(5-Phenyl-2-ureido)thiophene-3-carboxamide

Description

Inhibitor of NF-κB kinase 2 (IKK2, also known as IKKβ) acts as part of an IKK complex in the canonical NF-κB pathway, phosphorylating inhibitors of NF-κB (IκBs) to initiate signaling. NF-κB signaling can also occur through a non-canonical, IKK/IκB-independent pathway. IKK2 Inhibitor VI is a potent, cell-permeable, reversible inhibitor of IKK2 (IC₅₀ = 13 nM). It is used to evaluate the role of the canonical, IκB-dependent NF-κB signaling pathway in cellular responses.

Uses

(5-PHENYL-2-UREIDO)THIOPHENE-3-CARBOXAMIDE is an inhibitor of NF-κB kinase 2 (IKK2, also known as IKKβ) acts as part of an IKK complex in the canonical NF-κB pathway, phosphorylating inhibitors of NF-κB (IκBs) to initiate signaling. NF-κB signaling can also occur through a non-canonical, IKK/IκB-independent pathway. IKK2 Inhibitor VI is a potent, cell-permeable, reversible inhibitor of IKK2 (IC50 = 13 nM). It is used to evaluate the role of the canonical, IκB-dependent NF-κB signaling pathway in cellular responses.

Uses

An ureido-thiophenecarboxamide compound that acts as a potent inhibitor of IKK-2 (InhibitorVI).

IC 50

IKK-2: 25 nM (IC₅₀)

References

[1] ANDREW BAXTER  et al. et al. Hit-to-Lead Studies: The Discovery of Potent, Orally Active, Thiophenecarboxamide IKK-2 Inhibitors.[J]. ChemInform, 2004, 35 39. DOI: 10.1002/chin.200439220
[2] LUCY A MCNAMARA  Kathleen L C  Janani A Ganesh. Latent HIV-1 infection occurs in multiple subsets of hematopoietic progenitor cells and is reversed by NF-κB activation.[J]. Journal of Virology, 2012: 9337-9350. DOI: 10.1128/jvi.00895-12
[3] VASU PUNJ  Preet M C  Hittu Matta. A computational profiling of changes in gene expression and transcription factors induced by vFLIP K13 in primary effusion lymphoma.[J]. PLoS ONE, 2012: e37498. DOI: 10.1371/journal.pone.0037498