Fulvene-5

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Fulvene-5 

Fulvene-5 是一种有效的 NADPH 氧化酶 4 (NOX4) 抑制剂,具有抗氧化特性。Fulvene-5 是一种活性氧 (ROS) 修饰剂和有效的辐射防护剂,并具有抗肿瘤活性。

Fulvene-5

Fulvene-5 Chemical Structure

CAS No. : 1075723-01-1

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生物活性

Fulvene-5 is a potent NADPH oxidase 4 (NOX4) inhibitor with antioxidant properties. Fulvene-5 is a reactive oxygen species (ROS) modifying agent and a potent radioprotector. Fulvene-5 has antitumor activity[1][2][3].

IC50 & Target

NADPH oxidase 4 (NOX4)[1]; Reactive oxygen species (ROS)[2]

体外研究
(In Vitro)

Fulvene-5 (10 µM; 1 hour) facilitates the reversal of HCT116 TP53 wild type (WT) and HCT116 isogenic TP53 null mutant (Mut) cell cultures adaptive responses from pro-survival to radio-sensitization and vice versa. These changes are accompanied by corresponding reversals in the translocation of survivin to the nuclei of TP53 WT and to the cytoplasm of TP53 Mut cells. The potential role of NOX4 in the expression of the survivin-associated adaptive response is investigated by transfecting HCT116 cells with NOX4 siRNA oligomers to inhibit NOX4 expression. Under these conditions NOX4 expression is inhibited by about 50%[1].
Fulvene-5 (0.5-1.0 μM) treatment decreases the expression of Ang2, delta-like ligand 4 (DLL4), placental growth factor (PLGF), and Nrarp in a dose-dependent manner in bEnd.3 cells[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Fulvene-5 (120 mg/kg/d; intraperitoneal injection; daily; for 2 weeks; nude mice) treatment potently inhibits hemangioma growth in mice[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude mice injected with bEnd.3 cells[2]
Dosage: 120 mg/kg/d
Administration: Intraperitoneal injection; daily; for 2 weeks
Result: Tumor growth in mice was significantly reduced.

分子量

358.43

Formula

C26H18N2

CAS 号

1075723-01-1

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.

参考文献
  • [1]. Murley JS, et al. ROS modifiers and NOX4 affect the expression of the survivin-associated radio-adaptive response. Free Radic Biol Med. 2018 Aug 1;123:39-52.

    [2]. Bhandarkar SS, et al. Fulvene-5 potently inhibits NADPH oxidase 4 and blocks the growth of endothelial tumors in mice. J Clin Invest. 2009 Aug;119(8):2359-65.

    [3]. Weyemi U, et al. Inactivation of NADPH oxidases NOX4 and NOX5 protects human primary fibroblasts from ionizing radiation-induced DNA damage. Radiat Res. 2015 Mar;183(3):262-70.

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