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(CAS: 132911-47-8 )

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Background Information of Fascaplysin

Fascaplysin, a bis-indole alkaloid, is isolated from a marine sponge Fascaplysinopsis Bergquist sp.. Fascaplysin is a specific kinase inhibitor for CDK4. Fascaplysin chloride (0.4 μM) protects rat neuronal pheochromocytoma 12 cells from death induced by nerve growth factor deprivation, an in vitro model of Alzheimer disease (AD).

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Mechanism and Indications

Signaling Pathways Cell Cycle/DNA Damage
Target CDK
Research Area Cancer Neurological Disease

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase

Chemical Information

M.Wt Formula CAS No. Synonyms
271.29 C18H11N2O 132911-47-8

Structure Information of Fascaplysin

Smiles C1C=CC2C3C=C[N+]4C5C=CC=CC=5C(=O)C=4C=3NC=2C=1
InChI InChI=1S/C18H10N2O/c21-18-13-6-2-4-8-15(13)20-10-9-12-11-5-1-3-7-14(11)19-16(12)17(18)20/h1-10H/p+1

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Chemical and Physical Properties

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[1].Ning C, et al. Marine-derived protein kinase inhibitors for neuroinflammatory diseases. Biomed Eng Online. 2018 Apr 24;17(1):46.
Neuroinflammation is primarily characterized by overexpression of proinflammatory mediators produced by glial activation or immune cell infiltration. Several kinases have been shown to be critical mediators in neuroinflammation. One of the largest groups of kinases is protein kinases, which have been the second most studied group of drug targets after G-protein-coupled receptors. Thus far, most of the approved kinase inhibitor drugs are adenosine triphosphate-competitive inhibitors with various off-target liabilities because of cross-reactivities; however, marine-derived compounds provide opportunities for discovering allosteric kinase inhibitors. This review summarizes the potential of marine-derived protein kinase inhibitors in the field of neuroinflammatory diseases, such as Parkinson disease, Alzheimer disease, multiple sclerosis, and pain. The previous studies from 1990 to 2017 in this review have shown that marine-derived protein kinase inhibitors have great potential to elicit anti-neuroinflammatory or neuroprotective responses in in vitro and in vivo models of neuroinflammatory diseases. This suggests that further exploration and investigation of these marine-derived protein kinase inhibitors on neuroinflammatory diseases are warranted. Therefore, this review may inspire further discovery of new protein kinase inhibitors from a marine origin and additional neuroscience studies focusing on these valuable marine-derived protein kinase inhibitors.

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