货号:A350584
同义名:
哈尔碱
/ Telepathine
Harmine是一种天然的双特异性酪氨酸磷酸化调节激酶(DYRK)抑制剂,具有抗癌和抗炎活性。它对5-HT2A血清素受体具有高亲和力,Ki值为397 nM。


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| 产品名称 | MAO ↓ ↑ | MAO-A ↓ ↑ | MAO-B ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sennoside A |
++
MAO, IC50: 17 μM |
98%+ | |||||||||||||||||
| Glycyrrhizic acid |
++++
MAO, IC50: 0.16 μM |
80% HPLC | |||||||||||||||||
| Rasagiline |
++++
MAO-A, IC50: 412 nM |
++++
MAO-B, IC50: 4.43 nM |
97% | ||||||||||||||||
| Isatin |
++
MAO, IC50: 15 μM |
+
MAO-A, IC50: 58 μM |
++
MAO-B, IC50: 14 μM |
98% | |||||||||||||||
| Paeonol |
+
MAO-A, IC50: 54.6 μM |
+
MAO-B, IC50: 42.5 μM |
98% | ||||||||||||||||
| Tranylcypromine HCl |
+++
MAO-A, IC50: 11.5 μM |
+++
MAO-B, IC50: 7 μM |
97% | ||||||||||||||||
| Moclobemide |
+++
MAO-A (5-HT), IC50: 6.1 μM |
99%+ | |||||||||||||||||
| Pargyline HCl |
++
MAO-A, Ki: 13 μM |
+++
MAO-B, Ki: 0.5 μM |
99%+ | ||||||||||||||||
| Safinamide |
++++
MAO-B, IC50: 98 nM |
98% | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 靶点 |
|
| 描述 | Harmine is a beta-carboline alkaloid found in medicinal plant Peganum Harmala, which has served as a folk anticancer medicine. Harmine decreased the survival of HepG2 Cells and the cell survival rates were decreased with increasing the compounds concentrations (from 0 to 10 μM). In vivo,the mice receiving 100 mg/kg harmine exhibited neurotoxic behaviors immediately[3].In addition, harmine administration was associated with neuroprotective effects and also improved memory/learning in several animal models[4]. |
| Concentration | Treated Time | Description | References | |
| R7T1 mouse insulinoma cells | 10 µM | 24 hours | To evaluate the effect of Harmine and its analogs on NFAT2-GFP nuclear translocation, the results showed that some analogs significantly increased NFAT2-GFP nuclear translocation at 10 μM concentration. | J Med Chem. 2020 Mar 26;63(6):2986-3003. |
| B16-F10 melanoma cells | 5 and 10 µM | 24 hours | ACB1801 upregulates the mRNA expression of genes involved in MHC-I antigen presentation, such as TAP1, TAP2, Tapasin, and Lmp2. | Front Immunol. 2022 Nov 15;13:980704. |
| CT26 colorectal cancer cells | 10 µM | 24 hours | ACB1801 upregulates the mRNA expression of TAP1, TAP2, and Tapasin. | Front Immunol. 2022 Nov 15;13:980704. |
| A375 melanoma cells | 5 and 10 µM | 24 hours | ACB1801 upregulates the mRNA and protein expression of TAP1. | Front Immunol. 2022 Nov 15;13:980704. |
| HCT116 colorectal cancer cells | 5 and 10 µM | 24 hours | ACB1801 upregulates the mRNA and protein expression of TAP1. | Front Immunol. 2022 Nov 15;13:980704. |
| U87 and U251 glioblastoma cells | 5 and 10 µM | 24 hours | ACB1801 upregulates the mRNA and protein expression of TAP1. | Front Immunol. 2022 Nov 15;13:980704. |
| Spodoptera frugiperda Sf9 cells | 5, 10, 25, 50, 100 μg/mL | 24, 48 hours | Harmine and ZC-14 inhibited the proliferation of Sf9 cells in a dose-dependent manner, and ZC-14 exhibited higher cytotoxicity than Harmine. | Int J Mol Sci. 2018 Mar 11;19(3):811. |
| SH-SY5Y cells | 0.1 to 1 µM | 48 hours | To evaluate the toxicity of compounds 13 and 17d on SH-SY5Y cells. The results showed that compound 13 exhibited negligible cytotoxicity at concentrations ranging from 0.1 to 1 µM. | J Enzyme Inhib Med Chem. 2023 Dec;38(1):2281893. |
| SH-SY5Y cells | 1, 5, and 10 µM | 48 hours | To evaluate the neuroprotective effects of compounds 13 and 17d against Al 1−42-induced damage in SH-SY5Y cells. The results showed that compound 13 demonstrated exceptional cellular recovery even at the lowest concentration of 1 µM. | J Enzyme Inhib Med Chem. 2023 Dec;38(1):2281893. |
| Spodoptera frugiperda Sf9 cells | 7.5 μg/mL | 6, 12, 18, 24 hours | ZC-14 induced apoptosis in Sf9 cells, while Harmine did not show this effect at the same concentration. | Int J Mol Sci. 2018 Mar 11;19(3):811. |
| Human pancreatic islets | 10 µM | 96 hours | To evaluate the effect of Harmine and its analogs on the proliferation of human pancreatic islet β-cells, the results showed that some analogs significantly increased β-cell proliferation at 10 μM concentration. | J Med Chem. 2020 Mar 26;63(6):2986-3003. |
| Administration | Dosage | Frequency | Description | References | ||
| C57BL6N mice | Diabetes model | Intraperitoneal injection | 1 mg/kg, 3 mg/kg, 6 mg/kg, 10 mg/kg | Daily for 7 days | To evaluate the effect of Harmine and its analogs on the proliferation of mouse pancreatic islet β-cells, the results showed that some analogs significantly increased β-cell proliferation at 1 mg/kg and 3 mg/kg doses. | J Med Chem. 2020 Mar 26;63(6):2986-3003. |
| C57BL/6 mice | B16-F10 melanoma model | Oral | 10 mg/kg | Once daily for 9 days | ACB1801 significantly inhibited the growth and weight of B16-F10 tumors and prolonged the survival of tumor-bearing mice. When combined with anti-PD-1, ACB1801 significantly enhanced the therapeutic efficacy of anti-PD-1. | Front Immunol. 2022 Nov 15;13:980704. |
| Mice | ΑDKRC::RLTG mice | Osmotic minipump | 10 mg/kg/day | Two weeks | Harmine improved left ventricular ejection fraction (LVEF) and increased cardiomyocyte cycling | Circ Res. 2022 Apr 29;130(9):1345-1361 |
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT02914769 | Major Depression | Phase 1 Phase 2 | Completed | - | Brazil ... 展开 >> Draulio B de Araujo Natal, Rio Grande do Norte, Brazil, 59012-300 收起 << |
| NCT02379767 | - | Unknown | February 2018 | Austria ... 展开 >> Department of Psychiatry and Psychotherapy Recruiting Vienna, Austria, 1090 Contact: Rupert Lanzenberger, Assoc. Prof. PD MD +43-1-40400-35760 rupert.lanzenberger@meduniwien.ac.at 收起 << | |
| NCT02715232 | Gender Dysphoria | Phase 4 | Recruiting | December 2020 | Austria ... 展开 >> Department of Psychiatry and Psychotherapy, Medical University of Vienna Recruiting Vienna, Austria, 1090 Contact: Rupert Lanzenberger, A/Prof. +43 40400 ext 3825 rupert.lanzenberger@meduniwien.ac.at Principal Investigator: Rupert Lanzenberger, A/Prof. MD 收起 << |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
4.71mL 0.94mL 0.47mL |
23.56mL 4.71mL 2.36mL |
47.11mL 9.42mL 4.71mL |
|
| CAS号 | 442-51-3 |
| 分子式 | C13H12N2O |
| 分子量 | 212.25 |
| SMILES Code | COC1=CC2=C(C=C1)C1=C(N2)C(C)=NC=C1 |
| MDL No. | MFCD00004958 |
| 别名 | 哈尔碱 ;Telepathine |
| 运输 | 蓝冰 |
| InChI Key | BXNJHAXVSOCGBA-UHFFFAOYSA-N |
| Pubchem ID | 5280953 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry,2-8°C |
| 溶解方案 |
DMSO: 30 mg/mL(141.34 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的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
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