您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > ERK5-IN-4
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
ERK5-IN-4
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ERK5-IN-4图片
CAS NO:1888305-17-6
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
ERK5-IN-4 (compound 34b) 是细胞外信号相关激酶 5 (ERK5) 的选择性抑制剂。ERK5-IN-4 抑制剂在 HEK293 细胞中抑制ERK5全长激酶 和截断ERK5(ERK5ΔTAD) 激酶活性的IC50分别为 77 nM 和 300 nM。
生物活性

ERK5-IN-4 (compound 34b) is a potent and selective inhibitor ofextracellular signal-related kinase 5(ERK5). ERK5-IN-4 inhibitsERK5(full-length) and truncatedERK5(ERK5 ΔTAD) kinase activity in HEK293 cells with anIC50of 77 nM and 300 nM, respectively[1].

IC50& Target

ERK5

 

体外研究
(In Vitro)

ERK5-IN-4 (compound 34b) is selective against MAP3K, p38 (IC50>30 μM) and BRD4 (IC50>20 μM), in contrast to many reported ERK5 inhibitors[1].
ERK5-IN-4 (0-100 μM; 72 h) suppresses ERK5 kinase activity in HEK293 cells and (0-1 μM; 72 h) induces paradoxical activation of ERK5 transcriptional activity, thus resulting in C-terminal transcriptional activation domain (TAD) separated from the nuclear localization sequence (NLS) and results ERK5 nuclear translocation[1].
ERK5-IN-4 inhibits cancer cells with GI50of 19.6 μM (HEK293), 22.3 μM (A498), 25 μM (SJSA-1), 26.6 μM (MDA-MB-231) following a 72 h incubation[1].
ERK5-IN-4 exhibits kinome selectivity Kdof 1.2 μM, 0.29 μM, 0.046 μM, 0.061 μM, 0.18 μM, 0.38 μM, 1.3 μM, 0.42 μM, 0.22 μM, 2.8 μM against ABL1-nonphosphorylated, AURKA, CSF1R, DCAMKL1 (DCLK1), ERK5 (MAPK7), FGFR1, JAK3 (JH1domain-catalytic), KIT, LRRK2, MEK5 (MAP2K5)[1].

Western Blot Analysis[1]

Cell Line:HeLa cells
Concentration:0.01, 0.03, 0.1, 0.3, 1, 3 μM
Incubation Time:1 h
Result:Resulted upper phospho-ERK5 band with EGF stimulation and inhibition.
体内研究
(In Vivo)

ERK5-IN-4 (compound 34b) (p.o.; 10 mg/kg) has low clearance and an oral bioavailability of 42% in the mouse[1].

Animal Model:Pharmacokinetic Parameters for ERK5-IN-4[1]
Dosage:
Administration:
Result:
RouteDose (mg/kg)Cl (mL/min/kg)Vd(L/kg)t1/2(min)BA (%)
i.v.orp.o.10140.68042
分子量

381.19

Formula

C16H11Cl2FN4O2

CAS 号

1888305-17-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.