For research use only. Not for therapeutic Use.
ERK1/2 Inhibitor 9 (CAT: I040919) is a covalent inhibitor targeting ERK1/2, key components of the MAPK signaling pathway, which are often dysregulated in various cancers. This compound shows sub-micromolar activity in cellular assays (A375 GI50 = 0.47 μM) and effectively downregulates phospho-ERK1/2, a marker of ERK1/2 activation. Additionally, ERK1/2 Inhibitor 9 is equipped with a trans-cyclo-octene (TCO) and Tz-Thalidomide (tetrazine-tagged Thalidomide), enabling the formation of an ERK-CLIPTAC, a targeted protein degrader. By inducing the degradation of ERK1/2, this compound holds promise for Cancer Disease Research, particularly for cancers driven by aberrant ERK1/2 signaling.
| CAS Number | 2169302-75-2 |
| Synonyms | [(4Z)-cyclooct-4-en-1-yl] N-[4-[4-[[5-chloro-4-[2-(prop-2-enoylamino)anilino]pyrimidin-2-yl]amino]pyridin-2-yl]but-3-ynyl]carbamate |
| Molecular Formula | C31H32ClN7O3 |
| Purity | ≥95% |
| IUPAC Name | [(4Z)-cyclooct-4-en-1-yl] N-[4-[4-[[5-chloro-4-[2-(prop-2-enoylamino)anilino]pyrimidin-2-yl]amino]pyridin-2-yl]but-3-ynyl]carbamate |
| InChI | InChI=1S/C31H32ClN7O3/c1-2-28(40)37-26-15-8-9-16-27(26)38-29-25(32)21-35-30(39-29)36-23-17-19-33-22(20-23)12-10-11-18-34-31(41)42-24-13-6-4-3-5-7-14-24/h2-4,8-9,15-17,19-21,24H,1,5-7,11,13-14,18H2,(H,34,41)(H,37,40)(H2,33,35,36,38,39)/b4-3- |
| InChIKey | MEGBFSKPEJSVCC-ARJAWSKDSA-N |
| SMILES | C=CC(=O)NC1=CC=CC=C1NC2=NC(=NC=C2Cl)NC3=CC(=NC=C3)C#CCCNC(=O)OC4CCCC=CCC4 |
