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||73 mg/mL in DMSO|
Discovery of novel and selective SIRT6 inhibitors.
Parenti MD, et al. J Med Chem. 2014 Jun 12;57(11):4796-804. PMID: 24785705.
|Related Sirtuin Products|
3-TYP is a selective SIRT3 inhibitor, more potent over SIRT1 and SIRT2, with IC50 values of 88 nM, 92 nM, 16 nM for SITR1, SIRT2, SIRT3, respectively.
Thiomyristoyl is a potent and specific SIRT2 inhibitor with an IC50 of 28 nM. It inhibits SIRT1 with an IC50 value of 98 μM and does not inhibit SIRT3 even at 200 μM.
Nicotinamide is an active component of coenzymes NAD and NADP, and also act as an inhibitor of sirtuins.
Fisetin (Fustel) is a potent sirtuin activating compound (STAC) and an agent that modulates sirtuins.
Sirtinol is a specific SIRT1 and SIRT2 inhibitor with IC50 of 131 μM and 38 μM, respectively.
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