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BMS-345541(free base)

Catalog No.
B4655
IKK-1/IKK-2 inhibitor,potent and selective
Grouped product items
SizePriceStock Qty
5mg
$105.00
In stock
10mg
$160.00
In stock
50mg
$470.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

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Background

BMS-345541 (free base; CAS 445430-58-0) is a selective inhibitor of IκB kinases IKK-1 and IKK-2, central enzymes involved in cytokine-induced NF-κB signaling. It inhibits IKK-1 and IKK-2 with reported IC50 values of approximately 4 μM and 0.3 μM, respectively. In cell-based assays utilizing THP-1 monocytes, pretreatment with BMS-345541 decreases cytokine-induced phosphorylation of IKK and suppresses production of inflammatory cytokines, including TNF-α, IL-1β, IL-6, and IL-8. Additionally, in glioma and melanoma cell lines, this compound reduces proliferation and induces apoptotic cell death. BMS-345541 serves as a relevant pharmacological tool for studying IKK-NF-κB pathway modulation and disease mechanisms involving inflammation or apoptosis.

Product Citation

Chemical Properties

StorageStore at -20°C
M.Wt255.32
Cas No.445430-58-0
FormulaC14H17N5
Solubilityinsoluble in H2O; ≥70 mg/mL in DMSO; ≥2.49 mg/mL in EtOH with gentle warming and ultrasonic
Chemical NameN1-(1,8-dimethylimidazo[1,2-a]quinoxalin-4-yl)ethane-1,2-diamine
SDFDownload SDF
Canonical SMILESNCCNC1=NC2=CC=C(C)C=C2N3C1=NC=C3C
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment [1]:

Cell lines

THP-1 cells

Preparation method

The solubility of this compound in DMSO is >70mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

1-100μM for 1 h

Applications

In THP-1 cells, only the stimulus-induced phosphorylation of IκB was inhibited by BMS-345541 whereas other signal transduction cascades were unaffected. BMS-345541 inhibited IKK (Iκ B kinase) in cells in the micromolar range and was effective in THP-1 cells at inhibiting the stimulated production of a number of cytokines from THP-1 cells including TNF, IL-1, IL-8, and IL-6.

Animal experiment [2]:

Animal models

18–22-g female BALB/c mice

Dosage form

2mg/kg (1 ml/kg) intravenous bolus or 10 mg/kg (5 ml/kg) peroral gavage.

Application

In BALB/c mice, BMS-345541 dose-dependently inhibited LPS (intraperitoneal)-induced serum TNF production in mice at doses in the 3 to 100 mg/kg range. Approximately 50% inhibition was observed at 10 mg/kg, near complete inhibition of serum TNF was observed at a dose of 100 mg/kg BMS-345541.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Burke, J.R., et al. 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, 2003. 278(3): p. 1450-6.

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