Erythrosin B exhibits multifaceted bioactivities, including inhibition of several enzymes and proteins such as Ubiquitin-specific Protease USP2a, Menin-MLL interaction, Thyroid Hormone Receptor, Steroid Receptor Coregulator 2, RecQ-Like DNA Helicase 1, Tyrosyl-DNA Phosphodiesterase (TDP1), Schistosoma Mansoni Peroxiredoxins, Bacillus subtilis Sfp phosphopantetheinyl transferase (PPTase), Fructose-1,6-bisphosphate Aldolase, L3MBTL1, AmpC Beta-Lactamase, Bloom's syndrome helicase (BLM), GCN5L2, T. brucei phosphofructokinase, Chronic Active B-Cell Receptor Signaling, Eya2, and polymerase Kappa. The compound also modulates lipid storage in Drosophila S3 cells and activates the Relaxin Receptor RXFP1. It shows inhibitory effects on the growth of various human tumor cell lines, including those from renal, non-small cell lung, leukemia, melanoma, colon, prostate, central nervous system, ovarian, and breast cancers.
Additionally, Erythrosin B affects protein-protein interactions, particularly between human Fc-conjugated CD40 and FLAG-tagged biotinylated CD40L costimulatory proteins, with a ratio IC50 of 1.04 in the presence of Triton-X 100. The compound inhibits the Zika virus NS2B-NS3 protease with an IC50 of 1700.0 nM and displays an EC50 of 600.0 nM in a cell-based assay.
Binding affinity studies via isothermal titration calorimetry reveal that Erythrosin B has a strong affinity to human N-terminal His6-tagged and thrombin cleavage fused BLVRB protein, with a dissociation constant (Kd) around 160.0 nM. The associated thermodynamic parameters include a deltaH of -6.38 kcal/mol, TdeltaS of 2.91 kcal/mol, and deltaG of -9.28 kcal/mol.
Moreover, Erythrosin B demonstrates antiviral activities against DENV2, Zika virus, and West Nile virus, with respective EC50 values of 1200.0 nM, 620.0 nM, and 660.0 nM in human A549 cells after 48 hours, as measured by plaque reduction assays..
Note: Summary generated by AI. Data source: ChEMBL 