Acriflavine
Based on 7 publication(s) in Google Scholar
Acriflavine (Acriflavinium chloride) is a fluorescent acridine dye that can be used to label nucleic acid. Acriflavine is an antiseptic agent. Acriflavine is a potent HIF-1 inhibitor that prevents the dimerization of HIF-1α and HIF-1β subunits. Acriflavine inhibits the interaction between monocarboxylate transporter 4 (MCT4) and Basigin. Acriflavine is used in cancer research, such as breast cancer, brain tumor and chronic myeloid leukemia. Acriflavine is a potent papain-like protease (PLpro) inhibitor, which inhibits SARS-CoV-2.
For research use only. We do not sell to patients.
- Purity: 98.0%
- CAS No.: 8048-52-0
- Formula: C27H25ClN6
- Molecular Weight:468.98
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Acriflavine
More- EBioMedicine. 2019 Nov;49:291-304. [Abstract]
- EBioMedicine. 2018 May:31:202-216. [Abstract]
- Diabetes Metab J. 2026 Jan;50(1):62-76. [Abstract]
- Pharmaceutics. 2024 May 5;16(5):619. [Abstract]
- Int J Mol Sci. 2024 Apr 2;25(7):3944. [Abstract]
- J Clin Endocrinol Metab. 2023 Jan 17;108(2):368-384. [Abstract]
- J Photochem Photobiol B. 2022 Sep:234:112537. [Abstract]
Biological Activity
Acriflavine inhibits MCT4-Basigin dependent Rluc activity in a dose-dependent fashion with an IC50 of 4.6 μM. The IC50 for Acriflavine inhibiting NhRL-MCT1/ Basigin-ChRL interaction is calculated to be ~19.5 μM[3].
Acriflavine (5 μM; treatment for 24 hours) does not significantly affect hypoxia-induced lactate production and secretion in HSR-GBM1 cells[3].
Acriflavine (1-25 μM; treatment for 72 hours) reduces the clonogenic potential of several neurosphere-derived cells and is more obvious under hypoxic conditions[3].
Acriflavine (1-10 μM; treatment for 24 hours) inhibits the replication of SARS-CoV-2 in Vero and A549ACE2+ cells and has low cytotoxicity[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Vero, A549ACE2+
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Concentration:400 nM, 500 nM
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Incubation Time:24 h, 48 h
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Result:Eliminated SARS-CoV-2 compared with untreated cells at 24 h and 48 h post-infection. The IC50 values were 86 nM for A549ACE2+ cells and 64 nM for Vero cells.
Acriflavine (8 mg/kg; intraperitoneal injection; once a day; 15 administrations) inhibits tumor growth in NOG mice bearing small HSR-GBM1-Luc cell-derived xenografts[3].
Acriflavine (8 mg/kg; intraperitoneal injection; once a day; 10 days of administration) reduces the development of chronic myeloid leukemia and the maintenance of leukemia stem cells in C57BL/6J-CD45.1 mice transplanted with BCR/abl-transduced bone marrow cells[5].
Acriflavine (100 mg/kg orally; 5-15 mg/kg intramuscularly; once a day orally, twice a day intramuscularly; 6 days of administration) inhibits the replication of SARS-CoV-2 in the brain and lungs of K18-ACE2 transgenic mice[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOG mice (male and female, 6-8-week-old) with HSR-GBM1-Luc cell - derived xenografts (subcutaneous injection of HSR-GBM1-Luc cells into the left and right flanks)[5].
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Dosage:8 mg/kg
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Administration:Intraperitoneal injection, once a day, 13 times or 15 times
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Result:Inhibited tumor growth.
Also reduced tumor microvessel density, indicating inhibition of tumor vascularization.
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Animal Model:C57BL/6J-CD45.1 mice (8-10-week-old) with BCR/abl-induced chronic myeloid leukemia (retroviral transduction of BCR/abl into bone marrow cells and transplantation into recipient mice)[3].
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Dosage:8 mg/kg
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Administration:Intraperitoneal injection, once a day, 10 days
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Result:Reduced splenomegaly, lung infiltrate with myeloid cells, and white blood cell count in peripheral blood.
Decreased the percentage and number of GFP+/CD34-/LSK cells in bone marrow, indicating a reduction in leukemia stem cells.
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Animal Model:K18-ACE2 transgenic mice (female, 8-10-week-old) infected with SARS-CoV-2 (intranasal infection with the virus)[6]
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Dosage:100 mg/kg, 5 mg/kg or 15 mg/kg
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Administration:Oral administration once a day, intramuscular injection twice a day, 6 days
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Result:Blocked the infection in the brain and significantly reduced the viral load in the lungs. The effect was more pronounced with oral administration.
Chemical Information
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CAS No. 8048-52-0
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Appearance Solid
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Molecular Weight 468.98
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Formula C27H25ClN6
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Color Light brown to brown
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SMILES
NC(C=C1)=CC(C1=C2)=NC3=C2C=CC(N)=C3.NC(C=C4)=CC(C4=C5)=[N+](C)C6=C5C=CC(N)=C6.[Cl-]
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Synonyms
Acriflavinium chloride 3,6-Acridinediamine mix
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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 and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (7)
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Journal Impact Factor
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Most Recent
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EBioMedicine
Macrophage metabolic reprogramming aggravates aortic dissection through the HIF1α-ADAM17 pathway✰. [Abstract]2019 Nov;49:291-304. PMID: 31640947 -
EBioMedicine
Adipocyte-derived Lysophosphatidylcholine Activates Adipocyte and Adipose Tissue Macrophage Nod-Like Receptor Protein 3 Inflammasomes Mediating Homocysteine-Induced Insulin Resistance. [Abstract]2018 May:31:202-216. PMID: 29735414 -
Diabetes Metab J
Serpina3c Mitigates Adipose Tissue Inflammation by Inhibiting the HIF1α-Mediated Endoplasmic Reticulum Overoxidation in Adipocytes. [Abstract]2026 Jan;50(1):62-76. PMID: 40403760 -
Pharmaceutics
Cell-Membrane-Coated Metal-Organic Framework Nanocarrier Combining Chemodynamic Therapy for the Inhibition of Hepatocellular Carcinoma Proliferation. [Abstract]2024 May 5;16(5):619. PMID: 38794281 -
Int J Mol Sci
Epstein-Barr Virus Latent Membrane Protein 2A (LMP2A) Enhances ATP Production in B Cell Tumors through mTOR and HIF-1α. [Abstract]2024 Apr 2;25(7):3944. PMID: 38612754 -
J Clin Endocrinol Metab
Targeting tumor hypoxia inhibits aggressive phenotype of dedifferentiated thyroid cancer. [Abstract]2023 Jan 17;108(2):368-384. PMID: 36190930 -
J Photochem Photobiol B
Inhibition of hypoxia-inducible factor 1 by acriflavine renders glioblastoma sensitive for photodynamic therapy. [Abstract]2022 Sep:234:112537. PMID: 35939916
Solvent & Solubility
H2O : ≥ 25 mg/mL (53.31 mM)
* "≥" means soluble, but saturation unknown.
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 and light). 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 and light). 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 (287 KB)
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SDS (761 KB)
- English - EN (761 KB)
- Français - FR (761 KB)
- Deutsch - DE (761 KB)
- Norwegian - NO (761 KB)
- Español - ES (761 KB)
- Swedish - SV (761 KB)
- Italian - IT (761 KB)
- Korean - KR (761 KB)
- Portuguese - PT (761 KB)
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Handling Instructions (2659 KB)
References
[1]. Chan LM, et al. Interaction of acriflavine with DNA and RNA. J Mol Biol. 1969 Mar 28;40(3):491-5. [Content Brief]
[3]. Voss DM, et al. Disruption of the monocarboxylate transporter-4-basigin interaction inhibits the hypoxic response, proliferation, and tumor progression. Sci Rep. 2017 Jun 27;7(1):4292. [Content Brief]
[4]. Yin T, et al. HIF-1 Dimerization Inhibitor Acriflavine Enhances Antitumor Activity of Sunitinib in Breast Cancer Model. Oncol Res. 2014;22(3):139-45. [Content Brief]
[5]. Cheloni G, et al. Targeting chronic myeloid leukemia stem cells with the hypoxia-inducible factor inhibitor acriflavine. Blood. 2017 Aug 3;130(5):655-665. [Content Brief]
[6]. Napolitano V, et al. Acriflavine, a clinically approved drug, inhibits SARS-CoV-2 and other betacoronaviruses. Cell Chem Biol. 2022 May 19;29(5):774-784.e8. [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 and light). 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 |
|---|---|---|---|---|---|
| H2O | 1 mM | 2.1323 mL | 10.6614 mL | 21.3229 mL | 53.3072 mL |
| 5 mM | 0.4265 mL | 2.1323 mL | 4.2646 mL | 10.6614 mL | |
| 10 mM | 0.2132 mL | 1.0661 mL | 2.1323 mL | 5.3307 mL | |
| 15 mM | 0.1422 mL | 0.7108 mL | 1.4215 mL | 3.5538 mL | |
| 20 mM | 0.1066 mL | 0.5331 mL | 1.0661 mL | 2.6654 mL | |
| 25 mM | 0.0853 mL | 0.4265 mL | 0.8529 mL | 2.1323 mL | |
| 30 mM | 0.0711 mL | 0.3554 mL | 0.7108 mL | 1.7769 mL | |
| 40 mM | 0.0533 mL | 0.2665 mL | 0.5331 mL | 1.3327 mL | |
| 50 mM | 0.0426 mL | 0.2132 mL | 0.4265 mL | 1.0661 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.
Acriflavine Related Classifications
HY-100575 Related Classifications
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