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OSS_128167

Cat. No. M6254
OSS_128167 Structure
Synonym:

SIRT6-IN-1; OSS-128167

Size Price Availability Quantity
5mg USD 120 In stock
10mg USD 190 In stock
25mg USD 230 In stock
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Quality Control
Biological Activity

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.

Protocol
Cell Experiment
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.
Concentrations 100 μM
Incubation time 0, 2, 6, 18, 24 h
Animal Experiment
Animal models
Formulation
Dosages
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 366.32
Formula C19H14N2O6
CAS Number 887686-02-4
Purity 99.96%
Solubility 60 mg/mL in DMSO
Storage at -20°C
References

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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: OSS_128167, SIRT6-IN-1; OSS-128167 supplier, Sirtuin, inhibitors

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