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531535 AP-1/NF-κB Dual Inhibitor, SP100030 - CAS 154563-54-9 - Calbiochem

Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
154563-54-9C₁₄H₅ClF₉N₃O

Products

Catalog NumberPackaging Qty/Pack
5.31535.0001 Glass bottle 10 mg
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
CAS number154563-54-9
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
Global Trade Item Number
Catalog Number GTIN
5.31535.0001 04055977260359

Documentation

AP-1/NF-κB Dual Inhibitor, SP100030 - CAS 154563-54-9 - 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.

Brochure

Title
NPI Flyer- Epigenetics and Nuclear Function Feature
New Products - Antibodies, Small Molecule, Inhibitors

Technical Info

Title
White Paper: Further considerations of antibody validation and usage.
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
CAS number154563-54-9
Chemical formulaC₁₄H₅ClF₉N₃O
Purity≥95% by HPLC
SolubilityDMSO (100 mg/ml). Use only fresh DMSO for reconstitution.
Storage Protect from light
+2°C to +8°C
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.