KF 38789
目录号 : GC14589
KF 38789是一种新型的低分子量P选择素抑制剂，IC50为1.97µM。
Cas No.:257292-29-8
Sample solution is provided at 25 µL, 10mM.
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KF 38789 is a novel, low molecular weight P-selectin inhibitors displayed an IC50 of 1.97µM. P-selectin is a cell adhesion molecule of the selectin family[1][5]. KF 38789 can effectively inhibit P-selectin-dependent cell adhesion and leukocyte recruitment[2][3][5]. KF 38789 also has potential in reducing inflammation and inhibiting tumor growth[4][6][7].
In vitro, KF 38789 (0.5μM) incubating gastric cancer MKN-74 and MGC-803 cells for 24h dose-dependently decreased the cell viability ratio. KF 38789 treatment decreased the level of epithelial-mesenchymal transition (EMT)-related proteins and significantly decreased the migration of MKN-74 and MGC-803 cells by inhibiting P-selectin[2]. Corneal epithelial HCE-T cell cultures were established in regular serum-supplemented growth medium using 2-well culture inserts (0.22cm2 per well) in 35mm diameter culture dishes to expose a cell free gap of approximately 500μm in width. Cells were then cultured for an additional 8h in growth medium with or without 5μM of KF 38789. KF 38789 treatment reduced HCE-T cell migration and culture gap-closure[3]. Human mesothelial cell LP-9 in coculture devices were treated with 10μM of the KF 38789 1 hour prior to the addition ovarian cancer cells. KF 38789 significantly reduced the adhesion of cancer cells to mesothelial cells and effectively inhibited the rolling behavior of cancer cells on mesothelial surfaces[4].
In vivo, The thioglycollate (TG)-induced accumulation of leukocytes in mice was measured 6h after the treatment. KF 38789 (1mg/kg) injected intravenously prior to TG injection and at 3h following initial injection specifically inhibited P-selectin-dependent leukocyte recruitment in mouse peritonitis[5]. KF 38789 (10, 1 and 0.1mg/kg) administered to mouse carrageenan-injected model of hyperalgesia via intraperitoneal injection for 12 days, while others received a vehicle control (1% DMSO). The results showed that mice treated with the KF 38789 exhibited significantly reduced mechanical allodynia from the 3rd to the 9th day after carrageenan injection[6]. KF 38789 (10mg/kg) administered i.p. into human intrahepatic cholangiocarcinoma (ICC) cell line HUCCT1 xenograft mouse model decreased the volumes and weights of HUCCT1 formed tumor nodes in vivo. KF 38789 reduced the level of Ki67, but increased cleaved-caspase3 in tumor tissue[7].
References:
[1] Chhabra S R, Abdul Rahim A S A, Kellam B.Recent progress in the design of selectin inhibitors. Mini Rev Med Chem. 2003 Nov;3(7):679-87.
[2] Wu Y, Liu J Y, Yin T, et al. SELP can affect the immune microenvironment of gastric cancer and is associated with poor prognosis. Discov Oncol. 2025 May 21;16(1):846.
[3] Gillies P J, Richardson N A, Walshe J, et al. Demonstration of P-selectin expression and potential function in human corneal epithelial cells. Exp Eye Res. 2018 Nov:176:196-206.
[4] Carroll M J, Fogg K C, Patel H A, et al. Alternatively-Activated Macrophages Upregulate Mesothelial Expression of P-Selectin to Enhance Adhesion of Ovarian Cancer Cells. Cancer Res. 2018 Jul 1;78(13):3560-3573.
[5] Ohta S, Inujima Y, Abe M,et al. Inhibition of P-selectin specific cell adhesion by a low molecular weight, non-carbohydrate compound, KF 38789. Inflamm Res. 2001 Nov;50(11):544-51.
[6] Poh K W, Lutfun N, Manikandan J,et al. Global gene expression analysis in the mouse brainstem after hyperalgesia induced by facial carrageenan injection--evidence for a form of neurovascular coupling?. Pain. 2009 Mar;142(1-2):133-41.
[7] Du X J, Qi Z R, Chen S N, et al. Synthetic Retinoid Sulfarotene Selectively Inhibits Tumor-Repopulating Cells of Intrahepatic Cholangiocarcinoma via Disrupting Cytoskeleton by P-Selectin/PSGL1 N-Glycosylation Blockage. Adv Sci (Weinh). 2025 Jan;12(3):e2407519.
KF 38789是一种新型的低分子量P选择素抑制剂，IC50为1.97µM。P选择素是选择素家族的一种细胞黏附分子[1][5]。KF 38789能够有效抑制依赖P选择素的细胞黏附和白细胞募集[2][3][5]。KF 38789还具有减轻炎症和抑制肿瘤生长的潜力[4][6][7]。
体外实验中，KF 38789（0.5µM）与胃癌MKN-74和MGC-803细胞共孵育24小时，呈剂量依赖性地降低细胞存活率。KF 38789处理降低了上皮-间充质转化（EMT）相关蛋白水平，并通过抑制P选择素显著降低MKN-74和MGC-803细胞的迁移能力[2]。在35mm直径培养皿中，使用2孔培养插件（每孔0.22cm²）建立角膜上皮HCE-T细胞培养体系，并在培养皿中形成约500µm宽的无细胞间隙。然后，细胞在含或不含5µM KF 38789的生长培养基中继续培养8小时。KF 38789处理降低了HCE-T细胞的迁移能力，并减少了培养间隙的闭合[3]。在共培养装置中，人腹膜间皮细胞LP-9在卵巢癌细胞加入前1小时用10μM KF 38789处理。KF 38789显著降低了癌细胞对间皮细胞的黏附，并有效抑制了癌细胞在间皮细胞表面的滚动行为[4]。
体内实验中，测量了小鼠经硫代乙醇酸（TG）诱导后6小时白细胞的聚集情况。KF 38789（1mg/kg）在TG注射前通过静脉注射，以及在初次注射后3小时，特异性地抑制了小鼠腹膜炎中依赖P选择素的白细胞募集[5]。在小鼠角叉菜胶注射模型中，KF 38789（10、1和0.1mg/kg）通过腹腔注射给药12天，而其他小鼠接受载体对照（1% DMSO）。结果显示，经KF 38789处理的小鼠在角叉菜胶注射后第3天至第9天显著减少了机械性痛觉过敏[6]。KF 38789（10mg/kg）通过腹腔注射进入人肝内胆管癌（ICC）细胞系HUCCT1异种移植小鼠模型，降低了体内HUCCT1形成的肿瘤结节的体积和重量。KF 38789降低了肿瘤组织中Ki67的水平，但增加了裂解的caspase3水平[7]。
| Cell experiment [1]: | |
Cell lines | Gastric cancer MKN-74 and MGC-803 cells |
Preparation Method | We used the scratch assay to test the migratory abilities of MKN-74 and MGC-803 cells were seeded in 6-well plates (5×105 cells/well), and after adherence, the cells were treated with 0.5μM of KF 38789 for 24h. |
Reaction Conditions | 0.5μM; 24h |
Applications | Under the effect of KF 38789, the colonies of MKN-74 and MGC-803 cells were smaller than those in the control group. The western blot experiments showed that the levels of EMT-related proteins in gastric cancers cells changed significantly after 24h of KF 38789 treatment. Transwell and wound healing assays were performed to determine the effect of KF 38789 on the migration of MKN-74 and MGC-803 cells. The results indicated that culture in KF 38789 significantly decreased the migration of MKN-74 and MGC-803 cells compared to the control groups. |
| Animal experiment [2]: | |
Animal models | Male C57BL/6J mice |
Preparation Method | Seven groups of mice were used in this portion of the study. The first five groups (4 mice per group) received right facial carrageenan injection and daily intraperitoneal injection of 10, 1, 0.1, 0.01 or 0.001mg/kg of P-selectin inhibitor, KF 38789 (dissolved in 1% DMSO) for 12 days. The sixth group (4 mice) received right facial carrageenan injection and daily intraperitoneal injection of 1% DMSO (vehicle control) for 12 days. The last group (4 mice) did not receive facial carrageenan injection, but received daily intraperitoneal injection of 10mg/kg of KF 38789 in 1% DMSO for 12 days. |
Dosage form | 10, 1, 0.1, 0.01 or 0.001mg/kg; i.p.; 12 days |
Applications | Mice treated with the higher doses of KF 38789 (10, 1 and 0.1mg/kg) exhibited significantly reduced mechanical allodynia from the 3rd to the 9th day after carrageenan injection. Mice treated with the lower doses (0.01 and 0.001mg/kg) did not show a significant difference from the vehicle-treated group. |
References: | |
| Cas No. | 257292-29-8 | SDF | |
| 化学名 | 3-(7-(2,4-dimethoxyphenyl)-2,3,6,7-tetrahydro-1,4-thiazepin-5-yl)-4-hydroxy-6-methyl-2H-pyran-2-one | ||
| Canonical SMILES | CC(O1)=CC(O)=C(C1=O)C2=NCCSC(C3=C(OC)C=C(OC)C=C3)C2 | ||
| 分子式 | C19H21NO5S | 分子量 | 375.44 |
| 溶解度 | <37.54mg/ml in DMSO | 储存条件 | Store at -20°C |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6635 mL | 13.3177 mL | 26.6354 mL |
| 5 mM | 0.5327 mL | 2.6635 mL | 5.3271 mL |
| 10 mM | 0.2664 mL | 1.3318 mL | 2.6635 mL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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2.
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