Pitstop2
目录号 : GC45549
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。
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 |
| 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 | 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 |
| 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。
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- Purity: >99.50%
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