6-Aminonicotinamide, a potent antimetabolite of nicotinamide, is competitive NADP+-dependent enzyme glucose-6-phosphate dehydrogenase (G6PD) inhibitor (Ki=0.46 μM) [1]. Immediately following 45 min i.v. infusion of [2-(13)C]glucose to controls and 6-AN-treated (50 mg/kg i.p. given 4 h previously) Sprague-Dawley rats (n = 5 for both groups), metabolism was arrested using freeze-funnel fixation. Chloroform-methanol-water neocortical extracts from animals administered with 6-AN demonstrated elevated levels of 6-phosphogluconate and 6-phosphoglucono-delta-lactone, both of which demonstrated labeling through metabolism of [2-(13)C]glucose[2]. 6-Aminonicotinamide (100 nM; 7 days) causes a significant decrease in the human AR+, hormone-sensitive prostate cancer cell lines LNCaP and LAPC4, as well as the CRPC-derivative C4-2 and 22Rv1 cell models. 6-Aminonicotinamide (100 nM ± 10 nM R1881 as indicated for 3 days) increases both basal- and R1881-mediated ROS levels, suggesting 6-Aminonicotinamide is blocking the cells' antioxidant defense. 6-Aminonicotinamide also increases ROS levels in C4-2 cells[3]. 6-Aminonicotinamide (20 mg/kg; i.p.; thress times; days 1, 10 or 11, and 21) alone induces a small but significant tumor growth delay (4.3+/-0.8 days). Treatment with 6-Aminonicotinamide followed by radiation induces a tumor growth delay of 57.0+/-3.8 days in CD8F1 breast tumor model[4].
6-Aminonicotinamide/6-氨基烟酰胺 细胞实验
Cell Line
Concentration
Treated Time
Description
References
ES2 cells
10 µM
To study the effect of 6-Aminonicotinamide on CMA activity, results showed that 6-AN, as a CMA activator, could decrease the protein levels of EIF4A1, EIF4H, and DDX3X.
Autophagy. 2019 Sep;15(9):1558-1571.
SUM159 cells
10 µM
To study the effect of 6-Aminonicotinamide on CMA activity, results showed that 6-AN, as a CMA activator, could decrease the protein levels of EIF4A1, EIF4H, and DDX3X.
Autophagy. 2019 Sep;15(9):1558-1571.
C33A cells
26.78 μM
6 days
Inhibit HPV16 E6-induced cell proliferation
Redox Biol. 2024 May;71:103108.
PHKs cells
81.06 μM
6 days
Inhibit HPV16 E6-induced cell proliferation
Redox Biol. 2024 May;71:103108.
Mouse microglia-enriched cultures
10 μM
2 days
Inhibition of G6PD activity, reducing LPS-induced oxidative stress
J Neuroinflammation. 2019 Dec 5;16(1):255.
Rat mesencephalic neuron-glia co-cultures
10 μM
7 days
Inhibition of G6PD activity, attenuating LPS-induced dopaminergic neurodegeneration
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