CCG-1423 是 Rho/MRTF/SRF 通路的抑制剂。 CCG-1423 在几种癌细胞中显示出活性。 CCG-1423是一种很有前途的先导化合物,可用于开发新型药理学工具,可用于癌症和糖尿病的研究。
Cas No. | 285986-88-1 |
化学名 | N-((1-((4-chlorophenyl)amino)-1-oxopropan-2-yl)oxy)-3,5-bis(trifluoromethyl)benzamide |
Canonical SMILES | FC(F)(F)C1=CC(C(F)(F)F)=CC(C(NOC(C)C(NC2=CC=C(Cl)C=C2)=O)=O)=C1 |
分子式 | C18H13ClF6N2O3 |
分子量 | 454.75 |
溶解度 | ≥ 21mg/mL in DMSO |
储存条件 | Store at -20℃ |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | CCG-1423 is a small-molecule inhibitor of RhoA transcriptional signaling. The interaction between MRTF-A and importin a/b1 was inhibited by CCG-1423, but monomeric G-actin binding to MRTF-A was not inhibited [4]. Multiple members of the Rho family of small GTPases play important roles in these cellular processes and in some human tumors (e.g., colon, esophageal, lung, pancreatic, and inflammatory breast cancers), up-regulation of RhoA or RhoC is associated with a poor clinical outcome (2, 3). CCG-1423 has nanomolar to low micromolar potency as well as selectivity toward Rho-overexpressing and invasive cancer cell lines for inhibition of DNA synthesis, cell growth, and/or invasion. Caspase-3 activation in the highly metastatic RhoC-overexpressing A375M2 melanoma cell line was enhanced by CCG-1423 whereas a smaller increase was seen with the parental A375 cell line, whereas just the opposite pattern was seen with daunorubicin [2]. References: [1]. Minami T, Kuwahara K, Nakagawa Y et al. Reciprocal expression of MRTF-A and myocardin is crucial for pathological vascular remodelling in mice. EMBO J. 2012 Nov 28;31(23):4428-40. doi: 10.1038/emboj.2012.296. Epub 2012 Oct 26. [2]. Hayashi K, Watanabe B, Nakagawa Y et al. RPEL proteins are the molecular targets for CCG-1423, an inhibitor of Rho signaling. PLoS One. 2014 Feb 18;9(2):e89016. doi: 10.1371/journal.pone.0089016. eCollection 2014. |