| Description | Phenylmethanesulfonyl fluoride (PMSF (Phenylmethylsulfonyl fluoride)) is an enzyme inhibitor that inactivates IRC-50 arvin, subtilisin, and the fatty acid synthetase complex. |
| In vitro | 用PMSF（i.p.）处理小鼠能产生大麻素的效果,可以抗伤害（ED50：86 mg/kg）、降低体温（ED50：224 mg/kg）、保持不动性（ED50：206 mg/kg）.用PMSF（i.p.）处理Sprague-Dawley大鼠能产生剂量依赖的止痛效果.在大鼠体内,PMSF能明显提升β-内啡肽的镇痛效果.通过抑制脂肪酸酰胺水解酶活性,PMSF能抑制ICR小鼠的大麻素或Δ(9)- 四氢大麻酚典型性拟大麻效应.在注射1或10 mg/kg 3H标记的大麻素前用腹腔注射30 mg/kg PMSF预处理,待注射大麻素5分钟后,对比注射的3H H标记的大麻素,大脑中大麻素的水平显著升高.用PMSF（30 mg/kg）预处理可以增强大麻素对甩尾反应（抗伤害效应）、移动性和自发活动性产生的作用,其增强效果分别是原来的5、8和10倍.在PSP前12小时用PMSF处理母鸡可以完全防御迟发性神经毒性,但是在之后4小时处理则会加强神经毒性效应.用PMSF预处理可预防母鸡的有机磷酸酯诱导的延迟性神经病和抑制三邻甲苯基磷酸酯诱导的神经丝退化. |
| In vivo | PMSF是特定磷脂酰肌醇磷脂酶C的抑制剂。在豚鼠回肠的纵行平滑肌中,PMSF（2 mM）几乎完全抑制卡巴胆碱激活的肌糖形成磷脂酰肌醇,但不影响由钾激活的肌糖形成磷脂酰肌醇的通路。但PMSF对钾和卡巴胆碱刺激产生的肌肉收缩都能产生短暂的抑制效果。PMSF是鼠源乙酰胆碱酯酶最好的抑制剂,因为BSF（8倍于PMSF量）的抑制效果要比PMSF低6倍。PMSF可迅速抑制从人胰腺纯化的胰凝乳蛋白酶活性,也可以迅速地抑制人红细胞中的胰腺胆碱酯酶,但几乎不影响人胰蛋白酶。在布氏锥虫体内,PMSF还抑制乙醇胺磷酸添加到糖基磷脂酰肌醇中间产物的形成和血液中GPI中间产物的肌糖残基的酰化作用,以及前循环形式的乙醇胺磷酸的添加和肌糖的酰化,但是对哺乳动物HeLa细胞中最后一种没有抑制作用。 |
| Synonyms | Phenylmethylsulfonyl fluoride, Benzylsulfonyl fluoride, 苯甲基磺酰氟 |
| molecular weight | 174.19 |
| Molecular formula | C7H7FO2S |
| CAS | 329-98-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | Ethanol: 17.4 mg/mL (100 mM) DMSO: 55 mg/mL (315.75 mM) |
| References | 1. Turini P, et al. J Pharmacol Exp Ther, 1969, 167(1), 98-104. 2. Pinsky C, et al. Life Sci, 1982, 31(12-13), 1193-1196. 3. Sekar MC, et al. Cell Calcium, 1984, 5(3), 191-203. 4. Güther ML, et al. J Biol Chem. 1994 Jul 15;269(28):18694-701. 5. Compton DR, et al. J Pharmacol Exp Ther, 1997, 283(3), 1138-1143. 6. Wen Q L, Yi H Q, Yang K, et al. Role of oncogene PIM-1 in the development and progression of papillary thyroid carcinoma: involvement of oxidative stress[J]. Molecular and Cellular Endocrinology. 2020: 111144. 7. Xu Guang, Ting Li, Jiayi Chen, Changyan Li, Haixin Zhao, Chengcheng Yao, Hua Dong et al. Autosomal dominant retinitis pigmentosa-associated gene PRPF8 is essential for hypoxia-induced mitophagy through regulating ULK1mRNA splicing [J]. Autophagy. 2018;14(10):1818-1830. |
| Citations | 1. Xu G, Li T, Chen J, et al. Autosomal dominant retinitis pigmentosa-associated gene PRPF8 is essential for hypoxia-induced mitophagy through regulating ULK1mRNA splicing. Autophagy. 2018, 14(10): 1818-1830 2. Li X, Zhang H, Qiao S, et al Melatonin administration alleviates 2,2,4,4-tetra-brominated diphenyl ether (PBDE-47)-induced necroptosis and secretion of inflammatory factors via miR-140-5p/TLR4/NF-κB axis in fish kidney cells. Fish & Shellfish Immunology. 2022 3. Wen Q L, Yi H Q, Yang K, et al. Role of oncogene PIM-1 in the development and progression of papillary thyroid carcinoma: involvement of oxidative stress. Molecular and Cellular Endocrinology. 2021 Mar 1;523:111144. doi: 10.1016/j.mce.2020.111144 4. Song N, Guan X, Zhang S, et al.Discovery of a pyrrole-pyridinimidazole derivative as novel SIRT6 inhibitor for sensitizing pancreatic cancer to gemcitabine.Cell Death & Disease.2023, 14(8): 499. 5. Yan Y, Yu L, Chen B, et al.Mastoparan M Suppressed NLRP3 Inflammasome Activation by Inhibiting MAPK/NF-κB and Oxidative Stress in Gouty Arthritis.Journal of Inflammation Research.2023: 6179-6193. |