ERK1/2 inhibitor 9

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].

Product Specifications

CAS Number

[2169302-75-2]

UNSPSC

12352005

Target

ERK

Type

Reference compound

Related Pathways

MAPK/ERK Pathway; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/erk1-2-inhibitor-9.html

Purity

95.91

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

O=C(NCCC#CC1=NC=CC(NC2=NC=C(C(NC3=C(NC(C=C)=O)C=CC=C3)=N2)Cl)=C1)OC4CC/C=C\CCC4

Molecular Formula

C31H32ClN7O3

Molecular Weight

586.08

References & Citations

[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.