AX-15836

Name: AX-15836
Brand: MedChemExpress
SKU: HY-101846
Rating: 5.0 (4 reviews)

Cat. No.: HY-101846 Purity: 99.41%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 2035509-96-5

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 214	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 214	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 220	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 380	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 540	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 760	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 4 publication(s) in Google Scholar

4 Publications Citing Use of MCE AX-15836

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View All ERK Isoform Specific Products:

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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)

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	IC₅₀	8 nM Compound: 3; AX15836	Inhibition of ERK5 in human HeLa cells by KiNativ profiling method Inhibition of ERK5 in human HeLa cells by KiNativ profiling method	[PMID: 31212132]
SN12C	IC₅₀	86 nM Compound: AX15836	Inhibition of ERK5 in human SN12C cells transduced with MEF2-responsive transcription element assessed as reduction in MEF2 transcription by measuring luciferase signal after 16 hrs by luciferase reporter gene assay Inhibition of ERK5 in human SN12C cells transduced with MEF2-responsive transcription element assessed as reduction in MEF2 transcription by measuring luciferase signal after 16 hrs by luciferase reporter gene assay	[PMID: 30563338]

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 (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.

2035509-96-5

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
10 mM	0.1541 mL	0.7707 mL	1.5414 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (3.85 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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%

Select Batch:

Data Sheet (277 KB) SDS (393 KB)

COA (252 KB) LCMS (122 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

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

[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. [Content Brief]

Complete Stock Solution Preparation Table

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

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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AX-15836

Customer Review

AX-15836 Related Antibodies

4 Publications Citing Use of MCE AX-15836

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All ERK Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

AX-15836 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

AX-15836 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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