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Compounds/plate: 80
Plate price: US$640
Catalogue number: BQ-PS

Availability: in stock

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Statistics

Average Mw:366
Lowest Mw: 254
Highest Mw:563

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Arylsulfonyl Piperazines

80 compounds

This compound collection is a screening set of 80 small molecules combining 15 aryl- or alkyl-piperazines with different aryl- and/or alkyl sulfonyl groups.

The library format is a polypropylene 96-well deep well (1mL) plate consisting of 80 compounds, deposited in 2.5 micromole quantities per well. Adding 250 microliter of DMSO will yield a 10mM solution.

Click HERE to view all 80 chemical structures present in this collection.

Pharmacology of Piperazine Sulfonamides

The sulfonamide (R-N-SO2-R) moiety itself occurs in many approved and investigational drugs. Well-known examples of drugs having a sulfonamide moiety incorporated include Sildenafil, Rosuvastatin, Naratriptan and Delaviridine shown below.

The combination of piperazines and sulfonamides is widespread in drug discovery research and has led to the discovery of many compounds with a wide array of biological activities. Piperazine sulfonamides are reported to have activity against more than 200 protein targets.

Examples of reported bioactivities of sylfonyl piperazines in the NIH's PubChem bioassay database include:

  • inhibition of ROCK (example: compound "BA1049")
  • modulation of D1 Receptors
  • inhibition of TNFa specific NF-kB induction
  • inhibition of polo-like kinase, antagonists of GPR7
  • inhibition of MEK kinase
  • inhibition of the Epstein-Barr virus nuclear antigen 1 (EBNA-1)
  • inhibition of nucleotide-binding oligomerization domain containing 2 [Homo sapiens]
  • Inhibition of the interaction of Thyroid Hormone Receptor and Steroid Receptor Coregulator 2
  • inhibition of KCNQ2 potassium channels
  • inhibition of Tau Fibril Formation
  • modulation of the M1 muscarinic receptor
  • down-regulation of Insulin Promoter Activity in MIN6 Cells
  • inhibition of Hepatitis C Virus (HCV) core protein dimerization
  • inhibition and activation of N370S glucocerebrosidase as a potential chaperone treatment of Gaucher Disease
  • antagonism of the Sphingosine 1-Phosphate Receptor 4 (S1P4)
  • potentiation or agonism of NPY-Y2
  • inhibition of the Janus kinase 2 mutant JAK2V617F
  • inhibition of the Hepatitis C Virus non-structural protein 3 helicase (NS3)
  • inhibition of protein kinase D1
  • inhibition of trypanosoma brucei hexokinase, etc...

Below are furtherdepicted some other examples of piperazine sulfonamides with known bioactivity. Note that these molecules are not part of our libraries. Our libraries do contain analogues of these molecules: