OSS-128167 proves to be a selective compounds toward SIRT6, its IC50 values toward SIRT1 and SIRT2 being approximately 20 times higher. It is cell permeable and active in cultured cells. OSS-128167 increases H3K9 acetylation and GLUT-1 expression.
|Cell lines||BxPC3 cells|
|Preparation method||4 × 10^5 BxPC3 cells are plated in six-well plates and allowed to adhere for 24 h. There after, cells are stimulated with 100 μM OSS-128167 or the respective amounts of vehicle DMSO for the indicated time amounts. Finally, cells are used for protein lysate generation, and total H3 and acetylated H3K9 levels are detected by immunoblotting.|
|Incubation time||0, 2, 6, 18, 24 h|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||60 mg/mL in DMSO|
Evidence for a role of the histone deacetylase SIRT6 in DNA damage response of multiple myeloma cells.
Cea M, et al. Blood. 2016 Mar 3;127(9):1138-50. PMID: 26675349.
Discovery of novel and selective SIRT6 inhibitors.
Parenti MD, et al. J Med Chem. 2014 Jun 12;57(11):4796-804. PMID: 24785705.
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