2. Anti-infection Apoptosis Metabolic Enzyme/Protease Cell Cycle/DNA Damage Cytoskeleton
  3. Fungal Apoptosis Antibiotic Endogenous Metabolite Microtubule/Tubulin Wee1 Caspase Bcl-2 Family
  4. 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.

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Griseofulvin Chemical Structure

Griseofulvin Chemical Structure

CAS No. : 126-07-8

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Based on 1 publication(s) in Google Scholar

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Griseofulvin Related Antibodies

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  • 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

 

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.

Griseofulvin Related Antibodies

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
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Concentration
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Volume
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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%

COA (255 KB) LCMS (93 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, 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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Griseofulvin 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:

Griseofulvin126-07-8FungalApoptosisAntibioticEndogenous MetaboliteMicrotubule/TubulinWee1CaspaseBcl-2 FamilyInhibitorinhibitorinhibit

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