ERK1/2 inhibitor 9

Names

[ CAS No. ]:
2169302-75-2

[ Name ]:
ERK1/2 inhibitor 9

Biological Activity

[Description]:

ERK1/2 inhibitor 9 (Probe 1) is a covalent ERK1/2 inhibitor. ERK1/2 inhibitor 9 shows sub-micromolar activity in cells (A375 GI50=0.47 μM). ERK1/2 inhibitor 9 causes the downregulation of phospho-ERK1/2. ERK1/2 inhibitor 9 tagged trans-cyclo-octene (TCO) and Tz-Thalidomide (tetrazine tagged Thalidomide) can form the corresponding ERK-CLIPTAC to elicit degradation of ERK1/2[1].

[Related Catalog]:

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

[Target]

ERK1

ERK2


[References]

[1]. Honorine Lebraud, et al. Protein Degradation by In-Cell Self-Assembly of Proteolysis Targeting Chimeras. ACS Cent Sci. 2016 Dec 28;2(12):927-934.  

Chemical & Physical Properties

[ Molecular Formula ]:
C31H32ClN7O3

[ Molecular Weight ]:
586.08

Related Compounds