T-448

CAS No. 1597426-53-3

T-448( T448 | T 448 )

Catalog No. M12284 CAS No. 1597426-53-3

T-448 (T448) is a specific inhibitor of LSD1 enzyme activity, enhances H3K4 methylation in primary cultured rat neurons but has little impact on LSD1-GFI1B complex in human TF-1a erythroblasts.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    T-448
  • Note
    Research use only, not for human use.
  • Brief Description
    T-448 (T448) is a specific inhibitor of LSD1 enzyme activity, enhances H3K4 methylation in primary cultured rat neurons but has little impact on LSD1-GFI1B complex in human TF-1a erythroblasts.
  • Description
    T-448 (T448) is a specific inhibitor of LSD1 enzyme activity, enhances H3K4 methylation in primary cultured rat neurons but has little impact on LSD1-GFI1B complex in human TF-1a erythroblasts; increases brain H3K4 methylation and partially restored learning function in mice with NMDA receptor hypofunction, shows unique therapeutic approaches for central nervous system disorders associated with epigenetic dysregulation.
  • 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. RT-PCR.Cell Line:Primary cultured rat neurons. Concentration:0-10 μM.Incubation Time:1 day treatment.Result:Increased Ucp2 H3K4me2 and Ucp2 mRNA significantly.
  • 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. Animal Model:NR1-hypo mice.Dosage:1, 10 mg/kg.Administration:Orally, 3 weeks.Result:Dose-dependently increased the H3K4me2 levels around Bdnf, Arc, and Fos genes in the mouse hippocampus. Resulted in partial but statistically significant and dosedependent rescue effects on the rate of correct choices in NR1-hypo mice.
  • Synonyms
    T448 | T 448
  • Pathway
    Chromatin/Epigenetic
  • Target
    Histone Demethylase
  • Recptor
    Histone Demethylase
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1597426-53-3
  • Formula Weight
    444.506
  • Molecular Formula
    C21H24N4O5S
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 16.67 mg/mL (43.13 mM)
  • SMILES
    CC1=NN=C(S1)NC(=O)C2=CC=CC(=C2)C3CC3NC4CCC4.C(=CC(=O)O)C(=O)O
  • Chemical Name
    3-((1S,2R)-2-(cyclobutylamino)cyclopropyl)-N-(5-methyl-1,3,4-thiadiazol-2-yl)benzamide fumarate

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Matsuda S, et al. Neuropsychopharmacology. 2018 Dec 22. doi: 10.1038/s41386-018-0300-9.
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