Description: |
A2ti-1 is a selective and high-affinity annexin A2/S100A10 heterotetramer (A2t) inhibitor with an IC50 of 24 μM. A2ti-1 specifically disrupts the protein-protein interaction (PPI) between A2 and S100A10. A2ti-1 prevents human papillomavirus type 16 (HPV16) infection. |
Target: |
IC50: 24 μM (A2t)[1] |
In Vitro: |
A2ti-1 (compound 1 b) is an annexin A2-S100A10 protein-protein interaction blocker[1]. A2ti-1 (100 μM; for 72 hours) reduces HPV16 PsV infection of HeLa cells in a dose-dependent manner[2]. A2ti-1 (10, 25, 50, 75, 100 μM; 24 hours) significantly reduces CFDA-SE-labelled HPV16 PsV entry into HeLa cells in a dose-dependent manner[2]. Cell Viability Assay[2] Cell Line: HeLa cells Concentration: 100 μM Incubation Time: For 72 hours Result: Reduced HPV16 PsV infection of HeLa cells in a dose-dependent manner with 100% inhibition of infection observed at 100 μM and similar results were observed in HaCaT cells. |
References: |
[1]. Tummala R K Reddy, et al.Three-dimensional Pharmacophore Design and Biochemical Screening Identifies Substituted 1,2,4-triazoles as Inhibitors of the Annexin A2-S100A10 Protein Interaction. ChemMedChem. 2012 Aug;7(8):1435-46.
[2]. Andrew W Woodham, et al. Small Molecule Inhibitors of the Annexin A2 Heterotetramer Prevent Human Papillomavirus Type 16 Infection. J Antimicrob Chemother. 2015;70(6):1686-90. |