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BIX02188 {[allProObj[0].p_purity_real_show]}

货号:A665681 Ambeed 开学季,买赠积分,赢豪礼

BIX-02188 is a selective inhibitor of MEK5 with IC50 of 4.3 nM, also inhibits ERK5 catalytic activity with IC50 of 810 nM, and does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2.

BIX02188 化学结构 CAS号:334949-59-6
BIX02188 化学结构
CAS号:334949-59-6
BIX02188 3D分子结构
CAS号:334949-59-6
BIX02188 化学结构 CAS号:334949-59-6
BIX02188 3D分子结构 CAS号:334949-59-6
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BIX02188 纯度/质量文件 产品仅供科研

货号:A665681 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 MEK MEK1 MEK1/2 MEK2 MEK5 其他靶点 纯度
Honokiol {[allProObj[0].p_purity_real_show]}
Mirdametinib ++++

MEK, IC50: 0.33 nM

{[allProObj[0].p_purity_real_show]}
Binimetinib +++

MEK, IC50: 12 nM

{[allProObj[0].p_purity_real_show]}
BI-847325 ++

MEK1, IC50: 25 nM

+++

MEK2, IC50: 4 nM

{[allProObj[0].p_purity_real_show]}
U0126-EtOH +

MEK1, IC50: 0.07 μM

++

MEK2, IC50: 0.06 μM

{[allProObj[0].p_purity_real_show]}
GDC-0623 ++++

MEK1, IC50: 0.13 nM

{[allProObj[0].p_purity_real_show]}
TAK-733 ++++

MEK1, IC50: 3.2 nM

{[allProObj[0].p_purity_real_show]}
Trametinib ++++

MEK1, IC50: 0.92 nM

++++

MEK2, IC50: 1.8 nM

{[allProObj[0].p_purity_real_show]}
Selumetinib +++

MEK1, Kd: 99 nM

MEK1, IC50: 14 nM

+

MEK2, Kd: 530 nM

{[allProObj[0].p_purity_real_show]}
CI-1040 ++

MEK1, IC50: 17 nM

++

MEK2, IC50: 17 nM

{[allProObj[0].p_purity_real_show]}
Myricetin {[allProObj[0].p_purity_real_show]}
Refametinib ++

MEK1, IC50: 19 nM

++

MEK2, IC50: 47 nM

{[allProObj[0].p_purity_real_show]}
Cobimetinib +++

MEK1, IC50: 4.2 nM

{[allProObj[0].p_purity_real_show]}
PD98059 +

MEK1, IC50: 2 μM

{[allProObj[0].p_purity_real_show]}
SL327 +

MEK1, IC50: 0.18 μM

+

MEK2, IC50: 0.22 μM

AP-1 {[allProObj[0].p_purity_real_show]}
PD318088 {[allProObj[0].p_purity_real_show]}
AZD8330 +++

MEK1/2, IC50: 7 nM

{[allProObj[0].p_purity_real_show]}
Pimasertib {[allProObj[0].p_purity_real_show]}
(E/Z)-BIX02189 ++++

MEK5, IC50: 1.5 nM

{[allProObj[0].p_purity_real_show]}
(E/Z)-BIX02188 +++

MEK5, IC50: 4.3 nM

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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

BIX02188 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].

BIX02188 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.

BIX02188 实验方案

计算器
存储液制备 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

BIX02188 技术信息

CAS号334949-59-6
分子式C25H24N4O2
分子量 412.484
别名
运输蓝冰
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
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