OSS_128167 |
| Katalog-Nr.GC32745 |
OSS_128167 ist ein potenter selektiver Sirtuin 6 (SIRT6)-Inhibitor mit IC50-Werten von 89 μM, 1578 μM und 751 μM fÜr SIRT6, SIRT1 bzw. SIRT2.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 887686-02-4
Sample solution is provided at 25 µL, 10mM.
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OSS_128167 is a potent selective silencing regulatory protein 6 (SIRT6) inhibitor with an IC50 of 89 μM[1]. OSS_128167 can inhibit HBV transcription and replication, and has antiviral and anti-inflammatory effects[2-3].
OSS_128167(0-200 μM;24h) can promote the increase of H3K9 acetylation, the decrease of TNF-α secretion, the up-regulation of GLUT-1, and the increase of glucose uptake in BxPC-3 cells[1]. OSS_128167(10 μM-50 μM OSS_128167; 24 h) can reverse the protective effect of Oridonin (Ori) on Doxorubicin induced cardiotoxicity (DIC) [4]. OSS_128167 attenuated ROS generation and protective polarization caused by Caffeic acid phenethyl ester (CAPE) pretreatment[5].
OSS_128167(OSS-128167 in a final concentration of 12 mg/mL in a solution containing 2% DMSO, 40% PEG 300, and 2% Tween-80; 100 mg/kg; i.v) treatment caused increased toe swelling in collagen-induced arthritis (CIA) rats, and the proportion of CD38+ NK cells in peripheral blood of CIA rats increased[6]. OSS_128167(80 mg/kg;i.p;1h) significantly accelerated LPS-induced loss of tight junction proteins, lung inflammation, and apoptosis[7].
References:
[1]. Parenti MD, Grozio A, et,al. Discovery of novel and selective SIRT6 inhibitors. J Med Chem. 2014 Jun 12;57(11):4796-804. doi: 10.1021/jm500487d. Epub 2014 May 19. PMID: 24785705.
[2]. Jiang H, Cheng ST, et,al. SIRT6 Inhibitor, OSS_128167 Restricts Hepatitis B Virus Transcription and Replication Through Targeting Transcription Factor Peroxisome Proliferator-Activated Receptors α. Front Pharmacol. 2019 Oct 25;10:1270. doi: 10.3389/fphar.2019.01270. PMID: 31708789; PMCID: PMC6823301.
[3]. Cea M, Cagnetta A, 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. doi: 10.1182/blood-2015-06-649970. Epub 2015 Dec 16. PMID: 26675349; PMCID: PMC4778164.
[4]. Yu D, Li J, et,al. Oridonin ameliorates doxorubicin induced-cardiotoxicity via the E2F1/Sirt6/PGC1α pathway in mice. Food Chem Toxicol. 2023 Nov;181:114050. doi: 10.1016/j.fct.2023.114050. Epub 2023 Sep 20. PMID: 37734463.
[5]. Wang Y, Cai Z, et,al. Caffeic Acid Phenethyl Ester Suppresses Oxidative Stress and Regulates M1/M2 Microglia Polarization via Sirt6/Nrf2 Pathway to Mitigate Cognitive Impairment in Aged Mice following Anesthesia and Surgery. Antioxidants (Basel). 2023 Mar 13;12(3):714. doi: 10.3390/antiox12030714. PMID: 36978961; PMCID: PMC10045012.
[6]. Wang H, Li S, et,al. Potential therapeutic effects of cyanidin-3-O-glucoside on rheumatoid arthritis by relieving inhibition of CD38+ NK cells on Treg cell differentiation. Arthritis Res Ther. 2019 Oct 28;21(1):220. doi: 10.1186/s13075-019-2001-0. PMID: 31661005; PMCID: PMC6819496.
[7]. Liu H, Wang S, et,al. SIRT6 ameliorates LPS-induced apoptosis and tight junction injury in ARDS through the ERK1/2 pathway and autophagy. Int J Med Sci. 2023 Mar 5;20(5):581-594. doi: 10.7150/ijms.80920. PMID: 37082736; PMCID: PMC10110478.
Average Rating: 5 (Based on Reviews and 8 reference(s) in Google Scholar.)
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