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.
Shipping Conditions
Blue Ice
Storage Conditions
-20°C (Powder, protect from light)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
ERK1; ERK2
Available Sizes
Frequently Asked Questions
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