ERK1/2 inhibitor 10

ERK1/2 inhibitor 10 (Compound 36c) is a potent ERK1 and ERK2 inhibitor (IC50: 0.11 and 0.08 nM respectively) . ERK1/2 inhibitor 10 inhibits ERK1/2 and blocks the phosphorylation expression of their downstream substrates p90RSK and c-Myc. ERK1/2 inhibitor 10 induces cell apoptosis and incomplete autophagy-related cell death. ERK1/2 inhibitor 10 shows potent antitumor efficacy against triple-negative breast cancer and colorectal cancer models harboring BRAF and RAS mutations[1].

Product Specifications

CAS Number

[3056077-07-4]

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-10.html

Solubility

10 mM in DMSO

Smiles

O=C(C1=CC(C2=NC(NC3=CC=NC(C)=C3)=NC=C2Cl)=CS1)N[C@@H](C4=CC=CC=C4)CO

Molecular Formula

C23H20ClN5O2S

Molecular Weight

465.96

References & Citations

[1]Shuai W, et al. Structure-Guided Discovery and Preclinical Assessment of Novel (Thiophen-3-yl) aminopyrimidine Derivatives as Potent ERK1/2 Inhibitors. J Med Chem. 2024 Apr 25;67 (8) :6425-6455.