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AX-15836 is an inhibitor of ERK5 (IC50 : 8 nM).

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $52 | In Stock | In Stock | |
| 2 mg | $74 | In Stock | In Stock | |
| 5 mg | $123 | In Stock | In Stock | |
| 10 mg | $179 | In Stock | In Stock | |
| 25 mg | $313 | In Stock | In Stock | |
| 50 mg | $446 | In Stock | In Stock | |
| 100 mg | $629 | In Stock | In Stock | |
| 500 mg | $1,290 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $176 | In Stock | In Stock |
| Description | AX-15836 is an inhibitor of ERK5 (IC50 : 8 nM). |
| Targets&IC50 | ERK5:8 nM |
| In vitro | 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. AX-15836 shows more than 1,000-fold selectivity for ERK5 over a panel of over 200 kinases and it also shows similar intracellular potency (4–9 nM) across all cells tested, including peripheral blood mononuclear cells (PBMCs), endothelial cells, and oncogenic cell lines. It also exhibits selectivity over BRD4 with a Kd of 3,600 nM. 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]. |
| Molecular Weight | 648.78 |
| Formula | C32H40N8O5S |
| Cas No. | 2035509-96-5 |
| Smiles | CCOc1cc(ccc1Nc1ncc2N(C)C(=O)c3ccccc3N(c2n1)S(C)(=O)=O)C(=O)N1CCC(CC1)N1CCN(C)CC1 |
| Relative Density. | 1.42 g/cm3 (Predicted) |
| Storage | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 100 mg/mL (154.14 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (6.17 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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