Harmine hydrochloride
Based on 29 publication(s) in Google Scholar
Harmine Hydrochloride (Telepathine Hydrochloride) is a natural DYRK inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM.
For research use only. We do not sell to patients.
- Purity: 99.98%
- CAS No.: 343-27-1
- Formula: C13H13ClN2O
- Molecular Weight:248.71
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
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Publications Citing Use of MedChemExpress (MCE) Harmine hydrochloride
More- Cell Stem Cell. 2022 Apr 7;29(4):545-558.e13. [Abstract]
- J Clin Invest. 2024 Jul 18:e179472. [Abstract]
- Sci Adv. 2023 Dec 22;9(51):eadi5683. [Abstract]
- J Biomed Sci. 2022 Jun 2;29(1):34. [Abstract]
- Cancer Biol Med. 2020 May 15;17(2):387-400. [Abstract]
- Phytomedicine. 2025 Sep 24:148:157306. [Abstract]
- Phytomedicine. 2025 May:140:156484. [Abstract]
- Biochem Pharmacol. 2025 Oct 7;242(Pt 4):117391. [Abstract]
- J Ethnopharmacol. 2025 Jan 30;337(Pt 3):118896. [Abstract]
- Int J Oncol. 2022 Apr;60(4):45. [Abstract]
- Int Immunopharmacol. 2026 Jan 1;168(Pt 2):115902. [Abstract]
- Eur J Pharmacol. 2024 Dec 30:177223. [Abstract]
- Eur J Pharmacol. 2024 Jul 31:980:176828. [Abstract]
- Int Immunopharmacol. 2023 Jun:119:110208. [Abstract]
- Front Cell Dev Biol. 2022 Jan 17;9:792257. [Abstract]
- J Cell Mol Med. 2019 Nov;23(11):7427-7437. [Abstract]
- J Biol Chem. 2025 Feb 2:108254. [Abstract]
- Sci Rep. 2024 Mar 18;14(1):6504. [Abstract]
- Biomedicines. 2024 Jan 16;12(1):197. [Abstract]
- Prog Neuropsychopharmacol Biol Psychiatry. 2017 Jun 15;79(Pt B):258-267. [Abstract]
- Sci Rep. 2015 Aug 3;5:12728. [Abstract]
- BMC Infect Dis. 2024 Jul 31;24(1):760. [Abstract]
- Onco Targets Ther. 2019 Jun 12:12:4585-4593. [Abstract]
- J Integr Neurosci. 2025 Jun 23;24(6):38100. [Abstract]
- Exp Ther Med. 2022 Mar;23(3):209. [Abstract]
- Res Sq. 2025 Jul 08.
- bioRxiv. 2023 Dec 1.
- SSRN. 2023 Mar 8.
- Research Square Preprint. 2021 Aug.
Customer Validation & Images
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WB
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In Vivo Efficacy Study
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IF
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Cell Migration/Invasion Assay
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All 5-HT Receptor Isoforms
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Biological Activity
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5-HT2A Receptor |
5-HT2A Receptor 397 nM (Ki) |
DYRK1A |
Harmine inhibits tau phosphorylation by DYRK1A by selected DANDYs, with an IC50 of 190 nM[2]. Harmine negatively regulates homologous recombination (HR) by interfering Rad51 recruitment, resulting in severe cytotoxicity in hepatoma cells. Furthermore, NHEJ inhibitor Nu7441 markedly sensitizes Hep3B cells to the anti-proliferative effects of Harmine[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 343-27-1
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Appearance Solid
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Molecular Weight 248.71
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Formula C13H13ClN2O
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Color Off-white to light yellow
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SMILES
CC1=NC=CC2=C1NC3=C2C=CC(OC)=C3.Cl
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Synonyms
Telepathine hydrochloride
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (29)
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Journal Impact Factor
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Most Recent
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Cell Stem Cell
A small-molecule cocktail promotes mammalian cardiomyocyte proliferation and heart regeneration. [Abstract]2022 Apr 7;29(4):545-558.e13. PMID: 35395187 -
J Clin Invest
2024 Jul 18:e179472. PMID: 39024569
Harmine hydrochloride purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2024 Jul 18:e179472. [Abstract]
Western blotting images showing the expression of ECM-related genes in primary human intestinal fibroblasts with or without TGF-β (5 ng/mL, 48 hours) and Harmine administration (5 μM or 10 μM, 48 hours).
Harmine hydrochloride purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2024 Jul 18:e179472. [Abstract]
Masson’s trichrome staining showing collagen deposition in mouse colons across the 4 indicated groups. Twist1fl/fl mice and Col1a2-CreERT2Twist1fl/fl cohoused littermates (8 weeks old) were injected intraperitoneally with tamoxifen daily for 4 days (100 mg per kg body weight each time). The mice were subjected to 3 cycles of DSS administration (7 days of DSS administration followed by 14 days of regular drinking water). Harmine (10 mg/kg) was injected intraperitoneally twice a week during each DSS cycle (regularly on Tuesday and Friday weekly).
Harmine hydrochloride purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2024 Jul 18:e179472. [Abstract]
Representative IF staining of mouse colons across the 4 indicated groups (original magnification, ×20). DAPI (blue), COL1A1 (red), and vimentin (green) in merged channels are shown. Twist1fl/fl mice and Col1a2-CreERT2Twist1fl/fl cohoused littermates (8 weeks old) were injected intraperitoneally with tamoxifen daily for 4 days (100 mg per kg body weight each time). The mice were subjected to 3 cycles of DSS administration (7 days of DSS administration followed by 14 days of regular drinking water). Harmine (10 mg/kg) was injected intraperitoneally twice a week during each DSS cycle (regularly on Tuesday and Friday weekly).
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Sci Adv
Haploid-genetic screening of trophectoderm specification identifies Dyrk1a as a repressor of totipotent-like status. [Abstract]2023 Dec 22;9(51):eadi5683. PMID: 38117886 -
J Biomed Sci
DYRK1A reinforces epithelial-mesenchymal transition and metastasis of hepatocellular carcinoma via cooperatively activating STAT3 and SMAD. [Abstract]2022 Jun 2;29(1):34. PMID: 35655269
Harmine hydrochloride purchased from MedChemExpress. Usage Cited in: J Biomed Sci. 2022 Jun 2;29(1):34. [Abstract]
HepG2 cells were incubated with Harmine (0, 2, 4, 8 μM) and were then cultured in the upper compartment of Transwell chambers for 24 h. Then, the cells were stained with crystal violet solution.
Harmine hydrochloride purchased from MedChemExpress. Usage Cited in: J Biomed Sci. 2022 Jun 2;29(1):34. [Abstract]
Following treatment with Harmine (0, 5, 10, 20 μM) for 24 h at the indicated concentrations, total protein was extracted from HEPG2 and Hep3B cells and analysed by western blotting.
Harmine hydrochloride purchased from MedChemExpress. Usage Cited in: J Biomed Sci. 2022 Jun 2;29(1):34. [Abstract]
HCC cells were serum-starved overnight, a scratch was created, and the cells were then incubated with 10 μM harmine and/or 10 ng/mL TGF-β for 6 h. Images were acquired under a microscope.
Harmine hydrochloride purchased from MedChemExpress. Usage Cited in: J Biomed Sci. 2022 Jun 2;29(1):34. [Abstract]
Cells were serum-starved overnight and were then treated with Harmine (10 μM) or 10 ng/mL TGF-β for 6 h. Western blot analysis was then performed.
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Cancer Biol Med
DYRK1A suppression restrains Mcl-1 expression and sensitizes NSCLC cells to Bcl-2 inhibitors. [Abstract]2020 May 15;17(2):387-400. PMID: 32587776 -
Phytomedicine
Genkwanin reduces airway epithelial cell ferroptosis and alleviates asthma symptoms in mice. [Abstract]2025 Sep 24:148:157306. PMID: 41046685 -
Phytomedicine
Fangchinoline suppresses nasopharyngeal carcinoma progression by inhibiting SQLE to regulate the PI3K/AKT pathway dysregulation. [Abstract]2025 May:140:156484. PMID: 40090046 -
Biochem Pharmacol
Harmine inhibits ovarian cancer migration and invasion and epithelial-mesenchymal transition (EMT) by inhibiting HDAC7 to restore RECK expression. [Abstract]2025 Oct 7;242(Pt 4):117391. PMID: 41061932 -
J Ethnopharmacol
Qianyang Yuyin granules alleviate hypertension-induced vascular remodeling by inhibiting the phenotypic switch of vascular smooth muscle cells. [Abstract]2025 Jan 30;337(Pt 3):118896. PMID: 39393558 -
Int J Oncol
DYRK1A suppression attenuates HIF‑1α accumulation and enhances the anti‑liver cancer effects of regorafenib and sorafenib under hypoxic conditions. [Abstract]2022 Apr;60(4):45. PMID: 35244188 -
Int Immunopharmacol
Harmine attenuates renal fibrosis via Twist1 suppression: A novel anti-fibrotic strategy for chronic kidney disease with efficacy/safety profiling. [Abstract]2026 Jan 1;168(Pt 2):115902. PMID: 41273846 -
Eur J Pharmacol
Harmine-induced disruption of the blood-brain barrier via excessive mitophagy in zebrafish. [Abstract]2024 Dec 30:177223. PMID: 39742937 -
Eur J Pharmacol
MFN2-dependent mitochondrial dysfunction contributes to Relm-β-induced pulmonary arterial hypertension via USP18/Twist1/miR-214 pathway. [Abstract]2024 Jul 31:980:176828. PMID: 39094924 -
Int Immunopharmacol
Harmine exerts anxiolytic effects by regulating neuroinflammation and neuronal plasticity in the basolateral amygdala. [Abstract]2023 Jun:119:110208. PMID: 37150016 -
Front Cell Dev Biol
Harmine Alleviated Sepsis-Induced Cardiac Dysfunction by Modulating Macrophage Polarization via the STAT/MAPK/NF-κB Pathway. [Abstract]2022 Jan 17;9:792257. PMID: 35111758 -
J Cell Mol Med
DYRK1A inhibition suppresses STAT3/EGFR/Met signalling and sensitizes EGFR wild-type NSCLC cells to AZD9291. [Abstract]2019 Nov;23(11):7427-7437. PMID: 31454149 -
J Biol Chem
2025 Feb 2:108254. PMID: 39904483 -
Sci Rep
The roles of autophagy, ferroptosis and pyroptosis in the anti-ovarian cancer mechanism of harmine and their crosstalk. [Abstract]2024 Mar 18;14(1):6504. PMID: 38499622 -
Biomedicines
A Novel Druggable Dual-Specificity tYrosine-Regulated Kinase3/Calmodulin Kinase-like Vesicle-Associated Signaling Module with Therapeutic Implications in Neuroblastoma. [Abstract]2024 Jan 16;12(1):197. PMID: 38255303 -
Prog Neuropsychopharmacol Biol Psychiatry
2017 Jun 15;79(Pt B):258-267. PMID: 28625859
Harmine hydrochloride purchased from MedChemExpress. Usage Cited in: Prog Neuropsychopharmacol Biol Psychiatry. 2017 Jun 15;79(Pt B):258-267. [Abstract]
Representative images showing the restoration effect of Harmine on CUS-induced decrease in hippocampal DCX protein expressions. The Fluoxetine administration (20 mg/kg) is used as a positive control, and all data are shown as mean±SEM.
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Sci Rep
Identification of a DYRK1A Inhibitor that Induces Degradation of the Target Kinase using Co-chaperone CDC37 fused with Luciferase nanoKAZ. [Abstract]2015 Aug 3;5:12728. PMID: 26234946 -
BMC Infect Dis
Harmine acts as a quorum sensing inhibitor decreasing the virulence and antibiotic resistance of Pseudomonas aeruginosa. [Abstract]2024 Jul 31;24(1):760. PMID: 39085766 -
Onco Targets Ther
Harmine suppresses the proliferation of pancreatic cancer cells and sensitizes pancreatic cancer to gemcitabine treatment. [Abstract]2019 Jun 12:12:4585-4593. PMID: 31354292 -
J Integr Neurosci
Harmine-mediated Reduction of Bone Cancer Pain in Rats Correlates With Suppressed DYRK1A/NF-κB Signaling Axis. [Abstract]2025 Jun 23;24(6):38100. PMID: 40613372 -
Exp Ther Med
Harmine reinforces the effects of regorafenib on suppressing cell proliferation and inducing apoptosis in liver cancer cells. [Abstract]2022 Mar;23(3):209. PMID: 35126712 -
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Solvent & Solubility
H2O : 10 mg/mL (40.21 mM; ultrasonic and warming and heat to 60°C)
DMSO : 5 mg/mL (20.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (275 KB)
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SDS (584 KB)
- English - EN (584 KB)
- Français - FR (584 KB)
- Deutsch - DE (584 KB)
- Norwegian - NO (584 KB)
- Español - ES (584 KB)
- Swedish - SV (584 KB)
- Italian - IT (584 KB)
- Portuguese - PT (584 KB)
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Handling Instructions (2659 KB)
References
[1]. Glennon RA, et al. Binding of beta-carbolines and related agents at serotonin (5-HT(2) and 5-HT(1A)), dopamine (D(2)) and benzodiazepine receptors. Drug Alcohol Depend. 2000 Aug 1;60(2):121-32. [Content Brief]
[2]. Neumann F, et al. DYRK1A inhibition and cognitive rescue in a Down syndrome mouse model are induced by new fluoro-DANDY derivatives. Sci Rep. 2018 Feb 12;8(1):2859. [Content Brief]
[3]. Zhang L, et al. Harmine suppresses homologous recombination repair and inhibits proliferation of hepatoma cells. Cancer Biol Ther. 2015;16(11):1585-92. [Content Brief]
[4]. Zhong Z, et al. Treatment with harmine ameliorates functional impairment and neuronal death following traumatic brain injury. Mol Med Rep. 2015 Dec;12(6):7985-91. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 4.0207 mL | 20.1037 mL | 40.2075 mL | 100.5187 mL |
| 5 mM | 0.8041 mL | 4.0207 mL | 8.0415 mL | 20.1037 mL | |
| 10 mM | 0.4021 mL | 2.0104 mL | 4.0207 mL | 10.0519 mL | |
| 15 mM | 0.2680 mL | 1.3402 mL | 2.6805 mL | 6.7012 mL | |
| 20 mM | 0.2010 mL | 1.0052 mL | 2.0104 mL | 5.0259 mL | |
| H2O | 25 mM | 0.1608 mL | 0.8041 mL | 1.6083 mL | 4.0207 mL |
| 30 mM | 0.1340 mL | 0.6701 mL | 1.3402 mL | 3.3506 mL | |
| 40 mM | 0.1005 mL | 0.5026 mL | 1.0052 mL | 2.5130 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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