Bioactivity | T-448 is a specific, orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM. T-448 enhances H3K4 methylation in primary cultured rat neurons[1]. |
Target | IC50: 22 nM (LSD1). |
Invitro | 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[1]. RT-PCR[1]. Cell Line: |
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[1].T-448 increases H3K4 methylation in the brain without causing hematological side effects even at 100 mg/kg[1]. Animal Model: |
Name | T-448 |
CAS | 1597426-53-3 |
Formula | C17H20N4OS.1/2C4H4O4 |
Molar Mass | 386.50 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | -20°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
Reference | [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. |