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Home > Inhibitors & Agonists > NF-κB Pathway > IκB kinase (IKK)

BMS-345541

  Cat. No.:  DC8761   Featured
Chemical Structure
547757-23-3
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Field of application
BMS-345541 is a highly selective inhibitor of the catalytic subunits of IKK-2 and IKK-1 with IC50 of 0.3 μM and 4 μM, respectively.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 547757-23-3
Chemical Name: BMS-345541 HCl
Synonyms: BMS345541 hydrochloride; BMS-345541 hydrochloride; BMS 345541 hydrochloride
SMILES: Cl.NCCNC1=NC2C=CC(=CC=2N2C(=CN=C12)C)C
Formula: C14H18ClN5
M.Wt: 291.78
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.
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]. BMS-345541 (30 and 100 mg/kg, p.o.) is effective in blocking both clinical and histological endpoints of inflammation and injury in mice[3].
In Vitro: BMS-345541 inhibits IKK-2 and IKK-1 in dose-dependent manner. BMS-345541 fails to inhibit a panel of both serine/threonine and tyrosine kinases at concentrations as high as 100 μM. MS-345541 at concentrations as high as 100 μM fails to block both the anisomycin-stimulated phosphorylation of c-Jun and LPS-stimulated activation of MAPKAP K2 in THP-1 cells, as well as the EGF-stimulated phosphorylation of STAT3 in H292 cells[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].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC8761 BMS-345541 BMS-345541 is a highly selective inhibitor of the catalytic subunits of IKK-2 and IKK-1 with IC50 of 0.3 μM and 4 μM, respectively.
DC7759 WS6 WS6 is a β cell proliferation inducer via modulation of Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.
DC7760 WS3 WS3 is a novel small molecule that promotes β cell proliferation with EC50 of 28 nM(induced R7T1 proliferation).
DC8065 LY2409881 trihydrochloride LY2409881 is a novel inhibitor of IκB kinase β (IKK2).
DC8770 IMD-0354 IMD-0354 is a synthetic selective NF-kB inhibitor.
DC7802 IKK(epsilon)-IN-1 (IKKE-IN-1) IKKε-IN-1 is a potent IKKε inhibitor; inhibit the in-situ ΙKΚ ε-mediated phosphorylation of IRF3 with an IC50 value of less than about 100 nM.
DC9485 IKK-16(free base) IKK 16 is a selective IκB kinase (IKK) inhibitor for IKK-2, IKK complex and IKK-1 with IC50 of 40 nM, 70 nM and 200 nM, respectively.
DC7158 IKK-16 HCl IKK 16 is a selective IκB kinase (IKK) inhibitor for IKK-2, IKK complex and IKK-1 with IC50 of 40 nM, 70 nM and 200 nM, respectively.
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