AX-15836

SKU: orb1308620

Description

AX-15836 is a potent and selective ERK5 inhibitor with an IC50 of 8 nM. This small molecule is a valuable research tool for investigating the MAPK7/ERK5 signaling pathway in both cellular and in vivo models of cancer, inflammation, and cardiovascular disease.

Research Area

Signal Transduction

Key Properties

• CAS Number: 2035509-96-5
• MW: 648.78
• Purity: 99.03% (May vary between batches)
• Formula: C₃₂H₄₀N₈O₅S
• SMILES: CCOc1cc(ccc1Nc1ncc2N(C)C(=O)c3ccccc3N(c2n1)S(C)(=O)=O)C(=O)N1CCC(CC1)N1CCN(C)CC1
• Target: ERK
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (6.17 mM);DMSO:100 mg/mL (154.14 mM)

Bioactivity

• Target IC50:
  ERK5:8 nM
• In Vitro:
  AX15836 was completely ineffective (EC50>10 μM) to suppress inflammatory cytokine response, suggesting that it was the BRD inhibition component of the compounds that mediated cytokine reduction. AX-15836 shows more than 1,000-fold selectivity for ERK5 over a panel of over 200 kinases and it also shows similar intracellular potency (4–9 nM) across all cells tested, including peripheral blood mononuclear cells (PBMCs), endothelial cells, and oncogenic cell lines. It also exhibits selectivity over BRD4 with a Kd of 3,600 nM. In HUVEC and HeLa cell types, samples treated with AX15836 shows very few genes to be differentially expressed. AX15836 could clearly inhibit the EGF-stimulated, phosphorylated form of ERK5 in HeLa cells.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, Extracellular signal regulated kinases, ERK5, ERK, AX 15836, AX15836, AX-15836

Compound Identifiers

PubChem CID

122705989