BIX02188 - CAS:334949-59-6 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	BIX02188 一键复制产品信息
英文名称:	BIX02188
别名:	(3Z)-3-[[[3-[(二甲基氨基)甲基]苯基]氨基]苯亚甲基]-2,3-二氢-2-氧代-1H-吲哚-6-甲酰胺;BIX02188 国华试剂 (Z)-3-(((3-((dimethylamino)methyl)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxamide
CAS No:	334949-59-6	分子式:	C₂₅H₂₄N₄O₂	分子量:	412.49
CAS No:	334949-59-6
分子式:	C₂₅H₂₄N₄O₂
分子量:	412.49

产品说明书产品使用指南

B10403 BIX02188 ≥98% (普西唐-psaitong)

相关产品

包装规格：

5mg 25mg 100mg in glass bottle

溶解性：

溶于DMSO(≥40mg/mL)

产品描述：

基本信息

产品编号：	B10403
产品名称：	BIX02188
CAS:	334949-59-6	储存条件	粉末	-20℃	四年

分子式：	C25H24N4O2		溶于液体	-80℃	六个月
分子量	412.49			-20℃	一个月
化学名：	(Z)-3-(((3-((dimethylamino)methyl)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxamide
Solubility (25°C)：
体外:	DMSO	≥45mg/mL(109.10mM)
	Ethanol
	Water
体内(现配现用):	1.请依序添加每种溶剂：10% DMSO→40% PEG300→5% Tween-80→45% saline，Solubility:≥1.67mg/mL(4.05mM);Clear solution
	此⽅案可获得≥1.67mg/mL(4.05mM，饱和度未知)的澄清溶液。以1mL⼯作液为例，取100μL16.699999mg/mL的澄清DMSO储备液加到400μL PEG300中，混合均匀；向上述体系中加⼊50μL Tween-80，混合均匀；然后继续加⼊450μL⽣理盐⽔定容⾄1mL。
	2.请依序添加每种溶剂：10% DMSO→90% corn oil Solubility:≥1.67mg/mL(4.05mM);Clear solution
	此⽅案可获得≥1.67mg/mL(4.05mM，饱和度未知)的澄清溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。以1mL⼯作液为例，取100μL16.699999mg/mL的澄清DMSO储备液加到900μL⽟⽶油中，混合均匀。
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	2.4244mL	12.1218mL	24.2436mL
5mM	0.4849mL	2.4244mL	4.8487mL
10mM	0.2424mL	1.2122mL	2.4244mL

生物活性

产品描述

一种MEK5抑制剂。

靶点

MEK5

4.3nM(IC50)

ERK5

810nM(IC50)

CSF1R(FMS)

280nM(IC50)

LCK

390nM(IC50)

KIT

550nM(IC50)

TGFβR1

1.8μM(IC50)

ABL1

2.1μM(IC50)

RPS6KA6(RSK4)

3.2μM(IC50)

RPS6KA3(RSK2)

4.1μM(IC50)

MAPK14(p38alpha)

3.9μM(IC50)

JAK3

7.8μM(IC50)

SRC

8.9μM(IC50)

体外研究

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 0.1-10μM BIX02188 for 30 min, and then stimulated with 300μM 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±1.0μM, and maximal inhibition at concentrations >3μM. To examine the specificity of BIX02188, The effect of 0.1-10μM BIX02188 is measured on the activity of ERK1/2 and JNK. There is no significant inhibition of ERK1/2 and JNK at these concentrations. These observations confirm the selectivity of BIX02188 for MEK5-induced BMK1 phosphorylation . BIX02188 inhibits MEK5 and ERK5 activity, with IC50s of 4.3nM and 810nM, respectively. BIX02188 does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2. BIX02188 inhibits ERK5 phosphorylation in a dose dependent manner. To assess the proliferation of podocytes in response to the pro-fibrotic stimulus of TGFβ1, podocytes are pre-incubated in the presence and absence of BIX02188 (10μM) for 60 min after which cells are co-treated with TGFβ1 (2.5ng/mL) for 48 h to provide adequate time for proliferation to occur and a colorimetric cell proliferation assay is employed where metabolic activity is directly proportional to cell number. Inhibition of Erk5 activation with BIX02188 incubation reduces podocyte cell number. TGFβ1 stimulation increases podocyte cell number which is prevented following BIX02188 co-treatment

推荐实验方法(仅供参考)

Cell Assay

Human podocyte cell lines are treated at 37°C with the growth factor TGFβ1 (2.5ng/mL in serum-free media containing BSA (0.1% w/v)). Inhibitors are applied at 37°C in serum-free media. To diminish Erk5 activation the upstream activator Mek5 is chemically inhibited by BIX02188 (10μM) with an additional 60 min pre-incubation. TGFβ1-mediated signaling is stopped with SB431542 (10μM), targeting the type I TGFβ receptor Alk5, with a further 30 min pre-incubation. Transmembrane receptor-induced Ras function is prevented with an additional 30 min pre-incubation using farnesylthiosalicylic acid (FTS; 10μM). Controls (vehicles) are treated with serum-free media containing DMSO (0.1% v/v) and BSA (0.1% w/v).

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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