg/mL (199.37 mM); Water: Insoluble; Ethanol: Insoluble; |
|---|
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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