AX 15836

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Cat.No. 5843 - AX 15836 | C32H40N8O5S
Description: Potent and selective ERK5 inhibitor
Alternative 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
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature
Pathways

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
Storage Store at -20°C
Purity ≥98% (HPLC)
PubChem ID 122705989
InChI Key HTFNVAVTYILUCF-UHFFFAOYSA-N
Smiles CCOC1=C(NC2=NC=C3N(C)C(=O)C4=C(C=CC=C4)N(C3=N2)S(C)(=O)=O)C=CC(=C1)C(=O)N1CCC(CC1)N1CCN(C)CC1

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
1eq. HCl 64.88 100
DMSO 64.88 100
ethanol 64.88 100

Preparing Stock Solutions

The following data is based on the product molecular weight 648.78. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.54 mL 7.71 mL 15.41 mL
5 mM 0.31 mL 1.54 mL 3.08 mL
10 mM 0.15 mL 0.77 mL 1.54 mL
50 mM 0.03 mL 0.15 mL 0.31 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Lin et al (2016) ERK5 kinase activity is dispensable for cellular immune response and proliferation. Proc.Natl.Acad.Sci.U.S.A. 113 11865 PMID: 27679845

Gilbert et al (2017) Vomocytosis of live pathogens from macrophages is regulated by the atypcial MAP kinase ERK5. Science Advances 3 e1700898 PMID:


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Keywords: AX 15836, supplier, AX15836, potent, selective, ERK5, inhibitors, inhibits, vomocytosis, XMD17-109, ERK, Tocris Bioscience

Citations for AX 15836

Citations are publications that use Tocris products.

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Reviews

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Immunology

Immunology Product Listing

A collection of over 190 products for immunology research, the guide includes research tools for the study of:

  • Chemokine and Cytokine Signaling
  • Chemotaxis
  • Complement System
  • Immune Cell Signaling
  • Inflammation
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Neurodegeneration

Neurodegeneration Product Guide

A collection of over 275 products for neurodegeneration research, the guide includes research tools for the study of:

  • Alzheimer's disease
  • Parkinson's disease
  • Huntington's disease
MAPK Signaling

MAPK Signaling Scientific Review

MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.

Pathways for AX 15836

MAPK

MAPK Signaling Pathway

The mitogen-activated protein kinase pathway evokes an intracellular signaling cascade in response to extracellular stimuli such as heat and stress. It can influence cell division, metabolism and survival.

Protocols

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