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Extracellular signal-related protein kinase 5 ERK5 Small Molecule (Collaborative Toolkit)

Invented by Steve Wedge

Info

Antigen/Gene or Protein Targets ERK5
Relevance An inhibitor of extracellular signal-related protein kinase 5 (ERK5). Mitogen/extracellular signal regulated kinase kinase-5 (MEK5) specifically activates ERK5, also known as Big MAP kinase 1 (BMK1). The MEK5/ERK5 pathway is activated by EGF and is required for EGF-induced proliferation and connexin 43 gap junction communication in certain cellular contexts. ERK5 is comprised of 815 amino acids with a unique C-terminal tail containing a myocyte enhancer factor 2 (MEF2)-interacting domain and a potent transcriptional activation domain. ERK5 regulates several transcriptional factors such as MEF2C, c-Fos, Fra-1, Sap-1, cMyc and NFκB.

ERK5 activation has a potential role in tumorigenesis and is implicated in breast, prostate and hepatic cancer. ERK5 also plays a key role in embryogenesis; ERK5 knock-out embryos die between day 9.5 and 11.5 due to a loss of vascular integrity.
Modulatory Function Inhibitor
On Target IC50 A potent inhibitor of ERK5 in enzyme (IC50 = 79 nM) and whole cell (IC50 =970 nM) assays.
Selectivity Tested in the DiscoveRx panel of 456 kinases at a concentration of 10 μM. Seventeen kinases were inhibited by >99% at this concentration, including ERK5, and the S(35) selectivity score ((number of non-mutant kinases with % of control <35)/(number of non-mutant kinases tested)) was 0.205. Ten representative kinases were selected for Kd determinations and the three most sensitive kinases were CSF1R (46nM), DCAMKL1 (61 nM) and ERK5 (180 nM).
Solubility and Solvent 100μM
Molecular Weight (kDa) 381
Cell Permeability Caco2 Papp A2B/B2A (Efflux ratio) = 27/26 (0.94)
Notes Tested in vitro and in vivo.
Research Area Cancer, Cell Signaling & Signal Transduction, Drug Discovery & Development
Relevant Indications Breast cancer
Prostate cancer
Hepatic cancer
Relevant Signalling Pathways ERK5 signaling
MEK5 signaling
Epidermal growth factor (EGF) signaling
Negative Control Available No

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Steve Wedge

Steve Wedge

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