2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. CCG-100602

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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CCG-100602 Chemical Structure

CCG-100602 Chemical Structure

CAS No. : 1207113-88-9

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Based on 1 publication(s) in Google Scholar

CCG-100602 Related Antibodies

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Description

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[1][2].

Cellular Effect
Cell Line Type Value Description References
PC-3 IC50
17 μM
Compound: 2
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
[PMID: 23707258]
PC-3 IC50
9.8 μM
Compound: 2
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
[PMID: 23707258]
PC-3 IC50
9.8 μM
Compound: 4g
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
[PMID: 19963382]
In Vitro

CCG-100602 (3-30 μM) decreases the number of adherent hASC cells[2].
CCG-100602 blocks the expression of MRTF-A/SRF-activated genes[2].
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].
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].
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].
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.

CCG-100602 Related Antibodies

Cell Viability Assay[2]

Cell Line: Human adipose stem cell (hASC)
Concentration: 3, 8, 15, or 30 μM
Incubation Time: 7 days
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.

RT-PCR[1]

Cell Line: Human intestinal myofibroblasts (HIMFs)
Concentration: 5, 10, 20, and 40 μM
Incubation Time: 30 min prior to the addition of TGF-β1 (5 ng/mL) for 24 hours
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.

Western Blot Analysis[1]

Cell Line: Human intestinal myofibroblasts (HIMFs)
Concentration: 5, 10, 20, and 40 μM
Incubation Time: 30 min prior to the addition of TGF-β1 (5 ng/mL) for 48 hours
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.
In Vivo

Treatment with CCG-100602 (7.5 mg/kg/day, continuously administered for 2 weeks by osmotic minipumps) abrogates the increase of aortic stiffness represented by reduced arterial compliance and strain, indicating a significant anti-stiffening effect resulting from the inhibition of SRF/myocardin[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Adult (4 month-old) male spontaneously hypertensive rats (SHR) and normotensive control Wistar-Kyoto (WKY) rats[3]
Dosage: 7.5 mg/kg/day
Administration: Continuously administered for 2 weeks by osmotic minipumps.
Result: Abrogated the increase of aortic stiffness represented by reduced arterial compliance and strain.
Molecular Weight

478.82

Formula

C21H17ClF6N2O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC=C(NC(C2CN(C(C3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)=O)CCC2)=O)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0885 mL 10.4423 mL 20.8847 mL
5 mM 0.4177 mL 2.0885 mL 4.1769 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, 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 0.83 mg/mL (1.73 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.83 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 (8.3 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
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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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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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
References

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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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:

CCG-1006021207113-88-9CCG100602CCG 100602RasmyocardintranscriptionserumMRTF-ASRFnuclearlocalizationInhibitorinhibitorinhibit

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