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533641 CHOP Activator, Cpd12 - Calbiochem

533641
  
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Aperçu

Replacement Information

Tableau de caractéristiques principal

Empirical Formula
C₁₆H₁₆ClN₃O₆S
Description
Overview

This product has been discontinued.



A 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 SegmentMQ100
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
Global Trade ITEM Number
Référence GTIN
533641 0

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 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 3 months at -20°C.
Toxicity Standard Handling
ReferencesFlaherty, D. P., et al. 2014. ACS Med Chem Lett. 5, 1278.