CCG-100602
Based on 2 publication(s) in Google Scholar
CCG-100602 is a specific inhibitor of myocardin-related transcription factor A/serum response factor (MRTF-A/SRF) signaling. CCG-100602 specifically block MRTF-A nuclear localization and thus inhibit the fibrogenic transcription factor SRF.
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- Pureza: 99.29%
- No. CAS: 1207113-88-9
- Fòrmula: C21H17ClF6N2O2
- Peso molecular:478.82
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) CCG-100602
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
16.7 μM
Compound: 3-3d
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Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 method
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 method
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[PMID: 38329974] |
| PC-3 | IC50 |
17 μM
Compound: 2
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Antimetastatic activity against human PC3 cells after 24 hrs by scratch wound assay
Antimetastatic activity against human PC3 cells after 24 hrs by scratch wound assay
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[PMID: 23707258] |
| PC-3 | IC50 |
9.8 μM
Compound: 2
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Inhibition of RhoC-mediated pathway in human PC3 cells assessed as inhibition of SRE-regulated gene transcription by luciferase reporter gene assay
Inhibition of RhoC-mediated pathway in human PC3 cells assessed as inhibition of SRE-regulated gene transcription by luciferase reporter gene assay
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[PMID: 23707258] |
| PC-3 | IC50 |
9.8 μM
Compound: 4g
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Inhibition of RhoA/C-mediated transcriptional response in human PC3 cells by serum response factor-luciferase reporter gene assay
Inhibition of RhoA/C-mediated transcriptional response in human PC3 cells by serum response factor-luciferase reporter gene assay
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[PMID: 19963382] |
CCG-100602 (3-30?μM) decreases the number of adherent hASC cells[2].
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CCG-100602 blocks the expression of MRTF-A/SRF-activated genes[2].
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CCG-100602 (5-40?μM) diminishes the TGF-β1 (5?ng/mL)-induced increase in COL1A1, FN1, and ACTA2 transcription in a dose-dependent manner[1].
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CCG-100602 (5-40?μM) reduces the TGF-β1-induced increase in MRTFA and SRF mRNA expression in the HIMFs in a dose-dependent manner [1].
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CCG-100602 (5-40?μM) significantly reduces the protein expression levels of the ECM and α-SMA in TGF-β1 (5?ng/mL)-stimulated cells in a dose-dependent manner[1].
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CCG-100602 (5-40?μM) also significantly represses the MRTF-A and SRF protein expression, which were induced by TGF-β1, in the nuclear fraction of the HIMFs in a dose-responsive manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human adipose stem cell (hASC)
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Concentration:3, 8, 15, or 30 μM
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Incubation Time:7 days
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Result:The number of adherent cells decreased as a response to increasing inhibitor amount. The effect was also dependent on the culture media because the osteogenic medium condition supported the viability over basic culture medium and adipogenic medium conditions.
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Cell Line:Human intestinal myofibroblasts (HIMFs)
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Concentration:5, 10, 20, and 40 μM
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Incubation Time:30 min prior to the addition of TGF-β1 (5 ng/mL) for 24 hours
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Result:Diminished the TGF-β1-induced increase in COL1A1, FN1, and ACTA2 transcription in a dose-dependent manner.
Reduced the TGF-β1-induced increase in MRTFA and SRF mRNA expression in the HIMFs in a dose-dependent manner.
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Cell Line:Human intestinal myofibroblasts (HIMFs)
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Concentration:5, 10, 20, and 40 μM
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Incubation Time:30 min prior to the addition of TGF-β1 (5 ng/mL) for 48 hours
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Result:The protein expression levels of the ECM and α-SMA in TGF-β1-stimulated cells are significantly reduced.
Repressed the MRTF-A and serum response factor (SRF) protein expression, which were induced by TGF-β1, in the nuclear fraction of the HIMFs.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult (4 month-old) male spontaneously hypertensive rats (SHR) and normotensive control Wistar-Kyoto (WKY) rats[3]
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Dosage:7.5 mg/kg/day
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Administration:Continuously administered for 2 weeks by osmotic minipumps.
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Result:Abrogated the increase of aortic stiffness represented by reduced arterial compliance and strain.
Chemical Information
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No. CAS 1207113-88-9
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Appearance Solid
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Peso molecular 478.82
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Fòrmula C21H17ClF6N2O2
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Color White to off-white
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SMILES
ClC1=CC=C(NC(C2CN(C(C3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)=O)CCC2)=O)C=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (2)
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Journal Impact Factor
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Most Recent
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Stem Cell Res Ther
Activin B-activated Cdc42 signaling plays a key role in regulating adipose-derived mesenchymal stem cells-mediated skin wound healing. [Abstract]2022 Jun 11;13(1):248. PMID: 35690801 -
Solvente y solubilidad
DMSO : 100 mg/mL (208.85 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 (protect from light). 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 0.83 mg/mL (1.73 mM); Clear solution
This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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.
Pureza y Documentación
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Ficha de datos (277 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Yoon Jeong Choi, et al. Umbilical cord/placenta-derived mesenchymal stem cells inhibit fibrogenic activation in human intestinal myofibroblasts via inhibition of myocardin-related transcription factor A. Stem Cell Res Ther. 2019 Sep 23;10(1):291. [Content Brief]
[2]. Laura Hyväri, et al. Myocardin-Related Transcription Factor A (MRTF-A) Regulates the Balance between Adipogenesis and Osteogenesis of Human Adipose Stem Cells. Stem Cells Int. 2020 Sep 22;2020:8853541. [Content Brief]
[3]. Ning Zhou, et al. Rho Kinase Regulates Aortic Vascular Smooth Muscle Cell Stiffness Via Actin/SRF/Myocardin in Hypertension. Cell Physiol Biochem. 2017;44(2):701-715. [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 (protect from light). 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 | 2.0885 mL | 10.4423 mL | 20.8847 mL | 52.2117 mL |
| 5 mM | 0.4177 mL | 2.0885 mL | 4.1769 mL | 10.4423 mL | |
| 10 mM | 0.2088 mL | 1.0442 mL | 2.0885 mL | 5.2212 mL | |
| 15 mM | 0.1392 mL | 0.6962 mL | 1.3923 mL | 3.4808 mL | |
| 20 mM | 0.1044 mL | 0.5221 mL | 1.0442 mL | 2.6106 mL | |
| 25 mM | 0.0835 mL | 0.4177 mL | 0.8354 mL | 2.0885 mL | |
| 30 mM | 0.0696 mL | 0.3481 mL | 0.6962 mL | 1.7404 mL | |
| 40 mM | 0.0522 mL | 0.2611 mL | 0.5221 mL | 1.3053 mL | |
| 50 mM | 0.0418 mL | 0.2088 mL | 0.4177 mL | 1.0442 mL | |
| 60 mM | 0.0348 mL | 0.1740 mL | 0.3481 mL | 0.8702 mL | |
| 80 mM | 0.0261 mL | 0.1305 mL | 0.2611 mL | 0.6526 mL | |
| 100 mM | 0.0209 mL | 0.1044 mL | 0.2088 mL | 0.5221 mL |
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