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ERK Inhibitor

Names

[ CAS No. ]:
1049738-54-6

[ Name ]:
ERK Inhibitor

[Synonym ]:
(5Z)-3-(2-Aminoethyl)-5-(4-ethoxybenzylidene)-1,3-thiazolidine-2,4-dione hydrochloride (1:1)
erk inhibitor
2,4-Thiazolidinedione, 3-(2-aminoethyl)-5-[(4-ethoxyphenyl)methylene]-, (5Z)-, hydrochloride (1:1)

Biological Activity

[Description]:

ERK-IN-4 is an ERK inhibitor binds preferentially to ERK2 with a Kd of 5 μM. ERK-IN-4 specificity inhibits ERK Rsk-1 and Elk-1 phosphorylation. ERK-IN-4 has little effect on ERK protein phosphorylation by its upstream activator MEK1/2[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> MAPK/ERK Pathway >> ERK
Signaling Pathways >> Stem Cell/Wnt >> ERK

[Target]

ERK2:5 μM (Kd)


[In Vitro]

ERK-IN-4（化合物 76；10-75 µM；10 天）完全抑制细胞增殖，并减少细胞集落数量[1]。 ERK-IN-4（化合物 76；100 µM）抑制 ERK 介导的 Thr573 上 Rsk-1 磷酸化和 ERK 介导的 HeLa 细胞中的 Elk-1 磷酸化[1]。 Cell Proliferation Assay[1] Cell Line: HeLa, A549, or SUM-159 cells Concentration: 10 µM, 20 µM, 30 µM, 40 µM, 150 µM for A549, or SUM-159 cells; 25 µM, 50 µM, 75 µM for HeLa cells Incubation Time: 10 days Result: Completely inhibited cell proliferation.

[References]

[1]. Chad N Hancock, et al. Identification of novel extracellular signal-regulated kinase docking domain inhibitors. J Med Chem. 2005 Jul 14;48(14):4586-95.  

Chemical & Physical Properties

[ Molecular Formula ]:
C14H17ClN2O3S

[ Molecular Weight ]:
328.814

[ Exact Mass ]:
328.064850

[ PSA ]:
97.93000

[ LogP ]:
3.52050

[ Storage condition ]:
-20°C

Related Compounds