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OSS_128167

Catalog No.: GC32745

A SIRT6 inhibitor

OSS_128167 Chemical Structure

Size Price Stock Qty
10mM (in 1mL DMSO)
$84.00
In stock
5mg
$70.00
In stock
10mg
$101.00
In stock
25mg
$182.00
In stock
50mg
$308.00
In stock
100mg
$490.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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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].

References:

[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.

Background

OSS_128167 is a selective SIRT6 inhibitor with IC50s of 89, 1578 and 751 μM for SIRT6, SIRT1 and SIRT2, respectively.

OSS_128167 is a selective SIRT6 inhibitor with IC50s of 89, 1578 and 751 μM for SIRT6, SIRT1 and SIRT2, respectively. OSS_128167 inhibits SIRT6 in the micromolar range, but shows promising selectivity, since its IC50 value for SIRT6 is approximately 17 times lower compare to the IC50 for SIRT1 and 9 times lower compare to SIRT2[1]. OSS_128167 (200 μM) induces chemosensitization in primary multiple myeloma (MM) cells (NCI-H929), as well as in melphalan-resistant (LR-5) and doxorubicin-resistant (Dox40) MM cell lines[2].

[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.

Chemical Properties

Cas No. 887686-02-4 SDF
Synonyms N/A
Chemical Name N/A
Canonical SMILES O=C(C1=CC(NC(C2=CC=CO2)=O)=CC=C1)NC3=CC(C(O)=O)=C(O)C=C3
Formula C19H14N2O6 M.Wt 366.32
Solubility DMSO : 103.3 mg/mL (281.99 mM) Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Average Rating: 5 ★★★★★ (Based on Reviews and 8 reference(s) in Google Scholar.)

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