OSS_128167 是一种有效的选择性沉默调节蛋白 6 (SIRT6) 抑制剂，对SIRT6，SIRT1 和 SIRT2 的IC50分别为 89 μM，1578 μM 和 751 μM。OSS_128167 具有抗HBV活性，可抑制HBV的转录和复制。OSS_128167 具有抗癌，抗炎和抗病毒作用。
| 生物活性 | OSS_128167 is a potent selectivesirtuin6 (SIRT6)inhibitor withIC50s of 89 μM, 1578 μM and 751 μM forSIRT6,SIRT1andSIRT2, respectively. OSS_128167 has anti-HBVactivity that inhibitsHBVtranscription and replication. OSS_128167 has anti-acncer, anti-inflammation and anti-viral effects[1][2]. |
| IC50& Target[1][2] | SIRT6 89 μM (IC50) | SIRT2 751 μM (IC50) | SIRT1 1578 μM (IC50) | HBV |
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体外研究
(In Vitro) | OSS_128167 (Compound 9; 100 μM; 0-24 hours; BxPC3 cells) treatment increases H3K9 acetylation. And also increases GLUT-1 expression in BxPC-3 cells[1].
OSS_128167 (Compound 9) effectively blunts phorbol myristate acetate (PMA)-induced TNF-α secretion in cultured BxPC-3 cells. OSS_128167 increases glucose uptake in cells[1].
OSS_128167 (100 μM; 96 hours; HepG2.2.15 and HepG2-NTCP cells) treatment significantly decreaseS HBV core DNA and 3.5-Kb RNA levels. OSS_128167 treatment also inhibits hepatitis B surface antigen (HBsAg) and hepatitis B envelope antigen (HBeAg) secretions, as well as HBsAg expression in cell lysates[2].
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[3].
Western Blot Analysis[1] | Cell Line: | BxPC3 cells | | Concentration: | 100 μM | | Incubation Time: | 0 hours, 2 hours, 6 hours, 18 hours, 24 hours | | Result: | Increased H3K9 acetylation. |
RT-PCR[2] | Cell Line: | HepG2.2.15 and HepG2-sodium taurocholate cotransporting polypeptide (NTCP) cells | | Concentration: | 100 μM | | Incubation Time: | 96 hours | | Result: | Significantly decreased HBV core DNA and 3.5-Kb RNA levels. |
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体内研究
(In Vivo) | OSS_128167 (50 mg/kg; intraperitoneal injection; every 4 days; for 12 days; male HBV transgenic mice) treatment markedly suppresses the level of HBV DNA and 3.5-Kb RNA in HBV transgenic mice[2].
| Animal Model: | Male HBV transgenic mice (6-8-week-old)[2] | | Dosage: | 50 mg/kg | | Administration: | Intraperitoneal injection; every 4 days; for 12 days | | Result: | The level of HBV DNA and 3.5-Kb RNA were markedly suppressed in HBV transgenic mice. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 103.3 mg/mL(281.99 mM;Need ultrasonic and warming) 配制储备液 | 1 mM | 2.7299 mL | 13.6493 mL | 27.2985 mL | | 5 mM | 0.5460 mL | 2.7299 mL | 5.4597 mL | | 10 mM | 0.2730 mL | 1.3649 mL | 2.7299 mL |
*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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (5.68 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.68 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (5.68 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.68 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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