A selective inhibitor of IKKα and IKKβ
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BMS 345541 (hydrochloride)

Item No. 16667

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N1-(1,8-dimethylimidazo[1,2-a]quinoxalin-4-yl)-1,2-ethanediamine, monohydrochloride
CAS Number
547757-23-3
Synonyms
  • IKK Inhibitor III
Molecular Formula
C14H17N5 • HCl
Formula Weight
291.8
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
PBS (pH 7.2): 10 mg/ml
λmax
211, 226, 241, 261, 271, 291, 303, 316, 330 nm
SMILES
CC1=CN=C2N1C3=C(C=CC(C)=C3)N=C2NCCN.Cl
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

    $190

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    10 mg

    $306

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    25 mg

    $587

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    Product Description

    BMS 345541 is a cell permeable inhibitor of the IκB kinases IKKα and IKKβ (IC50s = 4 and 0.3 µM).1 It is without effect against a panel of other serine/threonine and tyrosine kinases at 100 µM.1 BMS 345541 inhibits signaling through nuclear factor-κB (NF-κB) both in cells and in vivo, showing excellent pharmacokinetics in mice.1 It blocks joint inflammation and damage in collagen-induced arthritis in mice and induces apoptosis in melanoma cells both in vitro and in vivo.2,3 BMS 345541 is used to explore novel roles for IKK phosphorylation and NF-κB signaling.4,5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Burke, J.R., Pattoli, M.A., Gregor, K.R., et al. BMS-345541 is a highly selective inhibitor of IκB kinase that binds at an allosteric site of the enzyme and blocks NF-κB-dependent transcription in mice. The Journal of Biological Chemisty 278(3), 1450-1456 (2003).

    2. McIntyre, K.W., Shuster, D.J., Gillooly, K.M., et al. A highly selective inhibitor of IκB kinase, BMS-345541, blocks both joint inflammation and destruction in collagen-induced arthritis in mice. Arthritis Rheum. 48(9), 2652-2659 (2003).

    3. Yang, J., Amiri, K.I., Burke, J.R., et al. BMS-345541 targets inhibitor of κB kinase and induces apoptosis in melanoma: Involvement of nuclear factor κB and mitochondria pathways. Clin. Cancer Res. 12(3 Pt 1), 950-960 (2006).

    4. Karim, Z.A., Zhang, J., Bangerjee, M., et al. IκB kinase phosphorylation of SNAP-23 controls platelet secretion. Blood 121(22), 4567-4574 (2013).

    5. Wen, L., Zhu, M., Madigan, M.C., et al. Immunomodulatory effects of bone marrow-derived mesenchymal stem cells on pro-inflammatory cytokine-stimulated human corneal epithelial cells. PLoS One 9(7), 1-12 (2014).

    Product Citations

    Yang, W., Yu, Z., Chiyoya, M., et al. Menaquinone-4 accelerates calcification of human aortic valve interstitial cells in high-phosphate medium through PXR. J. Pharm. Exp. Ther. 372, 277-284 (2020).