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- 文献和实验
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1443235-95-7
- 规格：
1 mg/5 mg/10 mg/25 mg/50 mg/100 mg
| 规格： | 1 mg | 产品价格： | ￥318.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥700.0 |
| 规格： | 10 mg | 产品价格： | ￥1100.0 |
| 规格： | 25 mg | 产品价格： | ￥2063.0 |
| 规格： | 50 mg | 产品价格： | ￥3300.0 |
| 规格： | 100 mg | 产品价格： | ￥4900.0 |
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JAK3-IN-6
CAS No. : 1443235-95-7
MCE 国际站：JAK3-IN-6
产品活性：JAK3-IN-6 是 JAK3 的一个有效的、选择性的、不可逆的抑制剂，其 IC50 值为 0.15 nM。
研究领域：Epigenetics | Protein Tyrosine Kinase/RTK | JAK/STAT Signaling | Stem Cell/Wnt
作用靶点：JAK
In Vitro: JAK3-IN-6 (compound 2), a potent inhibitor of JAK3 (0.15 nM) is 4300-fold selective for JAK3 over JAK1 in enzyme assays, 67-fold (IL-2 vs. IL-6) or 140-fold (IL-2 vs. EPO or GMCSF) selective in cellular reporter assays and >35-fold selective in human PBMC assays (IL-7 vs. IL-6 or GMCSF). Irreversible JAK3-IN-6 with a JAK1 selective inhibitor 3 (JAK1: 0.96 nM, JAK2: 14 nM, JAK3: >1500 nM, TYK2: 10 nM) are cross titrated to determine if there is an additive or synergistic effect of co-inhibiting JAK1 and JAK3 enzymes on IL-7 signaling in CD3+, CD4+ PBMCs. As shown, the predicted levels of pSTAT5 inhibition based on addition of JAK1 and JAK3 inhibition are very close to the measured effects of cross titrating each compound, demonstrating that there is an additive effect but no synergistic effect of inhibiting JAK1 and JAK3 on blocking STAT5 phosphorylation. Furthermore inhibition of either JAK1 or JAK3 alone is sufficient to fully inhibit pSTAT5.
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文献和实验1. IL-9结构 一、信号通路 IL-9 与异源二聚体受体 IL-9R 结合，并招募 Janus 激酶 JAK1 和 JAK3。磷酸化的 JAK 激酶激活 STAT1 和 STAT5 同源二聚体，以及 STAT1:STAT3 异源二聚体；这些二聚体随后转位进入细胞核并与 DNA 结合，从而调控基因表达。此外，JAK1 还能激活 IRS-1；IRS-1 进而激活依赖于 PI3-K/Akt 的抗凋亡通路，以及调控基因表达的 Ras/MAPK 信号通路。
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