Pitstop2
目录号 : GC45549Pitstop2是一种网格蛋白抑制剂,可抑制网格蛋白末端结构域的两性结合,IC50值为12μM。
Cas No.:1419320-73-2
Sample solution is provided at 25 µL, 10mM.
Pitstop2 is a clathrin inhibitor that inhibits amphoteric binding of clathrin terminal domains with an IC50 value of 12μM[1-2].
In Hela cells, Pitstop2 (5-30µM) inhibits clathrin-independent endocytosis in a dose-dependent manner. In BEAS-2B and COS-7 cells, Pitstop2 (20μM) inhibits the uptake of transferrin and major histocompatibility complex class I (MHCI) proteins[3]. Pitstop2 inhibits gridin-mediated transferrin uptake in HeLa and U2OS cells with IC50 values of 12-15μM and 9.7μM, respectively [1].
Pitstop2 (10µg/kg) pretreatment can partially prevent nitroglycerin (NTG)-induced hyperalgesia in rat chronic migraine (CM) model. Compared with NTG+ vehicle group, Pitstop2 can significantly reduce the expression of CGRP and c-Fos in trigeminal ganglion (TG) and reduce the activation of trigeminovascular system (TVS) in CM rats [4].
References:
[1] von Kleist, L., Stahlschmidt, W., Bulut, H., et al. Role of the clathrin terminal domain in regulating coated pit dynamics revealed by small molecule inhibition. Cell 146(3), 471-484 (2012).
[2] Smith CM, Haucke V, McCluskey A, Robinson PJ, Chircop M. Inhibition of clathrin by pitstop 2 activates the spindle assembly checkpoint and induces cell death in dividing HeLa cancer cells. Mol Cancer. 2013 Jan 17;12:4.
[3] Dutta D, Williamson C D, Cole N B, et al. Pitstop 2 is a potent inhibitor of clathrin-independent endocytosis[J]. 2012.
[4] Zhang L, Zhou Y, Wang Y, Yang L, Wang Y, Shan Z, Liang J, Xiao Z. Inhibiting PAC1 receptor internalization and endosomal ERK pathway activation may ameliorate hyperalgesia in a chronic migraine rat model. Cephalalgia. 2023 Apr;43(4):3331024231163131.
Pitstop2是一种网格蛋白抑制剂,可抑制网格蛋白末端结构域的两性结合,IC50值为12μM[1-2]。
在Hela细胞中,Pitstop2(5-30µM)以剂量依赖性方式抑制网格蛋白独立的内吞作用。在BEAS-2B和COS-7细胞中,Pitstop2(20μM)可抑制转铁蛋白和主要组织相容性复合物I类蛋白(MHCI)的摄取[3]。Pitstop2可抑制HeLa和U2OS细胞中网格蛋白介导的转铁蛋白摄取,IC50值分别为12-15μM和9.7μM[1]。
在大鼠慢性偏头痛(CM)模型中,Pitstop2(10µg/kg)预处理可部分预防硝酸甘油(NTG)诱导的痛觉过敏,与NTG+载体组相比,Pitstop2可以显著降低三叉神经节(TG)中CGRP、c-Fos的表达,减轻CM大鼠的三叉神经血管系统(TVS)激活[4]。
Cell experiment [1]: | |
Cell lines | ARPE-19 cells |
Preparation Method | ARPE-19 cells were treated with 10μM pitstop2, 30μM dyngo4A, 80μM dynasore or vehicle control (DMSO) for 30 min. The expression of p-AKT was detected by western blot assay. |
Reaction Conditions | 10μΜ, 30min |
Applications | ARPE-19 cells treated with 10μM pitstop2 ablated epidermal growth factor (EGF)-stimulated Akt phosphorylation. |
Animal experiment [2]: | |
Animal models | Rat model of chronic migraine |
Preparation Method | The rats were divided into four groups: Saline, Nitroglycerin (NTG, i.p.), NTG + vehicle and NTG + Pitstop2 (i.n.). The NTG + Pitstop2 group was given Pitstop2 every other day, followed by NTG 30 minutes later. Behavioral tests were performed 20 minutes before i.n. administration and two hours after i.p. injection. |
Dosage form | 10µg/kg, Two days a day for nine days, i.n. |
Applications | Pitstop2 can significantly increase the threshold of basic mechanical pain and thermal pain, and reverse NTG-induced acute mechanical pain and thermal pain allergy. |
References: [1] Garay C, Judge G, Lucarelli S, Bautista S, Pandey R, Singh T, Antonescu CN. Epidermal growth factor-stimulated Akt phosphorylation requires clathrin or ErbB2 but not receptor endocytosis. Mol Biol Cell. 2015 Oct 1;26(19):3504-19. [2] Zhang L, Zhou Y, Wang Y, Yang L, Wang Y, Shan Z, Liang J, Xiao Z. Inhibiting PAC1 receptor internalization and endosomal ERK pathway activation may ameliorate hyperalgesia in a chronic migraine rat model. Cephalalgia. 2023 Apr;43(4):3331024231163131. |
Cas No. | 1419320-73-2 | SDF | |
化学名 | N-[5-[(4-bromophenyl)methylene]-4,5-dihydro-4-oxo-2-thiazolyl]-1-naphthalenesulfonamide | ||
Canonical SMILES | O=C1/C(SC(NS(C2=C(C=CC=C3)C3=CC=C2)(=O)=O)=N1)=C/C4=CC=C(Br)C=C4 | ||
分子式 | C20H13BrN2O3S2 | 分子量 | 473.4 |
溶解度 | 20mg/mL in DMSO | 储存条件 | 4°C, protect from light |
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1 mg | 5 mg | 10 mg | |
1 mM | 2.1124 mL | 10.5619 mL | 21.1238 mL |
5 mM | 0.4225 mL | 2.1124 mL | 4.2248 mL |
10 mM | 0.2112 mL | 1.0562 mL | 2.1124 mL |
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