2. Epigenetics Neuronal Signaling
  3. Histone Demethylase Amyloid-β
  4. LSD1-IN-43

LSD1-IN-43 是一种高选择性、可逆性、口服活性且具有血脑屏障通透性的 LSD1 抑制剂，其 IC50 值为 0.8 μM。LSD1-IN-43 对 LSD1 的两个同源物 MAO-A 和 MAO-B 的抑制活性较低。LSD1-IN-43 显著抑制 Aβ 聚集并增强 Aβ 诱导的神经元细胞活力。LSD1-IN-43 可用于阿尔茨海默病 (AD) 的研究[1]。

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LSD1-IN-43 Chemical Structure

LSD1-IN-43 Chemical Structure

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LSD1-IN-43 相关抗体

Top Publications Citing Use of Products

查看 Histone Demethylase 亚型特异性产品:

查看所有亚型
KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LSD1-IN-43 is a highly selective, reversible, orally active and brain-penetrant LSD1 inhibitor with an IC50 value of 0.8 μM. LSD1-IN-43 has low inhibitory activity against MAO-A and MAO-B, two homologs of LSD1. LSD1-IN-43 significantly inhibits Aβ aggregation and enhances Aβ-induced neuronal cell viability. LSD1-IN-43 can be used for the study of Alzheimer’s disease (AD)[1].

体外研究
(In Vitro)


LSD1-IN-43 (10 μM) 对 LSD1 具有高度选择性和可逆抑制作用，对单胺氧化酶 A (抑制率 7%) 和单胺氧化酶 B (抑制率 4.9%) 几乎没有作用[1]。

LSD1-IN-43 (25-100 μM) 表现出低毒性，并能有效减少 HT22 细胞中 Aβ1-42 的产生[1]。

LSD1-IN-43 (10 μM) 对 Aβ1-42 聚集表现出显著的抑制作用，抑制率为 66.19%，远高于 Curcumin (HY-N0005) 的 49.98%[1]。

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

LSD1-IN-43 相关抗体:
体内研究
(In Vivo)

LSD1-IN-43 (125-500 μM, 24-56 h) 在 CL4176 转基因线虫模型中表现出浓度依赖性的延长寿命情况，并且可以减少瘫痪的发生[1]。

LSD1-IN-43 (40-80 mg/kg, i.g.) 可恢复 LSD1 调控的组蛋白标记物 (H3K9me2) 的水平，同时改善阿尔茨海默病小鼠的学习、记忆以及认知功能缺陷[1]。

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

Animal Model: APP/PS1 Mice (5 weeks)[1]
Dosage: 40, 80 mg/kg
Administration: Intragastric administration (i.g.)
Result: Improved performance in the Morris Water Maze compared to the saline-treated APP/PS1 group.
Reduced escape latency and improved ability to locate the hidden platform compared to the saline-treated APP/PS1 group.
Increased correct alternations and better spatial recognition compared to the saline-treated APP/PS1 group.
Reduced the expression of neuroinflammatory markers (IBAI for microglia and GFAP for astrocytes) and inflammatory cytokines (IL-1β and TNF-α) in the hippocampal CA1 region of APP/PS1 mice compared to the saline-treated group.
Reduced Aβ 1-42 deposition in the hippocampus ,with high-dose treatment (80 mg/kg) showing a more pronounced reduction compared to the saline-treated APP/PS1 group.
Restored the expression of H3K9me2,which is a histone marker regulated by LSD1 compared to the saline-treated APP/PS1 group.
Increased inneuron density and compact arrangement, reduced inuclear pyknosis and cytoplasmic vacuolation compared to the saline-treated APP/PS1 group.
分子量

377.43

Formula

C23H23NO4
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

LSD1-IN-43 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

Keywords:

LSD1-IN-43Histone DemethylaseAmyloid-ββ-amyloid peptideAβAbetaAlzheimer’s diseaseLSD1 inhibitorAtractylodes macrocephalaamyloid βneuroinflammationcognitionInhibitorinhibitorinhibit

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