| Bioactivity | 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]. | ||||||||||||
| Invitro | 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: | ||||||||||||
| In Vivo | INCA-6 (5.0, or 25.0 μM) treatment significantly reduces pathologic neovascularization in oxygen-induced retinopathy (OIR)[4]. Animal Model: | ||||||||||||
| Name | INCA-6 | ||||||||||||
| CAS | 3519-82-2 | ||||||||||||
| Formula | C20H12O2 | ||||||||||||
| Molar Mass | 284.31 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |