531535 AP-1/NF-κB Dual Inhibitor, SP100030 - Calbiochem

531535
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₄H₅ClF₉N₃O

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      Glass bottle 10 mg
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      Description
      OverviewA cell-permeable, non-toxic, conformationally restricted pyrimidinecarboxamide compound that acts as a potent, reversible T-cell specific inhibitor of both AP-1 and NF-κB transcriptional activation (IC50 = 50 nM). Reduces DNA binding activity of NF-κB and downregulates NF-κB driven cytokine gene expression. Displays only trivial inhibitory effect against cytokine induction in a variety of other cells. Exhibits anti-inflammatory activity in a murine model of collagen-induced arthritis (~ 10 mg/kg/d, i.p.) and suppresses the expansion of AH-130 Yoshida ascites hepatoma in rats (~ 5 mg/kg/d, i.p.).

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number531535
      Brand Family Calbiochem®
      SynonymsSP-100030, Nuclear Factor-κB Activation Inhibitor XI, 2-Chloro-4-(trifluoromethyl)pyrimidine-5-N-(3ʹ,5ʹ-bis(trifluoromethyl)phenyl)-carboxamide, N-(3,5-bis(Trifluoromethyl)phenyl)-2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxamide, Activator Protein-1 Activation Inhibitor; AP-1 Activation Inhibitor, NF-κB Activation Inhibitor XI
      References
      ReferencesYe, N., et al. 2014. J. Med. Chem. 57, 6930.
      Moore-Carrasco, R., et al. 2009. Anticancer Res. 29, 1315.
      Huang, T.J., et al. 2001. Br. J. Pharmacol. 134, 1029.
      Gerlag, D.M., et al. 2000. J. Immunol. 165,1652.
      Sullivan, R.W., et al. 1998. J. Med. Chem. 41, 413.
      Goldman, M.E., et al. 1996. Transplant. Proc. 28, 3106.
      Product Information
      FormOff-white solid
      Hill FormulaC₁₄H₅ClF₉N₃O
      Chemical formulaC₁₄H₅ClF₉N₃O
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetAP-1 and NF-κB
      Purity≥95% 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 (-70°C). Stock solutions are stable for up to 6 months at -70°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      AP-1/NF-κB Dual Inhibitor, SP100030 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Ye, N., et al. 2014. J. Med. Chem. 57, 6930.
      Moore-Carrasco, R., et al. 2009. Anticancer Res. 29, 1315.
      Huang, T.J., et al. 2001. Br. J. Pharmacol. 134, 1029.
      Gerlag, D.M., et al. 2000. J. Immunol. 165,1652.
      Sullivan, R.W., et al. 1998. J. Med. Chem. 41, 413.
      Goldman, M.E., et al. 1996. Transplant. Proc. 28, 3106.
      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.

      Revision12-September-2014 JSW
      SynonymsSP-100030, Nuclear Factor-κB Activation Inhibitor XI, 2-Chloro-4-(trifluoromethyl)pyrimidine-5-N-(3ʹ,5ʹ-bis(trifluoromethyl)phenyl)-carboxamide, N-(3,5-bis(Trifluoromethyl)phenyl)-2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxamide, Activator Protein-1 Activation Inhibitor; AP-1 Activation Inhibitor, NF-κB Activation Inhibitor XI
      DescriptionA cell-permeable, conformationally restricted pyrimidinecarboxamide compound that is reported to inhibit against the activation of AP-1- & NF-κB-, but not &beta-actin-, mediated transcriptions (IC50 = 50 nM in Jurkat-based reporter assays; 0.5 h drug pretreatment prior to 5 h stimulation with 1 µg/mL PHA/526511 & 50 ng/mL PMA/500582 & 524400) and target genes expressions, including IL-2, IL-8, TNF-α, in 6 T cell cultures (by >85% at 3 µM), while exhibiting little inhibitory potency against cytokine inductions in 10 non-T cell cultures (by <5% at 10 µM), including endothelial, epithelial, fibroblast, monocytic, and osteoblast cultures. Intraperitoneal injection is shown to display in vivo anti-inflammatory efficacy in a murine model of collagen-induced arthritis (10 mg/kg/d) and a rodent model of Ova-induced asthma response (20 mg/kg/d). Dual AP-1 & NF-κB inhibition via daily SP100030 subcutaneous injection is also reported to suppress AH-130 Yoshida ascites hepatoma tumor expansion in rats in vivo (5 mg/kg/d).
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₄H₅ClF₉N₃O
      Purity≥95% 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 (-70°C). Stock solutions are stable for up to 6 months at -70°C.
      Toxicity Standard Handling
      ReferencesYe, N., et al. 2014. J. Med. Chem. 57, 6930.
      Moore-Carrasco, R., et al. 2009. Anticancer Res. 29, 1315.
      Huang, T.J., et al. 2001. Br. J. Pharmacol. 134, 1029.
      Gerlag, D.M., et al. 2000. J. Immunol. 165,1652.
      Sullivan, R.W., et al. 1998. J. Med. Chem. 41, 413.
      Goldman, M.E., et al. 1996. Transplant. Proc. 28, 3106.