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. 2008 Oct 6;121(1):1–13. doi: 10.1016/j.pharmthera.2008.09.003

Table 2.

Available small molecule IKK-β inhibitors

Compound IC50, assay Reference
TPCA-1 0.17–0.32 μM, pro-inflammatory cytokine expression in monocytes (Podolin et al., 2005)
2-[(Aminocarbonyl)amino]-5-[4-fluorophenyl]-3-thiophenecarboxamide
PS-1145 Data not provided (Hideshima et al., 2002)
N-(6-chloro-9H-beta-carbolin-8-ly) nicotinamide
ML120B 3.3 μM TNF-α expression in PBMCs (Wen et al., 2006)
N-(6-chloro-7-methoxy-9H-beta-carbolin-8-yl)-2-methyl-nicotinamide
SC-514 8–20 μM pro-inflammatory cytokine expression in synovial fibroblasts (Kishore et al., 2003)
5-(Thien-3-yl)-3-aminothiophene-2-carboxamide
IMD-0354 Data not provided (Onai et al., 2004)
N-[3,5-bis-trifluoromethyl-phenyl]-5-chloro-2-hydroxy-benzamide
BMS-345541 4 μM IκB phosphorylation in THP-1 cells (Burke et al., 2003)
4(2′-aminoethyl)amino-1,8-dimethylimidazo(1,2-aquinoxaline)
BAY 11-7085 10 μM, adhesion molecule expression in HuVEC cells (Pierce et al., 1997)
3-[4-t-butylphenyl)-sulfonyl]-2-propenenitrile
AS602868 1–2 μM, NF-κB activation in Jurkat T cells (Frelin et al., 2003)