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Spautin-1

产品编号 T1937 CAS 1262888-28-7

别名: Spautin 1

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

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Spautin-1, CAS 1262888-28-7

规格	价格/CNY	货期
5 mg	￥ 457	现货
10 mg	￥ 581	现货
50 mg	￥ 1,995	现货
100 mg	￥ 3,717	现货
1 mL * 10 mM (in DMSO)	￥ 497	现货

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Spautin-1 is a novel autophagy inhibitor, IM inhibited the growth of K562 cells with IC50 of 1.03 μM. In contrast, co-treatment with Spautin-1 increased IM-induced inhibition of cell viability with IC50 of 0.45 μM.
靶点活性	K562:1.03 μM
体外活性	In Bcap-37 cells, Spautin-1 dramatically enhanced cell death in glucose-free media and induces apoptotic morphology. In Bax-Bak DKO cells, spautin-1 inhibits etoposide induced autophagic cell death. Spautin-1 promots the degradation of Vps34 complexes by regulating the deubiquitination activity of USP10 and USP13, and reduces the levels of PtdIns3P. [1] In PDGF-treated cells, spautin-1 stabilizes α-smooth muscle cell actin and calponin, prevents actin filament disorganization, diminishes production of extracellular matrix, and abrogates VSMC hyperproliferation and migration. [2] In CML cells, spautin-1 markedly inhibits IM-induced autophagy by downregulating Beclin-1, and enhances IM-induced apoptosis by inactivating PI3K/AKT and activating downstream GSK3β. [3] Spautin-1 also specifically reduces infectious dengue virus titers in BHK-21 cells. [4]
体内活性	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. The treatment of Spautin-1 can ameliorate the inflammation damage induced by cerulein, like edema, degeneration, coagulative necrosis and infiltration of inflammatory cells[5].
激酶实验	Kinase inhibitory assays in Vitro: The inhibitory ability against each kinase except for MEK1 and Raf-1 is evaluated by examining their ability to phosphorylate various substrate peptides in the presence of CH5424802 using time-resolved fluorescence resonance energy transfer (TR-FRET) assay or fluorescence polarization (FP) assay. The inhibitory activity against MEK1 is evaluated by quantitative analysis of the phosphorylation of a substrate peptide by a recombinant ERK2 protein in the presence of CH5424802. The inhibitory activity against Raf-1 is evaluated by examining the ability of the kinases to phosphorylate MEK1 in the presence of CH5424802.
细胞实验	Spautin-1 is dissolved in DMSO. Cell proliferation is evaluated using CCK-8 kit. K562 cells (1x105/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].

别名	Spautin 1
分子量	271.26
分子式	C15H11F2N3
CAS No.	1262888-28-7

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 27.1 mg/mL (100 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.6865 mL	18.4325 mL	36.865 mL	92.1625 mL
	5 mM	0.7373 mL	3.6865 mL	7.373 mL	18.4325 mL
	10 mM	0.3687 mL	1.8433 mL	3.6865 mL	9.2163 mL
	20 mM	0.1843 mL	0.9216 mL	1.8433 mL	4.6081 mL
	50 mM	0.0737 mL	0.3687 mL	0.7373 mL	1.8433 mL
	100 mM	0.0369 mL	0.1843 mL	0.3687 mL	0.9216 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Liu J, et al. Cell. 2011, 147(1), 223-234. 2. Salabei JK, et al. Biochem J. 2013, 451(3), 375-388. 3. Shao S, et al. Int J Oncol. 2014, 44(5), 1661-1668. 4. Mateo R, et al. J Virol. 2013, 87(3), 1312-1321. 5. Xiao J, et al. Spautin-1 Ameliorates Acute Pancreatitis via Inhibiting Impaired Autophagy and Alleviating Calcium Overload. Mol Med. 2016 Aug 18;22. 6. Yuan T, Chen Z, Yan F, et al. Deubiquitinating Enzyme USP10 Promotes Hepatocellular Carcinoma Metastasis through Deubiquitinating and Stabilizing Smad4 Protein[J]. Molecular oncology. 2020, 14(1): 197-210

文献引用

1. Wu W, Xu H, Liao C, et al. Blockade of USP14 potentiates type I interferon signaling and radiation-induced antitumor immunity via preventing IRF3 deubiquitination. Cellular Oncology. 2022: 1-15 2. Yuan T, Chen Z, Yan F, et al. Deubiquitinating Enzyme USP10 Promotes Hepatocellular Carcinoma Metastasis through Deubiquitinating and Stabilizing Smad4 Protein. Molecular Oncology. 2020, 14(1): 197-210 3. Yue X, Liu T, Wang X, et al.Pharmacological inhibition of BAP1 recruits HERC2 to competitively dissociate BRCA1–BARD1, suppresses DNA repair and sensitizes CRC to radiotherapy.Acta Pharmaceutica Sinica B.2023

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Spautin-1 1262888-28-7 Apoptosis Autophagy Cell Cycle/Checkpoint DNA Damage/DNA Repair Ubiquitination DUB inhibit Spautin1 Inhibitor Spautin 1 inhibitor

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Spautin-1

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords