2. Others Metabolic Enzyme/Protease Anti-infection Membrane Transporter/Ion Channel
  3. Fluorescent Dye Fungal Monocarboxylate Transporter HIF/HIF Prolyl-Hydroxylase Environmental Pollutants Bacterial SARS-CoV
  4. Acriflavine

Acriflavine  (Synonyms: Acriflavinium chloride 3,6-Acridinediamine mix)

Cat. No.: HY-100575 Purity: 98.0%
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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.

Acriflavine

Acriflavine Chemical Structure

CAS No. : 8048-52-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
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10 mM * 1 mL in Water In-stock
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Based on 7 publication(s) in Google Scholar

Other Forms of Acriflavine:

Acriflavine Related Antibodies

Top Publications Citing Use of Products

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MCT1 MCT2 MCT4

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HIF-1α HIF PHD1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2][3][4][5][6].

In Vitro

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.

Acriflavine Related Antibodies

Cell Viability Assay[6]

Cell Line: Vero, A549ACE2+
Concentration: 400 nM, 500 nM
Incubation Time: 24 h, 48 h
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.
In Vivo

Acriflavine (8 mg/kg; intraperitoneal injection; once a day; 13 administrations) inhibits tumor growth and angiogenesis in NOG mice bearing large HSR-GBM1-Luc cell-derived xenografts[3].
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.

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].
Dosage: 8 mg/kg
Administration: Intraperitoneal injection, once a day, 13 times or 15 times
Result: Inhibited tumor growth.
Also reduced tumor microvessel density, indicating inhibition of tumor vascularization.
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].
Dosage: 8 mg/kg
Administration: Intraperitoneal injection, once a day, 10 days
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.
Animal Model: K18-ACE2 transgenic mice (female, 8-10-week-old) infected with SARS-CoV-2 (intranasal infection with the virus)[6]
Dosage: 100 mg/kg, 5 mg/kg or 15 mg/kg
Administration: Oral administration once a day, intramuscular injection twice a day, 6 days
Result: Blocked the infection in the brain and significantly reduced the viral load in the lungs. The effect was more pronounced with oral administration.
Molecular Weight

468.98

Formula

C27H25ClN6
CAS No.
Appearance

Solid

Color

Light brown to brown

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-]
Shipping

Room temperature in continental US; may vary elsewhere.
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)

Solvent & Solubility
In Vitro: 

H2O : ≥ 25 mg/mL (53.31 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1323 mL 10.6614 mL 21.3229 mL
5 mM 0.4265 mL 2.1323 mL 4.2646 mL
View the 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.

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

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.

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Acriflavine Related Classifications

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  • 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:

Acriflavine8048-52-0Acriflavinium chloride 3,6-Acridinediamine mixFluorescent DyeFungalMonocarboxylate TransporterHIF/HIF Prolyl-HydroxylaseEnvironmental PollutantsBacterialSARS-CoVHypoxia-inducible factorsHIFsHIF-PHEnvironmental ContaminantsSARS coronavirusInhibitorinhibitorinhibit

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