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Submit ReviewAX 15836
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)
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 (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 for AX 15836
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.
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.
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 Data 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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Product Datasheets for AX 15836
References for AX 15836
References are publications that support the biological activity of the product.
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. Sci.Adv. 3 e1700898 PMID: 28835924
If you know of a relevant reference for AX 15836, please let us know.
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Keywords: AX 15836, AX 15836 supplier, AX15836, potent, selective, ERK5, inhibitors, inhibits, vomocytosis, ERK, 5843, Tocris Bioscience
1 Citation for AX 15836
Citations are publications that use Tocris products. Selected citations for AX 15836 include:
Ignacio et al (2020) CDK8 Fine-Tunes IL-6 Transcriptional Activities by Limiting STAT3 Resident Time at the Gene Loci. Cell Rep 33 108545 PMID: 33357429
Do you know of a great paper that uses AX 15836 from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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
