Spautin-1 |
カタログ番号GC13526
One-Click Copy Product Info
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Spautin-1はUSP10とUSP13の脱ユビキチン化活性を阻害し、IC50値は0.6-0.7µMである。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1262888-28-7
Sample solution is provided at 25 µL, 10mM.
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Spautin-1はUSP10とUSP13の脱ユビキチン化活性を阻害し、IC50値は0.6-0.7µMである[1]。オートファジー阻害剤として、Spautin-1は様々な癌細胞モデルで、細胞死の誘発に広く使われている[2]。
体外で、72時間の処理は、黒色腫細胞の成長を著しく阻害し、A375とSK-Mel-28に対するIC50値はそれぞれ1.830と2.062μMである[3]。10μM Spautin-1でU87MG細胞を48時間処理した結果、細胞の生存率、RAF-ERK経路、解糖機能を著しく阻害した[4]。10μM Spautin-1でPC12細胞を24時間事前処理した結果、酸素-グルコース欠乏/再酸素化（OGD/R）による活性酸素種（ROS）の蓄積とオートファジーミクロソームの数を減らし、細胞の生存率を増やした[5]。
体内で、A20細胞異種移植のマウスモデルに、20mg/kg/日のSpautin-1を14日間腹腔内注射した結果、腫瘍体積の増加を著しく阻害し、腫瘍細胞の萎縮、断片化と混乱を起こし、PCNAの発見を減らした[6]。急性肺損傷（ALI）のマウスモデルで、Spautin-1 (0.5mg/kg)を72時間単回気管内投与し、リポ多糖類（LPS）誘発の肺組織の構造の損傷、肺胞中隔肥厚と末梢好中球浸潤を効果的に逆転させた[7]。前立腺癌のマウスモデルで、30日間のSpautin-1(20mg/kg/日；腹腔内注射)の処理は、マウスの体重を影響せず、腫瘍の重量と体積を著しく減らした[8]。
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] Schott C R, Ludwig L, Mutsaers A J, et al. The autophagy inhibitor spautin-1, either alone or combined with doxorubicin, decreases cell survival and colony formation in canine appendicular osteosarcoma cells[J]. PloS one, 2018, 13(10): e0206427.
[3] Guo J, Zhang J L, Liang L, et al. Potent USP10/13 antagonist spautin‐1 suppresses melanoma growth via ROS‐mediated DNA damage and exhibits synergy with cisplatin[J]. Journal of Cellular and Molecular Medicine, 2020, 24(7): 4324-4340.
[4] Kona S V, Kalivendi S V. The USP10/13 inhibitor, spautin-1, attenuates the progression of glioblastoma by independently regulating RAF-ERK mediated glycolysis and SKP2[J]. Biochimica et Biophysica Acta (BBA)-Molecular Basis of Disease, 2024, 1870(7): 167291.
[5] Liu H, Zhao Z, Wu T, et al. Inhibition of autophagy‐dependent pyroptosis attenuates cerebral ischaemia/reperfusion injury[J]. Journal of Cellular and Molecular Medicine, 2021, 25(11): 5060-5069.
[6] Wu J, Deng Y, Gao Y, et al. Spautin-1 inhibits the growth of diffuse large B-cell lymphoma by inducing mitochondrial damage-mediated PANoptosis and anti-tumor immunity[J]. Cancer Immunology, Immunotherapy, 2025, 74(9): 293.
[7] Wen H, Miao W, Liu B, et al. SPAUTIN-1 alleviates LPS-induced acute lung injury by inhibiting NF-κB pathway in neutrophils[J]. International Immunopharmacology, 2024, 130: 111741.
[8] Liao Y, Guo Z, Xia X, et al. Inhibition of EGFR signaling with Spautin-1 represents a novel therapeutics for prostate cancer[J]. Journal of Experimental & Clinical Cancer Research, 2019, 38(1): 157.
| 細胞実験[1]: | |
細胞株 | A375細胞 |
準備方法 | A375細胞（2×103/ウェル）を96ウェルのプレートに播種し、10%のウシ胎児血清を含有する培地で一晩中培養した。その後、細胞を様々な濃度のSpautin-1 (対照物、2.5、5、10、20μMに、それぞれ24、48と72時間）で処理した。MTSアッセイを使い、細胞の増殖におけるSpautin-1の効果をテストした。 |
反応条件 | 2.5、5、10、20μM；24、48と72時間 |
アプリケーション | Spautin-1の処理は、A375細胞の増殖を用量と時間依存的に阻害した。 |
| 動物実験 [2]: | |
動物モデル | 雌のBALB/cヌードマウス |
準備方法 | 雌のBALB/cヌードマウス（5週齢）には、A20細胞（100μL PBS, 1 × 107の細胞）を皮下注射した。腫瘍の体積が50mm3に達した時、Spautin-1 (20mg/kg)を毎日腹腔内注射した。全体の実験を14日間持続けた。腫瘍のサイズ（最長軸/短軸）を、精密なノギスで記録し、体積を0.5 × 最長 × 最短2という式で算出した。腫瘍標本を採取し、組織学的な染色とH&E染色で分析した。 |
投与形態 | 0mg/kg/日、14日間；腹腔内注射 |
アプリケーション | Spautin-1の処理はマウスで、腫瘍体積の増加を著しく阻害し、腫瘍細胞の萎縮、断片化と混乱を起こし、PCNAの発見をも減らした。 |
References: | |
| Cas No. | 1262888-28-7 | SDF | |
| Chemical Name | (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 | ||
| Formula | C15H11F2N3 | M.Wt | 271.26 |
| 溶解度 | ≥ 13.5mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.6865 mL | 18.4325 mL | 36.865 mL |
| 5 mM | 737.3 μL | 3.6865 mL | 7.373 mL |
| 10 mM | 368.7 μL | 1.8433 mL | 3.6865 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)