Acriflavine hydrochloride
Based on 7 publication(s) in Google Scholar
Acriflavine (Acriflavinium chloride) hydrochloride is a fluorescent acridine dye that can be used to label nucleic acid. Acriflavine hydrochloride is an antiseptic agent. Acriflavine hydrochloride is a potent HIF-1 inhibitor that prevents the dimerization of HIF-1α and HIF-1β subunits. Acriflavine hydrochloride inhibits the interaction between monocarboxylate transporter 4 (MCT4) and Basigin. Acriflavine hydrochloride is used in cancer research, such as breast cancer, brain tumor and chronic myeloid leukemia. Acriflavine hydrochloride 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.: 69235-50-3
- Formula: C27H27Cl3N6
- Molecular Weight:541.90
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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)
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 hydrochloride
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 hydrochloride inhibits MCT4-Basigin dependent Rluc activity in a dose-dependent fashion with an IC50 of 4.6 μM. The IC50 for Acriflavine hydrochloride inhibiting NhRL-MCT1/ Basigin-ChRL interaction is calculated to be ~19.5 μM[3].
Acriflavine (5 μM; treatment for 24 hours) hydrochloride does not significantly affect hypoxia-induced lactate production and secretion in HSR-GBM1 cells[3].
Acriflavine (1-25 μM; treatment for 72 hours) hydrochloride 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) hydrochloride 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) hydrochloride 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) hydrochloride 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) hydrochloride 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)[3].
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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)[5]
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 69235-50-3
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Appearance Solid
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Molecular Weight 541.90
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Formula C27H27Cl3N6
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Color Brown to reddish brown
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SMILES
C[N+]1=C2C=C(N)C=CC2=CC3=C1C=C(N)C=C3.[H]Cl.NC4=CC=C5C(N=C6C=C(N)C=CC6=C5)=C4.[H]Cl.[Cl-]
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Synonyms
Acriflavinium chloride hydrochloride
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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 (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
DMSO : 25 mg/mL (46.13 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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (4.61 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.61 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (286 KB)
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SDS (620 KB)
- English - EN (620 KB)
- Français - FR (620 KB)
- Deutsch - DE (620 KB)
- Norwegian - NO (620 KB)
- Español - ES (620 KB)
- Swedish - SV (620 KB)
- Italian - IT (620 KB)
- Korean - KR (620 KB)
- Portuguese - PT (620 KB)
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Handling Instructions (2659 KB)
References
[1]. L M Chan, 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]. Tao Yin, et al. HIF-1 Dimerization Inhibitor Acriflavine Enhances Antitumor Activity of Sunitinib in Breast Cancer Model. Oncol Res. 2015; 22(3): 139-145. [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]
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 |
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| DMSO | 1 mM | 1.8454 mL | 9.2268 mL | 18.4536 mL | 46.1340 mL |
| 5 mM | 0.3691 mL | 1.8454 mL | 3.6907 mL | 9.2268 mL | |
| 10 mM | 0.1845 mL | 0.9227 mL | 1.8454 mL | 4.6134 mL | |
| 15 mM | 0.1230 mL | 0.6151 mL | 1.2302 mL | 3.0756 mL | |
| 20 mM | 0.0923 mL | 0.4613 mL | 0.9227 mL | 2.3067 mL | |
| 25 mM | 0.0738 mL | 0.3691 mL | 0.7381 mL | 1.8454 mL | |
| 30 mM | 0.0615 mL | 0.3076 mL | 0.6151 mL | 1.5378 mL | |
| 40 mM | 0.0461 mL | 0.2307 mL | 0.4613 mL | 1.1533 mL |
Acriflavine hydrochloride Related Classifications
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