Griseofulvin

Name: Griseofulvin
Brand: MedChemExpress
SKU: HY-17583
Rating: 4.5 (1 reviews)

Cat. No.: HY-17583 Purity: 99.05%: FAQs
Data Sheet SDS COA Handling Instructions Technical Support

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

CAS No. : 126-07-8

Size	Stock	Quantity

Free Sample (0.1 - 0.5 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
500 mg	In-stock	Estimated Time of Arrival: December 31
5 g	In-stock	Estimated Time of Arrival: December 31
10 g	In-stock	Estimated Time of Arrival: December 31
25 g	In-stock	Estimated Time of Arrival: December 31
50 g	Get quote

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Based on 1 publication(s) in Google Scholar

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

Biological Activity
Purity & Documentation
References
Customer Review

Description

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.

126-07-8

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

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

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
10 mM	0.2835 mL	1.4174 mL	2.8347 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
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

mg/kg

Animal weight
(per animal)

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%

Select Batch:

Data Sheet (299 KB) SDS (419 KB)

COA (255 KB) LCMS (93 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]

Complete Stock Solution Preparation Table

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

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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Griseofulvin

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Complete Stock Solution Preparation Table

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