Pitstop2 |
Katalog-Nr.GC45549 |
Pitstop2 ist ein selektiver Inhibitor der Clathrin-vermittelten Endozytose (CME).
Products are for research use only. Not for human use. We do not sell to patients.
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.
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