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- 2025年12月05日
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- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1443437-74-8
- 规格：
10 mM * 1 mL/5 mg/10 mg/25 mg/50 mg/100 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥363.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥330.0 |
| 规格： | 10 mg | 产品价格： | ￥600.0 |
| 规格： | 25 mg | 产品价格： | ￥1200.0 |
| 规格： | 50 mg | 产品价格： | ￥1800.0 |
| 规格： | 100 mg | 产品价格： | ￥2880.0 |
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CCG-203971
CAS No. : 1443437-74-8
MCE 国际站：CCG-203971
产品活性：CCG-203971 是第二代 Rho/MRTF/SRF 通路抑制剂。CCG-203971 有效靶向 RhoA/C 激活的 SRE 荧光素酶 (IC50=6.4 μM)。CCG-203971 抑制 PC-3 细胞迁移，IC50 为 4.2 μM。CCG-203971 具有潜在的抗转移作用。
研究领域：GPCR/G Protein
作用靶点：Ras
In Vitro: CCG-203971, a second-generation Ras homolog gene family, member A (RhoA)/myocardin-related transcription factor A (MRTF-A)/serum response factor (SRF) pathway inhibitor, represses both matrix-stiffness and transforming growth factor beta–mediated fibrogenesis as determined by protein and gene expression in a dose-dependent manner. CCG-203971 significantly represses TGF-β- induced MKL1 expression at 25 μM concentration. Human dermal fibroblasts are plated onto 96-well plates and allowed to grow for 3 days in the presence of 30 μM CCG-203971 or DMSO vehicle. Viable cell density is assessed through enzymatic reduction of the water-soluble tetrazolium dye WST-1. Scleroderma dermal fibroblasts proliferate faster than normal cells, and this is inhibited by CCG-203971.
In Vivo: CCG-203971 is tested in a Bleomycin skin injury model. Bleomycin is administered in 50 μL of DMSO intraperitoneally. Preliminary studies show that Bleomycin administered in this manner is well tolerated at 100 mg/kg twice a day. Intradermal Bleomycin for 2 weeks along with the DMSO control (50 μL i.p.) results in marked dermal thickening (P<0.0001) compared with the PBS+DMSO group, which does not receive Bleomycin. CCG-203971 treatment strongly and significantly (P<0.001) suppresses the Bleomycin-induced skin thickening in this model. Skin collagen amounts, assessed by measurement of hydroxyproline content, show similar results. Bleomycin injections promote collagen deposition (P<0.01) and CCG-203971 is able to block this effect (P<0.05).
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文献和实验GAA 393 53.26 0.74 Asp GAT 341 46.21 0.76 Asp GAC 106 14.37 0.24 Val
种方法都有其各自的缺陷。Merten等通过构建一基于λPL调节的反转衰减T7 RNA多聚酶表达盒阐明了这一问题。可以通过在启动子和编码T7多聚酶的基因之间插入三个串联排列的转录终止子来削弱T7多聚酶的基础表达水平。在诱导的情况下，噬菌体λ来源的nutL依赖的抗终止功能也可以协同来阻止转录终止[74]。来源于E.colirrnB rRNA操纵子的转录抗终止区已被用于某些表达载体如pSE420。该载体应用trc启动子[75]。其基本原理是使得转录通过重度二级结构区，从而减少宿主RNA 多聚酶引起的转录
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