Catalog Number: 5843
Alternate Names: XMD17-109
Chemical Name: 5,11-Dihydro-2-[[2-ethoxy-4-[[4-(4-methyl-1-piperazinyl)-1-piperidinyl]carbonyl]phenyl]amino]-5-methyl,11-(methylsulfonyl)-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one
Biological Activity
Potent and selective ERK5 inhibitor (IC50 = 8 nM). Exhibits >1,000-fold selectivity for ERK5 over a panel of over 200 kinases. Also exhibits selectivity over bromodomain BRD4 (Kd = 3,600 nM). Increases vomocytosis in human macrophages in vitro, as well as in an in vivo zebrafish model of cryptococcal disease, reducing spread of infection.
External Portal Information
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of AX15836 is reviewed on the chemical probes website.
Technical Data
  • M.Wt:
    648.78
  • Formula:
    C32H40N8O5S
  • Solubility:
    Soluble to 100 mM in 1eq. HCl and to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at -20°C
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. ERK5 kinase activity is dispensable for cellular immune response and proliferation.
    Lin et al.
    Proc.Natl.Acad.Sci.U.S.A., 2016;113:11865
  2. Vomocytosis of live pathogens from macrophages is regulated by the atypcial MAP kinase ERK5.
    Gilbert et al.
    Science Advances, 2017;3:e1700898
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