AX 15836

Name: AX 15836
Brand: Tocris Bioscience
SKU: 5843

Tocris Bioscience, part of Bio-Techne | Catalog # 5843

Citations (9)

COA / SDS

Potent and selective ERK5 inhibitor

Key Product Details

Description:	Potent and selective ERK5 inhibitor
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)
Molecular Weight:	648.78

View Full Technical Details for AX 15836

Technical Data
Citations

Biological Activity for AX 15836

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 (K_d = 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.

Compound Libraries for AX 15836

AX 15836 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.

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 for AX 15836

M. Wt	648.78
Formula	C₃₂H₄0N₈O₅S
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	2035509-96-5
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for AX 15836

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

Preparing Stock Solutions for AX 15836

The following data is based on the product molecular weight 648.78.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

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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References for AX 15836

References are publications that support the biological activity of the product.

Gilbert Vomocytosis of live pathogens from macrophages is regulated by the atypcial MAP kinase ERK5. Sci.Adv. 2017 PMID: 28835924
Lin ERK5 kinase activity is dispensable for cellular immune response and proliferation. Proc.Natl.Acad.Sci.U.S.A. 2016 PMID: 27679845