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Harringtonolide is a potent RACK1 inhibitor ( IC 50 =39.66 μM in A375 cells). Harringtonolide inhibits the epithelial-mesenchymal transition (EMT) process and cell proliferation by affecting the interaction between FAK and RACK1 . Harringtonolide has plant growth inhibitory, antiviral, anti-inflammatory, and antiproliferation activities
In Vitro
Harringtonolide (0-50 μM; 24 hours) exhibits good antiproliferation activity in A375 cells with IC 50 of 39.66 μM. Harringtonolide (0-20 μM; 1 hour) restrains the proteolysis of RACK1 by Pronase, and protects temperature-dependent degradation of RACK1. Harringtonolide (0-4 μM; 24 hours) suppresses the phosphorylation of FAK dose-dependently and inhibits Src and STAT3, the downstream proteins of FAK. Harringtonolide (0-4 μM; 24 hours) dose-dependently inhibits the RACK1–FAK interaction in A375 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation Assay Cell Line: A375 melanoma cellsConcentration: 0-50 μM Incubation Time: 24 hours Result: Showed good antiproliferation activity with IC 50 of 39.66 μM. Western Blot Analysis Cell Line: A375 melanoma cellsConcentration: 0, 0.5, 1, 2, 4 μM Incubation Time: 24 hours Result: Suppressed the phosphorylation of FAK dose-dependently and inhibited Src and STAT3, the downstream proteins of FAK.
Form:Solid
IC50& Target:IC 50 : 39.66 μM (RACK1) in A375 cells
Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Organoheterocyclic compounds |
| 分類 | Furopyrans |
| Subclass | Not available |
| Intermediate Tree Nodes | Not available |
| Direct Parent | Furopyrans |
| Alternative Parents | Tropones Oxepanes Delta valerolactones Pyrans Oxanes Tetrahydrofurans Furans Cyclic ketones Carboxylic acid esters Oxacyclic compounds Monocarboxylic acids and derivatives Dialkyl ethers Organic oxides |
| Molecular Framework | Aromatic heteropolycyclic compounds |
| Substituents | Furopyran - Tropone - Oxepane - Delta_valerolactone - Delta valerolactone - Pyran - Oxane - Tetrahydrofuran - Furan - Cyclic ketone - Lactone - Carboxylic acid ester - Oxacycle - Monocarboxylic acid or derivatives - Ether - Dialkyl ether - Carboxylic acid derivative - Organic oxygen compound - Organic oxide - Hydrocarbon derivative - Organooxygen compound - Carbonyl group - Aromatic heteropolycyclic compound |
| 説明 | This compound belongs to the class of organic compounds known as furopyrans. These are organic polycyclic compounds containing a furan ring fused to a pyran ring. Furan is a five-membered aromatic ring with four carbon atoms and one oxygen atom. Pyran a six-membered heterocyclic, non-aromatic ring, made up of five carbon atoms and one oxygen atom and containing two double bonds. |
| External Descriptors | Not available |