IKK Inhibitor III, BMS-345541

Bezeichnung:IKK Inhibitor III, BMS-345541

CAS-Nr445430-58-0

Englisch Name:IKK Inhibitor III, BMS-345541

CBNumberCB12618570

SummenformelC14H17N5

Molgewicht255.32

MOL-Datei445430-58-0.mol

IKK Inhibitor III, BMS-345541 physikalisch-chemischer Eigenschaften

Siedepunkt	449.5±45.0 °C(Predicted)
Dichte	1.32±0.1 g/cm3(Predicted)
storage temp.	under inert gas (nitrogen or Argon) at 2–8 °C
Löslichkeit	insoluble in H2O; ≥70 mg/mL in DMSO; ≥2.49 mg/mL in EtOH with gentle warming and ultrasonic
Aggregatzustand	Powder
pka	9.02±0.10(Predicted)
Farbe	White to off-white
CAS Datenbank	445430-58-0

Gefahreninformationscode (GHS)

IKK Inhibitor III, BMS-345541 Chemische Eigenschaften,Einsatz,Produktion Methoden

Charakteristisch
Allosteric IKK inhibitors have anti-inflammatory activity.
Verwenden
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.
Biologische Aktivität
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 p21^CIP1 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

IKK Inhibitor III, BMS-345541 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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Target	Value
IKK2 (Cell-free assay)	0.3 μM
IKK1 (Cell-free assay)	4 μM