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AX-15836

Catalog No.GC31667

AX-15836 es un inhibidor de ERK5 potente y selectivo con una IC50 de 8 nM.

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AX-15836 Chemical Structure

Cas No.: 2035509-96-5

Tamaño Precio Disponibilidad Cantidad
10mM (in 1mL DMSO)
249,00 $
Disponible
2mg
101,00 $
Disponible
5mg
175,00 $
Disponible
10mg
258,00 $
Disponible
25mg
534,00 $
Disponible
50mg
901,00 $
Disponible

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Sample solution is provided at 25 µL, 10mM.

Description Protocol Chemical Properties Product Documents Related Products

AX-15836 is a potent and selective ERK5 inhibitor with an IC50 of 8 nM.

AX-15836 shows more than 1,000-fold selectivity for ERK5 over a panel of over 200 kinases. It also exhibits selectivity over BRD4 with a Kd of 3,600 nM. AX15836 shows similar intracellular potency (4-9 nM) across all cells tested, including peripheral blood mononuclear cells (PBMCs), endothelial cells, and oncogenic cell lines. 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. 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[1].

[1]. Lin EC, et al. ERK5 kinase activity is dispensable for cellular immune response and proliferation. Proc Natl Acad Sci U S A. 2016 Oct 18;113(42):11865-11870.

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