AX 15836
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
Purity: ≥98%
Biological Activity
AX 15836 is a 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
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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ERK5 kinase activity is dispensable for cellular immune response and proliferation.
Lin et al.
Proc.Natl.Acad.Sci.U.S.A., 2016;113:11865
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Citation for AX 15836
The citations listed below are publications that use Tocris products. Selected citations for AX 15836 include:
1 Citation: Showing 1 - 1
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CDK8 Fine-Tunes IL-6 Transcriptional Activities by Limiting STAT3 Resident Time at the Gene Loci.
Authors: Ignacio Et al.
Cell Rep 2020;33:108545
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