14-3-3 Protein Inhibitor

WS3 is an allosteric inhibitor of 14-3-3 (14-3-3ζ: K_d = 2.29 μM). WS3 activates GSK3β by disrupting the binding of 14-3-3-pGSK3β, promotes the ubiquitination and degradation of NRF2, and inhibits the NRF2-ARE signaling pathway (IC₅₀ = 135 nM). It exerts antioxidant inhibition and chemotherapeutic/ferroptosis sensitizing effects in tumors with hyperactivated NRF2. WS3 binds to EBP1/IKKε and promotes the proliferation of β cells and retinal pigment epithelial (RPE) cells, which can be applied to islet regeneration and RPE expansion transplantation. WS3 is applicable to research related to age-related macular degeneration, retinal degeneration and non-small cell lung cancer.

(E)-FOBISIN101 is a 14-3-3 protein-protein interaction (14-3-3 protein-protein interaction) inhibitor, with IC₅₀ values of 9.3 and 16.4 μM for disrupting the binding of 14-3-3ζ or 14-3-3γ to PRAS40, respectively. (E)-FOBISIN101 inhibits the binding of 14-3-3 to Raf-1 and proline-rich AKT substrate, and neutralizes the ability of 14-3-3 to activate exotoxin S ADP-ribosyltransferase. (E)-FOBISIN101 is applicable to 14-3-3-mediated cancer research.

14-3-3η Protein inhibitor 1 (Compound C11) is a 14-3-3η protein inhibitor with a K_D of 35 µM. 14-3-3η Protein inhibitor 1 shows inhibitory activities against several typical human liver cancer cell lines. 14-3-3η Protein inhibitor 1 induces cell apoptosis and G1-S cell cycle arrest with good metabolic stability.

14-3-3-IN-2 is a 14-3-3 protein inhibitor with an IC₅₀ of 15 nM. 14-3-3-IN-2 can disrupt the interaction of 14-3-3α with aminopeptidase N and down-regulate 14-3-3α increased MMP-1 mRNA levels.

UTKO1 (Compound 2) is a derivate of Moverastin.UTKO1 has optical activity and significant inhibitory activity against tumor cell migration by abrogating the binding of 14-3-3ζ/Tiam1. UTKO1 can be used for cancers like esophageal cancer and epidermoid carcinoma research.