For research use only. Not for therapeutic Use.
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].
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].
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].
| Catalog Number | I005889 |
| CAS Number | 1207113-88-9 |
| Synonyms | 1-[3,5-bis(trifluoromethyl)benzoyl]-N-(4-chlorophenyl)piperidine-3-carboxamide |
| Molecular Formula | C21H17ClF6N2O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C21H17ClF6N2O2/c22-16-3-5-17(6-4-16)29-18(31)12-2-1-7-30(11-12)19(32)13-8-14(20(23,24)25)10-15(9-13)21(26,27)28/h3-6,8-10,12H,1-2,7,11H2,(H,29,31) |
| InChIKey | MOQCFMZWVKQBAP-UHFFFAOYSA-N |
| SMILES | C1CC(CN(C1)C(=O)C2=CC(=CC(=C2)C(F)(F)F)C(F)(F)F)C(=O)NC3=CC=C(C=C3)Cl |
| 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. |
