533641 CHOP Activator, Cpd12 - Calbiochem

533641
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₆H₁₆ClN₃O₆S

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.33641.0001
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          Glass bottle 10 mg
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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 SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Flaherty, D. P., et al. 2014. ACS Med Chem Lett. 5, 1278.
          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.

          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.