SC-514 354812-17-2

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Molecular Weight:

224.3 SC-514 is an orally active, ATP-competitive IKK-2 inhibitor with IC50 of 3-12 μM, blocks NF-κB-dependent gene expression, does not inhibit other IKK isoforms or Other serine-threonine and tyrosine kinases.

Biological Activity

SC-514 inhibits the native IKK complex or recombinant human IKK-1/IKK-2
heterodimer and IKK-2 homodimer similarly. SC-514 inhibits transcription
of NF-κB-dependent IL-6, IL-8, and COX-2 genes in IL-1β-induced
rheumatoid arthritis-derived synovial fibroblasts (RASFs) with IC50s of
20, 20 and 8 μM.


100 μM SC-514 blocks the phosphorylation and
degradation of IκBα and also reduces the level of translocation of p65
into the nucleus in IL-1β-treated RASFs SC-514 does not inhibit the
phosphorylation and activation of the IKK complex.


SC-514 induces a
delay but not a complete blockade in IκBα phosphorylation and
degradation. SC-514 treatment cells shows a slightly slowed, decreased
import of p65 into the nucleus and a faster export of p65 from the
nucleus. SC-514 inhibits the phosphorylation of either IκBα or p65
similarly.


SC-514 is efficacious in an acute model of inflammation, namely
LPS-induced serum TNF-α production. SC-514 (50 mg/kg, i.p.) inhibits
TNF-αproduction in vivo by ~70%.

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Product Categories : NF-κB > IκB/IKK Inhibitor