1. Epigenetics
  2. Histone Demethylase
  3. T-448 free base

T-448 free base 是赖氨酸特异性去甲基化酶1 (LSD1,一种H3K4去甲基化酶) 不可逆的、口服有效的抑制剂,IC50 值为 22 nM。T-448 free base能够加强原代培养的大鼠神经元中H3K4的甲基化。

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T-448 free base Chemical Structure

T-448 free base Chemical Structure

CAS No. : 1597426-52-2

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  • 生物活性

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生物活性

T-448 free base 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 free base enhances H3K4 methylation in primary cultured rat neurons[1].

IC50 & Target

IC50: 22 nM (LSD1)[1].

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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line: Primary cultured rat neurons.
Concentration: 0-10 μM.
Incubation Time: 1 day treatment.
Result: Increased Ucp2 H3K4me2 and Ucp2 mRNA significantly.
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[1].
T-448 increases H3K4 methylation in the brain without causing hematological side effects even at 100 mg/kg[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NR1-hypo mice[1].
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.
分子量

328.43

Formula

C17H20N4OS

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献

T-448 free base 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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T-448 free base
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HY-122635
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