Incyclinide

Modify Date: 2024-01-12 14:25:16

Incyclinide Structure
Incyclinide structure
Common Name Incyclinide
CAS Number 15866-90-7 Molecular Weight 371.34100
Density N/A Boiling Point N/A
Molecular Formula C19H17NO7 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Incyclinide


Incyclinide (CMT-3, COL-3) is a matrix metalloproteinase (MMP) inhibitor, thereby inducing extracellular matrix degradation, and inhibiting angiogenesis, tumor growth and invasion, and metastasis.

 Names

Name 4-Desmethylamino-6-desmethyl-6-desoxy-tetracyclin
Synonym More Synonyms

 Incyclinide Biological Activity

Description Incyclinide (CMT-3, COL-3) is a matrix metalloproteinase (MMP) inhibitor, thereby inducing extracellular matrix degradation, and inhibiting angiogenesis, tumor growth and invasion, and metastasis.
Related Catalog
In Vitro Incyclinide has been shown to experimentally suppress prostate cancer, colon adenocarcinoma and melanoma invasiveness in cell culture. Adding incyclinide at final concentrations of 5 to 20 μM inhibits MT1-MMP gelatinolytic and caseinolytic activity, blocks MT1-MMPactivation of pro-MMP-2, and decreases invasiveness of HT-1080 fibrosarcoma cells[1]. Incyclinide is an especially effective inhibitor of the growth and viability of filamentous fungi. Most of the MICs of CMT-3 against filamentous fungi are found to be between 0.25 and 8 μg/mL, and the inhibition of viability of these fungi by incyclinide is routinely higher than 90%[2].
In Vivo Incyclinide inhibits tooth movement in the rat, probably by reducing the number of osteoclasts at the compression side. This might be due to induction of apoptosis in activated osteoclasts or reduced osteoclast migration. Reduced MMP activity by incyclinide might also directly inhibit degradation of the organic bone matrix[3].
Cell Assay Determination of C. albicans growth inhibition by CMT-3 is carried out by a modified turbidity assay. A series of tubes containing PDB (5 mL) and different concentrations of incyclinide (0, 0.125, 0.25, 0.5, 1.0, and 2.0 μg/mL) are each inoculated with a 100 μL suspension of C. albicans in late log phase to yield a final cell concentration of 106/mL. The tubes are aerobically incubated at 35°C, and at each time point (0, 1, 2, 4, 6, 12, and 24 h), the turbidity in each tube is determined spectrophotometrically at 600 nm[2].
Animal Admin Rats: Eighteen Wistar rats receive a standardized orthodontic appliance at one side of the maxilla. During 14 days, three groups of six rats receive a daily dose of 0, 6 or 30 mg/kg incyclinide, and tooth displacement is measured. Thereafter, osteoclasts are counted on histological sections using an ED-1 staining. Multi- and mononuclear ED-1-positive cells in the PDL are also counted. In addition, sections are stained for MMP-9[3].
References

[1]. Lee HM, et al. CMT-3, a non-antimicrobial tetracycline (TC), inhibits MT1-MMPactivity: relevance to cancer. Curr Med Chem. 2001 Feb;8(3):257-60.

[2]. Liu Y, A chemically modified tetracycline (CMT-3) is a new antifungal agent. Antimicrob Agents Chemother. 2002 May;46(5):1447-54.

[3]. Bildt MM, et al. CMT-3 inhibits orthodontic tooth displacement in the rat. Arch Oral Biol. 2007 Jun;52(6):571-8.

 Chemical & Physical Properties

Molecular Formula C19H17NO7
Molecular Weight 371.34100
Exact Mass 371.10100
PSA 158.15000
LogP 1.28080
Storage condition 2-8℃

 Synonyms

Incyclinide
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