STF 31是一种具有细胞通透性的葡萄糖转运蛋白1（GLUT1）的抑制剂，IC₅₀为1μM。
Cas No.:724741-75-7
Sample solution is provided at 25 µL, 10mM.
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STF 31 is a cell-permeable inhibitor of glucose transporter 1 (GLUT1) with an IC₅₀ of 1μM[1]. GLUT1 is a key transporter responsible for glucose uptake and plays an essential role in maintaining glycolytic metabolism[2]. STF 31 can inhibit nicotinamide phosphoribosyltransferase (NAMPT), thereby disrupting glycolysis and inducing cytotoxicity[3].
In vitro, STF 31 (0-10μM) treatment inhibited the glucose uptake capacity of B6M7 cells in a dose-dependent manner within 24h without significantly affecting cell viability[4]. STF 31 (30μM) treatment of MCF-7 cells for 48h significantly suppressed glycolysis and induced apoptosis[5]. STF 31 (2, 4, and 8μM) treatment of rheumatoid arthritis fibroblast-like synoviocytes (RAFLs) for 24-72h inhibited cell proliferation in a time- and dose-dependent manner[6].
In vivo, STF 31 (10mg/kg), administered via intraperitoneal injection (twice daily for the first 2 days, followed by once daily for the next 3 days), had no significant effects on body weight, behavior, or ERG responses in normal mice. In a light-induced model, STF 31 significantly inhibited microglial activation in CX3CR1gfp/+ mice and alleviated retinal degeneration[4]. Intraperitoneal co-administration of STF 31 (10mg/kg) and dexamethasone in normal mice for 4h significantly promoted the accumulation of necrotic thymocytes[7].
References:
[1] Chan D A, Sutphin P D, Nguyen P, et al. Targeting GLUT1 and the Warburg Effect in Renal Cell Carcinoma by Chemical Synthetic Lethality[J]. Sci Transl Med, 2011, 3(94).
[2] Wu Q, ba-alawi W, Deblois G, et al. GLUT1 inhibition blocks growth of RB1-positive triple negative breast cancer[J]. Nat Commun, 2020, 11(1).
[3] Adams D J, Ito D, Rees M G, et al. NAMPT Is the Cellular Target of STF 31-Like Small-Molecule Probes[J]. Acs Chem Biol, 2014, 9(10): 2247-2254.
[4] Wang L X, Pavlou S, Du X, et al. Glucose transporter 1 critically controls microglial activation through facilitating glycolysis[J]. Mol Neurodegener, 2019, 14.
[5] Xintaropoulou C, Ward C, Wise A, et al. A comparative analysis of inhibitors of the glycolysis pathway in breast and ovarian cancer cell line models[J]. Oncotarget, 2015, 6(28): 25677-25695.
[6] Hou Hou, Lü Xing, Zhang Na, et al. Mechanism Analysis of the Effect of STF 31 on Proliferation and Apoptosis of Fibroblast-like Synoviocytes in Rheumatoid Arthritis [J]. Anatomical Research, 2022, 44(06): 525-531
[7] Morioka S, Perry JSA, Raymond MH, et al. Efferocytosis induces a novel SLC program to promote glucose uptake and lactate release[J]. Nature, 2018, 563(7733): 714-718.
STF 31是一种具有细胞通透性的葡萄糖转运蛋白1（GLUT1）的抑制剂，IC₅₀为1μM[1]。GLUT1是介导葡萄糖摄取的重要转运蛋白，参与维持糖酵解代谢[2]。STF 31还可抑制烟酰胺磷酸核糖转移酶（NAMPT），从而干扰糖酵解过程并产生细胞毒性[3]。
在体外，STF 31（0-10μM）处理B6M7细胞24h，可剂量依赖性抑制细胞的葡萄糖摄取能力，而对细胞存活率无明显影响[4]。STF 31（30μM）处理MCF-7细胞48h，可显著抑制糖酵解过程并诱导细胞凋亡[5]。STF 31（2、4、8μM）处理类风湿关节炎成纤维样滑膜细胞（RAFLs）24-72h，以时间和剂量依赖性方式抑制细胞增殖[6]。
在体内，STF 31（10mg/kg）通过腹腔注射给药（前2天每日两次，随后3天每日一次），对正常小鼠的体重、行为及ERG反应无明显影响。在光诱导模型中，STF 31可显著抑制CX3CR1gfp/+小鼠小胶质细胞的活化，并减轻视网膜变性[4]。STF 31（10mg/kg）与地塞米松通过腹腔联合注射正常小鼠4h，可显著促进坏死胸腺细胞的积累[7]。
| Cell experiment [1]: | |
Cell lines | B6M7 |
Preparation Method | B6M7 cells were seeded into 96-well plates with 6000 cells per well and cultured for 24h. They were treated with different concentrations of STF 31(0, 0.01, 0.1, 1, 5, and 10μM).for 24 h to 48 h.Cells were washed twice with PBS and incubated in serum-free DMEM overnight prior to the assay. Glucose uptake was measured using a Glucose Uptake Assay Kit (ab136955, Abcam) according to the manufacturer’s instructions, and fluorescence was detected using a FLUOstar Omega microplate reader (BMG Labtech). Cell viability was assessed using the AlamarBlue® assay (Thermo Fisher Scientific) following the manufacturer’s protocol. |
Reaction Conditions | 0, 0.01, 0.1, 1, 5, and 10μM; 24 h, 48 h. |
Applications | STF 31 dose-dependently suppressed glucose uptake in B6M7 cells without affecting cell viability. |
| Animal experiment [1]: | |
Animal models | C57BL/6J and CX3CR1gfp/+ mice |
Preparation Method | C57BL/6 J mice received intraperitoneal STF 31 at 10 mg/kg twice daily for 2 days and once daily for a further 3 days, with DMSO-treated mice as controls. Body weight and electroretinography were assessed on day 6, and eyes were collected for immunohistochemistry (4 mice per group). CX3CR1gfp/+mice were given the same STF 31 regimen starting 1 day prior to light exposure. After 16 h of dark adaptation, pupil dilation, and anesthesia, mice were exposed to 50,000 lx focal white light for 10 min. Clinical and immunohistochemical analyses were performed after treatment (5 mice per group). |
Dosage form | 10mg/kg, twice daily for 2 days, followed by once daily for another 3 days; i.p. |
Applications | STF 31 treatment improved photoreceptor survival and attenuated microglial activation in CX3CR1gfp/+ mice, without inducing retinal cell death in C57BL/6J mice. |
References: | |
| Cas No. | 724741-75-7 | SDF | |
| 化学名 | 4-((4-(tert-butyl)phenylsulfonamido)methyl)-N-(pyridin-3-yl)benzamide | ||
| Canonical SMILES | O=S(NCC1=CC=C(C(NC2=CC=CN=C2)=O)C=C1)(C3=CC=C(C=C3)C(C)(C)C)=O | ||
| 分子式 | C23H25N3O3S | 分子量 | 423.53 |
| 溶解度 | ≥ 42.4mg/mL in DMSO | 储存条件 | Store at RT |
| 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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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3611 mL | 11.8055 mL | 23.6111 mL |
| 5 mM | 472.2 μL | 2.3611 mL | 4.7222 mL |
| 10 mM | 236.1 μL | 1.1806 mL | 2.3611 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，
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2.
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