SRT 2183 是一种选择性Sirtuin-1 (SIRT1)激活剂，其EC1.5值为 0.36 μM。SRT 2183 诱导生长停滞和凋亡，同时伴随 STAT3 和 NF-κB 去乙酰化，并降低 c-Myc 蛋白水平。
| 生物活性 | SRT 2183 is a selectiveSirtuin-1 (SIRT1)activator with anEC1.5value of 0.36 μM[1]. SRT 2183 induces growth arrest andapoptosis, concomitant with deacetylation ofSTAT3andNF-κB, and reduction ofc-Mycprotein levels[2]. |
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体外研究
(In Vitro) | SRT 2183 (1-10 μM; 24-72 hours) inhibits the growth of Reh and Nalm-6 cells in a time- and dose-dependent manner[2].
SRT 2183 (5-10 μM in Reh cells; 10 μM in Ly3 cells; 24 hours) induces expression of DNA-damage response genes associated with accumulation of phospho-H2A.X levels[2].
SRT2183 inhibits RANKL-induced osteoclast differentiation, fusion and resorptive capacity without affecting osteoclast survival[3].
Cell Proliferation Assay[2] | Cell Line: | Reh cells, Nalm-6 cells (pre-B acute lymphoblastic leukemia (ALL) cell lines) | | Concentration: | 1 μM, 5 μM, 10 μM | | Incubation Time: | 24 hours, 48 hours, 72 hours | | Result: | Inhibited the growth of Reh and Nalm-6 cells in a time- and dose-dependent manner. The IC50(median inhibition concentration) values for SRT 2183-mediated inhibition of proliferation at 48 h are approximately 8.7 μM for Reh cells and approximately 3.2 μM for Nalm-6 cells. |
Western Blot Analysis[2] | Cell Line: | Reh cells, Ly3 cells | | Concentration: | 5μM and 10μM (Reh cells); 10μM (Ly3 cells) | | Incubation Time: | 24 hours | | Result: | Induced accumulation of phospho-H2A.X in Reh as well as in Ly3 cells. |
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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 : 250 mg/mL(533.54 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.1342 mL | 10.6708 mL | 21.3415 mL | | 5 mM | 0.4268 mL | 2.1342 mL | 4.2683 mL | | 10 mM | 0.2134 mL | 1.0671 mL | 2.1342 mL |
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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 (4.44 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.44 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。 *以上所有助溶剂都可在本网站选购。
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