IκB/IKK

PDE inhibitor

A kinase inhibitor

IκB kinase inhibitor

IKK inhibitor

A selective inhibitor of NF-κB activation

BI-605906 is an inhibitor of inhibitor of kappa B kinase subunit β (IKKβ; IC50 = 380 nM).

BI605906 is a novel IKKβ inhibitor with an IC50 value of 380 nM when assayed at 0.1 mM ATP.

Ginsenoside CK, a secondary ginsenoside biotransformed from major ginsenosides, is more bioavailable and soluble than its parent ginsenosides and holds great significance.

Amlexanox (AA673), a tricyclic amine carboxylic acid with oral activity, can effectively inhibit TANK-binding kinase 1 (TBK1) (IC 50 = 0.8μM) and inhibitor-kappaB kinase epsilon (IKK-ɛ) (IC 50 = 5.8μM)

BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor, with IC50s of 9 nM and 72 nM, respectively.

IMD-0560 is a novel IκB kinase β inhibitor.

Ertiprotafib (PTP 112) is an inhibitor of PTP1B, IkB kinase β (IKK-β), and a dual PPARα and PPARβ agonist, with an IC50 of 1.6 μM for PTP1B, 400 nM for IKK-β, an EC50 of ~1 μM for PPARα/PPARβ.

INH14 is a cell permeable inhibitor of IKKα/IKKβ, with IC50s of 8.97 and 3.59 μM, respectively.

Bay 65-1942 free base is an ATP-competitive and selective IKKβ inhibitor.

Bay 65-1942 R form is the less active R-form of Bay 65-1942.

Chicanine is a lignan compound of Schisandra chinesis, inhibits LPS-induced phosphorylation of p38 MAPK, ERK 1/2 and IκB-α, with anti-inflammatory activity.

TBK1/IKKε-IN-1 is a dual TBK1 and IKKε inhibitor extracted from patent US20160376283 A1, Compound 274 in Example 60, has IC50s of <100 nM.

TBK1/IKKε-IN-5 (compound 1) is an orally active TBK1 and IKKε dual inhibitor, with IC50 values of 1 and 5.6 nM, respectively. TBK1/IKKε-IN-5 enhances the blockade response to PD-1 and induces immune memory in rats when combines with anti-PD-L1. TBK1/IKKε-IN-5 can be used in cancer research, especially in tumour immunity.

GS-143 is an inhibitor of IκBα ubiquitylation.

Potent TBK inhibitor

A dual inhibitor of TBK1 and IKKε

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.

HOIPIN-1 (JTP-0819958) is a selective linear ubiquitin chain assembly complex (LUBAC) inhibitor with an IC50 of 2.8 μM. HOIPIN-1 suppress LUBAC-mediated NF-kB activation in vitro.

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.