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401480
Sigma-AldrichIKK Inhibitor III, BMS-345541 - CAS 445430-58-0 - Calbiochem
IKK Inhibitor III, BMS-345541, CAS 445430-58-0, is a cell-permeable, potent, selective, and allosteric site-binding inhibitor of IKK-2 (IC₅₀ = ~ 300 nM).
More>>IKK Inhibitor III, BMS-345541, CAS 445430-58-0, is a cell-permeable, potent, selective, and allosteric site-binding inhibitor of IKK-2 (IC₅₀ = ~ 300 nM). Less<<
MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.
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Description
Overview
A cell-permeable quinoxaline compound that displays anti-inflammatory properties. Acts as a potent, selective, and allosteric site-binding inhibitor of IKK-2 (IC50 = ~ 300 nM). Exhibits ~10-fold greater selectivity over IKK-1 (IC50 = ~ 4 µM) and no activity towards IKKε and a panel of more than 15 unrelated protein kinases even at concentrations as high as 100 µM. Inhibits cellular IκBα phosphorylation (IC50 = 4 µM in THP-1 cells) and LPS-induced cytokine production both in vitro (IC50 = 1-5 µM in THP-1 cells) and in vivo (IC50 = 10 mg/kg in mice). Effectively blocks inflammation and joint destruction in a murine arthritis model.
Townsend, R.M., et al. 2004. Transplantation77, 1090. MacMaster, J.F., et al. 2003. Inflamm. Res.52, 508. McIntyre, K.W., et al. 2003. Arthritis Rheum.48, 2652. Burke, J. R., et al. 2003. J. Biol. Chem.278, 1450.
~300 nM against IKK-2; 4 µM against cellular IκBα phosphorylation in THP-1 cells; 1-5 µM LPS-induced cytokine production in THP-1 cells
Purity
≥96% by HPLC
Physicochemical Information
Cell permeable
Y
Storage and Shipping Information
Ship Code
Ambient Temperature Only
Toxicity
Standard Handling
Storage
+2°C to +8°C
Protect from Light
Protect from light
Hygroscopic
Hygroscopic
Do not freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas
Packaged under inert gas
Global Trade Item Number
Catalogue Number
GTIN
401480-1MGCN
04055977211955
Documentation
IKK Inhibitor III, BMS-345541 - CAS 445430-58-0 - Calbiochem Certificates of Analysis
Title
Lot Number
401480
References
Reference overview
Townsend, R.M., et al. 2004. Transplantation77, 1090. MacMaster, J.F., et al. 2003. Inflamm. Res.52, 508. McIntyre, K.W., et al. 2003. Arthritis Rheum.48, 2652. Burke, J. R., et al. 2003. J. Biol. Chem.278, 1450.
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.
A cell-permeable, potent, selective, and allosteric site-binding inhibitor of IKK-2 (IC50 ~300 nM) that displays anti-inflammatory properties. Exhibits ~10-fold greater selectivity for IKK-2 over IKK-1 (IC50 ~4.0 µM) and does not inhibit IKKε and a panel of more than 15 unrelated protein kinases even at concentrations as high as 100 µM. Inhibits cellular IκBα phosphorylation (IC50 = 4 µM in THP-1 cells) and LPS-induced cytokine production both in vitro (IC50 = 1-5 µM in THP-1 cells) and in vivo (IC50 = 10 mg/kg in mice). Effectively blocks inflammation and joint destruction in a murine arthritis model.
Form
Off-white solid
Formulation
Supplied as bis-TFA salt.
Intert gas (Yes/No)
Packaged under inert gas
CAS number
445430-58-0
Chemical formula
C₁₄H₁₇N₅•2CF₃CO₂H
Structure formula
Purity
≥96% by HPLC
Solubility
DMSO (5 mg/ml)
Storage
Protect from light +2°C to +8°C Hygroscopic
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity
Standard Handling
References
Townsend, R.M., et al. 2004. Transplantation77, 1090. MacMaster, J.F., et al. 2003. Inflamm. Res.52, 508. McIntyre, K.W., et al. 2003. Arthritis Rheum.48, 2652. Burke, J. R., et al. 2003. J. Biol. Chem.278, 1450.
