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401480 IKK 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).

IKK Inhibitor III, BMS-345541 - CAS 445430-58-0 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 4-(2ʹ-Aminoethyl)amino-1,8-dimethylimidazo[1,2-a]quinoxaline

Primary Target: IKK-2
401480
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Tabulka spec. kláve

CAS #Empirical Formula
445430-58-0C₁₄H₁₇N₅•2CF₃CO₂H

Products

Katalogové čísloBalení ks/bal.
401480-1MG Plastová ampulka 1 mg
Přidat k oblíbeným položkám
Description
OverviewA 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.
Catalogue Number401480
Brand Family Calbiochem®
Synonyms4-(2ʹ-Aminoethyl)amino-1,8-dimethylimidazo[1,2-a]quinoxaline
References
ReferencesTownsend, R.M., et al. 2004. Transplantation 77, 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.
Product Information
CAS number445430-58-0
ATP CompetitiveN
FormOff-white solid
FormulationSupplied as bis-TFA salt.
Hill FormulaC₁₄H₁₇N₅•2CF₃CO₂H
Chemical formulaC₁₄H₁₇N₅•2CF₃CO₂H
Hygroscopic Hygroscopic
ReversibleN
Structure formula ImageStructure formula Image
Quality LevelMQ100
Biological Information
Primary TargetIKK-2
Primary Target IC<sub>50</sub>~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 permeableY
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 InstructionsFollowing 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
Katalogové číslo GTIN
401480-1MG 04055977211955