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- 详细信息
- 技术资料
- 保存条件：
Powder: -20℃，2 years
- 保质期：
Powder: -20℃，2 years
- 英文名：
INCA-6
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
3519-82-2
- 规格：
25mg/10mg/5mg/1mg
| 规格： | 25mg | 产品价格： | ￥2810.0 |
|---|---|---|---|
| 规格： | 10mg | 产品价格： | ￥1650.0 |
| 规格： | 5mg | 产品价格： | ￥1040.0 |
| 规格： | 1mg | 产品价格： | ￥423.0 |
| 基本信息 | |
| CAS | No.3519-82-2 |
| 英文名称 | INCA-6 |
| 分子式 | C20H12O2 |
| 分子量 | 284.31 |
| 溶解性 | Soluble in DMSO ≥0.1mg/mL(Need ultrasonic) |
| 纯度 | ≥98% |
| 外观(性状) | Solid |
| 储存条件 | Powder: -20℃，2 years |
| MDL | MFCD00226933 |
| SMILES | C1=CC=C2C3C4=CC=CC=C4C(C2=C1)C5=C3C(=O)C=CC5=O |
| InChIKey | GCHPUOHXXCNSQL-UHFFFAOYSA-N |
| InChI | InChI=1S/C20H12O2/c21-15-9-10-16(22)20-18-12-6-2-1-5-11(12)17(19(15)20)13-7-3-4-8-14(13)18/h1-10，17-18H |
| PubChem CID | 230748 |
| 靶点 | NFAT |
| 通路 | Immunology & Inflammation |
| 背景说明 | INCA-6是一种细胞渗透性 NFAT 抑制剂。INCA-6 特异性阻断 NFAT底物靶向钙调神经磷酸酶位点，是 calcineurin (CN)-NFAT 信号传导的有效抑制剂。 |
| 生物活性 | INCA-6 (Triptycene-1，4-quinone) is a cell-permeable NFAT inhibitor. INCA-6 specifically blocks targeting of NFAT(P) substrate to the calcineurin (CN) phosphatase site and is an effective inhibitor of CN-NFAT signaling[1][2][3]. |
| In Vitro | INCA-6 (5 μM; for 24-hour) prevents transient outward K+ current (Ito) downregulation in 3-Hz cells[1].Pre-treatment of BV-2 cells with INCA-6 (10 μM) significantly inhibits ATP-induced CXCL2 expression in BV-2 cells. INCA-6 also inhibits ATP-induced CXCL2 expression in rat primary microglia[2]. INCA-6 (5 μM) reduces SERCA2 transcript levels as well as protein expression， in the absence or in the presence of thapsigargin (TG)[3].INCA-6 (1.0 and 2.5 μM; 24 hours ) treatment significantly decreases both VEGF and serum-induced human retinal microvascular endothelial cells (HRMEC) proliferation， but does not affect baseline proliferation[4].Cell Proliferation Assay[4]Cell Line:Human retinal microvascular endothelial cells;Concentration:0.5， 1.0， or 2.5 μM;Incubation Time:24 hours;Result:Significantly inhibited VEGF-induced proliferation at 1.0 and 2.5 μM concentrations. |
| 细胞实验 | INCA-6 (5.0， or 25.0 μM) treatment significantly reduces pathologic neovascularization in oxygen-induced retinopathy (OIR)[4].Animal Model: Rats bearing OIR model[4];Dosage:2.5， 5.0， or 25.0 μM;Administration:Intravitreal injection on days 14(0) and 14(3);Result:Decreased the severity of OIR in a dose dependent manner. Significant inhibition was seen at 5.0 and 25.0 μM concentrations. |
| 数据来源文献 | [1]. Ling Xiao， et al. Mechanisms underlying rate-dependent remodeling of transient outward potassium current in canine ventricular myocytes. Circ Res. 2008 Sep 26;103(7):733-42. [2]. Miho Shiratori，et al. P2X7 receptor activation induces CXCL2 production in microglia through NFAT and PKC/MAPK pathways. J Neurochem. 2010 Aug;114(3):810-9. [3]. Anand Mohan Prasad， et al. Silencing calcineurin A subunit reduces SERCA2 expression in cardiac myocytes. Am J Physiol Heart Circ Physiol. 2011 Jan;300(1):H173-80. [4]. Colin A Bretz， et al. The role of the NFAT signaling pathway in retinal neovascularization. Invest Ophthalmol Vis Sci. 2013 Oct 25;54(10):7020-7. |
| 单位 | 瓶 |
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II1900 INCA-6 免疫学/炎症 索莱宝
￥423 - 2810
