Cat. No.: HY-17583

Griseofulvin

Name: Griseofulvin
Brand: MedChemExpress
SKU: HY-17583
Price: 50.00 USD
Availability: InStock
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2 Cited Publications

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Based on 2 publication(s) in Google Scholar

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.

Purity : 99.07%
CAS No.: 126-07-8
Formula: C₁₇H₁₇ClO₆
Molecular Weight:352.77

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Griseofulvin Chemical Structure

CAS No.: 126-07-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Solvent & Solubility
- In Vitro
- In Vivo
Protocols (8)
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

Microbial Metabolite

All Caspase Isoforms :

All Bcl-2 Family Isoforms :

All Antibiotic Isoforms :

All Endogenous Metabolite Isoforms :

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	25 μM Compound: 1	Cytotoxicity against human HeLa cells Cytotoxicity against human HeLa cells	[PMID: 22191585]
HeLa	IC₅₀	25 μM Compound: 18	Antimitotic activity against human HeLa cells Antimitotic activity against human HeLa cells	[PMID: 32652407]
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]
V79	IC₅₀	8 μM Compound: 1	Cytotoxicity against Chinese hamster V79 cells Cytotoxicity against Chinese hamster V79 cells	[PMID: 22191585]

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. Further protocols information, click here.

Apoptosis Analysis^[2]

View Protocol

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]

View Protocol

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.

Chemical Information

CAS No. 126-07-8
Appearance Solid
Molecular Weight 352.77
Formula C₁₇H₁₇ClO₆
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
- Others
Initial Source
- Microorganisms
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

Publications (2)

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Journal Impact Factor

Signal Transduct Target Ther

Large-scale and high-resolution mass spectrometry-based proteomics defines molecular subtypes of nasopharyngeal carcinoma for therapeutic targeting. [Abstract]

2026 Jun 23;11(1):244. PMID: 42331772
J Cell Sci

Selective disruption of microtubule formation at the nuclear envelope impairs the bone resorption capacity of osteoclasts. [Abstract]

2025 Dec 8:jcs.264166. PMID: 41355489

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.8347 mL

14.1735 mL

28.3471 mL

5 mM

0.5669 mL

2.8347 mL

5.6694 mL

10 mM

0.2835 mL

1.4174 mL

2.8347 mL

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (7.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protocols

All Cell Biology Signal Pathway Related Animals and Diseases

Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
Flow cytometric DNA-content cell-cycle staining
Flow cytometric DNA-content cell-cycle staining measures the fluorescence intensity of DNA-bound fluorochromes in single cells or nuclei to estimate DNA content distributions, allowing assignment of populations to G0/G1, S, and G2/M phases by DNA histogram deconvolution. Propidium iodide (PI) intercalates into DNA, and PI fluorescence is proportional to cellular DNA content when staining is performed under conditions that make DNA accessible and minimize non-DNA signal. Cells with G2/M DNA content are expected to show approximately twice the fluorescence intensity of G0/G1 cells, while S-phase cells occupy intermediate fluorescence values. PI-based DNA-content analysis can also detect cells with fractional DNA content, often reported as sub-G1, when DNA fragmentation and extraction during staining reduce retained DNA signal in apoptotic cells. DAPI is an alternative DNA fluorochrome for univariate DNA-content analysis, while bivariate approaches combining DNA content with proliferation
Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
BrdU Incorporation Assay
Bromodeoxyuridine (BrdU) incorporation assay is based on the principle that BrdU, a thymidine analog, is incorporated into newly synthesized DNA during the S phase of the cell cycle, thereby serving as a marker of DNA replication and cellular proliferation. Incorporated BrdU can be detected using anti-BrdU antibodies following DNA denaturation, enabling visualization or quantification of proliferating cells through immunochemical detection methods such as immunofluorescence or immunohistochemistry.
Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
Protocol for Cell Cycle
Cell-cycle analysis by flow cytometry measures DNA content in single cells to estimate the fraction of cells in G0/G1, S, and G2/M phases. Propidium iodide intercalates into DNA, and after RNA removal with RNase, fluorescence intensity reflects cellular DNA content: 2N cells are assigned to G0/G1, cells between 2N and 4N to S phase, and 4N cells to G2/M. DNA-content analysis alone cannot reliably separate G0 from G1 or G2 from M. Ki-67 can distinguish quiescent G0 cells from cycling cells, EdU or BrdU incorporation marks active DNA synthesis in S phase, and phospho-histone H3 staining identifies mitotic cells within the 4N population.
Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Brilhante RSN, et al. In vitro activity of azole derivatives and griseofulvin against planktonic and biofilm growth of clinical isolates of dermatophytes. Mycoses. 2018 Jul;61(7):449-454. [Content Brief]

[2]. Schmeel LC, et al. Griseofulvin Efficiently Induces Apoptosis in In Vitro Treatment of Lymphoma and Multiple Myeloma. Anticancer Res. 2017 May;37(5):2289-2295. [Content Brief]

[3]. Knasmüller S, et al. Toxic effects of griseofulvin: disease models, mechanisms, and risk assessment[J]. Critical reviews in toxicology, 1997, 27(5): 495-537. [Content Brief]

[4]. BEDFORD C, et al. Studies on the biological disposition of griseofulvin, an oral antifungal agent[J]. AMA Archives of Dermatology, 1960, 81(5): 735-745. [Content Brief]

[5]. Aldinger E E. Cardiovascular effects of griseofulvin[J]. Circulation Research, 1968, 22(5): 589-593. [Content Brief]

[6]. Ho Y S, et al. Griseofulvin potentiates antitumorigenesis effects of nocodazole through induction of apoptosis and G2/M cell cycle arrest in human colorectal cancer cells[J]. International journal of cancer, 2001, 91(3): 393-401. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Publications Citing Use of MedChemExpress (MCE) Griseofulvin

All Caspase Isoforms

All Bcl-2 Family Isoforms

All Antibiotic Isoforms

All Endogenous Metabolite Isoforms