BMS-345541 hydrochloride is an anti-inflammatory, cell-permeable quinoxaline compound with a highly selective IKKbeta inhibitory activity. BMS-345541 blocks both joint inflammation and destruction in collagen-induced arthritis in mice. BMS-345541 hydrochloride induced apoptosis and an accumulation of cells in the G 2/M phase of the cell cycle via inhibition of IKK/NFκB signaling. T-ALL cells treated with BMS-345541 displayed nuclear translocation of FOXO3a and restoration of its functions, including control of p21(Cip1) expression levels. BMS-345541 hydrochloride is an allosteric site-binding inhibitor with a primary target of IKK-2 and blocks the NF-κB-dependent transcription in mice.
| Molecular Weight | 291.78 |
| Formula | C14H17N5.HCl |
| CAS Number | 547757-23-3 |
| Solubility (25°C) | Water ≥ 30 mg/mL DMSO 15 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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.
[3] Oliver Herrmann, et al. Nat Med. IKK mediates ischemia-induced neuronal death
| Related IκB/IKK Products |
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| BMS-066
BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor, with IC50s of 9 nM and 72 nM, respectively. |
| Ainsliadimer A
Ainsliadimer A is a novel guaiacolide sesquiterpene dimer isolated from Ainsliaea macrocephala.Ainsliadimer A can block the NF-κB signaling pathway by binding to IKK α/β, and possesses anti-tumor and anti-inflammatory activities.Meanwhile, Ainsliadimer A can also Ainsliadimer A can also directly target peroxidase 1 and 2 (PRDX1 and PRDX2) and significantly inhibit their enzymatic activities. In addition, Ainsliadimer A can cause mitochondrial dysfunction by altering the permeability of mitochondrial membrane potential, inhibiting mitochondrial respiration and ATP production, inhibiting cell proliferation, promoting cell cycle arrest in G2/M phase, and inducing apoptosis. |
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| MRT67307 dihydrochloride
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| 4′-Hydroxywogonin
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