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Chemical Structure| 1419320-73-2 Chemical Structure| 1419320-73-2

Structure of pitstop 2
CAS No.: 1419320-73-2

Chemical Structure| 1419320-73-2

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Pitstop 2 is a potent inhibitor of clathrin-independent endocytosis.

4.5 *For Research Use Only !

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Product Details of pitstop 2

CAS No. :1419320-73-2
Formula : C20H13BrN2O3S2
M.W : 473.36
SMILES Code : O=S(C1=C2C=CC=CC2=CC=C1)(NC(S/C3=C\C4=CC=C(Br)C=C4)=NC3=O)=O
MDL No. :N/A

Safety of pitstop 2

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P264-P270-P271-P280-P301+P312-P302+P352-P304+P340-P305+P351+P338-P330-P332+P313-P337+P313-P362-P403+P233-P405-P501

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Mouse peritoneal macrophages 20 nM 1 hour Inhibition of clathrin-mediated endocytosis, significantly reducing the internalization rate of T. gondii Front Cell Infect Microbiol. 2020 Jun 30;10:294
Human foreskin fibroblast (HFF1) 20 nM 1 hour Inhibition of clathrin-mediated endocytosis, significantly reducing the internalization rate of T. gondii Front Cell Infect Microbiol. 2020 Jun 30;10:294
Xenopus laevis oocytes 30 µM 1 hour Inhibition of clathrin-mediated endocytosis significantly reduced the inhibitory effect of Cx30 on ENaC J Biol Chem. 2021 Jan-Jun;296:100404
HEK 293 TREx cells 10 µM 15 minutes Markedly reduced LPA-induced receptor internalization Int J Mol Sci. 2024 Jun 12;25(12):6491
A549 cells 15 µM 20 min Block clathrin-mediated endocytosis, reducing internalization of SARS-CoV-2 spike protein J Biol Chem. 2021 Jan-Jun;296:100306
VERO cells 15 µM 20 min Block clathrin-mediated endocytosis, reducing internalization of SARS-CoV-2 spike protein J Biol Chem. 2021 Jan-Jun;296:100306
HEK-293T cells 15 µM 20 min Block clathrin-mediated endocytosis, reducing internalization of SARS-CoV-2 spike protein J Biol Chem. 2021 Jan-Jun;296:100306
SH-SY5Y cells 10 µM 25 minutes To explore the uptake mechanisms of EPC-EXs in SH-SY5Y cells, Pitstop 2 partially decreased the relative fluorescence intensity of EPC-EXs (p < 0.05 vs. control) Stem Cell Res Ther. 2020 Oct 26;11(1):330
TmB cells 30 µM 3 hours To test the effect of pitstop 2 on TiLV entry into TmB cells, results showed no significant effect of pitstop 2 on TiLV entry Front Cell Dev Biol. 2022 Dec 16;10:1075364
RAW264.7 macrophages 10 µg/mL 30 minutes Inhibited the binding of PPM60-Tyr-FITC to the surface receptors of RAW264.7 macrophages Polymers (Basel). 2018 Mar 26;10(4):372
DRG neurons 20 µM 30 minutes Blocked the hyperexcitability induced by high concentrations of DAMGO and DADLE J Neurosci. 2022 Apr 20;42(16):3316-3328
Rat mesenchymal stem cells 5 µM 30 minutes Inhibited clathrin-mediated endocytosis, reduced internalization of S100B-Alexa488 Front Cell Dev Biol. 2021 Jul 26;9:674995.
Human umbilical vein endothelial cells (HUVECs) 5 µM 30 minutes Pitstop-2 significantly inhibited the entry of rhMG53 into endothelial cells, indicating that the cellular uptake of rhMG53 may be partly through clathrin-dependent endocytosis. J Cell Mol Med. 2025 Feb;29(4):e70439
HEK293 cells 15 µM 7-20 minutes Inhibited PAC1R endocytosis and blocked PACAP-induced increase in neuronal excitability J Neurosci. 2013 Mar 6;33(10):4614-22
Mouse auditory inner hair cells (IHCs) 30 µM at least 10 min To test the effect of pitstop 2 on clathrin-mediated endocytosis, it was found to selectively impair the linear component of endocytic Cm decline. J Neurosci. 2014 Jan 15;34(3):705-16.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Guinea pig Cardiac neurons Bath application 15 μM 7-20 minutes Inhibited PAC1R endocytosis and blocked PACAP-induced increase in neuronal excitability J Neurosci. 2013 Mar 6;33(10):4614-22

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.11mL

0.42mL

0.21mL

10.56mL

2.11mL

1.06mL

21.13mL

4.23mL

2.11mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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