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533641 CHOP Activator, Cpd12 - Calbiochem

533641
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Replacement Information

Tableau de caractéristiques principal

Empirical Formula
C₁₆H₁₆ClN₃O₆S

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      Description
      OverviewA cell-permeable sulfonamidebenzamide derivative that acts as a potent and selective inducer of C/EBP-homologous protein (CHOP; AC50 = 800 nM) without affecting XBP (AC50 > 80 µM). Displays a balanced profile in terms of its lipophilic profile (cLogP = 2.7), selectivity, and activation of CHO-CHOP luciferase reporter system. Exhibits high selectivity against a panel of 67 GPCR, nuclear receptors, transporters, and ion channels. Has significantly reduced activity towards dopamine receptor at high concentrations (68% at 10 µM). upregulates the expression of UPR target genes. Displays anti-proliferation properties in wild-type mouse embryonic fibroblasts (EC50 = 4.8 µM), but does not affect CHOP knock out cells even at high concentrations (EC50 > 20 µM). Inhibits the proliferation of several cancer cell lines at low micromolar levels. Exhibits favorable pharmacokinetic profile (Cmax = 140 nM; Tmax = 0.17 h at 30 mg/kg, i.p. single dose).
      Catalogue Number533641
      Brand Family Calbiochem®
      SynonymsN-(4-((4-chloropiperidin-1-yl)sulfonyl)phenyl)-5-nitrofuran-2-carboxamide, C/EBP-Homologous Protein Activator, Cpd12
      DescriptionCHOP Activator, Cpd12
      References
      ReferencesFlaherty, D. P., et al. 2014. ACS Med Chem Lett. 5, 1278.
      Product Information
      FormLight yellow solid
      Hill FormulaC₁₆H₁₆ClN₃O₆S
      Chemical formulaC₁₆H₁₆ClN₃O₆S
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetCHOP
      Purity≥96% 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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      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 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      CHOP Activator, Cpd12 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      Flaherty, D. P., et al. 2014. ACS Med Chem Lett. 5, 1278.
      Fiche technique

      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.

      Revision24-June-2016 JSW
      SynonymsN-(4-((4-chloropiperidin-1-yl)sulfonyl)phenyl)-5-nitrofuran-2-carboxamide, C/EBP-Homologous Protein Activator, Cpd12
      DescriptionA cell-permeable sulfonamidebenzamide derivative that acts as a potent and selective inducer of C/EBP-homologous protein (CHOP; AC50 = 800 nM) without affecting XBP (AC50 > 80 µM). Displays a balanced profile in terms of its lipophilic profile (cLogP = 2.7), selectivity, and activation of CHO-CHOP luciferase reporter system. Exhibits high selectivity against a panel of 67 GPCR, nuclear receptors, transporters, and ion channels. Has significantly reduced activity towards dopamine receptor at high concentrations (68% at 10 µM). upregulates the expression of UPR target genes. Displays anti-proliferation properties in wild-type mouse embryonic fibroblasts (EC50 = 4.8 µM), but does not affect CHOP knock out cells even at high concentrations (EC50 > 20 µM). Inhibits the proliferation of several cancer cell lines at low micromolar levels. Exhibits favorable pharmacokinetic profile (Cmax = 140 nM; Tmax = 0.17 h at 30 mg/kg, i.p. single dose).
      FormLight yellow solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₆H₁₆ClN₃O₆S
      Purity≥96% by HPLC
      SolubilityDMSO (50 mg/ml)
      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 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesFlaherty, D. P., et al. 2014. ACS Med Chem Lett. 5, 1278.