INCA-6 (Triptycene-1,4-quinone) 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-permeableNFATinhibitor. INCA-6 specifically blocks targeting of NFAT(P) substrate to the calcineurin(CN)phosphatasesite and is an effective inhibitor of CN-NFAT signaling[1][2][3]. |
体外研究
(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. |
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体内研究
(In Vivo) | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
