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BIX02188

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Chemical Structure| 334949-59-6 同义名 : -
CAS号 : 334949-59-6
货号 : A665681
分子式 : C25H24N4O2
纯度 : 98%
分子量 : 412.484
MDL号 : MFCD18157583
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 45 mg/mL(109.1 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Mitogen-activated protein kinases/extracellular signal-regulated kinase (MAPK/ERK) pathway, also known as MEK pathway, is reported to be associated with the cell proliferation, differentiation, migration, senescence and apoptosis[3]. BIX-02188 is a potent MEK5-selective inhibitor with an IC50 of 4.3 nM. BIX02188 inhibits ERK5 catalytic activity, with an IC50 of 810 nM[4]. In activated HeLa cells, BIX-02188 blocks phosphorylation of ERK5, without affecting phosphorylation of ERK1/2, c-Jun amino terminal kinase (JNK) and p38 MAP kinases. Phosphorylated BMK1 (ERK5) is inhibited by BIX-02188 in a dose-dependent manner, with an IC50 of 0.8±1.0 μM, and maximal inhibition at concentrations >3 μM, which confirms the selectivity of BIX-02188 for MEK5-induced BMK1 phosphorylation[5]. When podocytes are pre-incubated in the absence or presence of BIX-02188 (10 μM) for 60 min, Inhibition of Erk5 activation with BIX-02188 incubation reduces podocyte cell number[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.42mL

0.48mL

0.24mL

12.12mL

2.42mL

1.21mL

24.24mL

4.85mL

2.42mL
参考文献

[1]Li L, Tatake RJ, et al. Fluid shear stress inhibits TNF-mediated JNK activation via MEK5-BMK1 in endothelial cells. Biochem Biophys Res Commun. 2008 May 23;370(1):159-63.

[2]Tatake RJ, O'Neill MM, et al. Identification of pharmacological inhibitors of the MEK5/ERK5 pathway. Biochem Biophys Res Commun. 2008 Dec 5;377(1):120-5.

[3]Sun Y, Liu WZ, Liu T, Feng X, Yang N, Zhou HF. Signaling pathway of MAPK/ERK in cell proliferation, differentiation, migration, senescence and apoptosis. J Recept Signal Transduct Res. 2015;35(6):600-4. doi: 10.3109/10799893.2015.1030412. Epub 2015 Jun 22. PMID: 26096166.

[4]Badshah II, Baines DL, Dockrell ME. Erk5 is a mediator to TGFβ1-induced loss of phenotype and function in human podocytes. Front Pharmacol. 2014 Apr 21;5:71. doi: 10.3389/fphar.2014.00071. PMID: 24795631; PMCID: PMC4001011.

[5]Li L, Tatake RJ, Natarajan K, Taba Y, Garin G, Tai C, Leung E, Surapisitchat J, Yoshizumi M, Yan C, Abe J, Berk BC. Fluid shear stress inhibits TNF-mediated JNK activation via MEK5-BMK1 in endothelial cells. Biochem Biophys Res Commun. 2008 May 23;370(1):159-63. doi: 10.1016/j.bbrc.2008.03.051. Epub 2008 Mar 19. PMID: 18358237; PMCID: PMC2435412.

[6]Tatake RJ, O'Neill MM, Kennedy CA, Wayne AL, Jakes S, Wu D, Kugler SZ Jr, Kashem MA, Kaplita P, Snow RJ. Identification of pharmacological inhibitors of the MEK5/ERK5 pathway. Biochem Biophys Res Commun. 2008 Dec 5;377(1):120-5. doi: 10.1016/j.bbrc.2008.09.087. Epub 2008 Oct 1. PMID: 18834865.