Inhibitors, Agonists, Screening Libraries
www.MedChemExpress.com
Data Sheet
Product Name:Cat. No.:CAS No.:
Molecular Formula:Molecular Weight:Target:Pathway:Solubility:
OSS_128167HY-107454887686-02-4C19H14N2O6366.32Sirtuin
Cell Cycle/DNA Damage; EpigeneticsDMSO: 103.3 mg/mL
BIOLOGICAL ACTIVITY:
OSS_128167 is a selective SIRT6 inhibitor with IC50s of , 1578 and 751 μM for SIRT6, SIRT1 and SIRT2, respectively.IC50 & Target: IC50: μM (SIRT6), 1578 μM (SIRT1), 751 μM (SIRT2)[1]
In Vitro: OSS_128167 is a selective SIRT6 inhibitor with IC50s of , 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 17times lower compare to the IC50 for SIRT1 and 9 times lower compare to SIRT2[1]. OSS_128167 (200 μM) induces chemosensitizationin primary multiple myeloma (MM) cells (NCI-H929), as well as in melphalan-resistant (LR-5) and doxorubicin-resistant (Dox40) MMcell lines[2].
PROTOCOL (Extracted from published papers and Only for reference)
Kinase Assay:[1]TNF-a levels in supernatants from cells incubated for 18 h in the presence or absence of OSS_128167 (100 μM, finalconcentration) are measured by a commercially available ELISA kit according to the manufacturer's instructions[1]. Cell Assay: OSS_128167 is solubilized at 50 mM concentration in DMSO.[1]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.
Caution: Product has not been fully validated for medical applications. For research use only.
Tel: 609-228-68 Fax: 609-228-5909 E-mail: tech@MedChemExpress.com
Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA
www.MedChemExpress.com
