OSS_128167

A SIRT6 inhibitor

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1mg

￥375.00

300.00

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5mg

￥850.00

680.00

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10mg

￥1212.00

970.00

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25mg

￥2200.00

1760.00

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50mg

￥3687.00

2950.00

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100mg

￥5875.00

4700.00

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Background

OSS-128167 is an inhibitor of sirtuin 6 (SIRT6; IC₅₀ = 89 μM).¹ It is selective for SIRT6 over SIRT1 and SIRT2 (IC₅₀s = 1,578 and 751 μM, respectively). OSS-128167 increases acetylation of histone H3 lysine 9 (H3K9) and glucose uptake and decreases TNF-α release in BxPC-3 cells. In vivo, OSS-128167 (100 μg/animal, i.c.v.) prevents decreases in left hemisphere cerebral levels of IL-1β, TNF-α, and IL-6 and neutrophil infiltration induced by bexarotene in a rat model of subarachnoid hemorrhage.²

1.Damonte, P., Sociali, G., Parenti, M.D., et al.SIRT6 inhibitors with salicylate-like structure show immunosuppressive and chemosensitizing effectsBioorg. Med. Chem.25(20)5849-5858(2017) 2.Zuo, Y., Huang, L., Enkhjargal, B., et al.Activation of retinoid X receptor by bexarotene attenuates neuroinflammation via PPARγ/SIRT6/FoxO3a pathway after subarachnoid hemorrhage in ratsJ. Neuroinflammation16(1):47(2019)

Protocol

Kinase experiment:

TNF-a levels in supernatants from cells incubated for 18 h in the presence or absence of OSS_128167 (100 μM, final concentration) are measured by a commercially available ELISA kit according to the manufacturer’s instructions[1].

Cell experiment:

Glucose uptake is evaluated using a fluorescent D-glucose analog, 2-NBDG, in L6 cells incubated for 18 h in the presence or absence of OSS_128167 (100 μM, final concentration)[1].

参考文献:

[1]. Parenti MD, et al. Discovery of novel and selective SIRT6 inhibitors. J Med Chem. 2014 Jun 12;57(11):4796-804.
[2]. Cea M, et al. Evidence for a role of the histone deacetylase SIRT6 in DNA damage response of multiple myeloma cells. Blood. 2016 Mar 3;127(9):1138-50.