INCA-6|3519-82-2|(Triptycene-1,4-quinone)-陌孚医药/Medlife

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INCA-6 (Synonyms: Triptycene-1,4-quinone)

目录号: PC10105 纯度: ≥98%

CAS No. :3519-82-2

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中文名称

INCA-6

英文名称

INCA-6

英文别名

9,10-DIHYDRO-9,10[1',2']-BENZENOANTHRACENE-1,4-DIONE;INCA-6 NFAT Activation Inhibitor III;INCA-6;NFAT Activation Inhibitor III;9,10-dihydro-9,10-o-benzenoanthracene-1,4-dione;Inhibitor of NFAT-Calcineurin Association-6;triptycene quinone;triptycene-1,4-quinone;triptycene-quinine

Cas No.

3519-82-2

分子式

C₂₀H₁₂O₂

分子量

284.31

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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.

性状

Solid

体外研究(In Vitro)

INCA-6 (5 μM; for 24-hour) prevents transient outward K+ current (Ito) downregulation in 3-Hz cells.
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.
INCA-6 (5 μM) reduces SERCA2 transcript levels as well as protein expression, in the absence or in the presence of thapsigargin (TG).
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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

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.

体内研究(In Vivo)

INCA-6 (5.0, or 25.0 μM) treatment significantly reduces pathologic neovascularization in oxygen-induced retinopathy (OIR).

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Rats bearing OIR model
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.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[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. [Information]

[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. [Information]

[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. [Information]

[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. [Information]

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