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CCG-100602

CAS No. : 1207113-88-9

MCE 站：CCG-100602

产品活性：CCG-100602 是心肌蛋白相关转录因子 A/血清反应因子 (MRTF-A/SRF) 信号转导的特异性抑制剂。CCG-100602 特异性阻断 MRTF-A 核定位，从而抑制纤维生成转录因子 SRF。

研究领域：GPCR/G Protein

作用靶点：Ras

In Vitro: CCG-100602 (3-30?μM) decreases the number of adherent hASC cells.
CCG-100602 blocks the expression of MRTF-A/SRF-activated genes.
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.
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 .
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.
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.

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.

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