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Heparanase Inhibitor Heparastatin (SF4) Hydrochloride

Date:November 09 2020Web Page No:90008

Heparastatin is an inhibitor of heparanase.
Heparanase Inhibitor, Heparastatin (SF4) Hydrochloride Structure

Specification

CAS#153758-26-0
Molecular FormulaC8H11F3N2O5 HCl
Molecular Weight308.638
SourceChemically synthesized from natural siastatin B
Purity> 95%
Long Term Storageat -20℃
SolubilitySoluble in MeOH, DMSO, H2O. Insoluble in CHCl3

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Application Notes

  • Heparastatin(SF4) inhibits recombinant human heparanasefrom human melanoma A375M cells transfected with pBK-CMV expression vectors containing the heparanase cDNA (IC50=1.02μM) 3).
  • Heparastatin(SF4) inhibits β-D-glucuronidase from bovine liver (IC50=6.5 x10-2μM) 3).
  • In a in vitro HS degradation assay, 100μM Heparastatin(SF4) completely inhibits the enzyme activity of recombinant heparanase of murine mammary epitherialcells(NMuMG) transefected with a mouse heparanase expression vector pcDNA3.1(-)-Hygro-Hep at 0.15μg/mL 6).
  • Heparastatin(SF4) inhibits heparansulfate(HS) chain degradation of HSPGs of Matrigel by heparanase of the LPS-treated microgliallysates from the forebrain cells of Wistar rats and the in vitro transmigration of microglia through the Matrigel-coated insert in a dose-dependent manner 5).
  • Heparastatin(SF4) markedly inhibits degradation of HS by heparanasein the nucleus translocatedfrom the cytoplasm of the calcium-induced human esophageal keratinocyte cells and keratinocyte differentiation at 100μM 4).

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References

  1. Effect on spontaneous metastasis of mouse Lewis lung carcinoma by a trifluoroacetamideanalogue of siastatin B. Nishimura Y, Satoh T, Kondo S, Takeuchi T, AzetakaM, FukuyasuH, IizukaY, Shibahara S, J. Antibiotics, 1994, 47, 840-842
  2. Apracticalsynthesis of(3S,4S,5R,6R)-4,5-dihydroxy-6-(trifluoroacetamido)piperidine -3-carboxylic acid having antimetastaticactivity in mice from siastatinB. Satoh T., Nishimura Y., Kondo S., Takeuchi T. Carbohyd. Res., 1996,286, 173-178
  3. Flexible synthesis and biological activity of uronicacid-type gem-diamine1-N-iminosugars: a new family of glycosidase inhibitors. Nishimura Y, ShitaraE, Adachi H, Toyoshima M, Nakajima M, OkamiY, Takeuchi T J. Org. Chem., 2000, 65, 2-11
  4. Heparanaseregulates esophageal keratinocyte differentiation through nuclear translocation and heparin sulfate cleavage. Kobayashi M., NaomotoY., NobuhisaT., OkawaT., Takaoka M., ShirakawaY., YamatsujiT., Matsuoka J., MizushimaT., Matsuura H., Nakajima M., Nakagawa H., RustgiA., Tanaka N. Differentiation, 2006, 74, 235-243
  5. Involvement of heparanasein migration of microglial cells. Takahashi H., Matsumoto H., SmirkinA., ItaiT., Nishimura Y., Tanaka J., Biochim. Biophys. Acta., 2008, 1780, 709-715
  6. Heparanasedownmodulationin the process of epithelial-to-mesenchymaltransition of mouse mammary epithelial cells. KoganeY., Higashi N., Nishimura Y., Nakajima M., T.IrimuraT.,J. GlycomicsLipdomics,2013 (online publication), 3 (1), 1000107

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[Date : July 15 2024 00:05]

Detail Product Name Product Code Supplier Size Price
Heparastatin (Hydrochloride),SF4 Hydrochloride,Heparanase Inhibitor
DatasheetThis may not be the latest data sheet.
11829 IMCInstitute of Microbial Chemistry 1 mg $500

Description CAS# : 153758-25-9 Molecular Formula : C8H11F3N2O5・HCl Molecular Weight : 308.64 (hydrochloride) Heparastatin (SF4) inhibits recombinant human heparanase from human melanoma A375M cells transfected with pBK-CMV expression vectors containing the heparanase cDNA with IC50 1.02μM.
Storage -20°C CAS 153758-26-0 (hydrochloride salt), 153758-25-9 (salt free form)
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Bioactive Compounds

[Date : July 15 2024 00:05]

Heparastatin (Hydrochloride),SF4 Hydrochloride,Heparanase Inhibitor


  • Product Code: 11829
  • Supplier: IMC
  • Size: 1mg
  • Price: $500

Description CAS# : 153758-25-9 Molecular Formula : C8H11F3N2O5・HCl Molecular Weight : 308.64 (hydrochloride) Heparastatin (SF4) inhibits recombinant human heparanase from human melanoma A375M cells transfected with pBK-CMV expression vectors containing the heparanase cDNA with IC50 1.02μM.
Storage -20°C CAS 153758-26-0 (hydrochloride salt), 153758-25-9 (salt free form)
Link

Bioactive Compounds

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