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539225 Protein Disulfide Isomerase Inhibitor III, PACMA 31 - Calbiochem

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

539225
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539225-25MG
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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
      Applications
      Biological Information
      Primary TargetPDI
      Primary Target IC<sub>50</sub>10 µ
      Purity≥99% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      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
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Numero di catalogo GTIN
      539225-25MG 04055977268966

      Documentation

      Riferimenti bibliografici

      Panoramica delle referenze
      Xu, S., et al. 2012. Proc. Natl. Acad. Sci. USA 109, 16348.
      Scheda tecnica

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision04-July-2013 JSW
      SynonymsPDI Inhibitor III, Ethyl 2-(2-(N-(2,4-dimethoxyphenyl)propiolamido)-2-(thiophen-2-yl)acetamido)acetate
      DescriptionA 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, in insulin aggregation assays; 1h preincubation) by altering PDI secondary conformation via covalent modification of either of the two cysteine residues within the active site C(397)GHC(400) motif. Shown to inhibit the proliferation of human ovarian cancer cells in vitro, including OVCAR-3, OVCAR-8, and the doxorubicin- (Cat. No. 324380) and paclitaxel- (Cat. No. 580555 & 580556) resistant NCI/ADR-RES (GI50 (72 h) = 0.32, 0.9, and 1.4 µM, respectively), and suppress OVCAR-8-derived tumor growth in mice in vivo via either i.p. (by 85%; 100 mg/kg/5d/wk for 3 wks, 40 mg/kg/d for 7 days, then no treatment til day 62) or p.o. (by 65%; 20 mg/kg/d to 200 mg/kg/d with 20 mg increment every three 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.
      FormLight beige solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₁H₂₂N₂O₆S
      Structure formulaStructure formula
      Purity≥99% by HPLC
      SolubilityDMSO (100 mg/ml). Use only fresh DMSO for reconstitution.
      Storage Protect from light
      +2°C to +8°C
      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.
      Toxicity Standard Handling
      ReferencesXu, S., et al. 2012. Proc. Natl. Acad. Sci. USA 109, 16348.