Product Information
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.

Related Products & Applications

Categories

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > NF-κB Activation > NF-κB Activation Inhibitors