1. MAPK/ERK Pathway Stem Cell/Wnt
  2. ERK
  3. AX-15836

AX-15836 

Cat. No.: HY-101846 Purity: 99.41%
COA Handling Instructions

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

For research use only. We do not sell to patients.

AX-15836 Chemical Structure

AX-15836 Chemical Structure

CAS No. : 2035509-96-5

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 214 In-stock
Solution
10 mM * 1 mL in DMSO USD 214 In-stock
Solid
5 mg USD 150 In-stock
10 mg USD 220 In-stock
25 mg USD 380 In-stock
50 mg USD 540 In-stock
100 mg USD 760 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

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Description

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

IC50 & Target[1]

ERK5

8 nM (IC50)

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[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

648.78

Formula

C32H40N8O5S

CAS No.
Appearance

Solid

Color

Off-white to yellow

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

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

Preparing
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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (3.85 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (3.85 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (3.85 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.68%

References
Cell Assay
[1]

For proliferation studies, cells are treated with eight-point serial dilution series of AX-15836 (starting concentration of 15 μM) or with DMSO vehicle (0.25% final volume). For MM.1S cells, compound was added 1 h before adding recombinant human IL-6 at 5 nM. After 3 d, the relative number of viable cells was measured via quantitation of ATP using CellTiter-Glo 2.0 reagent. Luminescence was read on the Synergy 2 multimode reader[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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AX-15836 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
AX-15836
Cat. No.:
HY-101846
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