6-Aminonicotinamide (Synonyms: 6-AN,NSC 21206,SR 4388) |
Catalog No.GC10462 |
La 6-aminonicotinamida, un potente antimetabolito de la nicotinamida, es un inhibidor competitivo de la enzima glucosa-6-fosfato deshidrogenasa (G6PD) dependiente de NADP+- (Ki =0,46 μM). La 6-aminonicotinamida interfiere con la glucÓlisis, lo que da como resultado el agotamiento de ATP y actÚa en sinergia con los medicamentos de quimioterapia que reticulan el ADN, como el cisplatino, para matar las células cancerosas.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 329-89-5
Sample solution is provided at 25 µL, 10mM.
Ki: 0.46 μM
6-Aminonicotinamide is a 6-phosphogluconate dehydrogenase inhibitor.
6-Phosphogluconate dehydrogenase, an enzyme in the pentose phosphate pathway, can produce ribulose 5-phosphate from 6-phosphogluconate. 6-Phosphogluconate dehydrogenase is also an oxidative carboxylase catalyzing the decarboxylating reduction of 6-phosphogluconate into ribulose 5-phosphate in the presence of NADP.
In vitro: 6-Aminonicotinamide could be metabolized to 6-amino-NAD(P+), a competitive inhibitor of NAD(P+)-requiring processes, especially the pentose phosphate pathway enzyme, 6-phosphogluconate dehydrogenase. Moreove, 6-aminonicotinamide as a single agent could cause a significant inhibition of glycolytic flux but had no effect on the pentose phosphate pathway. 31P-NMR studies of perifused RIF-1 cells indicated that 4 h of exposure to 6-aminonicotinamide was enough to cause significant accumulation of 6-phosphogluconate, the substrate for this enzyme [1].
In vivo: The influence of 6-aminonicotinamide on the G-6-P-DH- and 6-PG-DH-levels of the pentose phosphate pathway in the kidney was investigated. Following i.p. administration of 6-aminonicotinamide at 6 mg/kg, the 6-PG-level rose from a value less than 10 nmoles/g to 1000 nmoles/g fresh weight within 24 h. In addition, at the end of the assay, after 7 days, a 6-PG-concentration of about 150 nmoles/g fresh weight was still seen. Moreove, the G-6-P level simultaneously rose with the 6-PG-level to about 150% of the control level and returned to normal on the 5th day [2].
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Street, J. C.,Alfieri, A.A. and Koutcher, J.A. Quantitation of metabolic and radiobiological effects of 6-aminonicotinamide in RIF-1 tumor cells in vitro. Cancer Research 57, 3956-3962 (1997).
[2] Lange, K. and Proft, E.R. Inhibition of the 6-phosphogluconate dehydrogenase in the rat kidney by 6-aminonicotinamide. Naunyn-Schmiedeberg's Archives of Pharmacology 267, 177-180 (1970).
Average Rating: 5
(Based on Reviews and 39 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *