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

531535
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₄H₅ClF₉N₃O

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.31535.0001
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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®
          Synonyms2-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, SP-100030, Nuclear Factor-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
          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
          Synonyms2-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, SP-100030, Nuclear Factor-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.