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) |