Vacuolin-1
目录号 : GC10325
Vacuolin-1一种有效的PIKfyve抑制剂，可保护溶酶体成熟来抑制细胞自噬。Vacuolin-1还可通过抑制细胞渗透溶酶体胞吐，特异性地调节细胞内的囊泡运输和溶酶体功能。
Cas No.:351986-85-1
Sample solution is provided at 25 µL, 10mM.
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Vacuolin-1 is an effective PIKfyve inhibitor that can protect lysosome maturation to inhibit autophagy[1]. Vacuolin-1 can also specifically regulate intracellular vesicle transport and lysosome function by inhibiting cell permeation and lysosome exocytosis[2]. Vacuolin-1 can be used to prevent viral infections, including Ebola virus and SARS-CoV-2[3]. Vacuolin-1 can protect nerve cells by reducing α-synuclein aggregation[4].
In vitro, after pre-treatment of HL-60 myeloid leukemia cells with Vacuolin-1 (0.25μM), followed by co-treatment with all-trans retinoic acid (1μM) for 24–72h, Vacuolin-1 significantly enhanced the expression of the cell differentiation marker CD11b, the production of reactive oxygen species (ROS), and G1/0 phase cell cycle arrest[5]. After pre-treatment of RBL-2H3 cells and mouse bone marrow-derived mast cells (BMMCs) with Vacuolin-1 (10μM) for 3h, Vacuolin-1 can induce the formation of a large number of vacuoles in both cell types. Vacuolin-1 significantly enhanced exocytosis and membrane repair capacity in RBL-2H3 cells, but inhibited these functions in BMMCs[6].
In vivo, Vacuolin-1 (15 or 30mg/kg) was administered orally once daily for 2 months to 1-month-old MMTV-PyMT transgenic mice. Vacuolin-1 significantly reduced the number of lung metastases, the weight of breast tumors, and the incidence of breast tumors in mice[7]. Vacuolin-1 (100mg/kg) was administered intraperitoneally once daily for 14 days to 1-month-old HA-DAT knock-in mice. Vacuolin-1 significantly blocked the Amphetamine (Amph)-induced loss of the dopamine transporter (DAT) in the striatum[8].
References:
[1] Sano O, Kazetani K, Funata M, et al. Vacuolin-1 inhibits autophagy by impairing lysosomal maturation via PIKfyve inhibition. FEBS Lett. 2016 Jun;590(11):1576-85.
[2] Pronk SD, Schooten E, Heinen J, et al. Single Domain Antibodies as Carriers for Intracellular Drug Delivery: A Proof of Principle Study. Biomolecules. 2021 Jun 22;11(7):927.
[3] Kang YL, Chou YY, Rothlauf PW, et al. Inhibition of PIKfyve kinase prevents infection by Zaire ebolavirus and SARS-CoV-2. Proc Natl Acad Sci U S A. 2020 Aug 25;117(34):20803-20813.
[4] Sanyal A, Scanavachi G, Somerville E, et al. Neuronal constitutive endolysosomal perforations enable α-synuclein aggregation by internalized PFFs. J Cell Biol. 2025 Feb 3;224(2):e202401136.
[5] Zhu K, Kazim N, Yue J, et al. Vacuolin-1 enhances RA-induced differentiation of human myeloblastic leukemia cells: evidence for involvement of a CD11b/FAK/LYN/SLP-76 axis subject to endosomal regulation that drives late differentiation steps. Cell Biosci. 2022 Nov 3;12(1):179.
[6] Shaik GM, Dráberová L, Heneberg P, et al. Vacuolin-1-modulated exocytosis and cell resealing in mast cells. Cell Signal. 2009 Aug;21(8):1337-45.
[7] Ye Z, Wang D, Lu Y, et al. Vacuolin-1 inhibits endosomal trafficking and metastasis via CapZβ. Oncogene. 2021 Mar;40(10):1775-1791.
[8] Bagalkot T, Sorkin A. Amphetamine Induces Sex-Dependent Loss of the Striatal Dopamine Transporter in Sensitized Mice. eNeuro. 2024 Jan 29;11(1):ENEURO.0491-23.2023.
Vacuolin-1一种有效的PIKfyve抑制剂，可保护溶酶体成熟来抑制细胞自噬[1]。Vacuolin-1还可通过抑制细胞渗透溶酶体胞吐，特异性地调节细胞内的囊泡运输和溶酶体功能[2]。Vacuolin-1可用预防病毒感染，包括埃博拉病毒和SARS-CoV-2[3]。Vacuolin-1可通过减少α-突触核蛋白聚集，保护神经细胞[4]。
在体外，Vacuolin-1（0.25μM）预处理HL-60髓样白血病细胞后，与all-trans retinoic acid（1μM）共同作用24–72h，Vacuolin-1显著增强细胞的分化标志物CD11b的表达、活性氧（ROS）的产生以及G1/0期细胞周期阻滞[5]。Vacuolin-1（10μM）预处理RBL-2H3细胞和小鼠骨髓来源的肥大细胞（BMMCs）3h，Vacuolin-1可诱导两种细胞类型形成大量囊泡，Vacuolin-1显著增强RBL-2H3细胞的胞吐作用、细胞膜修复能力，但在BMMCs中却抑制胞吐作用和细胞膜修复能力[6]。
在体内，Vacuolin-1（15或30mg/kg）通过口服给药，每天一次，用于处理1月龄的MMTV-PyMT转基因小鼠，持续2个月。Vacuolin-1显著减少了小鼠乳腺癌的肺部转移灶数量、乳腺肿瘤的重量，并降低了乳腺肿瘤的发生率[7]。Vacuolin-1（100mg/kg）通过腹腔注射，每天一次，用于处理1月龄的HA-DAT基因敲入小鼠，持续14天。Vacuolin-1显著阻断了Amphetamine（Amph）诱导的多巴胺转运体（DAT）在纹状体中的丢失[8]。
| Cell experiment [1]: | |
Cell lines | RBL-2H3 cells (rat basophilic leukemia cell line) and BMMCs (mouse bone marrow-derived mast cells). |
Preparation Method | RBL-2H3 cells were maintained in complete culture medium (CCM) consisting of Eagle's minimum essential medium with Earle's balanced salt solution, supplemented with 10% heat-inactivated fetal calf serum (FCS), 4mM L-glutamine, and antibiotics at 37°C in a humidified atmosphere with 5% CO₂. BMMCs were cultured in complete Iscove's medium (CIM) supplemented with antibiotics, 10% FCS, SCF (40ng/ml), and IL-3 (20ng/ml) at 37°C in 10% CO₂. Cells were treated with Vacuolin-1 (10μM) for 3 hours. |
Reaction Conditions | 10μM; 3h |
Applications | Vacuolin-1 can induce the formation of a large number of vacuoles in two types of cells. Vacuolin-1 significantly enhances exocytosis and membrane repair capacity in RBL-2H3 cells but inhibits these functions in BMMCs. |
| Animal experiment [2]: | |
Animal models | Male HA-DAT knock-in mice |
Preparation Method | Mice were intraperitoneally administered with Vacuolin-1 (2mg/kg) 2 hours before saline or amphetamine challenge on Day 14 of the sensitization protocol. Striatal synaptosomes were prepared 1 hour after saline/amphetamine challenge injections for analysis. |
Dosage form | 2mg/kg; i.p. |
Applications | Vacuolin-1 blocked the amphetamine-induced decrease in the HA-DAT protein in the striatal synaptosomes of sensitized male mice. |
References: | |
| Cas No. | 351986-85-1 | SDF | |
| 化学名 | 3-iodo-2-[4-(diphenylamino)-6-(4-morpholinyl)-1,3,5-triazin-2-yl]hydrazone, benzaldehyde | ||
| Canonical SMILES | IC1=CC(/C=N/NC2=NC(N(C3=CC=CC=C3)C4=CC=CC=C4)=NC(N5CCOCC5)=N2)=CC=C1 | ||
| 分子式 | C26H24IN7O | 分子量 | 577.4 |
| 溶解度 | ≤5mg/ml in DMSO;3mg/ml in dimethyl formamide | 储存条件 | Store at -20°C, stored under nitrogen |
| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7319 mL | 8.6595 mL | 17.319 mL |
| 5 mM | 0.3464 mL | 1.7319 mL | 3.4638 mL |
| 10 mM | 0.1732 mL | 0.866 mL | 1.7319 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
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- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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