XMD17-109
Based on 6 publication(s) in Google Scholar
XMD17-109 is a novel, specific ERK-5 inhibitor, with an IC50 of 162 nM.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.14%
- CAS. Nr.: 1435488-37-1
- Formel: C36H46N8O3
- Molecular Weight:638.80
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Lösungsmittel & Löslichkeit
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Publications Citing Use of MedChemExpress (MCE) XMD17-109
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Biologische Aktivität
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ERK5 162 nM (IC50) |
LRRK2[G2019S] 339 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| HEK293 | EC50 |
4.2 μM
Compound: 26, ERK5-IN-1
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Inhibition of GST-tagged full length human ERK5 transfected in HEK293 cells assessed as inhibition of AP1 transcriptional activity after 24 hrs by dual luciferase reporter gene assay
Inhibition of GST-tagged full length human ERK5 transfected in HEK293 cells assessed as inhibition of AP1 transcriptional activity after 24 hrs by dual luciferase reporter gene assay
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[PMID: 23656407] |
| HEK-293T | IC50 |
>10000 nM
Compound: ERK5-IN-1
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Inhibition of cell growth in HEK293T cells incubated for 72 hrs by CellTiter-blue reagent based assay
Inhibition of cell growth in HEK293T cells incubated for 72 hrs by CellTiter-blue reagent based assay
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[PMID: 34710325] |
| MM1.S | IC50 |
280 nM
Compound: ERK5-IN-1
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Inhibition of cell growth in human MM1.S cells incubated for 72 hrs by CellTiter-blue reagent based assay
Inhibition of cell growth in human MM1.S cells incubated for 72 hrs by CellTiter-blue reagent based assay
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[PMID: 34710325] |
XMD17-109 (Compound 26) inhibits ERK5 biochemically with an IC50 of 0.162 ± 0.006 μM, and blocks pidermal growth factor induced ERK5 autophosphorylation with an EC50 of 0.09 ± 0.03 μM in cells. XMD17-109 also inhibits LRRK2[G2019S] with an IC50 of 339 nM[1]. XMD17-109 demonstrats low nanomolar cellular activity judged by the significant dose-dependent reduction of mobility shifted phosphorylated ERK5 bands from sorbitol stimulated cells. XMD17-109 completely inhibits the ERK5-mediated AP1 transcriptional activity at 30 μM and has an EC50 of 4.2 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1435488-37-1
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Appearance Solid
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Molecular Weight 638.80
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Formel C36H46N8O3
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Color Light yellow to yellow
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SMILES
O=C1C2=C(C=CC=C2)N(C3CCCC3)C4=NC(NC5=C(OCC)C=C(C(N6CCC(N7CCN(C)CC7)CC6)=O)C=C5)=NC=C4N1C
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
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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Cancer Lett
Inhibition of MEK5/ERK5 signaling overcomes acquired resistance to the third generation EGFR inhibitor, osimertinib, via enhancing Bim-dependent apoptosis. [Abstract]2021 Oct 28:519:141-149. PMID: 34245854 -
Sci Signal
Extracellular signal-regulated kinase 5 promotes acute cellular and systemic inflammation. [Abstract]2015 Aug 25;8(391):ra86. PMID: 26307013 -
Int J Gen Med
PER1 Serves as a Tumor Suppressor in Breast Cancer by Regulating MEK5/ERK5 Signaling Pathway. [Abstract]2025 Aug 9:18:4337-4349. PMID: 40809954 -
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Ann Transl Med
Cortistatin exerts antiproliferation and antimigration effects in vascular smooth muscle cells stimulated by Ang II through suppressing ERK1/2, p38 MAPK, JNK and ERK5 signaling pathways. [Abstract]2019 Oct;7(20):561. PMID: 31807542 -
Oncotarget
MEK5/ERK5 signaling inhibition increases colon cancer cell sensitivity to 5-fluorouracil through a p53-dependent mechanism. [Abstract]2016 Jun 7;7(23):34322-40. PMID: 27144434
XMD17-109 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 Jun 7;7(23):34322-40. [Abstract]
HCT116 parental cells are treated for up to 48 h with increasing doses of 5-FU in combination with 4 μM XMD8-92 or 2 μM XMD17-109, two highly-selective ERK5 pharmacological inhibitors.
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (156.54 mM; ultrasonic and warming and heat to 60°C; 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (3.91 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 (3.91 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.
Protokoll
HeLa cells are maintained in DMEM supplemented with 10% FBS, 2 mM l-glutamine, 50 U/mL penicillin G, and 50 μg/mL streptomycin. Before use HeLa cells are serum starved for 16 h in DMEM supplemented with 2 mM l-glutamine, 50 U/mL penicillin G, and 50 μg/mL streptomycin. HeLa cells are then incubated with ERK5-IN-1 at the indicated concentrations for 1 h prior to stimulation with 0.5mol/Lsorbitol for 30 min. Cells are lysed in Triton lysis buffer (50 mM Tris-HCl, pH 7.5, 1 mM EGTA, 1 mM EDTA, 1 mM sodium orthovanadate, 50 mM sodium fluoride, 1 mM sodium pyrophosphate, 0.27mol/Lsucrose, 1 μM microcystin-LR, 1% (v/v) Triton X-100, 0.1% (v/v) 2-mercaptoethanol) and 20 μg of protein loaded per well. Samples are run on 8% polyacrylamide gels using standard methods. Proteins are transferred onto nitrocellulose membranes and specific proteins detected by immunoblotting.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (283 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Deng X, et al. Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones. Eur J Med Chem. 2013;70:758-67. [Content Brief]
[2]. Elkins, Jonathan M., et al. X-ray Crystal Structure of ERK5 (MAPK7) in Complex with a Specific Inhibitor. Journal of Medicinal Chemistry (2013), 56(11), 4413-4421. [Content Brief]
[3]. Wilhelmsen K, et al. Extracellular signal-regulated kinase 5 promotes acute cellular and systemic inflammation. Sci Signal. 2015 Aug 25;8(391):ra86. [Content Brief]
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 | 1.5654 mL | 7.8272 mL | 15.6544 mL | 39.1359 mL |
| 5 mM | 0.3131 mL | 1.5654 mL | 3.1309 mL | 7.8272 mL | |
| 10 mM | 0.1565 mL | 0.7827 mL | 1.5654 mL | 3.9136 mL | |
| 15 mM | 0.1044 mL | 0.5218 mL | 1.0436 mL | 2.6091 mL | |
| 20 mM | 0.0783 mL | 0.3914 mL | 0.7827 mL | 1.9568 mL | |
| 25 mM | 0.0626 mL | 0.3131 mL | 0.6262 mL | 1.5654 mL | |
| 30 mM | 0.0522 mL | 0.2609 mL | 0.5218 mL | 1.3045 mL | |
| 40 mM | 0.0391 mL | 0.1957 mL | 0.3914 mL | 0.9784 mL | |
| 50 mM | 0.0313 mL | 0.1565 mL | 0.3131 mL | 0.7827 mL | |
| 60 mM | 0.0261 mL | 0.1305 mL | 0.2609 mL | 0.6523 mL | |
| 80 mM | 0.0196 mL | 0.0978 mL | 0.1957 mL | 0.4892 mL | |
| 100 mM | 0.0157 mL | 0.0783 mL | 0.1565 mL | 0.3914 mL |
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