AX-15836

AX-15836 is a potent and selective ERK5 inhibitor with an IC50 of 8 nM.

Product information

CAS Number: 2035509-96-5

Molecular Weight: 648.78

Formula: C32H40N8O5S

Chemical Name: 5-({2-ethoxy-4-[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]phenyl}amino)-2-methanesulfonyl-9-methyl-2, 4, 6, 9-tetraazatricyclo[9.4.0.0, ]pentadeca-1(15), 3, 5, 7, 11, 13-hexaen-10-one

Smiles: CCOC1=CC(=CC=C1NC1=NC2=C(C=N1)N(C)C(=O)C1=CC=CC=C1N2S(C)(=O)=O)C(=O)N1CCC(CC1)N1CCN(C)CC1

InChiKey: HTFNVAVTYILUCF-UHFFFAOYSA-N

InChi: InChI=1S/C32H40N8O5S/c1-5-45-28-20-22(30(41)39-14-12-23(13-15-39)38-18-16-36(2)17-19-38)10-11-25(28)34-32-33-21-27-29(35-32)40(46(4,43)44)26-9-7-6-8-24(26)31(42)37(27)3/h6-11,20-21,23H,5,12-19H2,1-4H3,(H,33,34,35)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 100 mg/mL (154.14 mM; Need ultrasonic)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

AX-15836 shows more than 1, 000-fold selectivity for ERK5 over a panel of over 200 kinases. It also exhibits selectivity over BRD4 with a Kd of 3, 600 nM. AX15836 shows similar intracellular potency (4–9 nM) across all cells tested, including peripheral blood mononuclear cells (PBMCs), endothelial cells, and oncogenic cell lines. AX15836 was completely ineffective (EC50>10 μM) to suppress inflammatory cytokine response, suggesting that it was the BRD inhibition component of the compounds that mediated cytokine reduction. In HUVEC and HeLa cell types, samples treated with AX15836 shows very few genes to be differentially expressed. AX15836 could clearly inhibit the EGF-stimulated, phosphorylated form of ERK5 in HeLa cells.

References:

1. Lin EC, et al. ERK5 kinase activity is dispensable for cellular immune response and proliferation. Proc Natl Acad Sci U S A. 2016 Oct 18;113(42):11865-11870.

Products are for research use only. Not for human use.