CMPD1
Based on 1 Customer Validation
CMPD1 is a selective and non-ATP-competitive p38 MAPK-mediated MK2 phosphorylation inhibitor with apparent Ki (Kiapp) of 330 nM.
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- Reinheit: 99.81%
- CAS. Nr.: 41179-33-3
- Formel: C22H20FNO2
- Molecular Weight:349.40
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Kiapp: 330 nM (MK2 phosphorylation)[2]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A 172 | EC50 |
0.6 μM
Compound: 75; CMPD1
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Antiproliferative activity against human A-172 cells assessed as cell growth inhibition
Antiproliferative activity against human A-172 cells assessed as cell growth inhibition
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[PMID: 34101463] |
| U-251 | EC50 |
0.6 μM
Compound: 75; CMPD1
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Antiproliferative activity against human U-251 cells assessed as cell growth inhibition
Antiproliferative activity against human U-251 cells assessed as cell growth inhibition
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[PMID: 34101463] |
| U-87MG ATCC | EC50 |
<1 μM
Compound: CMPD1
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Inhibition of tubulin polymerization in human U87 cells assessed as decrease in cell viability after 72 hrs by Alamar blue assay
Inhibition of tubulin polymerization in human U87 cells assessed as decrease in cell viability after 72 hrs by Alamar blue assay
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[PMID: 28280261] |
| U-87MG ATCC | EC50 |
0.6 μM
Compound: 75; CMPD1
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Antiproliferative activity against human U87 cells assessed as cell growth inhibition
Antiproliferative activity against human U87 cells assessed as cell growth inhibition
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[PMID: 34101463] |
CMPD1 does not inhibit p38 MAPK-mediated phosphorylation of other two substrates, MBP and ATF2[1].
CMPD1 induced mitotic arrest and apoptosis in U87 cells[1].
CMPD1 inhibits tubulin polymerisation in glioblastoma cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 41179-33-3
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Appearance Solid
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Molecular Weight 349.40
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Formel C22H20FNO2
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Color Off-white to light brown
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SMILES
O=C(NC1=CC=C(O)C=C1)CCCC2=CC=C(C3=CC=CC=C3F)C=C2
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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 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (286.20 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 2.08 mg/mL (5.95 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.95 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Reinheit & Dokumentation
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Data Sheet (270 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Gurgis F, et al. Cytotoxic activity of the MK2 inhibitor CMPD1 in glioblastoma cells is independent of MK2. Cell Death Discov. 2015 Sep 7;1:15028. [Content Brief]
[2]. Davidson W, er al. Discovery and characterization of a substrate selective p38alpha inhibitor. Biochemistry. 2004 Sep 21;43(37):11658-71. [Content Brief]
[3]. Phoa AF, et al. Pharmacology of novel small-molecule tubulin inhibitors in glioblastoma cells with enhanced EGFR signalling. Biochem Pharmacol. 2015 Dec 15;98(4):587-601. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8620 mL | 14.3102 mL | 28.6205 mL | 71.5512 mL |
| 5 mM | 0.5724 mL | 2.8620 mL | 5.7241 mL | 14.3102 mL | |
| 10 mM | 0.2862 mL | 1.4310 mL | 2.8620 mL | 7.1551 mL | |
| 15 mM | 0.1908 mL | 0.9540 mL | 1.9080 mL | 4.7701 mL | |
| 20 mM | 0.1431 mL | 0.7155 mL | 1.4310 mL | 3.5776 mL | |
| 25 mM | 0.1145 mL | 0.5724 mL | 1.1448 mL | 2.8620 mL | |
| 30 mM | 0.0954 mL | 0.4770 mL | 0.9540 mL | 2.3850 mL | |
| 40 mM | 0.0716 mL | 0.3578 mL | 0.7155 mL | 1.7888 mL | |
| 50 mM | 0.0572 mL | 0.2862 mL | 0.5724 mL | 1.4310 mL | |
| 60 mM | 0.0477 mL | 0.2385 mL | 0.4770 mL | 1.1925 mL | |
| 80 mM | 0.0358 mL | 0.1789 mL | 0.3578 mL | 0.8944 mL | |
| 100 mM | 0.0286 mL | 0.1431 mL | 0.2862 mL | 0.7155 mL |
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