Description
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.
Product information
CAS Number: 1597426-53-3
Molecular Weight: 444.50
Formula: C21H24N4O5S
Chemical Name: (2E)-but-2-enedioic acid; 3-[(1R,2S)-2-(cyclobutylamino)cyclopropyl]-N-(5-methyl-1,3,4-thiadiazol-2-yl)benzamide
Smiles: CC1=NN=C(NC(=O)C2=CC(=CC=C2)[C@H]2C[C@@H]2NC2CCC2)S1.OC(=O)/C=C/C(O)=O
InChiKey: BNLKYWVPJPFTMA-YWNVCFPDSA-N
InChi: InChI=1S/C17H20N4OS.C4H4O4/c1-10-20-21-17(23-10)19-16(22)12-5-2-4-11(8-12)14-9-15(14)18-13-6-3-7-13;5-3(6)1-2-4(7)8/h2,4-5,8,13-15,18H,3,6-7,9H2,1H3,(H,19,21,22);1-2H,(H,5,6)(H,7,8)/b;2-1+/t14-,15+;/m1./s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 16.67 mg/mL (43.13 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
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.
Products are for research use only. Not for human use.
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