AX-15836
Based on 6 publication(s) in Google Scholar
AX-15836 is a potent and selective ERK5 inhibitor with an IC50 of 8 nM.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.79%
- CAS 番号: 2035509-96-5
- 分子式: C32H40N8O5S
- 分子量:648.78
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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ERK5 8 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
8 nM
Compound: 3; AX15836
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Inhibition of ERK5 in human HeLa cells by KiNativ profiling method
Inhibition of ERK5 in human HeLa cells by KiNativ profiling method
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[PMID: 31212132] |
| SN12C | IC50 |
86 nM
Compound: AX15836
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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
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[PMID: 30563338] |
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.
化学情報
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CAS 番号 2035509-96-5
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性状 Solid
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分子量 648.78
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分子式 C32H40N8O5S
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Color Off-white to yellow
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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
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
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Journal Impact Factor
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Most Recent
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MedComm (2020)
Tyrosine phosphatase SHP2 exacerbates psoriasis-like skin inflammation in mice via ERK5-dependent NETosis. [Abstract]2022 Mar 4;3(1):e120. PMID: 35281792 -
Phytomedicine
Licochalcone B targets neural cell adhesion molecule 1 to inhibit osteosarcoma progression and ferroptosis resistance via extracellular signal-regulated kinase 5 and nuclear factor kappa B pathways. [Abstract]2025 Nov 22:150:157584. PMID: 41349457 -
Toxicology
Hippocampal MEF2C phosphorylation mediates synaptic plasticity in lead-induced learning and memory impairments. [Abstract]2025 Feb 11:154082. PMID: 39947421 -
Cell Signal
2023 May:105:110607. PMID: 36690134 -
Mol Oncol
Importin subunit beta-1 mediates ERK5 nuclear translocation, and its inhibition synergizes with ERK5 kinase inhibitors in reducing cancer cell proliferation. [Abstract]2025 Jan;19(1):99-113. PMID: 38965815 -
溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
プロトコル
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (277 KB)
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SDS (393 KB)
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取扱説明書 (2659 KB)
参考文献
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 |
AX-15836 関連分類
HY-101846 関連分類
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