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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).

FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

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

Primary Target: IKK-2
401480
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Aperçu

Replacement Information

Tableau de caractéristiques principal

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

Products

RéférenceConditionnement Qté
401480-1MG Ampoule plast. 1 mg
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
Applications
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
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
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
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Référence GTIN
401480-1MG 04055977211955

Documentation

IKK Inhibitor III, BMS-345541 - CAS 445430-58-0 - Calbiochem FDS

Titre

Fiche de données de sécurité des matériaux (FDS) 

IKK Inhibitor III, BMS-345541 - CAS 445430-58-0 - Calbiochem Certificats d'analyse

TitreNuméro de lot
401480

Références bibliographiques

Aperçu de la référence bibliographique
Townsend, 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.
Fiche technique

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-April-2011 RFH
Synonyms4-(2ʹ-Aminoethyl)amino-1,8-dimethylimidazo[1,2-a]quinoxaline
DescriptionA 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.
FormOff-white solid
FormulationSupplied as bis-TFA salt.
Intert gas (Yes/No) Packaged under inert gas
CAS number445430-58-0
Chemical formulaC₁₄H₁₇N₅•2CF₃CO₂H
Structure formulaStructure formula
Purity≥96% by HPLC
SolubilityDMSO (5 mg/ml)
Storage Protect from light
+2°C to +8°C
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.
Toxicity Standard Handling
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.