ERK-IN-2 free base

Names

[ CAS No. ]:
2743576-55-6

[ Name ]:
ERK-IN-2 free base

Biological Activity

[Description]:

ERK-IN-2 free base is a ERK2 inhibitor with an IC50 value of 1.8 nM. ERK-IN-2 free base might lead to off-target toxicity and/or off-target activity at dose >10 μM[1].

[Related Catalog]:

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

[Target]

ERK2:1.8 nM (IC50)


[In Vitro]

ERK-IN-2 (ERKi) inhibits RSK phosphorylation with an IC50 of 280 nM[1]. ERK-IN-2 (ERKi, 1 μM) inhibits cell proliferation in cancer cell lines, with IC50 values of 214 nM; 305 nM; 91 nM and 201 nM for A375SM cell, SK-MEL 30 cell; Colo 205 cell and Lovo cell, respectively[1].

[In Vivo]

ERK-IN-2 (1 mpk, p.o.; or 0.5 mpk, i.v.; rat) shows a t1/2 of 0.4 h, and F% of 13%[1].

[References]

[1]. MRK-ERK Inhibitor and Negative Control.

Chemical & Physical Properties

[ Molecular Formula ]:
C16H17N5O2

[ Molecular Weight ]:
311.34

Related Compounds