OSS_128167 |
| カタログ番号GC32745 |
OSS_128167 は、強力な選択的サーチュイン 6 (SIRT6) 阻害剤であり、SIRT6、SIRT1、および SIRT2 に対してそれぞれ 89 μM、1578 μM、および 751 μM の IC50 を備えています。
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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