| Identification | Back Directory | [Name]
IKK Inhibitor III, BMS-345541 | [CAS]
445430-58-0 | [Synonyms]
CS-1910
BMS345541 (free base)
BMS-345541 (free base)
BMS 345541 (free base)
IKK Inhibitor III, BMS-345541
BMS345541;BMS 345541;IKK INHIBITOR III
IKK Inhibitor III, BMS-345541 USP/EP/BP
BMS-345541 free base
(BMS345541 (free base)
N-(1,8-Dimethylimidazo[1,2-a]quinoxalin-4-yl)-1,2-ethanediamine
N1-(1,8-Dimethylimidazo[1,2-a]quinoxalin-4-yl)ethane-1,2-diamine
N1-(1,8-Dimethylimidazo[1,2-a]quinoxalin-4-yl)-1,2-ethanediamine
1,2-Ethanediamine, N1-(1,8-dimethylimidazo[1,2-a]quinoxalin-4-yl)-
N-(1,8-Dimethylimidazo[1,2-a]quinoxalin-4-yl)-1,2-ethanediamine BMS345541 | [Molecular Formula]
C14H17N5 | [MDL Number]
MFCD18089812 | [MOL File]
445430-58-0.mol | [Molecular Weight]
255.318 |
| Chemical Properties | Back Directory | [Boiling point ]
449.5±45.0 °C(Predicted) | [density ]
1.32±0.1 g/cm3(Predicted) | [storage temp. ]
under inert gas (nitrogen or Argon) at 2–8 °C | [solubility ]
insoluble in H2O; ≥70 mg/mL in DMSO; ≥2.49 mg/mL in EtOH with gentle warming and ultrasonic | [form ]
Powder | [pka]
9.02±0.10(Predicted) | [color ]
White to off-white | [CAS DataBase Reference]
445430-58-0 |
| Hazard Information | Back Directory | [Characteristics]
Allosteric IKK inhibitors have anti-inflammatory activity. | [Uses]
BMS-345541 is a potent, selective, and allosteric site-binding inhibitor of IKK β (IKK-2) and shows 10 times greater selectivity over IKK α (IKK-1). BMS-345541 also inhibits cellular Iκβα phosphorylation and has some anti-inflammatory properties. | [Definition]
ChEBI: N'-(1,8-dimethyl-4-imidazo[1,2-a]quinoxalinyl)ethane-1,2-diamine is a quinoxaline derivative. | [Biological Activity]
BMS-345541 highly selectively inhibits the catalytic subunits of IKK-2 and IKK-1 with IC50s of 0.3 μM and 4 μM, respectively. | [in vitro]
BMS-34554 (5 μM) induces time-dependent dephosphorylation of IκBα and p65. Treatment of T-ALL cells with BMS-34554 resulted in nuclear translocation of FOXO3a, including control of the expression level of the p21CIP1 gene. In human umbilical vein endothelial cells, BMS-345541 inhibits TNFα-induced expression of ICAM-1 and VCAM-1 with IC50 of 5 μM. | [in vivo]
BMS-345541 (100 mg/kg) reduced the cumulative arthritis damage score from 4.4 to 0, along with low-grade degradation and inflammation of the tibiotarsal joint, synovial hyperplasia, bone resorption, and severity of cartilage erosion. There was no apparent damage to the joints of the animals, which was indistinguishable from the histological phenotype observed in those from age-matched, disease-free control animals. BMS-345541 dose-dependently inhibited IL-1β signaling, with animals in the 100 mg/kg dose group exhibiting levels consistent with disease-free control animals. | [target]
| Target | Value | IKK2
(Cell-free assay) | 0.3 μM | IKK1
(Cell-free assay) | 4 μM |
| [storage]
Store at -20°C |
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| Company Name: |
SPIRO PHARMA
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| Telephone: |
|
| Website: |
www.spiropharma.com.cn |
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