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539225 Protein Disulfide Isomerase Inhibitor III, PACMA 31 - Calbiochem

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

539225
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Descripción

Replacement Information

Products

Número de referenciaEmbalaje Cant./Env.
539225-25MG Frasco de vidrio 25 mg
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
Número de referencia GTIN
539225-25MG 04055977268966

Documentation

Referencias bibliográficas

Visión general referencias
Xu, S., et al. 2012. Proc. Natl. Acad. Sci. USA 109, 16348.
Ficha técnica

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.