Spautin-1
(Synonyms: Spautin-1抑制剂) 目录号 : GC13526
An autophagy inhibitor
Cas No.:1262888-28-7
Sample solution is provided at 25 µL, 10mM.
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Description:
IC50: 0.6 and 0.7 μM for USP10 and USP13 activity, respectively
Autophagy is an important intracellular catabolic mechanism which mediates the degradation of cytoplasmic proteins and organelles. USP10 mediates the deubiquitination of p53, regulating deubiquitination the activities of USP10 and USP13 by Beclin1 provides a mechanism for Beclin1 to control the levels of p53. Spautin-1 is a novel autophagy inhibitor.
In vitro: Spautin-1 promotes the degradation of Vps34 PI3 kinase complexes via inhibiting two ubiquitinspecific peptidases, USP10 and USP13, that target the Beclin1 subunit of Vps34 complexes. Spautin-1 had no effect on the growth and survival of Bcap-37 cells under normal culture conditions but dramatically enhanced cell death in glucose-free media. Under glucose-free conditions, western blotting for LC3 further confirmed that autophagy was induced, which was inhibited by spautin-1. Similar results were obtained with MCF-7 and BT549 cells. Therefore, spautin-1 can sensitize tumor cells to apoptosis under nutritional deprived conditions [1].
In vivo: So far, there is no report to investigate the in vivo animal efficacy of spautin-1.
Clinical trial: Up to now, spautin-1 is still in the preclinical development stage.
Reference:
[1] Liu J, Xia H, Kim M, Xu L, Li Y, Zhang L, Cai Y, Norberg HV, Zhang T, Furuya T, Jin M, Zhu Z, Wang H, Yu J, Li Y, Hao Y, Choi A, Ke H, Ma D, Yuan J. Beclin1 controls the levels of p53 by regulating the deubiquitination activity of USP10 and USP13. Cell. 2011 Sep 30;147(1):223-34.
| Cell experiment[1]: | |
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Cell lines |
Mouse MEF cells |
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Preparation method |
The solubility of this compound in DMSO is > 13.5 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
4 h, 10 µM |
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Applications |
Spautin-1 is a potent and specific small molecule inhibitor of autophagy. Spautin-1 inhibits two ubiquitin-specific peptidases, USP10 and USP13 ( IC50 values of 0.6 and 0.7 μM respectively), and promotes the ubiquitination and degradation of Vps34 PI3 kinase complexes, leading to an inhibition of autophagy. |
| Animal experiment [2]: | |
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Animal models |
Female KunMing (KM) mice |
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Dosage form |
Intraperitoneal injection, 2 mg/kg |
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Application |
Pretreating mice with spautin-1 significantly reduced the elevation of serum lipase and amylase levels, which are indicators of trypsin activity. Spautin-1 also inhibited the increasing levels of serum TNFα induced by cerulein. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Liu J, Xia H, Kim M, et al. Beclin1 controls the levels of p53 by regulating the deubiquitination activity of USP10 and USP13[J]. Cell, 2011, 147(1): 223-234. [2]. Xiao J, Feng X, Huang X Y, et al. Spautin-1 ameliorates acute Pancreatitis via inhibiting impaired autophagy and alleviating Calcium Overload[J]. Molecular Medicine, 2016, 22: 643. | |
| Cas No. | 1262888-28-7 | SDF | |
| 别名 | Spautin-1抑制剂 | ||
| 化学名 | (Z)-1-(4-fluorophenyl)-N-(6-fluoroquinazolin-4(3H)-ylidene)methanamine | ||
| Canonical SMILES | FC1=CC=C(C/N=C2C3=C(N=CN/2)C=CC(F)=C3)C=C1 | ||
| 分子式 | C15H11F2N3 | 分子量 | 271.26 |
| 溶解度 | ≥ 13.5mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.6865 mL | 18.4325 mL | 36.865 mL |
| 5 mM | 0.7373 mL | 3.6865 mL | 7.373 mL |
| 10 mM | 0.3687 mL | 1.8433 mL | 3.6865 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet