DFP00173是一种水通道蛋白3（aquaporin-3，AQP3）抑制剂，抑制小鼠和人 AQP3，IC50值约为0.1-0.4μM，具有抗肿瘤活性。
Cas No.:672286-03-2
Sample solution is provided at 25 µL, 10mM.
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DFP00173 is an aquaporin-3 (AQP3) inhibitor that inhibits mouse and human AQP3 with an IC50 value of approximately 0.1-0.4μM, exhibiting antitumor activity[1, 2]. DFP00173 effectively inhibits intracellular H2O2 uptake[3].
In vitro, treatment of multiple myeloma cell lines (RPMI8226, KMS-11, U266, KMS-27) with DFP00173 (1μM) for 1-6 days significantly reduced the survival rate of all four cell lines, but did not significantly increase the rate of apoptosis, and inhibited cellular mitochondrial respiration[4]. Treatment of HCT8 cells with DFP00173 (5μM) for 45min reduced cell viability and glycerol uptake[5].
In vivo, DFP00173 (20mg/kg) administered via intradiscal injection for 5 weeks in a rat model of intervertebral disc degeneration (IVDD) induced by annular puncture (AFP) restored the intervertebral disc space in IVDD rats[6].
References:
[1] Sonntag Y, Gena P, Maggio A, et al. Identification and characterization of potent and selective aquaporin-3 and aquaporin-7 inhibitors[J]. Journal of Biological Chemistry, 2019, 294(18): 7377-7387.
[2] Pimpão C, da Silva I V, Soveral G. The expanding role of aquaporin-1, aquaporin-3 and aquaporin-5 as transceptors: Involvement in cancer development and potential druggability[J]. International Journal of Molecular Sciences, 2025, 26(3): 1330.
[3] Mu K, Kitts D D. Application of a HyPer-3 sensor to monitor intracellular H2O2 generation induced by phenolic acids in differentiated Caco-2 cells[J]. Analytical Biochemistry, 2022, 659: 114934.
[4] Tanaka M, Yasui M, Hara-Chikuma M. Aquaporin 3 inhibition suppresses the mitochondrial respiration rate and viability of multiple myeloma cells[J]. Biochemical and Biophysical Research Communications, 2023, 676: 158-164.
[5] Angelini I, Centrone M, Caponio G R, et al. MOMAST® Downregulates AQP3 Expression and Function in Human Colon Cells[J]. Antioxidants, 2024, 14(1): 26.
[6] Sang Y, Zhao H, Wu J, et al. Downregulation of aquaporin 3 promotes hyperosmolarity-induced apoptosis of nucleus pulposus cells through PI3K/Akt/mTOR pathway suppression[J]. arXiv preprint arXiv:2507.02231, 2025.
DFP00173是一种水通道蛋白3（aquaporin-3，AQP3）抑制剂，抑制小鼠和人 AQP3，IC50值约为0.1-0.4μM，具有抗肿瘤活性[1, 2]。DFP00173能够有效抑制细胞内H2O2的摄取[3]。
在体外，DFP00173（1µM）处理多发性骨髓瘤细胞系（RPMI8226, KMS-11, U266, KMS-27）1-6天，均显著降低了4种细胞的存活数量，但并未显著提高细胞凋亡率，抑制了细胞线粒体呼吸作用[4]。DFP00173（5µM）处理HCT8细胞45min，降低了细胞活力和甘油摄取率[5]。
在体内，DFP00173（20mg/kg）通过椎间盘内注射治疗椎间盘穿刺（AFP）诱导的椎间盘退变（IVDD）大鼠模型5周，恢复了IVDD大鼠的椎间盘间隙[6]。
| Cell experiment [1]: | |
Cell lines | RPMI8226, KMS-11, U266, KMS-27 cells |
Preparation Method | Cells were incubated with anti-AQP3 mAb (1µg/mL), an equal concentration of control IgG (mouse IgG2a isotype control), DFP00173 (1µM), or vehicle (0.01% DMSO) for 1-6 days. Cell viability was quantified using the CellTiter-Glo Luminescent Cell Viability assay. |
Reaction Conditions | 1µM; 1-6 days |
Applications | Both anti-AQP3 mAb (1µg/mL) and DFP00173 (1µM) significantly reduced the numbers of viable RPMI8226, KMS-11, U266, and KMS-27 cells compared to corresponding controls treated with IgG. |
| Animal experiment [2]: | |
Animal models | Sprague-Dawley rats |
Preparation Method | Rats were randomly allocated into four experimental groups using stratified randomization based on body weight: Control, Annulus fibrosus puncture (AFP), AFP+AQP3 inhibitor DFP00173, AFP+AAV-AQP3. Animals were anesthetized via intraperitoneal injection of sodium pentobarbital (40mg/kg) and positioned prone on a warming pad. Under fluoroscopic guidance (C-arm Ziehm Vision RFD 3D), the caudal intervertebral disc (Co6/7 level) was exposed through a posterolateral approach. A 26-gauge spinal needle was inserted perpendicular to the annulus fibrosus at 5mm depth, followed by 360° rotation with 30-second dwell timeto induce controlled annular injury. DFP00173 (20mg/kg) or AAV-AQP3 solution were intradiscally injected using a microsyringe. Postoperative analgesia was maintained with meloxicam for 72h. Weekly booster injections were administered under isoflurane anesthesia. |
Dosage form | 20mg/kg; 5 weeks; intradiscally injected |
Applications | After 5 weeks of treatment with DFP00173, micro-CT imaging showed that the intervertebral disc space width was restored in rats. |
References: | |
| Cas No. | 672286-03-2 | SDF | |
| Canonical SMILES | O=C(NC1=CSC([N+]([O-])=O)=C1)NC2=C(Cl)C=CC=C2Cl | ||
| 分子式 | C11H7Cl2N3O3S | 分子量 | 332.16 |
| 溶解度 | DMSO: 125 mg/mL (376.32 mM) | 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.0106 mL | 15.053 mL | 30.106 mL |
| 5 mM | 602.1 μL | 3.0106 mL | 6.0212 mL |
| 10 mM | 301.1 μL | 1.5053 mL | 3.0106 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: >99.50% Appearance: A solid
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