A small molecule inhibitor of NEMO (IKKγ)-ubiquitin binding with EC50 of 9.3 uM, directly binds to NEMO with Kd of 2.14 uM.

AZD 3264 is an IkB-kinase IKK2 Inhibitor, IKK2 has been identified as one of the novel pathways to treat inflammatory conditions such as asthma, chronic pulmonary obstructive disorder (COPD) and rheumatoid arthritis.

BI605906 is a potent, specific IKKβ inhibitor with IC50 of 380 nM (0.1 mM ATP), does not suppress signaling downstream of mTOR or activate AMPK.

IKK 16 is a selective IκB kinase (IKK) inhibitor for IKK-2, IKK complex and IKK-1 with IC50 of 40 nM, 70 nM and 200 nM, respectively.

IKK 16 is a selective IκB kinase (IKK) inhibitor for IKK-2, IKK complex and IKK-1 with IC50 of 40 nM, 70 nM and 200 nM, respectively.

IKK-2 inhibitor VIII is a potent and selective IKK-2 inhibitor with IC50 of 8.5 nM.

IKKε-IN-1 is a potent IKKε inhibitor; inhibit the in-situ ΙKΚ ε-mediated phosphorylation of IRF3 with an IC50 value of less than about 100 nM.

IMD-0354 is a synthetic selective NF-kB inhibitor.

LY2409881 is a novel inhibitor of IκB kinase β (IKK2).

PS-1145 has been shown to be an IKK (IKB kinase) inhibitor.

TPCA-1 is potent, selective inhibitor of IKK-2 (IC50 = 17.9 nM) that displays>22-fold selectivity over IKK-1 and > 550-fold selectivity over other kinases and enzymes.

WS3 is a novel small molecule that promotes β cell proliferation with EC50 of 28 nM(induced R7T1 proliferation).

WS6 is a β cell proliferation inducer via modulation of Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.

BMS-345541 is a highly selective inhibitor of the catalytic subunits of IKK-2 and IKK-1 with IC50 of 0.3 μM and 4 μM, respectively.

BAY-985 is a highly potent, orally active and selective ATP-competitive dual inhibitor of TBK1 and IKKε with IC50s of 2/30 and 2 nM for TBK1 (low/high ATP) and IKKε, respectively. Antitumor efficacy.

(Rac)-BAY-985 (Compound Example 100.01) is a potent, ATP-competitive and selective TBK1 inhibitor with an IC50 of 1.5 nM. Antitumor efficacy.

HPN-01 is a potent and selective IKK inhibitor, with pIC50 values of 6.4, 7.0 and <4.8 for IKK-α, IKK-β and IKK-ε, respectively. HPN-01 displays greater 50-fold selectivity over a panel of more than 50 other kinases, including ALK5, CDK-2, EGFR, ErbB2, GSK3β, PLK1, Src, and VEGFR-2.

Malachite green oxalate is a triphenylmethane dye which can be used to detect the release of phosphate in enzymatic reactions. Malachite green oxalate is also a potent and selective inhibitor of IKBKE, and inhibits its downstream targets such as IκBα, p65 and IRF3. Malachite green oxalate exhibits antitumor activity in vitro and in vivo.

NF-κB-IN-1, a 4-arylidene crucumin analogue, is a potent NF-κB signaling pathway inhibitor. NF-κB-IN-1 directly inhibits IKK to block NF-κB activation. NF-κB-IN-1 effectively inhibits the viability of lung cancer cells and attenuates the clonogenic activity of A549 cells.

Siegesbeckialide I most potently inhibits LPS-induced NO production in RAW264.7 murine macrophages by directly binding to IKKα/β.

Glabrescone C possesses potent anti-inflammatory activity by directly bnding to IKKα/β.

AZ13102909 (AZ909) is a potent and selrctive TBK1 inhibitor with IC50 of 5 nM, 100-1000 fold greater for other related kinases.AZ909 combines with AZD6244 to enhance apoptosis in AZD6244-resistant lines in 3D culture.