Pitstop 2

Pitstop 2 is a clathrin inhibitor which inhibits clathrin-mediated endocytosis (CME) by associating with the terminal domain of clathrin. Pitstop 2 has the potential for anti-cancer research.

Product information

CAS Number: 1419320-73-2

Molecular Weight: 473.36

Formula: C20H13BrN2O3S2

Chemical Name: (Z)-N-(5-(4-bromobenzylidene)-4-oxo-4, 5-dihydrothiazol-2-yl)naphthalene-1-sulfonamide

Smiles: O=C1N=C(NS(=O)(=O)C2=CC=CC3=CC=CC=C32)S/C/1=C\C1C=CC(Br)=CC=1

InChiKey: CGDLWHGPJPVPDU-ATVHPVEESA-N

InChi: InChI=1S/C20H13BrN2O3S2/c21-15-10-8-13(9-11-15)12-17-19(24)22-20(27-17)23-28(25,26)18-7-3-5-14-4-1-2-6-16(14)18/h1-12H,(H,22,23,24)/b17-12-

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 62.5 mg/mL (132.03 mM; Need ultrasonic)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Pitstop 2 (20-40 μM; 30 min) inhibits the endocytosis of transferrin in J774A.1 macrophages and does not compromise cell viability. Pitstop 2 (20-40 μM; 30 min) does not affect the internalization of cholera toxin B in J774A.1 macrophages. Pitstop 2 (0.001-100 μM; 6 h) inhibits the mitotic spindle and impairs mitotic progression in HeLa cells. Pitstop 2 (1-30 μM; 24 h) induces apoptosis and inhibits cell growth in dividing cancer cells. Pitstop 2 (1-30 μM; 48 h) does not affect the growth and viability of non-tumourigenic NIH3T3 fibroblasts.

References:

1. Kumar GA, et, al. Leishmania donovani Internalizes into Host Cells via Caveolin-mediated Endocytosis. Sci Rep. 2019 Sep 2; 9(1): 12636.
2. Smith CM, et, al. 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.

Products are for research use only. Not for human use.