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MedKoo Cat#: 574007 | Name: Pitstop2
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Pitstop2 is an inhibitor of the interaction between the clathrin terminal domain and amphiphysin. It inhibits clathrin-mediated transferrin uptake and HIV-1 entry and infectivity reporter cell lines. It also inhibits clathrin-independent endocytosis of CD44, CD98, and CD147 in HeLa cells.

Chemical Structure

Pitstop2
Pitstop2
CAS#1332879-52-3

Theoretical Analysis

MedKoo Cat#: 574007

Name: Pitstop2

CAS#: 1332879-52-3

Chemical Formula: C20H13BrN2O3S2

Exact Mass: 471.9551

Molecular Weight: 473.36

Elemental Analysis: C, 50.75; H, 2.77; Br, 16.88; N, 5.92; O, 10.14; S, 13.55

Price and Availability

Size Price Availability Quantity
5mg USD 350.00
25mg USD 875.00
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Related CAS #
No Data
Synonym
Pitstop2
IUPAC/Chemical Name
N-[5-[(4-bromophenyl)methylene]-4,5-dihydro-4-oxo-2-thiazolyl]-1-naphthalenesulfonamide
InChi Key
CGDLWHGPJPVPDU-ATVHPVEESA-N
InChi Code
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-
SMILES Code
O=C1/C(SC(NS(C2=C(C=CC=C3)C3=CC=C2)(=O)=O)=N1)=C/C4=CC=C(Br)C=C4
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
λmax: 210, 212, 222, 344 nm

Preparing Stock Solutions

The following data is based on the product molecular weight 473.36 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Stefanello ST, Mizdal CR, Shahin V. Pitstop-2 Upsets The Integrity of Nuclear Pore Complexes (NPCs) by Interaction with β-Propeller Folds of Npc Scaffold Proteins. Adv Biol (Weinh). 2024 Mar;8(3):e2300360. doi: 10.1002/adbi.202300360. Epub 2023 Dec 21. PMID: 38129324. 2: Sharma M, Marin M, Wu H, Prikryl D, Melikyan GB. Human Immunodeficiency Virus 1 Preferentially Fuses with pH-Neutral Endocytic Vesicles in Cell Lines and Human Primary CD4+ T-Cells. ACS Nano. 2023 Sep 12;17(17):17436-17450. doi: 10.1021/acsnano.3c05508. Epub 2023 Aug 17. PMID: 37589658; PMCID: PMC10510587. 3: Liashkovich I, Stefanello ST, Vidyadharan R, Haufe G, Erofeev A, Gorelkin PV, Kolmogorov V, Mizdal CR, Dulebo A, Bulk E, Kouzel IU, Shahin V. Pitstop-2 and its novel derivative RVD-127 disrupt global cell dynamics and nuclear pores integrity by direct interaction with small GTPases. Bioeng Transl Med. 2022 Oct 19;8(4):e10425. doi: 10.1002/btm2.10425. PMID: 37476059; PMCID: PMC10354767. 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. doi: 10.1177/03331024231163131. PMID: 36946245. 5: Mavri M, Glišić S, Senćanski M, Vrecl M, Rosenkilde MM, Spiess K, Kubale V. Patterns of human and porcine gammaherpesvirus-encoded BILF1 receptor endocytosis. Cell Mol Biol Lett. 2023 Feb 21;28(1):14. doi: 10.1186/s11658-023-00427-y. Erratum in: Cell Mol Biol Lett. 2023 Nov 24;28(1):94. doi: 10.1186/s11658-023-00512-2. PMID: 36810008; PMCID: PMC9942385. 6: Paksoy A, Hoppe S, Dörflinger Y, Horstmann H, Sätzler K, Körber C. Effects of the clathrin inhibitor Pitstop-2 on synaptic vesicle recycling at a central synapse in vivo. Front Synaptic Neurosci. 2022 Nov 17;14:1056308. doi: 10.3389/fnsyn.2022.1056308. PMID: 36466146; PMCID: PMC9714552. 7: Iida A, Nomura J, Yoshida J, Suzuki T, Yokoi H, Hondo E. Endocytosis-mediated vitellogenin absorption and lipid metabolism in the hindgut-derived placenta of the viviparous teleost Xenotoca eiseni. Biochim Biophys Acta Mol Cell Biol Lipids. 2022 Sep;1867(9):159183. doi: 10.1016/j.bbalip.2022.159183. Epub 2022 Jun 2. PMID: 35660667. 8: Sun H, -Takebayashi YU, Motohashi H, Nagai J. Internalization of FITC-albumin in Human Adipose-derived Stem Cells: Involvement of Clathrin and Caveolin. Pharmazie. 2022 May 1;77(5):141-146. doi: 10.1691/ph.2022.2340. PMID: 35655384. 9: Jones BM, Mingin GC, Tykocki NR. Histamine receptors rapidly desensitize without altering nerve-evoked contractions in murine urinary bladder smooth muscle. Am J Physiol Renal Physiol. 2022 Mar 1;322(3):F268-F279. doi: 10.1152/ajprenal.00355.2021. Epub 2022 Jan 24. PMID: 35073211; PMCID: PMC8858670. 10: Zhang Y, Zhu J, Xu H, Yi Q, Yan L, Ye L, Zhang X, Xie M, Tan B. Time- Dependent Internalization of S100B by Mesenchymal Stem Cells via the Pathways of Clathrin- and Lipid Raft-Mediated Endocytosis. Front Cell Dev Biol. 2021 Jul 26;9:674995. doi: 10.3389/fcell.2021.674995. PMID: 34381770; PMCID: PMC8351554. 11: Arai M, Komori H, Fujita D, Tamai I. Uptake Pathway of Apple-derived Nanoparticle by Intestinal Cells to Deliver its Cargo. Pharm Res. 2021 Mar;38(3):523-530. doi: 10.1007/s11095-021-03018-8. Epub 2021 Mar 15. PMID: 33723795. 12: May V, Johnson GC, Hammack SE, Braas KM, Parsons RL. PAC1 Receptor Internalization and Endosomal MEK/ERK Activation Is Essential for PACAP-Mediated Neuronal Excitability. J Mol Neurosci. 2021 Aug;71(8):1536-1542. doi: 10.1007/s12031-021-01821-x. Epub 2021 Mar 6. PMID: 33675454; PMCID: PMC8450765. 13: Ilyaskin AV, Korbmacher C, Diakov A. Inhibition of the epithelial sodium channel (ENaC) by connexin 30 involves stimulation of clathrin-mediated endocytosis. J Biol Chem. 2021 Jan-Jun;296:100404. doi: 10.1016/j.jbc.2021.100404. Epub 2021 Feb 10. PMID: 33577799; PMCID: PMC7973139. 14: Riaz MA, Adang MJ, Hua G, Rezende TMT, Rezende AM, Shen GM. Identification of Lysinibacillus sphaericus Binary toxin binding proteins in a malarial mosquito cell line by proteomics: A novel approach towards improving mosquito control. J Proteomics. 2020 Sep 15;227:103918. doi: 10.1016/j.jprot.2020.103918. Epub 2020 Jul 24. PMID: 32712372. 15: Herrscher C, Pastor F, Burlaud-Gaillard J, Dumans A, Seigneuret F, Moreau A, Patient R, Eymieux S, de Rocquigny H, Hourioux C, Roingeard P, Blanchard E. Hepatitis B virus entry into HepG2-NTCP cells requires clathrin-mediated endocytosis. Cell Microbiol. 2020 Aug;22(8):e13205. doi: 10.1111/cmi.13205. Epub 2020 Apr 1. PMID: 32216005. 16: Li M, Zhang D, Li C, Zheng Z, Fu M, Ni F, Liu Y, Du T, Wang H, Griffin GE, Zhang M, Hu Q. Characterization of Zika Virus Endocytic Pathways in Human Glioblastoma Cells. Front Microbiol. 2020 Mar 6;11:242. doi: 10.3389/fmicb.2020.00242. PMID: 32210929; PMCID: PMC7069030. 17: Yamazaki S, Su Y, Maruyama A, Makinoshima H, Suzuki J, Tsuboi M, Goto K, Ochiai A, Ishii G. Uptake of collagen type I via macropinocytosis cause mTOR activation and anti-cancer drug resistance. Biochem Biophys Res Commun. 2020 May 21;526(1):191-198. doi: 10.1016/j.bbrc.2020.03.067. Epub 2020 Mar 20. PMID: 32201076. 18: Yu W, Yang W, Li X, Li X, Yu S. Alpha-synuclein oligomerization increases its effect on promoting NMDA receptor internalization. Int J Clin Exp Pathol. 2019 Jan 1;12(1):87-100. PMID: 31933723; PMCID: PMC6944010. 19: Bar-Yoseph H, Pressman S, Blatt A, Gerassy Vainberg S, Maimon N, Starosvetsky E, Ungar B, Ben-Horin S, Shen-Orr SS, Chowers Y; Israeli IBD Research Nucleus. Infliximab-Tumor Necrosis Factor Complexes Elicit Formation of Anti-Drug Antibodies. Gastroenterology. 2019 Nov;157(5):1338-1351.e8. doi: 10.1053/j.gastro.2019.08.009. Epub 2019 Aug 8. PMID: 31401142. 20: DiCello JJ, Rajasekhar P, Eriksson EM, Saito A, Gondin AB, Veldhuis NA, Canals M, Carbone SE, Poole DP. Clathrin and GRK2/3 inhibitors block δ-opioid receptor internalization in myenteric neurons and inhibit neuromuscular transmission in the mouse colon. Am J Physiol Gastrointest Liver Physiol. 2019 Aug 1;317(2):G79-G89. doi: 10.1152/ajpgi.00085.2019. Epub 2019 May 15. PMID: 31091149.