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CCG-100602 

Cat. No.: HY-120855 Purity: 99.66%
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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.

For research use only. We do not sell to patients.

CCG-100602 Chemical Structure

CCG-100602 Chemical Structure

CAS No. : 1207113-88-9

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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].

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].

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

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].

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.
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)

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
10 mM 0.2088 mL 1.0442 mL 2.0885 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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Keywords:

CCG-100602CCG100602CCG 100602RasmyocardintranscriptionserumMRTF-ASRFnuclearlocalizationInhibitorinhibitorinhibit

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Product Name:
CCG-100602
Cat. No.:
HY-120855
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