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Pitstop2 Sale

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。

Pitstop2 Chemical Structure

Cas No.:1419320-73-2

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥579.00
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2mg
¥316.00
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5mg
¥488.00
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10mg
¥885.00
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25mg
¥1,771.00
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50mg
¥2,798.00
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100mg
¥4,559.00
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200mg
¥6,711.00
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Sample solution is provided at 25 µL, 10mM.

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客户使用产品发表文献 2

Description

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]

实验参考方法

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.

化学性质

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 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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