Cycloleucine is a specific inhibitor of S-adenosyl-methionine mediated methylation. Cycloleucine is antagonist of NMDA receptor associated glycine receptor, with a K i of 600 μM. Cycloleucine is also a competitive inhibitor of ATP: L-methionine-S-adenosyl transferase in vitro. Cycloleucine has anxiolytic and cytostatic effects.
性状
Solid
IC50 & Target[1][2]
Ki: 600 μM (NMDA)
体外研究(In Vitro)
Cycloleucine (4-40 mM; 3 h) blocks internal methylation of viral RNA in B77 transformed chick embryo fibroblasts.Cycloleucine (40 mM; 24 h) blocks the formation of both mA and the penultimate G in B77 38S RNA subunits by greater than 90%.Cytostatic (10 μg/mL) inhibits the viability human KB and mouse L1210s leukemia cell lines. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Cycloleucine (0.5-4 μg; intracerebroventrical injection) increases time spent in open arms, open arm entries, and extreme arrivals in rats.
Cycloleucine reduces thymus and spleen weights in Semliki Forest virus (SFV) strain A7(74) infected and control mice. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Hood WF, et, al. 1-Aminocyclobutane-1-carboxylate (ACBC): a specific antagonist of the N-methyl-D-aspartate receptor coupled glycine receptor. Eur J Pharmacol. 1989 Feb 28;161(2-3):281-2.[2]. Caboche M, et, al. RNA methylation and control of eukaryotic RNA biosynthesis. Effects of cycloleucine, a specific inhibitor of methylation, on ribosomal RNA maturation. Eur J Biochem. 1977 Mar 15;74(1):19-29.
溶解度数据
In Vitro: H2O : 20 mg/mL (154.85 mM; Need ultrasonic)DMSO : < 1 mg/mL (ultrasonic) (insoluble or slightly soluble)配制储备液