Table 1. EC50 values for agonists and antagonists tested on HEK293 cells.
Inhibitor | EC50 (NF-kB reporter) nM | IC50 (cell viability) nM | Putative mechanism of Inhibition | Reference |
---|---|---|---|---|
Ro106–9920 | <1 | >100,000 | LPS- and TNF-a induced IkBa ubiquitination | (Swinney et al., 2002) |
TCPA-1 | <1 | > 00,000 | IKKβ | (Birrell et al., 2005; Nan et al., 2014) |
IMD 0354 | 292 | 1,560 | IKKβ | (Podolin, 2004; Tanaka et al., 2005) |
PF-184 | 901 | 1,230 | IKKβ | (Sommers et al., 2009) |
Pictalisib | 4,266 | 7,470 | PI3Kα/δ | (Folkes et al., 2008; Junttila et al., 2009) |
BAY 11–7085 | 31,700 | >100,000 | IκB phosphorylation | (Koedel et al., 2000; Pierce et al., 1997) |
Cardamonin | 3,290 | 27,520 | IκB phosphorylation | (Lee et al., 2006) |
PSI | 10 | 373 | IκBα phosphorylation | (Traenckner et al., 1994) |
Celastrol | 82 | 475 | IκBα phosphorylation | (Sethi et al., 2007) |
Artemisinin | >100,000 | >100,000 | IκBα phosphorylation | (Wang et al., 2017) |
Luteolin | 35,000 | >100,000 | IκBα phosphorylation | (Kim and Jobin, 2005) |
IKK-16 | 852 | 1,510 | IKKα, IKKβ, IKK complex | (Waelchli et al., 2006) |
CID 2858522 | 8,590 | 6,420 | Protein Kinase C induced IKKβ | (Shi et al., 2010) |
BAY 11–7082 | 16,930 | 2,730 | IκBα phosphorylation | (Keller et al., 2000) |
Piceatannol | >100,000 | >100,000 | IκBα phosphorylation | (Ashikawa et al., 2002) |