1. NF-κB
  2. IKK
  3. BMS-345541

BMS-345541 

Cat. No.: HY-10519 Purity: 99.17%
Handling Instructions

BMS-345541 is a selective inhibitor of the catalytic subunits of IKK (IKK-2 IC50=0.3 μM, IKK-1 IC50=4 μM). BMS-345541 binds at an allosteric site of IKK.

For research use only. We do not sell to patients.

BMS-345541 Chemical Structure

BMS-345541 Chemical Structure

CAS No. : 445430-58-0

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1  mL in DMSO USD 134 In-stock
Estimated Time of Arrival: December 31
5 mg USD 122 In-stock
Estimated Time of Arrival: December 31
50 mg USD 768 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 9 publication(s) in Google Scholar

Other Forms of BMS-345541:

Top Publications Citing Use of Products

    BMS-345541 purchased from MCE. Usage Cited in: Biomed Pharmacother. 2020 May.

    Relative NFκB, p-NFκB, p-IKBα and t-IKBα protein levels in spheres in the control, TNFα, TNFα + BMS-345541 and TNFα + resveratrol groups.

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    • Biological Activity

    • Protocol

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    • References

    • Customer Review

    Description

    BMS-345541 is a selective inhibitor of the catalytic subunits of IKK (IKK-2 IC50=0.3 μM, IKK-1 IC50=4 μM). BMS-345541 binds at an allosteric site of IKK.

    IC50 & Target[1]

    IKK-2

    0.3 μM (IC50)

    IKK-1

    4 μM (IC50)

    In Vitro

    BMS-345541 selectively inhibits the stimulated phosphorylation of IκBα in cells (IC50=4 μM). Consistent with the role of IKK/NF-κB in the regulation of cytokine transcription, BMS-345541 inhibits lipopolysaccharide-stimulated tumor necrosis factor α, interleukin-1β, interleukin-8, and interleukin-6 in THP-1 cells with IC50 values in the 1 to 5 μM range[1]. BMS-345541 treatment results in a concentration-dependent inhibition of melanoma cell proliferation in SK-MEL-5, A375, and Hs 294T cells. BMS-345541 (0, 100 μM) shows apoptotic features as revealed by TUNEL staining and nuclear condensation[2].

    In Vivo

    BMS-345541 (10 mg/kg, p.o.) results in prolonged serum drug levels, with concentrations sustained at or above 1 μM for many hours in mice. BMS-345541 dose-dependently inhibits the production of TNFα measured in the serum of animals challenged with an intraperitoneal administration of LPS[1]. BMS-345541 (0, 10, 25, and 75 mg/kg, p.o.) effectively inhibits SK-MEL-5 tumor growth in a dose-dependent manner in the mice. Tumor-bearing mice treated with 75 mg/kg of BMS-345541 show effective inhibition of growth of SK-MEL-5, A375, and Hs 294T tumors by 86±2.8%, 69±11% and 67±3.4%, respectively[2].

    Molecular Weight

    255.32

    Formula

    C₁₄H₁₇N₅

    CAS No.

    445430-58-0

    SMILES

    CC1=CN=C2C(NCCN)=NC3=CC=C(C)C=C3N21

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 10 mg/mL (39.17 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.9167 mL 19.5833 mL 39.1665 mL
    5 mM 0.7833 mL 3.9167 mL 7.8333 mL
    10 mM 0.3917 mL 1.9583 mL 3.9167 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 1 mg/mL (3.92 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 1 mg/mL (3.92 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 1 mg/mL (3.92 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Kinase Assay
    [1]

    Assays measuring the enzyme-catalyzed phosphorylation of GST-IκBα are performed by adding enzyme (IKK-2, IKK-1, or IKK-ε, typically to a final concentration of 0.5 μg/mL) at 30°C to solutions of 100 μg/mL GST-IκBα and 5 μM [33P]ATP in 40 mM Tris-HCl, pH 7.5, containing 4 mM MgCl2, 34 mM sodium phosphate, 3 mM NaCl, 0.6 mM potassium phosphate, 1 mM KCl, 1 mM dithiothreitol, 3% (w/v) glycerol, and 250 μg/mL bovine serum albumin. The specific activity of [33P]ATP used in the assay is 100 Ci/mmol. After 5 min, the kinase reactions are stopped by the addition of 2× LaemmLi sample buffer and heat-treated at 90°C for 1 min. The samples are then loaded on to NuPAGE 10% BisTris gels. After completion of SDS-PAGE, gels are dried on a slab gel dryer. The bands are then detected using a 445Si PhosphorImager, and the radioactivity is quantified using ImageQuant software. Under these conditions, the degree of phosphorylation of GST-IκBα is linear with time and concentration of enzyme[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [2]

    SK-MEL-5 cells are treated with BMS-345541 at different concentrations (0, 1.0, 10, and 100 μM) for different time periods. The cells are collected by trypsinization, fixed in 70% ethanol for 2 hours on ice and stained with PI solution (PBS containing 2 μg/mL PI, 0.1% Triton X-100, and 125 units/mL RNase A) at 37°C for 30 minutes. Cell fluorescence is measured by flow cytometry with 488 nm excitation and 620 nm emission filters and resulting data are analyzed using the software program MultiCycle[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    Mice[1]
    BMS-345541 is administered either by intravenous tail vein injection or by peroral gavage to groups of three 18-22 g female BALB/c mice. BMS-345541 is formulated as a 2 mg/mL solution in 3% Tween 80, water. Mice receive either a 2 mg/kg (1 mL/kg) intravenous bolus or a 10 mg/kg (5 mL/kg) peroral gavage. Whole blood samples are taken from individual mice by orbital bleed and cardiac puncture at 0, 0.05, 0.25, 0.5, 1.0, 3.0, 6.0, and 8.0 h after dosing. Whole blood is centrifuged at 20×103×g for 5 min. Serum is stored at -20°C until analysis.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
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    Keywords:

    BMS-345541BMS345541BMS 345541IKKIκB kinaseI kappa B kinaseInhibitorinhibitorinhibit

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    Cat. No.:
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