ns 5

NS2B/NS3-IN-5 (Compound 25b) is a variant of the DENV2 and ZIKV NS2B/NS3 protease inhibitor with IC50 values of 0.67 μM and 4.38 μM for the NS2B/NS3 protease of ZIKV and DENV2, respectively.

NS5A-IN-2 (Compound 33) serves as a potent NS5A inhibitor exhibiting exceptional efficacy against HCV genotype 1b, enhanced activity against genotype 3a (GT 3a), and notable metabolic stability [1].

NS5A-IN-3 (Compound 15) serves as a potent NS5A inhibitor, displaying exceptionally high efficacy against HCV genotype 1b, enhanced activity towards genotype 3a (GT 3a), and substantial metabolic stability. It also demonstrates a superior resistance barrier compared to daclatasvir in genotype 1b [1].

NS5A-IN-1 is a proagent of the HCV NS5A inhibitor Pibrentasvir (ABT-530).

NS5A-IN-4 (Compound 1.12) is a pan-genotypic, orally active inhibitor of the hepatitis C virus (HCV) NS5A, exhibiting IC50 values of 1.2, 2296, 4.6, 362, 10.3, and 693 pM against genotypes gT1b, gT1a, gT2a, gT3a, gT4a, and gT5a, respectively [1].

Burnettramic acid A is a fungal metabolite originally isolated fromA. burnettiithat has diverse biological activities.1It is active againstB. subtilis,S. aureus,C. albicans, andS. cerevisiae(IC50s = 2.3, 5.9, 0.5, and 0.2 μg/ml, respectively). Burnettramic acid A is cytotoxic to NS-1 murine myeloma cells but not neonatal foreskin fibroblasts (IC50s = 13.8 and >100 μg/ml, respectively). 1.Li, H., Gilchrist, C.L.M., Lacey, H.J., et al.Discovery and heterologous biosynthesis of the burnettramic acids: Rare PKS-NRPS-derived bolaamphiphilic pyrrolizidinediones from an Australian fungus, Aspergillus burnettiiOrg. Lett.21(5)1287-1291(2019)

Droxinostat (NS 41080) is a selective inhibitor of HDAC, mostly for HDACs 6 and 8 with IC50 of 2.47 μM and 1.46 μM, greater than 8-fold selective against HDAC3 and no inhibition to HDAC1, 2, 4, 5, 7, 9, and 10.

Burnettramic acid A aglycone is a fungal metabolite and an aglycone form of burnettramic acid A originally isolated fromA. burnettiithat has anticancer activity.1It is cytotoxic to NS-1 murine myeloma cells but not neonatal foreskin fibroblasts (IC50s = 8.4 and >100 μg/ml, respectively). 1.Li, H., Gilchrist, C.L.M., Lacey, H.J., et al.Discovery and heterologous biosynthesis of the burnettramic acids: Rare PKS-NRPS-derived bolaamphiphilic pyrrolizidinediones from an Australian fungus, Aspergillus burnettiiOrg. Lett.21(5)1287-1291(2019)