T-448 is a specific, orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC 50 of 22 nM. T-448 enhances H3K4 methylation in primary cultured rat neurons.
性状
Solid
IC50 & Target[1][2]
IC50: 22 nM (LSD1).
体外研究(In Vitro)
T-448 enhances the levels of H3K4 methylation, increased mRNA expression of neural plasticity-related genes including brain derived neurotrophic factor (Bdnf), and ameliorated learning dysfunction. has not independently confirmed the accuracy of these methods. They are for reference only.RT-PCR.
体内研究(In Vivo)
T-448 has minimal impact on the LSD1-GFI1B complex and a superior hematological safety profile in mice via the generation of a compact formyl-FAD adduct. T-448 increases brain H3K4 methylation and partially restored learning function in mice with NMDA receptor hypofunction.
T-448 increases H3K4 methylation in the brain without causing hematological side effects even at 100 mg/kg. 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
-20°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
参考文献
[1]. Matsuda S, et al. T-448, a specific inhibitor of LSD1 enzyme activity, improves learning function without causing thrombocytopenia in mice. Neuropsychopharmacology. 2018 Dec 22.
溶解度数据
In Vitro: DMSO : 16.67 mg/mL (43.13 mM; Need ultrasonic)配制储备液