OSS_128167
目录号 : GC32745
OSS_128167是一种有效的选择性沉默调节蛋白6 (SIRT6)抑制剂，IC50为89 μM。
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.
OSS_128167是一种有效的选择性沉默调节蛋白6 (SIRT6)抑制剂，IC50为89 μM[1]。OSS_128167能抑制HBV转录和复制，并具有抗病毒和抗炎作用[2-3]。
OSS_128167(0 ~ 200 μM;24h)能促进BxPC-3细胞H3K9乙酰化水平升高、TNF-α分泌减少、GLUT-1表达上调、葡萄糖摄取增加[1]。OSS_128167(10 μm -50 μm;24 h)可逆转Oriidonin (Ori)对阿霉素致心脏毒性(DIC)的保护作用[4]。OSS_128167可减弱咖啡酸苯乙酯(CAPE)预处理引起的ROS生成和保护性极化[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)处理导致胶原诱导性关节炎CIA大鼠足趾肿胀加重，外周血CD38+ NK细胞比例升高[6]。OSS_128167(80 mg/kg;i.p;1h)在小鼠中显著加速LPS诱导的紧密连接蛋白丢失、肺部炎症和细胞凋亡[7]。
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Cell experiment [1]: |
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Cell lines |
BxPC-3 cell |
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Preparation method |
Cells was plated in six-well plates and allowed to adhere for 24 h before being stimulated for 24 h with OSS_128167. |
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Reaction Conditions |
0-200 μM;24h |
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Applications |
OSS_128167 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. |
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Animal experiment [2]: |
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Animal models |
C57BL/6 male mice (6-8 weeks, weight 20-25 g) |
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Preparation method |
The mice were divided into four groups: the control group, OSS_128167 group, the LPS group, and LPS+OSS_128167 group. Mice were given an intraperitoneal injection of 1% sodium pentobarbital to induce anesthesia and then fixed to a 45-degree inclined board. LPS was dissolved in 0.9% normal saline and then instilled intratracheally at a dose of 5 mg/kg. To ensure that LPS was distributed evenly throughout the mouse lungs, the mice were placed in a prone position after 30 seconds of vertical rotation. Mice in the control group received the same volume of 0.9% saline and manipulations. To inhibit SIRT6, mice were intraperitoneally injected with 80 mg/kg OSS_128167 1 h before LPS administration. All mice were sacrificed 24 h after saline or drug administration, and the lungs and bronchoalveolar lavage fluid (BALF) were collected for further study. |
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Dosage form |
80 mg/kg; i.p;1h |
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Applications |
OSS_128167 significantly accelerated LPS-induced loss of tight junction proteins, lung inflammation, and apoptosis. |
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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]. 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. |
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| Cas No. | 887686-02-4 | SDF | |
| Canonical SMILES | O=C(C1=CC(NC(C2=CC=CO2)=O)=CC=C1)NC3=CC(C(O)=O)=C(O)C=C3 | ||
| 分子式 | C19H14N2O6 | 分子量 | 366.32 |
| 溶解度 | DMSO : 103.3 mg/mL (281.99 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7299 mL | 13.6493 mL | 27.2985 mL |
| 5 mM | 0.546 mL | 2.7299 mL | 5.4597 mL |
| 10 mM | 0.273 mL | 1.3649 mL | 2.7299 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet