Description
SC-514 is an orally active, ATP-competitive inhibitor of IKK-2 with an IC50 value of 3-12 μM.
Product Overview
SC-514 is a cell-permeable and selective inhibitor of IKK-2 with IC50 value of 3-12μM. SC-514 inhibits all forms of recombinant human IKK-2 with IC50 values in the 3-12μM range. It also inhibits the native IKK complex. SC-514 specifically binds at the ATP-binding site of IKK-2 and exerts a reversible and competitive inhibition with ATP. However, SC-514 shows non-competitive inhibition with the IκB site. As an inhibitor of IKK-2, SC-514 is found to block the phosphorylation and degradation of IκBα and reduce the translocation level of p65 into the nucleus in IL-1β-treated RASFs. Additionally, SC-514 shows dose-dependent inhibition in the transcription of NF-κB-induced genes, including IL-6, IL-8, and COX-2.Moreover, SC-514 shows efficacious in reduction of LPS-induced TNFα production in the acute model of inflammation. SC-514 is also reported to inhibit the osteoclastogenesis in BMM cells through attenuating RANKL-induced activation of NF-κB.
Targets
IKK-2; CDK2/CyclinA; AUR2; PRAK; p38α
IC50
3-12 μM; 61 μM; 71 μM; 75 μM; >100 μM
Molecular Formula
C9H8N2OS2
Chemical Name
3-amino-5-thiophen-3-ylthiophene-2-carboxamide
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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