AFMK

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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。

AFMK 

AFMK 是褪黑激素的一种抗氧化代谢物，可减弱 X 射线诱导的小鼠 DNA、蛋白质和脂质氧化损伤。AFMK 是效果稍低的一种清洁剂，在生理 pH 值下的 pKa 为 8.7。具有抗氧化活性。AFMK 可通过调节细胞凋亡途径提高 Gemcitabine 在 PANC-1 细胞中的抗肿瘤作用。

AFMK

AFMK Chemical Structure

CAS No. : 52450-38-1

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生物活性

AFMK, antioxidant metabolite of Melatonin, attenuates X-ray-induced oxidative damage to DNA, proteins and lipids in mice. AFMK is a poorer scavenger. The pKa of AFMK at physiological pH is 8.7. Antioxidant capacity[1][2]. AFMK improves the anti-tumor effect of Gemcitabine in PANC-1 cells through the modulation of apoptotic pathway[3].

IC50 & Target

Human Endogenous Metabolite

 

体外研究
(In Vitro)

AFMK is one of the metabolites of melatonin and can be formed by both enzymatic or pseudoenzymatic and nonenzymatic metabolic pathways[1].
AFMK pretreatment significantly inhibits DNA damage. AFMK shows a very high level of in vitro hydroxyl radical scavenging potential which was measured by an electron spin resonance (ESR) study. IC50 values resulting from ESR analysis was 338.08 nM. AFMK, a melatonin metabolite, is a sparingly investigated biogenic amine[2].
AFMK administered to PANC-1 in combination with Gemcitabine inhibits the production of HSP70 and cIAP-2 as compared to the results obtained with Gemcitabine alone[3].

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

Western Blot Analysis[3]

Cell Line: Human pancreatic carcinoma cell line (PANC-1)
Concentration: 0.001, 0.1, 10, 1000 nM
Incubation Time:
Result: Augmented the inhibitory effects on HSP70 expression from 0.47 (Gemcitabine alone) to 0.13 (10 nM AFMK), 0.08 (0.1 nM AFMK) and 0.01 (0.001 nM AFMK).

体内研究
(In Vivo)

AFMK is a potent antioxidant in vivo. AFMK significantly reverses radiation-induced decline in the total antioxidant capacity of plasma in mice[2].

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

Animal Model: Male C57BL mice 8 wk of age[2]
Dosage: 10 mg/kg body weight
Administration: Intraperitoneal injection
Result: Radiation-induced decline in the total antioxidant capacity of plasma was significantly reversed in AFMK pretreated mice.
AFMK-pretreated irradiated groups showed a significantly lower value of comet tail length and % DNA in tail.

分子量

264.28

Formula

C13H16N2O4
CAS 号

52450-38-1
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]. Annia Galano, et al. On the free radical scavenging activities of melatonin’s metabolites, AFMK and AMK. J Pineal Res. 2013 Apr;54(3):245-57.

    [2]. Kailash Manda, et al. AFMK, a melatonin metabolite, attenuates X-ray-induced oxidative damage to DNA, proteins and lipids in mice. J Pineal Res. 2007 Apr;42(4):386-93.

    [3]. Anna Leja-Szpak, et al. Melatonin and its metabolite N1-acetyl-N2-formyl-5-methoxykynuramine (afmk) enhance chemosensitivity to gemcitabine in pancreatic carcinoma cells (PANC-1). Pharmacol Rep. 2018 Dec;70(6):1079-1088.

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