[CAS NO. 2035509-96-5] AX-15836
PRODUCTS SPECIFICATIONS [2035509-96-5]
DESCRIPTION [2035509-96-5]
Overview
| MDL | MFCD30536368 |
|---|---|
| Molecular Weight | 648.78 |
| Molecular Formula | C32H40N8O5S |
| SMILES | O=C1N(C)C2=CN=C(NC3=CC=C(C(N4CCC(N5CCN(C)CC5)CC4)=O)C=C3OCC)N=C2N(S(=O)(C)=O)C6=CC=CC=C16 |
2 Publications Citing Use of MCE
Summary
AX-15836 is a potent and selective ERK5 inhibitor with an IC 50 of 8 nM.
IC50 & Target
|
ERK5 8 nM (IC 50 ) |
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 K d 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 (EC 50 >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 [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 100 mg/mL ( 154.14 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.5414 mL | 7.7068 mL | 15.4135 mL |
| 5 mM | 0.3083 mL | 1.5414 mL | 3.0827 mL |
| 10 mM | 0.1541 mL | 0.7707 mL | 1.5414 mL |