BMS-345541(free base)
BMS-345541 (free base; CAS 445430-58-0) is a selective inhibitor of IκB kinases IKK-1 and IKK-2, central enzymes involved in cytokine-induced NF-κB signaling. It inhibits IKK-1 and IKK-2 with reported IC50 values of approximately 4 μM and 0.3 μM, respectively. In cell-based assays utilizing THP-1 monocytes, pretreatment with BMS-345541 decreases cytokine-induced phosphorylation of IKK and suppresses production of inflammatory cytokines, including TNF-α, IL-1β, IL-6, and IL-8. Additionally, in glioma and melanoma cell lines, this compound reduces proliferation and induces apoptotic cell death. BMS-345541 serves as a relevant pharmacological tool for studying IKK-NF-κB pathway modulation and disease mechanisms involving inflammation or apoptosis.
- 1. Jingchun Du, Yougui Xiang, et al. "RIPK1 dephosphorylation and kinase activation by PPP1R3G/PP1γ promote apoptosis and necroptosis." Nat Commun. 2021 Dec 3;12(1):7067. PMID: 34862394
- 2. Shu min Lv, Hongwen Cai, et al. "Thymosin‑β 4 induces angiogenesis in critical limb ischemia mice via regulating Notch/NF‑κB pathway." Int J Mol Med. 2020 Oct;46(4):1347-1358. PMID: 32945357
| Storage | Store at -20°C |
| M.Wt | 255.32 |
| Cas No. | 445430-58-0 |
| Formula | C14H17N5 |
| Solubility | insoluble in H2O; ≥70 mg/mL in DMSO; ≥2.49 mg/mL in EtOH with gentle warming and ultrasonic |
| Chemical Name | N1-(1,8-dimethylimidazo[1,2-a]quinoxalin-4-yl)ethane-1,2-diamine |
| SDF | Download SDF |
| Canonical SMILES | NCCNC1=NC2=CC=C(C)C=C2N3C1=NC=C3C |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
THP-1 cells |
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Preparation method |
The solubility of this compound in DMSO is >70mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
1-100μM for 1 h |
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Applications |
In THP-1 cells, only the stimulus-induced phosphorylation of IκB was inhibited by BMS-345541 whereas other signal transduction cascades were unaffected. BMS-345541 inhibited IKK (Iκ B kinase) in cells in the micromolar range and was effective in THP-1 cells at inhibiting the stimulated production of a number of cytokines from THP-1 cells including TNF, IL-1, IL-8, and IL-6. |
| Animal experiment [2]: | |
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Animal models |
18–22-g female BALB/c mice |
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Dosage form |
2mg/kg (1 ml/kg) intravenous bolus or 10 mg/kg (5 ml/kg) peroral gavage. |
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Application |
In BALB/c mice, BMS-345541 dose-dependently inhibited LPS (intraperitoneal)-induced serum TNF production in mice at doses in the 3 to 100 mg/kg range. Approximately 50% inhibition was observed at 10 mg/kg, near complete inhibition of serum TNF was observed at a dose of 100 mg/kg BMS-345541. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Burke, J.R., 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. J Biol Chem, 2003. 278(3): p. 1450-6. |
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Quality Control & MSDS
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