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HomeProduct name listIKK Inhibitor III, BMS-345541

IKK Inhibitor III, BMS-345541

Synonym(s):4-(2ʹ-Aminoethyl)amino-1,8-dimethylimidazo[1,2-a]quinoxaline;IKK Inhibitor III, BMS-345541 - CAS 445430-58-0 - Calbiochem

IKK Inhibitor III, BMS-345541 Structural

What is IKK Inhibitor III, BMS-345541?

Characteristics

Allosteric IKK inhibitors have anti-inflammatory activity.

The Uses of IKK Inhibitor III, BMS-345541

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.

What are the applications of Application

BMS-345541 is a cell-permeable quinoxaline agent and a potent, selective, and allosteric site-binding inhibitor of IKK β

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.

Properties of IKK Inhibitor III, BMS-345541

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

Safety information for IKK Inhibitor III, BMS-345541

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H227:Flammable liquids
Precautionary Statement Codes P210:Keep away from heat/sparks/open flames/hot surfaces. — No smoking.
P280:Wear protective gloves/protective clothing/eye protection/face protection.
P370+P378:In case of fire: Use … for extinction.
P403+P235:Store in a well-ventilated place. Keep cool.

Computed Descriptors for IKK Inhibitor III, BMS-345541

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