T-448

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

T-448 (T448) 是 LSD1 酶活性的特异性抑制剂，可增强原代培养的大鼠神经元中的 H3K4 甲基化，但对人 TF-1a 成红细胞中的 LSD1-GFI1B 复合物几乎没有影响。

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.

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.

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.

T448 | T 448

Chromatin/Epigenetic

Histone Demethylase

Histone Demethylase

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1597426-53-3

444.506

C21H24N4O5S

>98% (HPLC)

In Vitro:?DMSO : 16.67 mg/mL (43.13 mM)

CC1=NN=C(S1)NC(=O)C2=CC=CC(=C2)C3CC3NC4CCC4.C(=CC(=O)O)C(=O)O

3-((1S,2R)-2-(cyclobutylamino)cyclopropyl)-N-(5-methyl-1,3,4-thiadiazol-2-yl)benzamide fumarate

(-20℃)

With Ice Pack

≥ 2 years