OSS_128167

OSS_128167 is a potent selective sirtuin 6 (SIRT6) inhibitor with IC₅₀s of 89 μM, 1578 μM and 751 μM for SIRT6, SIRT1 and SIRT2, respectively. OSS_128167 has anti-HBV activity that inhibits HBV transcription and replication. OSS_128167 has anti-cancer, anti-inflammation and anti-viral effects^[1][2]. IC50 & Target:IC50: 89 μM (SIRT6), 1578 μM (SIRT1), 751 μM (SIRT2)^[1] In Vitro:OSS_128167 (Compound 9; 100 µM; 0-24 hours; BxPC3 cells) treatment increases H3K9 acetylation. And also increases GLUT-1 expression in BxPC-3 cells^[1].
OSS_128167 (Compound 9) effectively blunts phorbol myristate acetate (PMA)-induced TNF-α secretion in cultured BxPC-3 cells. OSS_128167 increases glucose uptake in cells^[1].
OSS_128167 (100 µM; 96 hours; HepG2.2.15 and HepG2-NTCP cells) treatment significantly decreaseS HBV core DNA and 3.5-Kb RNA levels. OSS_128167 treatment also inhibits hepatitis B surface antigen (HBsAg) and hepatitis B envelope antigen (HBeAg) secretions, as well as HBsAg expression in cell lysates^[2].
OSS_128167 (200 μM) induces chemosensitization in primary multiple myeloma (MM) cells (NCI-H929), as well as in melphalan-resistant (LR-5) and doxorubicin-resistant (Dox40) MM cell lines^[3]. In Vivo:OSS_128167 (50 mg/kg; intraperitoneal injection; every 4 days; for 12 days; male HBV transgenic mice) treatment markedly suppresses the level of HBV DNA and 3.5-Kb RNA in HBV transgenic mice^[2].