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(R)-CCG-1423 目录号 GC10419

Rho inhibitor

规格 价格 库存 购买数量
1mg
¥416.00
现货
5mg
¥1,976.00
现货
10mg
¥3,744.00
现货

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Sample solution is provided at 25 µL, 10mM.

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Chemical Properties

Cas No. SDF
化学名 (R)-N-((1-((4-chlorophenyl)amino)-1-oxopropan-2-yl)oxy)-3,5-bis(trifluoromethyl)benzamide
Canonical SMILES O=C(NO[C@H](C)C(NC1=CC=C(Cl)C=C1)=O)C2=CC(C(F)(F)F)=CC(C(F)(F)F)=C2
分子式 C18H13ClF6N2O3 分子量 454.8
溶解度 ≤0.25mg/ml in ethanol;10mg/ml in DMSO;10mg/ml in dimethyl formamide 储存条件 Store at -20°C
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
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产品描述

(R)-CCG-1423 is a stereoisomer of CCG-1423. CCG-1423 is a Rho inhibitor involved in blocking signaling through myocardin-related transcription factor A (MRTF-A) and serum response factor (SRF) [1].

The Rho family of small GTPases plays an important role in cancer metastasis. Up-regulation of RhoA or RhoC has been associated with a poor clinical outcome. Rho GTPases are important for the actin cytoskeleton. The RhoA family plays an important role in multiple cellular processes central to tumor growth and metastasis [1].

CCG-14223 was an inhibitor for Rho/SRF pathway and displayed activity in several in vitro cancer cell functional assays. In PC-3 prostate cancer cells, CCG-1423(< 1 μmol/L) potently inhibited lysophosphatidic acid–induced DNA synthesis. CCG-1423 inhibited the growth of RhoC-overexpressing melanoma lines (A375M2 and SK-Mel-147) at nanomolar concentrations. CCG-1423 selectively stimulated apoptosis of the metastasis-prone, RhoC-overexpressing melanoma cell line (A375M2) when compared with the parental cell line (A375). CCG-1423 inhibited Rho-dependent invasion by PC-3 prostate cancer cells [1]. The R-isomer of CCG-1423 inhibited MRTF-A-dependent cellular events, including SRF-mediated gene expression and cell migration. The efficacy of (R)-CCG-1423 was less potent than the S-isomer [2].

References:
[1] Evelyn C R, Wade S M, Wang Q, et al.  CCG-1423: a small-molecule inhibitor of RhoA transcriptional signaling[J]. Molecular cancer therapeutics, 2007, 6(8): 2249-2260.
[2] Watanabe B, Minami S, Ishida H, et al.  Stereospecific inhibitory effects of ccg-1423 on the cellular events mediated by myocardin-related transcription factor a[J]. PloS one, 2015, 10(8): e0136242.