2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Apoptosis
  3. PPAR Apoptosis
  4. Ankaflavin

Ankaflavin, isolated from Monascus-Fermented red rice, is an orally active PPARγ agonist. Ankaflavin exhibits selective cytotoxic effect and induces cell death through apoptosis on cancer cells. Ankaflavin has anti-inflammatory, anti-cancer, antiatherosclerotic, and hypolipidemic effects.

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Ankaflavin Chemical Structure

Ankaflavin Chemical Structure

CAS No. : 50980-32-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 880 In-stock
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Solid
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5 mg USD 800 In-stock
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Based on 1 publication(s) in Google Scholar

Ankaflavin Related Antibodies

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PPARα PPARβ/δ PPARγ PPAR PPARδ

  • Biological Activity

  • Purity & Documentation

  • References

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Description

Ankaflavin, isolated from Monascus-Fermented red rice, is an orally active PPARγ agonist. Ankaflavin exhibits selective cytotoxic effect and induces cell death through apoptosis on cancer cells. Ankaflavin has anti-inflammatory, anti-cancer, antiatherosclerotic, and hypolipidemic effects[1][2].

IC50 & Target

PPARγ[2].
Cellular Effect
Cell Line Type Value Description References
A-431 IC50
7.05 μM
Compound: 6
Antiproliferative activity against human A431 cells after 72 hrs
Antiproliferative activity against human A431 cells after 72 hrs
[PMID: 20655237]
IGROV-1 IC50
5.08 μM
Compound: 6
Antiproliferative activity against human IGROV1 cells after 72 hrs
Antiproliferative activity against human IGROV1 cells after 72 hrs
[PMID: 20655237]
NCI-H460 IC50
30 μM
Compound: 6
Antiproliferative activity against human NCI-H460 cells after 72 hrs
Antiproliferative activity against human NCI-H460 cells after 72 hrs
[PMID: 20655237]
In Vitro

Ankaflavin (0-50 µg/mL, 48 h) shows cytotoxicity against cancer cells with no significant toxicity toward normal cells[1].
Ankaflavin (0-30 µg/mL, 0-48 h) arrests Hep G2 cell cycle at sub-G1 phase in a dose- and time-dependent manner[1].
Ankaflavin (25 µg/mL, 48 h) induces Hep G2 cell apoptosis[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Ankaflavin Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: A549, Hep G2, MRC-5 and WI-38
Concentration: 1, 10, 25, and 50 µg/mL
Incubation Time: 48 h
Result: Showed cytotoxicity against A549 and Hep G2 cells in a dose-dependent manner with no significant toxicity toward normal cells (MRC-5 and WI-38).

Cell Cycle Analysis[1]

Cell Line: Hep G2 cells
Concentration: 15, 20, 25, and 30 µg/mL
Incubation Time: 12, 24, 36, and 48 h
Result: Induced a distinct sub-G1 peak in Hep G2 cells in a dose- and time-dependent manner.

Apoptosis Analysis[1]

Cell Line: Hep G2 cells
Concentration: 25 µg/mL
Incubation Time: 48 h
Result: Exhibited significant chromatin condensation (fluorescent spot) through Hoechst staining.
In Vivo

Ankaflavin (10 mg/kg; p.o.; daily for 28 days) shows antidiabetic and anti-inflammatory activity, improves liver function and pancreatic function[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Wistar rats (4 weeks of age), diabetes was induced by treating them with Methylglyoxal (MG) (600 mg/kg; oral) for 4 weeks[2]
Dosage: 10 mg/kg
Administration: Oral administration for 28 days
Result: Exerted PPARγ agonist activity. Effectively reduced AGE (advanced glycation end-products) levels in serum, liver, and pancreas of MG-induced rats.
Molecular Weight

386.48

Formula

C23H30O5
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C([C@@H]1C(CCCCCCC)=O)O[C@]2(C)[C@]1([H])CC(C=C(/C=C/C)OC3)=C3C2=O
Structure Classification
Initial Source

Monascus
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (129.37 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 2.5875 mL 12.9373 mL 25.8746 mL
5 mM 0.5175 mL 2.5875 mL 5.1749 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 (protect from light). 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
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 1.25 mg/mL (3.23 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (3.23 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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:

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(per animal)

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Dosing volume
(per animal)

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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 (protect from light)

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: 98.33%

SDS (251 KB)

COA (251 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 (protect from 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
DMSO 1 mM 2.5875 mL 12.9373 mL 25.8746 mL 64.6864 mL
5 mM 0.5175 mL 2.5875 mL 5.1749 mL 12.9373 mL
10 mM 0.2587 mL 1.2937 mL 2.5875 mL 6.4686 mL
15 mM 0.1725 mL 0.8625 mL 1.7250 mL 4.3124 mL
20 mM 0.1294 mL 0.6469 mL 1.2937 mL 3.2343 mL
25 mM 0.1035 mL 0.5175 mL 1.0350 mL 2.5875 mL
30 mM 0.0862 mL 0.4312 mL 0.8625 mL 2.1562 mL
40 mM 0.0647 mL 0.3234 mL 0.6469 mL 1.6172 mL
50 mM 0.0517 mL 0.2587 mL 0.5175 mL 1.2937 mL
60 mM 0.0431 mL 0.2156 mL 0.4312 mL 1.0781 mL
80 mM 0.0323 mL 0.1617 mL 0.3234 mL 0.8086 mL
100 mM 0.0259 mL 0.1294 mL 0.2587 mL 0.6469 mL
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Ankaflavin 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:

Ankaflavin50980-32-0PPARApoptosisPeroxisome proliferator-activated receptorsHep G2A549anticancerantioxidantantidiabeticanti-inflammatoryantiatherosclerotichypolipidemic effectInhibitorinhibitorinhibit

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