Stattic 是一种有效的STAT3抑制剂，可以抑制 STAT3 磷酸化 (磷酸化位点为 Y705 和 S727)。Stattic 抑制高亲和力磷酸肽与 STAT3 的 SH2 域结合。Stattic 可改善 Alport 综合征 (AS) 小鼠的肾功能不全。
| 生物活性 | Stattic is a potentSTAT3inhibitor and inhibitsSTAT3phosphorylation (at Y705 and S727)[1]. Stattic inhibits the binding of a high affinity phosphopeptide for the SH2 domain ofSTAT3[2]. Stattic ameliorates the renal dysfunction in Alport syndrome (AS) mice[3]. |
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体外研究
(In Vitro) | Stattic (20 μM; 24 hours) inhibits STAT3 phosphorylation (Y705) and selectively inhibits P-STAT3 as demonstrated by the lack of inhibition of P-ERK1/2 in ALDH+and D44+/CD24+subpopulations of Panc-1 and HPAC pancreatic cancer cell lines[1].
Stattic (2.5, 5, 10 μM; for 4 h) significantly reduces the nuclear level of pSTAT3 and survivin in PC3M-1E8 cells at 10 μM. Stattic (2.5-10 μM; for 24 h) inhibits IL-6-induced STAT3 activation in a dose-dependent manner[2].
Stattic (2.5, 5, 10 μM; for 48 h) suppresses both the growth and induces apoptosis prostate cancer cells (PC3M-1E8 cells) with 10 μM. Stattic does not induce significant cell apoptosis with 2.5 μM, 5 μM[2].
Stattic (2.5, 5, 10 μM; for 48 h) shows significant S phase accumulation[2].
Stattic can not lead to significant morphological changes or apoptosis and has little STAT3 phosphorylation in A2780 cells and HUVECs[2].
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体内研究
(In Vivo) | Stattic (10 mg/kg; i.p.; three times per week for 10 week) ameliorates the renal dysfunction in Alport syndrome (AS) mice[3].
| Animal Model: | Age-matched wild-type (WT) C57BL/6 mice[3] | | Dosage: | 10 mg/kg | | Administration: | IP; three timesper week for 10 week | | Result: | Increased levels of proteinuria, BUN and serum creatinine.
Significantly suppressed the gene expression levels of renal injury markers (Lcn2, Kim-1), pro-inflammatory cytokines (Il-6, KC), pro-fibrotic genes (Tgf-β, Col1a1, α-Sma) and Mmp9. |
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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 : 50 mg/mL(236.75 mM;Need ultrasonic) 配制储备液 | 1 mM | 4.7351 mL | 23.6754 mL | 47.3507 mL | | 5 mM | 0.9470 mL | 4.7351 mL | 9.4701 mL | | 10 mM | 0.4735 mL | 2.3675 mL | 4.7351 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: ≥ 2.5 mg/mL (11.84 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (11.84 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (11.84 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (11.84 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 25.0 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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