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BMS-345541

Product #: TL0132
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l  General Information

Product Name

BMS-345541

General description

BMS-345541 is a highly selective inhibitor of the catalytic subunits of IKK-2 and IKK-1.

Synonym

N'-(1,8-dimethylimidazo[1,2-a]quinoxalin-4-yl)ethane-1,2-diamine; BMS345541

Purity

≥98%(HPLC)

CAS Number

445430-58-0

Formula

C14H17N5

Molecular Weight

255.325

Suitability

BioReagent, suitable for cell culture, etc.

l  Physical and Chemical Information

Appearance

White or Off-white solid

Solubility(25℃)

DMSO

~8mg/mL

Ethanol

Insoluble

Water

Insoluble

l  Biological Information

Biochem/Physiol   Actions

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.

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.

l  Packaging & Storage

Packaging

5mg; 25mg; 100mg

Storage temp.

0-5

l  Precautions and Disclaimer

This   product is for R&D use only, not for drug, household, or other uses.

l  References

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov

 


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