SAP2-IN-1

SAP2-IN-1 is a secreted aspartic protease 2 (SAP2) inhibitor and has potent SAP2 inhibitory activity with an IC50 value of 0.92 μM. SAP2-IN-1 also is a virulence factor inhibitor and is inactive in vitro. SAP2-IN-1 can be used for the research of infection[1].

Research Areas >> Infection

Signaling Pathways >> Metabolic Enzyme/Protease >> Proteasome

IC50: 0.92 μM (SAP2)[1]

SAP2-IN-1 (compound 24a) (100 μM) shows potent SAP2 inhibitory activity with an IC50 value of 0.92 μM[1]. SAP2-IN-1 (100 μM) has not inhibit the growth of C. albicans and inactive in vitro[1]. SAP2-IN-1 (64 μg/mL) blocks fungi biofilm and hypha formation by down-regulating the expression of genes SAP2, ECE1, ALS3 and EFG1[1]. RT-PCR[1] Cell Line: C. albicans cells Concentration: 64 μg/mL Incubation Time: Result: Inhibited hypha growth through the cAMP-dependent pathway.

SAP2-IN-1 (compound 24a) (i.p.; 10 mg/kg; once daily; for four days) shows potent in vivo efficacy in a murine model of invasive candidiasis[1]. Animal Model: a murine model of invasive candidiasis[1] Dosage: 10 mg/kg Administration: intraperitoneally administration, once daily, for four days Result: Significantly reduced the fungal burden in the kidney.

[1]. Chenglan Li, et al. Targeting fungal virulence factor by small molecules: Structure-based discovery of novel secreted aspartic protease 2 (SAP2) inhibitors. Eur J Med Chem. 2020 Sep 1;201:112515.