1443437-74-8
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- CAS号:
- 1443437-74-8
- 英文名:
- CCG-203971
- 英文别名:
- 3-Piperidinecarboxamide, N-(4-chlorophenyl)-1-[3-(2-furanyl)benzoyl]-;203971;CCG-203971;CC 203971;CCG-203971, 10 mM in DMSO;CCG 203971;CCG203971;CCG-203971;N-(4-Chlorophenyl)-1-[3-(2-furanyl)benzoyl]-3-piperidinecarboxamide;N-(4-chlorophenyl)-1-[3-(furan-2-yl)benzoyl]piperidine-3-carboxamide;Rho,Ras,Inhibitor,SRF,CCG 203971,CCG-203971,MKL1,inhibit,MRTF,anti-metastasis,PC-3,migration
- 中文名:
- 1443437-74-8
- 中文别名:
- 化合物CCG203971;PERFEMIKER]CCG-203971,98%;化合物CCG203971,10 MM DMSO 溶液;CCG 203971,抑制MRTF / SRF基因转录通路;N-(4-氯苯基)-1-(3-(2-呋喃基)苯甲酰基)-3-哌啶甲酰胺
- CBNumber:
- CB13067539
- 分子式:
- C23H21ClN2O3
- 分子量:
- 408.88
- MOL File:
- 1443437-74-8.mol
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1443437-74-8化学性质
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沸点:
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656.0±55.0 °C(Predicted)
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密度:
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1.305±0.06 g/cm3(Predicted)
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储存条件:
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2-8°C
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溶解度:
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DMSO:81.0(Max Conc. mg/mL);198.1(Max Conc. mM)
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酸度系数(pKa):
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13.69±0.70(Predicted)
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形态:
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powder
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颜色:
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white to beige
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1443437-74-8性质、用途与生产工艺
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。
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.
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).
1443437-74-8
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上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2025/02/08 | HY-108361 | CCG-203971 | 1443437-74-8 | 5 mg | 330元 |
| 2025/02/08 | HY-108361 | 1443437-74-8
CCG-203971 | 1443437-74-8 | 10mM * 1mLin DMSO | 363元 |
1443437-74-8, 1443437-74-8 相关搜索:
- 合成有机化合物配体
- 抑制剂
- 化合物CCG203971,10 MM DMSO 溶液
- PERFEMIKER]CCG-203971,98%
- CCG 203971,抑制MRTF / SRF基因转录通路
- N-(4-氯苯基)-1-(3-(2-呋喃基)苯甲酰基)-3-哌啶甲酰胺
- 化合物CCG203971
- 1443437-74-8
- CCG-203971, 10 mM in DMSO
- CC 203971
- Rho,Ras,Inhibitor,SRF,CCG 203971,CCG-203971,MKL1,inhibit,MRTF,anti-metastasis,PC-3,migration
- 3-Piperidinecarboxamide, N-(4-chlorophenyl)-1-[3-(2-furanyl)benzoyl]-
- 203971
- N-(4-chlorophenyl)-1-[3-(furan-2-yl)benzoyl]piperidine-3-carboxamide
- N-(4-Chlorophenyl)-1-[3-(2-furanyl)benzoyl]-3-piperidinecarboxamide
- CCG 203971;CCG203971;CCG-203971
- CCG-203971