539225 Protein Disulfide Isomerase Inhibitor III, PACMA 31 - Calbiochem

539225
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      Overview

      Replacement Information

      Pricing & Availability

      Catalog 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
          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

          Documentation

          References

          Reference overview
          Xu, S., et al. 2012. Proc. Natl. Acad. Sci. USA 109, 16348.
          Data Sheet

          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 +2°C to +8°C
          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.
          Toxicity Standard Handling
          ReferencesXu, S., et al. 2012. Proc. Natl. Acad. Sci. USA 109, 16348.