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

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
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 USD 214 In-stock
Solution
10 mM * 1 mL in DMSO USD 214 In-stock
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5 mg USD 150 In-stock
10 mg USD 220 In-stock
25 mg USD 380 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

AX-15836 Related Antibodies

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ERK ERK1 ERK2 ERK5 ERK8

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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.

AX-15836 Related Antibodies
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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.68%

COA (252 KB) LCMS (122 KB)

Handling Instructions (2659 KB)
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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5414 mL 7.7068 mL 15.4135 mL 38.5339 mL
5 mM 0.3083 mL 1.5414 mL 3.0827 mL 7.7068 mL
10 mM 0.1541 mL 0.7707 mL 1.5414 mL 3.8534 mL
15 mM 0.1028 mL 0.5138 mL 1.0276 mL 2.5689 mL
20 mM 0.0771 mL 0.3853 mL 0.7707 mL 1.9267 mL
25 mM 0.0617 mL 0.3083 mL 0.6165 mL 1.5414 mL
30 mM 0.0514 mL 0.2569 mL 0.5138 mL 1.2845 mL
40 mM 0.0385 mL 0.1927 mL 0.3853 mL 0.9633 mL
50 mM 0.0308 mL 0.1541 mL 0.3083 mL 0.7707 mL
60 mM 0.0257 mL 0.1284 mL 0.2569 mL 0.6422 mL
80 mM 0.0193 mL 0.0963 mL 0.1927 mL 0.4817 mL
100 mM 0.0154 mL 0.0771 mL 0.1541 mL 0.3853 mL
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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.

Keywords:

AX-158362035509-96-5AX15836AX 15836ERKExtracellular signal regulated kinasesInhibitorinhibitorinhibit

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