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- 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：
883065-90-5
- 规格：
10 mM * 1 mL/5 mg/10 mg/25 mg/50 mg/100 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥968.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥880.0 |
| 规格： | 10 mg | 产品价格： | ￥1350.0 |
| 规格： | 25 mg | 产品价格： | ￥2850.0 |
| 规格： | 50 mg | 产品价格： | ￥4950.0 |
| 规格： | 100 mg | 产品价格： | ￥8100.0 |
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BI-78D3
CAS No. : 883065-90-5
MCE 国际站：BI-78D3
产品活性：BI-78D3 是一种底物竞争性的 JNK 抑制剂，抑制 JNK 激酶活性，IC50 为 280 nM。
研究领域：MAPK/ERK Pathway
作用靶点：JNK
In Vitro: BI-78D3, dose-dependently inhibits the phosphorylation of JNK substrates both in vitro and in cell. BI-78D3 is able to compete with the D-domain of JIP1 (amino acids 153-163; pepJIP1) for JNK1 binding (IC50=500 nM). Using the same in vitro LanthaScreen kinase assay and the same ATF2 substrate, BI-78D3 is found to be 100-fold less active vs. p38α, a member of the MAPK family with high structural similarity to JNK, and completely inactive against mTOR and PI3-kinase (α-isoform), both unrelated protein kinases. Furthermore, Lineweaver-Burk analysis clearly indicates that BI-78D3 is competitive with ATF2 for binding to JNK1 with an apparent Ki value of 200 nM. In an attempt to profile the properties of BI-78D3 in the context of a complex cellular milieu, the cell-based LanthaScreen kinase assay is used. In this assay BI-78D3 is able to inhibit TNF-α stimulated phosphorylation of c-Jun in cell (EC50=12.4 μM).
In Vivo: The link between ConA-induced liver failure, TNF receptor signaling, and JNK function has been established by studies employing JNK1-/- and JNK2-/- mice. For this analysis, insulin insensitive mice are injected only once with 25 mg/kg BI-78D3, 30 min before insulin injection. The effect of insulin on blood glucose levels is then measured. BI-78D3 results in a statistically significant reduction in blood glucose levels as compared with the vehicle control. Thus, the ability of BI-78D3 to abrogate ConA-induced liver damage and restore insulin sensitivity is consistent with its proposed function as an effective JNK inhibitor. Liquid chromatography/mass spectrometry bio-availability analysis demonstrates that BI-78D3 has favorable microsome and plasma stability (T1/2=54 min).
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图 UCL（Upper contor limit）=x+A2R=73.25+1.88*2.85=78.10 LCL（Lower contor limit）=x-A2R=67.89 CL（Center limit）=x=73.25 R控制图 UCL=D4R=3.27*2.85=9.32 LCL=D3R=0 Cl=R=2.85 （n为每批检测时应用同浓度质控品的个数） 步骤4.根据一表1及步骤3提供
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