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home » Chemicals » PLA2 Inhibitors and Controls » HELSS (Haloenol lactone suicide substrate, BEL, Bromoenol lactone): sc-201418

HELSS (Haloenol lactone suicide substrate, BEL, Bromoenol lactone): sc-201418

  |  Datasheet  | MSDS
  • Specifications
    • Offered as 5 mg (sc-201418) and 25 mg (sc-201418A) sizes
    • CAS Number: 88070-98-8
    • Molecular Weight: 317.2
    • Molecular Formula: C16H13BrO2
    • Purity: 98%
    • Form: Solid
    • Physical Appearance: White solid
    • Solubility: Soluble in DMSO (25 mg/ml)
    • SMILES: C1C/C(=C\Br)/OC(=O)C1C2=CC=CC3=CC=CC=C32
  • Description
    • Haloenol lactone (HELSS) is a potent and irreversible inhibitor that selectively targets and forms a covalent bond with myocardial calcium-independent PLA2 (phospholipase A2). Calcium-independent phospholipase A2 is a mediator of arachidonic acid release from aortic smooth cells induced by vasopressin. Inhibition of arachidonic acid release was found to be saturable and specific due to HELSS's 1,000-fold selectivity for inhibition of calcium-independent versus calcium-dependent PLA2. HELSS has also been observed to inhibit cellular cytosolic magnesium-dependent PAP (phosphatidic acid phosphohydrolase) activity in intact P388D1 macrophages. It is noted that this compound is also a glutathione S-transferases (GST) inhibitor that could help prevent GST-mediated drug resistance.
  • Storage
    • Store as supplied at -20° C for up to 1 year
  • For Research Use Only
    • The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.
  • Reference Numbers
    • PubChem Compound ID: 5940264
    • MDL Number: MFCD00270871
  • References
    • 1. Hazen, S.L., et al. 1991. J. Biol. Chem. 266: 7227-7232. PMID: 2016324
      2. Lehman, J.J., et al. 1993. J. Biol. Chem. 268: 20713-20716. PMID: 8407892
      3. Balsinde, J. and Dennis, E.A. 1996. J. Biol. Chem. 271: 31937-31941. PMID: 8943239
      4. Zheng, J., et al. 1997. Biochem. Biophys. Res. Commun. 241: 13-17. PMID: 9405226
      5. Franchi, L., et al. 2009. J Innate Immun. 1: 607-617. PMID: 20160900
 
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Product NameCatalog #UnitPriceQtyAddFavorites
HELSS (Haloenol lactone suicide substrate, BEL, Bromoenol lactone) sc-201418 5 mg $113
HELSS (Haloenol lactone suicide substrate, BEL, Bromoenol lactone) sc-201418A 25 mg $453
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