SRT 2183

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SRT 2183  纯度: 98.48%

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。

SRT 2183

SRT 2183 Chemical Structure

CAS No. : 1001908-89-9

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10 mM * 1 mL in DMSO ￥1320 In-stock
5 mg ￥1200 In-stock
10 mg ￥3900 In-stock
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100 mg   询价  

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SRT 2183 相关产品

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生物活性

SRT 2183 is a selective Sirtuin-1 (SIRT1) activator with an EC1.5 value of 0.36 μM[1]. SRT 2183 induces growth arrest and apoptosis, concomitant with deacetylation of STAT3 and NF-κB, and reduction of c-Myc protein levels[2].

IC50 & Target[1]

SIRT1

0.36 μM (EC1.5)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

468.57

Formula

C27H24N4O2S
CAS 号

1001908-89-9
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
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (533.54 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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

*

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, 6 months; -20°C, 1 month。-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。

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。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Milne JC, et al. Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes. Nature. 2007 Nov 29; 450(7170): 712–716.

    [2]. Scuto A, et al. SIRT1 activation enhances HDAC inhibition-mediated upregulation of GADD45G by repressing the binding of NF-κB/STAT3 complex to its promoter in malignant lymphoid cells. Cell Death Dis. 2013 May; 4(5): e635.

    [3]. Gurt I, et al. The Sirt1 Activators SRT2183 and SRT3025 Inhibit RANKL-Induced Osteoclastogenesis in Bone Marrow-Derived Macrophages and Down-Regulate Sirt3 in Sirt1 Null Cells. PLoS One. 2015 Jul 30;10(7):e0134391.

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