BIX02188 是一种有效的选择性 MEK5 抑制剂，IC₅₀ 为 4.3 nM。 BIX02188 也选择性抑制 ERK5 活性, IC₅₀ 为 810 nM。

BIX02188 is a potent MEK5-selective inhibitor with an IC 50 of 4.3 nM. BIX02188 inhibits ERK5 catalytic activity, with an IC 50 of 810 nM.

Solid

MEK5 4.3 nM (IC50) ERK5 810 nM (IC50

BIX02188 is a potent inhibitor of catalytic function of purified, active MEK5 enzyme. In activated HeLa cells, BIX02188 blocks phosphorylation of ERK5, without affecting phosphorylation of ERK1/2, JNK and p38 MAP kinases. To characterize the effects of BIX02188 in cultured endothelial cells (EC), H2O2 is used to activate BMK1. Bovine lung microvascular endothelial cells (BLMECs) are pretreated with 0.1-10 μM BIX02188 for 30 min, and then stimulated with 300 μM H2O2. BMK1 is dramatically activated by H2O2, with peak at 20 min. Phosphorylated BMK1 is inhibited by BIX02188 in a dose-dependent manner, with an IC50=0.8±1.0 μM, and maximal inhibition at concentrations >3 μM. To examine the specificity of BIX02188, The effect of 0.1-10 μM BIX02188 is measured on the activity of ERK1/2 and JNK. There is no

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Li L, 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]. Badshah II, et al. Erk5 is a mediator to TGFβ1-induced loss of phenotype and function in human podocytes. Front Pharmacol. 2014 Apr 21;5:71.

In Vitro: DMSO : ≥ 45 mg/mL (109.10 mM)配制储备液