205807-59-6
Chemical Structure
PKF 242-484
Synonym(s): TNF484
- CAS No.: 205807-59-6
- Formula:C19H29N3O6
- Molecular Weight:395.45
InChIKey: IOLRUMINDIUCLJ-RRFJBIMHSA-N
SMILES: ONC([C@@H](CO)[C@@H](C1=CC=C(C=C1)OC)C(N[C@@H](C(C)(C)C)C(NC)=O)=O)=O
Biological Activity: PKF 242-484 (TNF484) is an orally active dual inhibitor of TACE/MMPs, with Ki values of 3.6, 0.1, 0.9, 1, and 4.5 nM against hMMP-1, hMMP-2, hMMP-3, hMMP-9, and hMMP-13, respectively. PKF 242-484 inhibits the enzymatic activities of MMPs and ADAM17, reduces the release of TNF-α, suppresses the proliferation, migration and invasion of cancer cells, and regulates inflammatory cell infiltration and cytokine production. PKF 242-484 can be used in studies related to airway inflammatory diseases such as asthma and chronic obstructive pulmonary disease, intestinal ischemia-reperfusion injury, epilepsy-induced neuronal damage, and hepatocellular carcinoma[1][2][3][4][5].
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PKF 242-484 | PKF 242-484 (TNF484) is an orally active dual inhibitor of TACE/MMPs, with Ki values of 3.6, 0.1, 0.9, 1, and 4.5 nM against hMMP-1, hMMP-2, hMMP-3, hMMP-9, and hMMP-13, respectively. PKF 242-484 inhibits the enzymatic activities of MMPs and ADAM17, reduces the release of TNF-α, suppresses the proliferation, migration and invasion of cancer cells, and regulates inflammatory cell infiltration and cytokine production. PKF 242-484 can be used in studies related to airway inflammatory diseases such as asthma and chronic obstructive pulmonary disease, intestinal ischemia-reperfusion injury, epilepsy-induced neuronal damage, and hepatocellular carcinoma. | |||||||||||||||||||||
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References
- [1]. Trifilieff A, et al. Pharmacological profile of PKF242-484 and PKF241-466, novel dual inhibitors of TNF-alpha converting enzyme and matrix metalloproteinases, in models of airway inflammation. British journal of pharmacology. 2002 Apr;135(7):1655-64. [Content Brief]
- [2]. Souza DG, et al. Effects of PKF242-484 and PKF241-466, novel dual inhibitors of TNF-alpha converting enzyme and matrix metalloproteinases, in a model of intestinal reperfusion injury in mice. European journal of pharmacology. 2007 Sep 24;571(1):72-80. [Content Brief]
- [3]. Thompson SJ et al. Suppression of TNF receptor-1 signaling in an in vitro model of epileptic tolerance. Int J Physiol Pathophysiol Pharmacol. 2011;3(2):120-132. [Content Brief]
- [4]. Morris A, et al. Comparison of cigarette smoke-induced acute inflammation in multiple strains of mice and the effect of a matrix metalloproteinase inhibitor on these responses. The Journal of pharmacology and experimental therapeutics. 2008 Dec;327(3):851-62. [Content Brief]
- [5]. Xia C, et al. Inhibition of hepatocellular carcinoma cell proliferation, migration, and invasion by a disintegrin and metalloproteinase-17 inhibitor TNF484. Journal of research in medical sciences : the official journal of Isfahan University of Medical Sciences. 2019;24:26. [Content Brief]
