Spautin-1

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Spautin-1  纯度: 99.26%

Spautin-1是一种特异性和有效的自噬抑制剂,可抑制泛素特异性肽酶USP10和 USP13,IC50s 约为0.6-0.7 μM。

Spautin-1

Spautin-1 Chemical Structure

CAS No. : 1262888-28-7

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥610 In-stock
5 mg ¥550 In-stock
10 mg ¥700 In-stock
50 mg ¥2500 In-stock
100 mg ¥4500 In-stock
200 mg   询价  
500 mg   询价  

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Spautin-1 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library

生物活性

Spautin-1 is a specific and potent autophagy inhibitor which inhibits ubiquitin-specific peptidases, USP10 and USP13 with IC50s of 0.6-0.7 μM.

体外研究
(In Vitro)

Spautin-1 enhances imatinib mesylate (IM)-induced CmL cell apoptosis by reducing the expression of the anti-apoptotic proteins Mcl-1 and Bcl-2. The pro-apoptotic activity of spautin-1 is associated with activation of GSK3β, an important downstream effector of PI3K/AKT. Spautin-1 enhances IM-induced cytotoxicity in CmL cell line K562, decreasing the IC50 from 1 to 0.5 μM[1]. The mechanism of spautin-1 acting on acute pancreatitis is associated with impaired autophagy inhibition[2].

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.

体内研究
(In Vivo)

Spautin-1 ameliorates the pathogenesis of acute pancreatitis induced by cerulein or L-arginine. Spautin-1 pretreatment significantly diminishes the elevation of serum amylase and lipase levels, which are indicative of trypsin activity. Increasing levels of serum TNFα caused by cerulein are inhibited in the presence of spautin-1. Spautin-1 treatment can ameliorate the inflammation damage induced by cerulein, such as edema, degeneration, coagulative necrosis and infiltration of inflammatory cells[2].

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.

分子量

271.26

Formula

C15H11F2N3

CAS 号

1262888-28-7

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 : 50 mg/mL (184.33 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.6865 mL 18.4325 mL 36.8650 mL
5 mM 0.7373 mL 3.6865 mL 7.3730 mL
10 mM 0.3687 mL 1.8433 mL 3.6865 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: ≥ 2.5 mg/mL (9.22 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.22 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。

    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

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (9.22 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.22 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 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Shao S, et al. Spautin-1, a novel autophagy inhibitor, enhances imatinib-induced apoptosis in chronic myeloid leukemia. Int J Oncol. 2014 May;44(5):1661-1668.

    [2]. Xiao J, et al. Spautin-1 Ameliorates Acute Pancreatitis via Inhibiting Impaired Autophagy and Alleviating Calcium Overload. Mol Med. 2016 Aug 18;22.

Cell Assay
[1]

Spautin-1 is dissolved in DMSO. Cell proliferation is evaluated using CCK-8 kit. K562 cells (1×105/mL) are seeded into 96-well plates in triplicate and then treated with 125 to 4,000 nM IM alone or in combi¬nation with spautin-1 (10 μM). After 48 h of incubation, 10 μL of CCK-8 reagent is added to each well. Four hours later, the absorbance is read at 450 nm using a microplate reader[1].

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.

Animal Administration
[2]

Mice: In this study, mice models with acute pancreatitis, including cerulein- and L-arginine-induced models, are constructed. For the cerulein-induced model, four intraperitoneal injections of cerulein (50 μg/kg body weight) are given consecutively at hourly intervals; The L-arginine-induced model received hourly intraperitoneal injections of 1.4 g/kg (optimal dosage for this study) L-arginine three times[2].

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.

参考文献
  • [1]. Shao S, et al. Spautin-1, a novel autophagy inhibitor, enhances imatinib-induced apoptosis in chronic myeloid leukemia. Int J Oncol. 2014 May;44(5):1661-1668.

    [2]. Xiao J, et al. Spautin-1 Ameliorates Acute Pancreatitis via Inhibiting Impaired Autophagy and Alleviating Calcium Overload. Mol Med. 2016 Aug 18;22.

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