Brief Description

LY2409881 is a novel selective inhibitor of IKK2 with IC50 of 30 nM; IC50 for IKK1 and other common kinases is at least one log higher.
IC50 value: 30 nM
Target: IKK2 inhibitor
in vitro: LY2409881 inhibited constitutively activated NF-κB, and caused concentration- and time-dependent growth inhibition and apoptosis in lymphoma cells. Pretreatment of LY10 with 10 umol/L of LY2409881 prevented the formation of phosphorylated IkB in samples treated with TNFa for 2, 20, and 60 minutes in the presence of abundant IkB protein.
in vivo: LY2409881 was safe to mice at three dose levels, 50, 100, and 200 mg/kg, all of which caused significant inhibition of tumor growth. LY2409881 suppressed the activity of the NF-κB subunit p65 in lymphoma cells treated by the HDAC inhibitor romidepsin, underlying a potential mechanism of the marked synergy observed of these two drugs.

Solubility

DMSO

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Storage conditions

Store at -20°C 2 years

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