Home Cytoskeletal Signaling Microtubule Associated inhibitor Griseofulvin

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Griseofulvin Microtubule Associated inhibitor

Cat.No.S4071

Griseofulvin, a production from some strains of the mold Penicillium griseofulvumam, is able to inhibit cell mitosis by interfering with microtubule function.
Griseofulvin Microtubule Associated inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 352.77

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Quality Control

Batch: S407101 DMSO]50 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.31%
99.31

Solubility

In vitro
Batch:

DMSO : 50 mg/mL (141.73 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 352.77 Formula

C17H17ClO6

 Storage (From the date of receipt)
CAS No. 126-07-8 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1CC(=O)C=C(C12C(=O)C3=C(O2)C(=C(C=C3OC)OC)Cl)OC

Mechanism of Action

Targets/IC50/Ki
Microtubules
In vitro
Griseofulvin is active against dermatophytes of different species in the genera Microsporum, Trichophyton and Epidermophyton. Other fungi such as Scopulariopsis brevicaulis and Hendersomula toruloidea are insensitive. This compound has little or no effect against yeasts and bacteria. The minimum inhibitory concentration of this chemical tested in vitro against various dermatophytes ranges between 0.14 and 0.6 μg/mL. Main effect of this compound on cell mitosis is disorganization of the spindle microtubules. It is also able to induce structural chromosomal aberrations in mammalian cells. This compound inhibits the viability of human colon adenocarcinoma cells COLO 205 and HT 29, hepatoma cells Hep G2 and Hep 3B, leukemia cells HL 60, and normal keratinocytes (#76 KhGH) with IC50s of ~1 and ~5 μM, 5 and 5 μM, 1 μM, and 50 μM, respectively after a 30 hr incubation,. It (20 μM) induces a marked presence of abnormal mitotic spindle formation with mono-, bi-, and tripolar spindles of varying lengths in HT 29 cells, and causes G2/M cell cycle arrest at 24h through elevation of cyclin B1/cdc2 kinase activity and down-regulation of myt-1 protein expression. This chemical is able to induce apoptosis of HT 29 cells via caspase3 activation, Bcl-2 hyperphosphorylation and inhibition of the normal function of Bcl-2 associated with Bax.
In vivo
Griseofulvin displays potent anti-infection activity in vivo. The minimum effective dose of this compound given daily per os is 250 mg/kg (6 days) in mice with a cutaneous infection of Trichophyton quinckeanum and 25 mg/kg (12 days) in guinea pigs with a cutaneous infection of Trichophyton mentagrophytes. This compound (50 mg/kg) is able to suppress COLO 205 tumor xenografts growth. Treatment with this chemical and nocodazole (5 mg/kg) together significantly enhances the efficacy of nocodazole, leading to cessation of tumor growth.
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