Bay 65-1942 free base

Short Summary : IKKβ kinase inhibitor,ATP-competitive

Category : Immunology/Inflammation|IκB/IKK

Purity : 0.98

CAS Number : 600734-02-9

Formula : C22H25N3O4

Molecular Weight : 395.45

SMILE : O=C(C=CC=C/1OCC2CC2)C1=C(NC3=C4COC(N3)=O)/C=C4C5CCCNC5

Solubility : DMSO

Storage : Store at -20°C

Description : Bay 65-1942 free base is a selective inhibitor of IKKβ with IC50 value of 10 μM and Ki value of 2 nM [1] [2].IKKβ (inhibitor of nuclear factor kappa-B kinase subunit beta) is a subunit of IκB kinase which regulates the NF-κB activation and plays an important role in triggering immune responses [3]. Bay 65-1942 is a potent IKKβ inhibitor. When tested with MYL-R cells, administration of Bay 65-1942 reduced cell viability and induced cell apoptosis by decreasing IKKβ expression[1]. In human alveolar type II epithelium-like lung adenocarcinoma cell line A549, treatment of Bay 65-1942 inhibited IKKβ –dependent signal transduction and NF-κB activation by inhibiting IKKβ [2].In acute ischemia-reperfusion C57BL/6 mice model, administration of Bay 65-1942 significantly reduced left ventricular infarct size and preserved cardiac function and finally prevented cardiac injury following IR by inhibiting IKKβ[4].References: [1.]Cooper, M.J., et al., Application of multiplexed kinase inhibitor beads to study kinome adaptations in drug-resistant leukemia. PLoS One, 2013. 8(6): p. e66755.[2].Ziegelbauer, K., et al., A selective novel low-molecular-weight inhibitor of IkappaB kinase-beta (IKK-beta) prevents pulmonary inflammation and shows broad anti-inflammatory activity. Br J Pharmacol, 2005. 145(2): p. 178-92.[3].Harken, A.H., The world of inhibitory kappaB. Am J Physiol Heart Circ Physiol, 2007. 293(5): p. H2624-5.[4].Moss, N.C., et al., IKKbeta inhibition attenuates myocardial injury and dysfunction following acute ischemia-reperfusion injury. Am J Physiol Heart Circ Physiol, 2007. 293(4): p. H2248-53.

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