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BMS-345541

Cat. No. M2462
BMS-345541 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
2mg USD 55  USD55 In stock
5mg USD 85  USD85 In stock
10mg USD 128  USD128 In stock
25mg USD 255  USD255 In stock
50mg USD 385  USD385 In stock
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Quality Control & Documentation
Biological Activity

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.

Customer Product Validations & Biological Datas
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
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Oliver Herrmann, et al. Nat Med. IKK mediates ischemia-induced neuronal death

[2] Xiaohua Zhu, et al. BMS‑345541 inhibits airway inflammation and epithelial‑mesenchymal transition in airway remodeling of asthmatic mice

[3] Venkata Lokesh Battula, et al. IKK inhibition by BMS-345541 suppresses breast tumorigenesis and metastases by targeting GD2+ cancer stem cells

[4] Lixian Wu, et al. BMS-345541 sensitizes MCF-7 breast cancer cells to ionizing radiation by selective inhibition of homologous recombinational repair of DNA double-strand breaks

[5] Jinming Yang, et al. BMS-345541 targets inhibitor of kappaB kinase and induces apoptosis in melanoma: involvement of nuclear factor kappaB and mitochondria pathways

[6] James R Burke, 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

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