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539225 Protein Disulfide Isomerase Inhibitor III, PACMA 31 - Calbiochem

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: PDI Inhibitor III, Ethyl 2-(2-(N-(2,4-dimethoxyphenyl)propiolamido)-2-(thiophen-2-yl)acetamido)acetate

539225
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Catalogue Number AvailabilityPackaging Qty/Pack Price Quantity
539225-25MG
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      		 Glass bottle 25 mg
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      Description
      OverviewA cell-permeable propynoic acid carbamoyl methyl amide (PACMA) that is more potent than PAO (Cat. No. 521000) in inhibiting PDI (protein disulfide isomerase) thioloxidoreductase activity (IC50 = 10 and 85 µM, respectively; 1h preincubation) by altering PDI secondary conformation via covalent modification of active site C(397)GHC(400) motif cysteines. Shown to inhibit the proliferation of human ovarian cancer cells in vitro (GI50 (72 h) = 0.32, 0.9, and 1.4 µM in OVCAR-3, OVCAR-8, and NCI/ADR-RES cultures, respectively), and suppress OVCAR-8 tumor growth in mice in vivo via either i.p. (100 mg/kg/5d/wk or 40 mg/kg/d) or p.o. (20 mg/kg/d to 200 mg/kg/d with 20 mg increment every 3 days; then 200 mg/kg/d til day 62). The commonly used PDI inhibitor Bacitracin (Cat. No. 1951) on the other hand is not suitable for in vivo studies due to its nephrotoxicity and low membrane permeability.
      Catalogue Number539225
      Brand Family Calbiochem®
      SynonymsPDI Inhibitor III, Ethyl 2-(2-(N-(2,4-dimethoxyphenyl)propiolamido)-2-(thiophen-2-yl)acetamido)acetate
      References
      ReferencesXu, S., et al. 2012. Proc. Natl. Acad. Sci. USA 109, 16348.
      Product Information
      FormLight beige solid
      Hill FormulaC₂₁H₂₂N₂O₆S
      Chemical formulaC₂₁H₂₂N₂O₆S
      ReversibleN
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Biological Information
      Primary TargetPDI
      Primary Target IC<sub>50</sub>10 µ
      Purity≥99% by HPLC
      Physicochemical Information
      Cell permeableY
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Catalogue Number GTIN
      539225-25MG 04055977268966