CCG-1423 是Rho/MRTF/SRF通路的抑制剂。CCG-1423 在多种癌细胞中具有活性。CCG-1423 是开发新型药物工具的先导化合物，可用于癌症和糖尿病的研究。
| 生物活性 | CCG-1423 is an inhibitor ofRho/MRTF/SRFpathway. CCG-1423 shows activities in severalcancercells. CCG-1423 is a promising lead compound for the development of novel pharmacologic tools, and it can be used for the research ofcancerand diabetes[1][2][3]. |
| IC50& Target | IC50: 1.5 μM (Rho-pathway selective serum response element-luciferase reporter)[1] |
体外研究
(In Vitro) | CCG-1423 (10 μM; 24 h) affects invasion by cultured PC-3 cells into a Matrigel matrix and inhibits 54% mitochondrial metabolism of WST-1[1].CCG-1423 (0-100 μM; 24 h) inhibits RhoA and RhoC signaling pathways with an IC50value of 1.5 μM for Rho-pathway selective serum response element-luciferase reporter[1].CCG-1423 (1 μM; 16 h) improves glucose uptake in both L6 cells and primary human myotubes[2].CCG-1423 (10 μM; 18-19 h) inhibits expression of Rho downstream[2].CCG-1423 (3 μM; 25 h) selectively stimulates apoptosis of RhoC-overexpressing melanoma cell line (A375M2) compared with the parental cell line (A375)[3].
Cell Invasion Assay[1] | Cell Line: | PC-3 cell line | | Concentration: | 10 μM | | Incubation Time: | 24 hours | | Result: | Inhibited 71% invasion by cultured PC-3 cells into a Matrigel matrix. |
Western Blot Analysis[2] | Cell Line: | L6 myotubes | | Concentration: | 1 μM | | Incubation Time: | 48 hours | | Result: | Increased insulin-stimulated Akt phosphorylation, blocked ERK phosphorylation, and increased IRS-1 tyrosine phosphorylation and its association with the p85 regulatory subunit of PI3K. |
Cell Proliferation Assay[3] | Cell Line: | PC-3 cell line | | Concentration: | 0.3 μM | | Incubation Time: | 8 days | | Result: | Inhibited growth of PC-3 prostate cancer cells with an IC50value of 1 μM with 30 μM LPA adding. |
Apoptosis Analysis[3] | Cell Line: | RhoC-overexpressing A375M2 and low RhoC-expressing A375 melanoma cell lines | | Concentration: | 3 μM | | Incubation Time: | 25 hours | | Result: | Stimulated apoptosis of A375M2 cell line compared with the parental cell line. |
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体内研究
(In Vivo) | CCG-1423 (0.15 mg/kg; i.p. once daily for two weeks) affects glucose tolerance and insulin levels in HFD-fed mice[1].
| Animal Model: | 16-week-old mice with HFD-induced obesity[1] | | Dosage: | 0.15 mg/kg | | Administration: | Intraperitoneal injection; 0.15 mg/kg once per day; for two weeks | | Result: | Improved glucose tolerance and reduced insulin levels at 30 minutes after glucose injection. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(219.90 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 2.1990 mL | 10.9951 mL | 21.9901 mL | | 5 mM | 0.4398 mL | 2.1990 mL | 4.3980 mL | | 10 mM | 0.2199 mL | 1.0995 mL | 2.1990 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.50 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.50 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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