產(chǎn)品描述: | BI-78D3 functions as a substrate competitive inhibitor of JNK, inhibit the JNK kinase activity (IC50=280 nM). |
靶點(diǎn): |
JNK:280 nM (IC50);JNK |
體內(nèi)研究: |
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) |
參考文獻(xiàn): |
1. Stebbins JL et al. Identification of a new JNK inhibitor targeting the JNK-JIP interaction site. Proc Natl Acad Sci U S A, 2008 Oct 28, 105(43):16809-13. |
溶解性: |
DMSO : 100 mg/mL (263.59 mM; Need ultrasonic) |
保存條件: |
-20℃ |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
2.639 ml |
13.193 ml |
26.385 ml |
5 mM |
0.528 ml |
2.639 ml |
5.277 ml |
10 mM |
0.264 ml |
1.319 ml |
2.639 ml |
50 mM |
0.053 ml |
0.264 ml |
0.528 ml |
|
注意: |
部分產(chǎn)品我司僅能提供部分信息,我司不保證所提供信息的權(quán)威性,僅供客戶參考交流研究之用。 |