CCG-203971 是一种第二代 Rho/MRTF/SRF 通路抑制剂,CCG-203971 可抑制 PC-3 细胞迁移(IC50值为4.2 μM)。 产品性质 英文别名(English Synonym) CCG-203971 中文名称(Chinese Name) / 靶点(Target) others 通路(Pathway) GPCR/G Protein CAS号(CAS NO.) ...
Rho/MRTF/SRFmitochondriabioenergeticshistone-4acetylationoxidative stressRhoA-regulated gene transcription by serum response factor (SRF) and its transcriptional cofactor myocardin-related transcription factors (MRTFs) signaling pathway has emerged as a promising therapeutic target for pharmacological intervention ...
CCG-257081 (MRTF SRF-IN-1) is an inhibitor of cardiac myosin-related transcription factor and serum response factor (MRTF SRF) that acts by inhibiting the Rho MRTF SRF pathway.CCG-257081 has shown efficacy in preventing bleomycin-induced fibrosis in several mouse models. CCG-257081 can be used...
Johnson LA, Rodansky ES, Haak AJ, Larsen SD, Neubig RR, Higgins PDR. Novel Rho/MRTF/SRF inhibitors block matrix-stiffness and TGF-β-induced fibrogenesis in human colonic myofibroblasts[J/OL]. Inflamm Bowel Dis. 2014;20:154–65. Article Google Scholar Horowitz S, Binion DG, Nelson VM,...
R.R.N. is a President and Founder of Fibrosix, Inc. R.R.N. and E.M.L. are part of the following patent “Inhibitors of Myocardin-Related Transcription Factor and Serum Response Factor (MRTF/SRF)-Mediated Gene Transcription and Methods for use of the same”, Serial Number 14/934,769...
Yuan等[43]研究发现巩膜成纤维细胞受到机械应力后可激活RhoA,通过RhoA/ROCK2-MRTF-A/SRF途径,使得心肌相关转录因子-A(MRTF-A)核转移,α-SMA表达增加,诱导其分化为肌成纤维细胞。另外,MDIA和ROCK在Rho引起的应力纤维形成过程中同时被激活,MDIA通过成核和聚合产生肌动蛋白细丝,而ROCK激活肌球蛋白使其交联,从而诱导...
CCG-1423, a selective RhoA pathway inhibitor, suppresses SRF-mediated transcription. 靶点活性 LRRK2 (WT):1.28 nM, LRRK2 (G2019S):1.85 nM 体内活性 在H9c2细胞中,CCG-1423抑制MRTF核定位,并完全阻断STARS近端报告基因活性。在人结肠肌成纤维细胞中,CCG-1423抑制TGF-β诱导的纤维增生。小鼠胚胎干细胞在...
localization of FLAG-MRTF-A, and the effect of MRTF-A overexpression on smooth muscle alpha-actin promoter activity was inhibited by dominant negative RhoA... K Lockman,JS Hinson,MD Medlin,... - 《Journal of Biological Chemistry》 被引量: 287发表: 2004年 EphrinA1 inactivates integrin-mediated...
localization of FLAG-MRTF-A, and the effect of MRTF-A overexpression on smooth muscle alpha-actin promoter activity was inhibited by dominant negative RhoA... K Lockman,JS Hinson,MD Medlin,... - 《Journal of Biological Chemistry》 被引量: 286发表: 2004年 ...
CCG-1423 is a Rho A pathway inhibitor which has been reported to inhibit Rho/SRF-mediated transcriptional regulation. SRF and SRF cofactors, which include ternary complex factors (TCFs) and myocardin-related transcription factor (MRTF), regulate various cellular functions. The Rho/SRF signaling ...