OSS-128167
SIRT6 inhibitor / OSS-128167 (887686-02-4) is an inhibitor of SIRT6 (IC50=89 µM) showing selectivity over SIRT1 and SIRT2 (IC50s=1,578 and 751 µM, respectively).1 In diffuse large B-cell lymphoma cells which overexpress SIRT6, treatment with OSS-128167 resulted in higher rates of apoptosis, arrested cell cycle progression and augmented sensitivity to chemotherapy.2 It exacerbates diabetic cardiomyopathy by aggravating inflammation and oxidative stress in a streptozotocin-induced diabetic mouse model3 and delays peripheral nerve recovery after injury by suppressing migration, phagocytosis and M2-polarization of macrophages4. OSS-128167 promotes cell senescence and aging in myocardial H9c2 cells.5
Biochemicals & reagents
887686-02-4
1 Damonte et al. (2017), SIRT6 inhibitors with salicylate-like structure show immunosuppressive and chemosensitizing effects; Bioorg. Med. Chem., 25 5849 2 Yang et al. (2020), Sirt6 promotes tumorigenesis and drug resistance of diffuse large B-cell lymphoma by mediating PI3K/Akt signaling; J. Exp. Cancer Res., 39 142 3 Huang et al. (2021), SIRT6-specific inhibitor OSS-128167 exacerbates diabetic cardiomyopathy by aggravating inflammation and oxidative stress; Mol. Med. Rep., 23 367 4 Zou et al. (2021), SIRT6 inhibition delays peripheral nerve recovery by suppressing migration, phagocytosis and M2-polarization of macrophages; Cell Biosci., 11 210 5 Zhou et al. (2022), Downregulation of Sirt6 by CD38 promotes cell senescence and aging; Aging (Albany NY), 14 9730
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TARGET: Protein deacetylase -- PATHWAY: Chromatin; Posttranslational modification; Senescence; Cytokine -- RESEARCH AREA: Epigenetics -- DISEASE AREA: Cancer; Ageing