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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. 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. BMS-345541 treatment results in a concentration-dependent inhibition of melanoma cell proliferation in SK-MEL-5, A375, and Hs 294T cells.
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Source | Eye Vis (Lond) (2017). Figure 1. BMS-345541 |
| Method | SEAP assay | |
| Cell Lines | HCET cells | |
| Concentrations | - | |
| Incubation Time | 24 h | |
| Results | SEAP assay showed that both Wedelolactone and BMS-345541 could significantly inhibit Pam3CSK4-induced NF-κB activity |
| Molecular Weight | 255.32 |
| Formula | C14H17N5 |
| CAS Number | 445430-58-0 |
| Solubility (25°C) | DMSO 9 mg/mL Water 4 mg/mL (ultrasonic and warming) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[5] Oliver Herrmann, et al. Nat Med. IKK mediates ischemia-induced neuronal death
| Related IκB/IKK Products |
|---|
| BAY 11-7082
BAY 11-7082 is an inhibitor of cytokine-induced IκB-α phosphorylation (IC50 ~ 10 μM). BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC50=0.19, 0.96 μM, respectively). |
| SC-514
SC-514 is a selective and reversible inhibitor of IκB kinase 2 (IKK2) with IC50 of 3-12 μM. |
| TPCA-1
TPCA-1 is an inhibitor of IKK-2 with IC50 of 17.9 nM. |
| BMS-345541 hydrochloride
BMS-345541 hydrochloride is a selective inhibitor of the catalytic subunits of IKK (IC50 values of 0.3 μM and 4 μM for IKK-2 and IKK-1 respectively). BMS-345541 binds at an allosteric site of IKK. |
| Bardoxolone Methyl
Bardoxolone Methyl is an IKK inhibitor with potent pro-apoptotic and anti-inflammatory activities, as well as an activator of the Nrf2 pathway and an inhibitor of the NF-κB pathway. |
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