| Bioactivity | 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]. |
| Invitro | 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]. Cell Viability Assay[2] Cell Line: |
| 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]. Animal Model: |
| Name | CCG-100602 |
| CAS | 1207113-88-9 |
| Formula | C21H17ClF6N2O2 |
| Molar Mass | 478.82 |
| Appearance | Solid |
| Transport | 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) |
| Reference | [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. [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. [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. |
CCG-100602
CAS: 1207113-88-9 F: C21H17ClF6N2O2 W: 478.82
CCG-100602 is a specific inhibitor of myocardin-related transcription factor A/serum response factor (MRTF-A/SRF) signal
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