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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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B126876-5mg | 5mg | In stock | $97.90 | |
B126876-10mg | 10mg | In stock | $157.90 | |
B126876-25mg | 25mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $355.90 | |
B126876-50mg | 50mg | In stock | $473.90 | |
B126876-100mg | 100mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $706.90 |
Selective allosteric inhibitor of IKK; anti-inflammatory
Synonyms | 4-methoxyphenyl methylbromide | N1-(1,8-Dimethylimidazo[1,2-a]quinoxalin-4-yl)-1,2-ethanediamine hydrochloride | N1-{1,8-DIMETHYLIMIDAZO[1,2-A]QUINOXALIN-4-YL}ETHANE-1,2-DIAMINE HYDROCHLORIDE | BMS-345541 hydrochloride | BMS-345541, >=98% (HPLC), powder | |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | Selective allosteric inhibitor of IKK (IC50values are 0.3 and 4.0μM for IKKβand IKKαrespectively). Exhibits no effect against a panel of 15 other kinases. Attenuates LPS-induced cytokine productionin vitroand blocks NFκB dependent transcription in mice. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | ALLOSTERIC MODULATOR |
Mechanism of action | Allosteric modulator of component of inhibitor of nuclear factor kappa B kinase complex;Allosteric modulator of inhibitor of nuclear factor kappa B kinase subunit beta |
Product Description | BMS-345541 has been used:
as an IκB kinase (IKK) complex inhibitor to study its effects on the interferon-γ (IFN-γ) production by natural killer (NK) cells
as an IKK inhibitor to study its effects on the expression of eotaxin and monocyte chemoattractant protein-1 (MCP-1) mRNA in gingival fibroblasts
as nuclear factor κB (NF-κB) pathway inhibitor to study its effects on tumor necrosis factor α (TNFα) production in human oral squamous carcinoma cells |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | N'-(1,8-dimethylimidazo[1,2-a]quinoxalin-4-yl)ethane-1,2-diamine;hydrochloride |
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INCHI | InChI=1S/C14H17N5.ClH/c1-9-3-4-11-12(7-9)19-10(2)8-17-14(19)13(18-11)16-6-5-15;/h3-4,7-8H,5-6,15H2,1-2H3,(H,16,18);1H |
InChi Key | MIDKPVLYXNLFGZ-UHFFFAOYSA-N |
Canonical SMILES | CC1=CC2=C(C=C1)N=C(C3=NC=C(N23)C)NCCN.Cl |
Isomeric SMILES | CC1=CC2=C(C=C1)N=C(C3=NC=C(N23)C)NCCN.Cl |
PubChem CID | 9926054 |
Molecular Weight | 291.78 |
CAS Registry No. | 547757-23-3 |
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Wikipedia | BMS-345541 |
DiscoveRx TREEspot | BMS-345541| |
PubChem CID | 9813758 |
ChEMBL Ligand | CHEMBL249697 |
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Solubility | Solvent:water, Max Conc. mg/mL: 29.18, Max Conc. mM: 100; Solvent:DMSO, Max Conc. mg/mL: 29.18, Max Conc. mM: 100 |
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Pictogram(s) | GHS07 |
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Hazard Statements | H315:Causes skin irritation H319:Causes serious eye irritation H335:May cause respiratory irritation |
Precautionary Statements | P261:Avoid breathing dust/fume/gas/mist/vapors/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing. |
1. Burke JR, Pattoli MA, Gregor KR, Brassil PJ, MacMaster JF, McIntyre KW, Yang X, Iotzova VS, Clarke W, Strnad J et al.. (2003) BMS-345541 is a highly selective inhibitor of I kappa B kinase that binds at an allosteric site of the enzyme and blocks NF-kappa B-dependent transcription in mice.. J Biol Chem, 278 (3): (1450-6). [PMID:12403772] [10.1021/op500134e] |