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. Author manuscript; available in PMC: 2022 Feb 24.
Published in final edited form as: Eur J Pharmacol. 2020 Jan 31;873:172981. doi: 10.1016/j.ejphar.2020.172981

Table 1. EC50 values for agonists and antagonists tested on HEK293 cells.

For NF-κB reporter luciferase activity, values <1nM indicate that NF-κB expression was less than 50% expression of untreated control cells even at the lowest concentration of inhibitor, while values >100,000nM indicate no decrease in luciferase expression was observed at the highest concentration of inhibitor. For cell viability, >100,000nM indicates that 50% cell death was not observed even at the highest concentration of inhibitor.

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)