1. Anti-infection Apoptosis Metabolic Enzyme/Protease Cell Cycle/DNA Damage Cytoskeleton
  2. Fungal Apoptosis Antibiotic Endogenous Metabolite Microtubule/Tubulin Wee1 Caspase Bcl-2 Family
  3. Griseofulvin

Griseofulvin is an orally active antifungal antibiotic with antitumor activity. Griseofulvin induces apoptosis and G2/M cell cycle arrest in cancer cells. Griseofulvin also has cardiovascular modulatory activity, reducing angina pectoris, relieving hand artery spasm associated with onychomycosis, and peripheral vascular diseases such as shoulder-hand syndrome.

For research use only. We do not sell to patients.

Griseofulvin Chemical Structure

Griseofulvin Chemical Structure

CAS No. : 126-07-8

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10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Griseofulvin:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Griseofulvin is an orally active antifungal antibiotic with antitumor activity. Griseofulvin induces apoptosis and G2/M cell cycle arrest in cancer cells. Griseofulvin also has cardiovascular modulatory activity, reducing angina pectoris, relieving hand artery spasm associated with onychomycosis, and peripheral vascular diseases such as shoulder-hand syndrome[1][2][3][4][5][6].

IC50 & Target

Microbial Metabolite

 

Cellular Effect
Cell Line Type Value Description References
A2780 IC50
> 10 μM
Compound: 8
Cytotoxicity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31359750]
CCRF-CEM IC50
10 μM
Compound: Griseofulvin
Cytotoxicity against human CEM cells after 96 hrs
Cytotoxicity against human CEM cells after 96 hrs
[PMID: 16124785]
HCC1937 IC50
> 10 μM
Compound: Griseofulvin
Antiproliferative activity against exponentially growing adherent human HCC1937 cells assessed as inhibition of cell proliferation after 72 hrs by luminescence detection based ATPlite assay
Antiproliferative activity against exponentially growing adherent human HCC1937 cells assessed as inhibition of cell proliferation after 72 hrs by luminescence detection based ATPlite assay
[PMID: 25872984]
HEK293 IC50
7.3 μM
Compound: Griseofulvin
Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay
Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay
[PMID: 28230985]
HeLa IC50
75 μM
Compound: 1
Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 24 hrs by MTT assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 24 hrs by MTT assay
[PMID: 27061984]
HT-29 IC50
> 20 μM
Compound: 15
Cytotoxicity against human HT-29 cells after 3 days by sulforhodamine B assay
Cytotoxicity against human HT-29 cells after 3 days by sulforhodamine B assay
[PMID: 28409637]
Huh7.5.1 IC50
10 μM
Compound: 1; isolated
Cytotoxicity against human Huh7.5.1 cells assessed as reduction in cell viability by cell titer 96 aqueous one solution cell proliferation assay
Cytotoxicity against human Huh7.5.1 cells assessed as reduction in cell viability by cell titer 96 aqueous one solution cell proliferation assay
[PMID: 28802670]
L5178Y IC50
> 10 μM
Compound: 8
Cytotoxicity against mouse L5178Y cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against mouse L5178Y cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31359750]
MCF7 IC50
13.9 μM
Compound: 15
Cytotoxicity against human MCF7 cells after 3 days by sulforhodamine B assay
Cytotoxicity against human MCF7 cells after 3 days by sulforhodamine B assay
[PMID: 28409637]
MDA-MB-231 IC50
18 μM
Compound: 1
Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 48 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 48 hrs by MTT assay
[PMID: 22191585]
MDA-MB-231 IC50
25 μM
Compound: 1
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by CellTiter-Glo luminescent assay
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by CellTiter-Glo luminescent assay
[PMID: 28258034]
MDA-MB-231 IC50
25.33 μM
Compound: 1
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by celltiter Glo assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by celltiter Glo assay
[PMID: 27061984]
MDA-MB-435 IC50
6.4 μM
Compound: 1; isolated
Cytotoxicity against human MDA-MB-435 cells assessed as reduction in cell viability by cell titer 96 aqueous one solution cell proliferation assay
Cytotoxicity against human MDA-MB-435 cells assessed as reduction in cell viability by cell titer 96 aqueous one solution cell proliferation assay
[PMID: 28802670]
OVCAR-3 IC50
48.5 μM
Compound: 1; isolated
Cytotoxicity against human OVCAR3 cells assessed as reduction in cell viability by cell titer 96 aqueous one solution cell proliferation assay
Cytotoxicity against human OVCAR3 cells assessed as reduction in cell viability by cell titer 96 aqueous one solution cell proliferation assay
[PMID: 28802670]
U2OS IC50
22.4 μM
Compound: 1
Antiproliferative activity against human U2OS cells after 72 hrs by CellTiter-Glo luminescent assay
Antiproliferative activity against human U2OS cells after 72 hrs by CellTiter-Glo luminescent assay
[PMID: 28258034]
U2OS IC50
22.44 μM
Compound: 1
Cytotoxicity against human U2OS cells assessed as reduction in cell viability after 72 hrs by celltiter Glo assay
Cytotoxicity against human U2OS cells assessed as reduction in cell viability after 72 hrs by celltiter Glo assay
[PMID: 27061984]
In Vitro

The minimum inhibitory concentrations (MICs) of Griseofulvin against T. rubrum, T tonsurans, and T mentagrophytes in planktonic and biofilm growth were 0.0078-0.0156 μg/ml, 1-4 μg/mL, and 1-4 μg/mL, respectively[1].
Griseofulvin inhibits the growth of KMS 18, OPM-2, RPMI-8226, U-266, MPC-11, Primary CLL cells, Raji, RAW 264,7, Oci Ly 8 Lam 53, SU DHL 4 cell lines with IC50 values ​​of 9 μM, 45 μM, 26 μM, 18 μM, 44 μM, 80 μM, 33 μM, 28 μM, 30 μM and 22 μM[2].
Griseofulvin (10-100 µM; 72 h) inhibits the viability of human myeloma cells in a concentration-dependent manner[2].
Griseofulvin (0-50 µM; 30 h) dose-dependently induces apoptosis in colon cancer cells (COLO 205 and HT 29), liver cancer cells (Hep G2 and Hep 3B) and leukemia cells HL 60[6].
Griseofulvin (0-20 µM; 24 h) induces abnormal microtubule polymerization in HT 29 cells[6].
Griseofulvin (5-60 µM; 24 h) induces apoptosis at lower doses[6].

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

Apoptosis Analysis[2]

Cell Line: OPM-2 and KMS-18 cells
Concentration: 10, 50 and 100 µM
Incubation Time: 72 h
Result: Induced apoptosis in KMS-18 cells at a dose of 10 mM.

Western Blot Analysis[6]

Cell Line: HT 29 cells
Concentration: 0, 1, 10, 20, 30, 40, 50 and 60 µM
Incubation Time: 24 h
Result: Down-regulated myt-1 protein expression, activated caspase 3 and caused hyperphosphorylation of Bcl-2.
In Vivo

Griseofulvin (0.5-3 mg/kg in crossbred dogs; 2 and 5 mg/kg in rats; i.v.) increases ventricular contractility and coronary blood flow in dogs and rats[5].
Griseofulvin (50 mg/kg; i.p.; 3 injections per week for 6 weeks) reduces tumor volume in COLO 205 xenograft mice[6].

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

Clinical Trial
Molecular Weight

352.77

Formula

C17H17ClO6

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1[C@]2(C(OC)=CC(C[C@H]2C)=O)OC3=C(Cl)C(OC)=CC(OC)=C13

Structure Classification
Initial Source

Penicillium

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (94.48 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 2.8347 mL 14.1735 mL 28.3471 mL
5 mM 0.5669 mL 2.8347 mL 5.6694 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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 (7.09 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    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 (7.09 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    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).
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: 99.05%

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8347 mL 14.1735 mL 28.3471 mL 70.8677 mL
5 mM 0.5669 mL 2.8347 mL 5.6694 mL 14.1735 mL
10 mM 0.2835 mL 1.4174 mL 2.8347 mL 7.0868 mL
15 mM 0.1890 mL 0.9449 mL 1.8898 mL 4.7245 mL
20 mM 0.1417 mL 0.7087 mL 1.4174 mL 3.5434 mL
25 mM 0.1134 mL 0.5669 mL 1.1339 mL 2.8347 mL
30 mM 0.0945 mL 0.4725 mL 0.9449 mL 2.3623 mL
40 mM 0.0709 mL 0.3543 mL 0.7087 mL 1.7717 mL
50 mM 0.0567 mL 0.2835 mL 0.5669 mL 1.4174 mL
60 mM 0.0472 mL 0.2362 mL 0.4725 mL 1.1811 mL
80 mM 0.0354 mL 0.1772 mL 0.3543 mL 0.8858 mL
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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.

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