"目录号: HY-13991
GPCR/G Protein-
CCG-1423是一种新型的RhoA/C介导的基因转录抑制剂，能抑制细胞的转移前列腺癌PC-3细胞侵袭模型。
Ras
相关产品
ARS-853-NSC 23766 trihydrochloride-EHT 1864-ML141-Salirasib-Rhosin hydrochloride-K-Ras G12C-IN-2-Y16-CASIN-ZCL278-BQU57-EHop-016-K-Ras G12C-IN-1-K-Ras G12C-IN-3-K-Ras(G12C) inhibitor 12-
生物活性
Description
CCG-1423 is a novel inhibitor of RhoA/C-mediated gene transcription that is capable of inhibiting invasion of PC-3 prostate cancer cells in a Matrigel model of metastasis.IC50 value: 1.5 uM [1]Target: Rho signaling inhibitorin vitro: CCG-1423 selectively inhibited spontaneous PC-3 prostate cancer cell invasion through a Matrigel matrix, but not the Gαi-dependent LPA-stimulated SKOV-3 ovarian cancer cell invasion, in vitro. At 100 μM, nearly complete inhibition of invasion was achieved with a lesser degree of toxicity than that induced by CCG-1423 at 10 μM [1]. SRF binds to this site in vivo and the SRF inhibitor CCG-1423 completely blocks STARS proximal reporter activity in H9c2 cells [3]. pharmacological MKL-inhibition with CCG-1423 significantly inhibited CCN1 promoter activity as well as mRNA and protein expression[4].in vivo: Pharmacological SRF inhibition by CCG-1423 reduced nuclear MKL1 and improved glucose uptake and tolerance in insulin-resistant mice in vivo [2].
References
[1].Evelyn CR, et al. Design, synthesis and prostate cancer cell-based studies of analogs of the Rho/MKL1 transcriptional pathway inhibitor, CCG-1423. Bioorg Med Chem Lett. 2010 Jan 15;20(2):665-72.
[2].Jin W, et al. Increased SRF transcriptional activity in human and mouse skeletal muscle is a signature of insulin resistance. J Clin Invest. 2011 Mar;121(3):918-29.
[3].Chong NW, et al. STARS is essential to maintain cardiac development and function in vivo via a SRF pathway. PLoS One. 2012;7(7):e40966.
[4].Duggirala A, et al. cAMP-induced actin cytoskeleton remodelling inhibits MKL1-dependent expression of the chemotactic and pro-proliferative factor, CCN1. J Mol Cell Cardiol. 2014 Nov 18;79C:157-168.