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

Acriflavine hydrochloride  (Synonyms: Acriflavinium chloride hydrochloride)

Cat. No.: HY-W088075 Purity: ≥97.0%
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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.

Acriflavine hydrochloride Chemical Structure

Acriflavine hydrochloride Chemical Structure

CAS No. : 69235-50-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
Solid
500 mg In-stock
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5 g   Get quote  

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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Acriflavine hydrochloride:

Acriflavine hydrochloride Related Antibodies

Top Publications Citing Use of Products

View All HIF/HIF Prolyl-Hydroxylase Isoform Specific Products:

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HIF-1α HIF

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MCT1 MCT2 MCT4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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

In Vitro

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.

Acriflavine hydrochloride 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) hydrochloride 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) 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.

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].
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)[5]
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.
Clinical Trial
Molecular Weight

541.90

Formula

C27H27Cl3N6
CAS No.
Appearance

Solid

Color

Brown to reddish brown

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-]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8454 mL 9.2268 mL 18.4536 mL
5 mM 0.3691 mL 1.8454 mL 3.6907 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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

Purity: ≥97.0%

SDS (620 KB)

COA (254 KB)

Handling Instructions (2659 KB)
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). 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 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
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Acriflavine hydrochloride Related Classifications

Help & FAQs
  • 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:

Acriflavine69235-50-3Acriflavinium chlorideFluorescent DyeHIF/HIF Prolyl-HydroxylaseBacterialSARS-CoVMonocarboxylate TransporterFungalHypoxia-inducible factorsHIFsHIF-PHSARS coronavirusDNARNAlabelingantisepticHIF-1antimicrobialantiviralSARS-CoV-2Inhibitorinhibitorinhibit

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