IKK-16

IKK-16 is a potent and selective small molecule inhibitor of IκB kinase (IKK), with IC50 values of 40 nM for IKKβ, 70 nM for IKK complex, and 200 nM for IKKα[1][2][4][7][14][15][16][18]. It inhibits TNF-α-stimulated IκB degradation and the expression of adhesion molecules (E-selectin, ICAM, VCAM), as well as LPS-induced TNF-α release in vivo and neutrophil extravasation in inflammatory models[1][2][7]. IKK-16 has shown efficacy in reducing multiple organ dysfunction in mouse sepsis models, protecting against cardiac, renal, hepatic, and lung injury likely through inhibition of NF-κB activity and subsequent iNOS suppression[6][8][10]. Additionally, IKK-16 has demonstrated an ability to enhance responses to kinase inhibitors in cancer cell lines, further inhibiting NF-κB/RELA target genes, reducing cell viability, and modulating signaling pathways including mTOR and GSK3β[4]. IKK-16 is mainly used as a tool compound in preclinical research and is not approved for clinical use.

Brand names

IKK-16IKK16IKK 16

Other names

IKK 16IKK16IKK-16IKK 16 hydrochlorideIKK16 hydrochlorideIKK-16 hydrochlorideIKK-16 HClIKK16 HClIKK 16 HClN-(4-Pyrrolidin-1-yl-piperidin-1-yl)-[4-(4-benzo[b]thiophen-2-yl-pyrimidin-2-ylamino)phenyl]carboxamide hydrochloride