2. Neuronal Signaling Autophagy Apoptosis
  3. Monoamine Oxidase Autophagy Apoptosis α-synuclein
  4. Harmol

Harmol 是 TFEB 激活剂，是一种可口服的单胺氧化酶抑制剂，有抗肿瘤，抗抑郁，延缓衰老的活性。Harmol 可诱导细胞有丝分裂，自噬和凋亡。Harmol 通过调节自噬-溶酶体通路，促进 α-突触核蛋白 (α-synuclein) 降解，改善小鼠帕金森模型运动损伤。

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Harmol Chemical Structure

Harmol Chemical Structure

CAS No. : 487-03-6

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥550
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1 mg ￥190
In-stock
5 mg ￥500
In-stock
10 mg ￥800
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25 mg ￥1500
In-stock
50 mg ￥2200
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200 mg   询价  

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Harmol 相关抗体

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MCE 顾客使用本产品发表的 1 篇科研文献

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Harmol is a TFEB activator, an orally active monoamine oxidase inhibitor that has anti-tumor, anti-depressant, and anti-aging effects. Harmol can induce cell mitosis, autophagy and apoptosis. Harmol promotes the degradation of α-synuclein through the regulation of the autophagy-lysosomal pathway, improving motor deficits in mouse models of Parkinson's disease[1][2][3][4].

IC50 & Target

MAO-B

 

体外研究
(In Vitro)

Harmol (3-30 μM，6-24 h) 在 PC12 细胞中，以剂量和时间依赖的方式降低 α-syn[1]。
Harmol (30 μM，24 h) 在 Hela 细胞中促进外源性 TFEB (转录因子 EB) 的核易位，在 N2a 促进内源性 TFEB 的核易位，并伴随自噬通量和溶酶体生物发生的恢复[1]。
Harmol (0-100 μM，24 和 48 h) 呈时间依赖性与剂量依赖性抑制 U251MG 细胞增殖，诱导细胞死亡[2]。
Harmol (0-100 μM，0-48 h) 在 U251MG 细胞中抑制 survivin 的表达，促进 LC3-Ⅰ 和 LC3-Ⅱ 蛋白的表达，抑制 Akt/mTOR 通路，诱导细胞自噬和细胞凋亡[2]。
Harmol (0-100 μM，0-24 h) 在 A549 和 H226 细胞中具有轻微细胞毒性，在 H596 中表现出很强的细胞毒性，抑制肿瘤增殖[3]。
Harmol (60 μM，3-6 h) 提高了 caspase-3，caspase-6，caspase-8，caspase-9 活性，增加了 RAPA (caspase-3 内源性底物) 裂解，诱导 H596 细胞凋亡[3]。
Harmol (1.3 μg/mL，1-3 h) 在 C2C12 细胞中激活了细胞自噬[4]。
Harmol (1.3 μg/mL，45-60 min) 在 C2C12 细胞中是线粒体特异性自噬，且仅发生在无活性的 TMRM 阴性线粒体中[4]。
Harmol (1.3 μg/mL，16 h) 在 C2C12 细胞中代表线粒体功能的标志物表达上调[4]。
Harmol (1.3 μg/mL，0-20 h) 对 MAO-B 有特异性抑制作用[4]。
Harmol 减少 GABA 能神经传递，但不能完全抑制 GABA 与 GABAAR 的结合，GABAAR 活性对 Harmol 介导的线粒体去极化至关重要，并依靠线粒体功能发挥作用[4]。

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

Harmol 相关抗体:

Western Blot Analysis[1][4]

Cell Line: Tet-on inducible PC12 cells[1]; Hela, N2a[1]; C2C12[4]
Concentration: 3, 10, 30 μM; 30 μM; 1.3 μg/mL; 1.3 μg/mL
Incubation Time: 6, 12, 24 h; 24 h; 16 h; 24 h
Result: Reduced the phosphorylation (p-) and total α-syn levels in PC12 cells in a dose-dependent and time-dependent manner, showing pro-degradation activity between 6 and 24 hours.
Enhanced the LC3B-Ⅱ/LC3B-Ⅰ ratio in PC12 cells, promoted TFEB expression, and increased AMPK phosphorylation at the THr172 site. It facilitated the nuclear translocation of exogenous TFEB in HeLa cells and the translocation of endogenous TFEB to the nucleus in N2a cells. This also increased the expression of the lysosomal marker LAMP1 (lysosomal-associated membrane protein 1) precursor and the mature form of CTSD (cathepsin D).
Showed in C2C12, the protein expression of the mitochondrial transcription and replication factor TFAM and components of complex III (UQCRC2) and complex V (ATP5a) was significantly elevated, along with an increase in polyamine spermidine levels, while DYRK1A phosphorylation remained unchanged.

Immunofluorescence[1]

Cell Line: Hela, PC12
Concentration: 30 μM
Incubation Time: 24 h
Result: Caused 60% of Flag-TFEB to undergo nuclear translocation and significantly increased the lysosomal content.

Cell Autophagy Assay[1][4]

Cell Line: PC12[1]; C2C12[4]
Concentration: 3, 10, 30 μM; 1.3 μg/mL
Incubation Time: 24 h; 45, 60 min
Result: Promoted the autophagic degradation of p62 in PC12 induced cells.
Showed strong co-localization of lysosomes and mitochondria in C2C12 cells.

Cell Viability Assay[2] [3]

Cell Line: U251MG[2]; A549, H226, H596[3]
Concentration: 0, 25, 50, 75, 100 μM
Incubation Time: 24, 48h; 8, 16, 24 h
Result: Showed after 24 hours of treatment, the survival rates of U251MG cells were 102.3%, 99.8%, 93.7%, 82.3%, and 66.7%. After 48 hours of treatment, the survival rates dropped to 98.0%, 93.6%, 72.5%, 38.2%, and 17.3%.
Showed slight cytotoxicity in A549 and H226 cells, while exhibiting strong cytotoxicity in H596.

Western Blot Analysis[2][4]

Cell Line: U251MG[2]; C2C12[4]
Concentration: 0, 12.5, 25, 50, 75, 100 μM; 1.3 μg/mL
Incubation Time: 0, 6, 12, 24, 36, 48 h; 1 and 3 h
Result: Showed the activity of caspase-3 and -9 increased in U251MG cells, while there was no significant change in the activity of caspase-8, and a cleaved form of PARP (an endogenous substrate of caspase-3) was detected. There was a dose- and time-dependent inhibition of survivin protein expression. Both LC3-I and LC3-II proteins were expressed, with LC3-II levels increasing over time, indicating that autophagy occurs before apoptosis.
Decreased the phosphorylation of Akt protein in U251MG cells, reduced the level of mTOR phosphorylation (activation), and lowered the expression of p-P70S6K and p-4E-BP1.
Showed in C2C12 cells, aa upregulated LC3 expression, induced PINK1, and activated AMPK.
体内研究
(In Vivo)

Harmol (10-40 mg/kg，i.g.，一天两次，一个月) 在 α-syn 转基因小鼠模型中，可改善运动缺陷，包括运动和协调。下调黑质和前额皮质 α-syn 水平，增强自噬介导的蛋白质聚集体降解[1]。
Harmol (100 mg/kg，灌胃，每日一次，三周) 在小鼠中有轻微的抗焦虑作用[4]。
Harmol (100 mg/kg，口服，三个月) 改善肥胖小鼠胰岛素，葡萄糖稳态和代谢适应性，且对肾功能无影响[4]。
Harmol (15 μg/kg，口服，0-50 天) 延长无脊椎动物的寿命[4]。
Harmol (100 mg/kg，口服，两个月) 在老年小鼠延缓衰弱[4]。

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

Animal Model: A53T α-syn mice[1]
Dosage: 10, 20, 40 mg/kg; twice a day; one month
Administration: i.g.
Result: Made mice climb the rod faster, spent more time on the spinning rod, travelled farther in open areas, increased their step frequency and standing posture, reduced posture width, stride, step length, swing, and showed recovery of autonomous movement behavior.
Reduced the expression of α-syn and p62 in the brain’s substantia nigra and prefrontal cortex.
Increased the phosphorylation levels of AMPK Thr172 and TFEB in the substantia nigra, while decreasing the phosphorylation level of mTOR Ser2448.Increased the expression of LC3B-II/LC3B-I, LAMP1, pro-CTSD, and mature ctsd in the substantia nigra, while reducing the expression of p62 and p-ULK1(Ser757)/ULK1.
Animal Model: Male mice[4]
Dosage: 100 mg/kg, single dose; 100 mg/kg, daily, 3 weeks
Administration: i.g.
Result: Showed no change in blood glucose levels, with no change in fasting-mediated ketone body increase, and low permeability of the blood-brain barrier. High levels in the liver and plasma, but low levels in the brain. The mitochondrial autophagy marker PINK1 was elevated, while the phosphorylation levels of AMPK target ACC1 or the autophagy marker LC3-II/LC3-I were unaffected.
Showed no change in the time mice spent in the aversive area (center) versus the non-aversive area (border), with no differences in elevated plus maze tests, and significantly less time spent in the dark/light box.
Increased phosphorylation of ACC2 in the liver and BAT, and levels of the mitochondrial autophagy marker PINK1 were also significantly elevated in the liver, BAT, and soleus.
Animal Model: HFD-fed obese mice[4]
Dosage: 100 mg/kg, 3 months
Administration: Oral
Result: Reduced the increase in mouse weight, decreased water intake, reduced fat levels, without causing weight loss, lowered fasting blood sugar levels, improved glucose tolerance, and improved insulin resistance without affecting insulin sensitivity. Energy expenditure and oxygen consumption decreased, respiratory quotient remained unchanged, and there were no changes in physical activity. There was less fatty liver, lighter liver weight, and significantly higher levels of serum adiponectin and spermidine in the liver.
Animal Model: Nematodes[4]
Dosage: 15 mg/ml; 0, 10, 20, 30, 40, 50 days
Administration: Oral
Result: Reduced AMPK phosphorylation levels, but not significantly, and extent lifespan.
Animal Model: 2-year-old mice[4]
Dosage: 100 mg/mL, two months
Administration: Oral
Result: Lowered fasting blood sugar, reduced total blood cholesterol, allowed for better coordination during exercise for a longer time, maintained grip strength over time, improved muscle strength, enhanced cardiovascular fitness, produced less lactic acid, and increased total myosin heavy chains.
分子量

198.22

Formula

C12H10N2O
CAS 号
性状

固体

颜色

Off-white to light yellow

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 83.33 mg/mL (420.39 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 5.0449 mL 25.2245 mL 50.4490 mL
5 mM 1.0090 mL 5.0449 mL 10.0898 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (10.49 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (10.49 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.77%

COA (287 KB) HNMR (218 KB) LCMS (264 KB)

产品使用指南 (1538 KB)
参考文献

Harmol 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 5.0449 mL 25.2245 mL 50.4490 mL 126.1225 mL
5 mM 1.0090 mL 5.0449 mL 10.0898 mL 25.2245 mL
10 mM 0.5045 mL 2.5224 mL 5.0449 mL 12.6122 mL
15 mM 0.3363 mL 1.6816 mL 3.3633 mL 8.4082 mL
20 mM 0.2522 mL 1.2612 mL 2.5224 mL 6.3061 mL
25 mM 0.2018 mL 1.0090 mL 2.0180 mL 5.0449 mL
30 mM 0.1682 mL 0.8408 mL 1.6816 mL 4.2041 mL
40 mM 0.1261 mL 0.6306 mL 1.2612 mL 3.1531 mL
50 mM 0.1009 mL 0.5045 mL 1.0090 mL 2.5224 mL
60 mM 0.0841 mL 0.4204 mL 0.8408 mL 2.1020 mL
80 mM 0.0631 mL 0.3153 mL 0.6306 mL 1.5765 mL
100 mM 0.0504 mL 0.2522 mL 0.5045 mL 1.2612 mL
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:

Harmol487-03-6Monoamine OxidaseAutophagyApoptosisα-synucleinMAOα-SynMitosisObese miceNematodesAntidepressantsSlowing down agingInhibitorinhibitorinhibit

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