Harringtonolide

Harringtonolide is a potent RACK1 inhibitor (IC50=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[1].

Research Areas >> Cancer

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FAK

Signaling Pathways >> Others >> Others

Research Areas >> Inflammation/Immunology

IC50: 39.66 μM (RACK1) in A375 cells[1]

Harringtonolide (0-50 μM; 24 hours) exhibits good antiproliferation activity in A375 cells with IC50 of 39.66 μM[1]. Harringtonolide (0-20 μM; 1 hour) restrains the proteolysis of RACK1 by Pronase, and protects temperature-dependent degradation of RACK1[1]. Harringtonolide (0-4 μM; 24 hours) suppresses the phosphorylation of FAK dose-dependently and inhibits Src and STAT3, the downstream proteins of FAK[1]. Harringtonolide (0-4 μM; 24 hours) dose-dependently inhibits the RACK1–FAK interaction in A375 cells[1]. Cell Proliferation Assay Cell Line: A375 melanoma cells[1] Concentration: 0-50 μM Incubation Time: 24 hours Result: Showed good antiproliferation activity with IC50 of 39.66 μM. Western Blot Analysis Cell Line: A375 melanoma cells[1] Concentration: 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.

[1]. Zhu TY, et al. Photoaffinity Probe Reveals the Potential Target of Harringtonolide for Cancer Cell Migration Inhibition. ACS Med Chem Lett. 2022;13(3):449-456. Published 2022 Feb 2.