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Licofelone

Catalog No. T6568 CAS 156897-06-2

Synonyms: ML-3000

Licofelone (ML-3000) is a dual COX/LOX inhibitor potentially for the treatment of osteoarthritis. Licofelone is both an analgesic and an anti-inflammatory. Inhibition of 5-LOX may reduce the gastrointestinal toxicity associated with other non-steroidal anti-inflammatory drugs, which only inhibit COX (cyclooxygenase).

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Licofelone, CAS 156897-06-2

Pack Size	Availability	Price/USD
5 mg	In stock	$ 39.00
10 mg	In stock	$ 64.00
25 mg	In stock	$ 128.00
50 mg	In stock	$ 197.00
100 mg	In stock	$ 293.00
200 mg	In stock	$ 437.00
500 mg	In stock	$ 693.00
1 mL * 10 mM (in DMSO)	In stock	$ 43.00

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Purity: 99.49%

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Chemical Properties

Storage & Solubility Information

Description	Licofelone (ML-3000) is a dual COX/LOX inhibitor potentially for the treatment of osteoarthritis. Licofelone is both an analgesic and an anti-inflammatory. Inhibition of 5-LOX may reduce the gastrointestinal toxicity associated with other non-steroidal anti-inflammatory drugs, which only inhibit COX (cyclooxygenase).
Targets&IC50	5-LOX:0.18 μM, COX:0.21 μM
In vitro	The dual COX/5-LOX inhibitor licofelone triggers apoptosis in a dose- and time-dependent manner in HCA-7 colon cancer cells.?Induction of apoptosis was related to the recruitment of the intrinsic mitochondrial apoptotic pathway, as shown by loss in mitochondrial membrane potential, cytochrome c release, caspase-9 and 3 activation and poly-(ADP-ribose)polymerase-1 cleavage.?Moreover, licofelone induced the cleavage of the full-length p21(Bax) into p18(Bax), a more potent inducer of the apoptotic process than the uncleaved form.?Pre-treatment of HCA-7 cells with the pan-caspase inhibitor z-VAD-fmk significantly blocked licofelone-induced apoptosis, confirming that this process occurred primarily in a caspase-dependent pathway.?Licofelone was able to affect the arachidonic acid (AA) cascade, as it blocked the activity of 5-LOX and COX enzymes, and it induced, through the phosphorylation of cytoplasmic phospholipase A(2) (cPLA(2)), the release of unesterified AA from HCA-7 membrane phospholipids.[1]

Synonyms	ML-3000
Molecular Weight	379.88
Formula	C23H22ClNO2
CAS No.	156897-06-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 25 mg/mL (65.81 mM), Sonification is recommended.

Ethanol: 10 mg/mL (26.32 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble) (< 1 mM)

References and Literature

1. Tavolari S, et al. Licofelone, a dual COX/5-LOX inhibitor, induces apoptosis in HCA-7 colon cancer cells through the mitochondrial pathway independently from its ability to affect the arachidonic acid cascade. Carcinogenesis. 2008 Feb;29(2):371-80. 2. https://www.ncbi.nlm.nih.gov/pubmed/8021931

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Metabolism Compound Library Bioactive Compound Library ReFRAME Related Library NO PAINS Compound Library Anti-Aging Compound Library Anti-Cancer Compound Library Apoptosis Compound Library Lipid Metabolism Compound Library Bioactive Compounds Library Max

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Keywords

Licofelone 156897-06-2 Apoptosis Immunology/Inflammation Metabolism Neuroscience Lipoxygenase COX LOX Inhibitor ML3000 inhibit ML 3000 Cyclooxygenase ML-3000 inhibitor

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