Signaling Pathway

IKK

IKK

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The IκB kinase (IKK) is an enzyme complex that is involved in propagating the cellular response to inflammation. An IκB kinase is an enzyme that catalyzes the chemical reaction: ATP + IκB protein ADP + IκB phosphoprotein. The IκB kinase enzyme complex is part of the upstream NF-κB signal transduction cascade. The IκBα (inhibitor of kappa B) protein inactivates the NF-κB transcription factor by masking the nuclear localization signals of NF-κB proteins and keeping them sequestered in an inactive state in the cytoplasm. IKK specifically, phosphorylates the inhibitory IκBα protein. This phosphorylation results in the dissociation of IκBα from NF-κB. NF-κB, which is free migrates into the nucleus and activates the expression of at least 150 genes; some of which are anti-apoptotic. IKK belongs to the family of transferases, specifically those transferring a phosphate group to the sidechain oxygen atom of serine or threonine residues in proteins.

IKK Inhibitors & Modulators (22)

Product Name Catalog No. Brief Description
ACHP Hydrochloride

HY-13060

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

Amlexanox

HY-B0713

Amlexanox (AA673; CHX3673) is a specific inhibitor of IKKε and TBK1; inhibition of IKKε and TBK1 activity as determined by MBP phosphorylation showing an IC50 of approximately 1–2 μM.

Apigenin

HY-N1201

Apigenin is a non-toxic and non-mutagenic flavone that exists abundantly in numerous herbs and vegetables.

AZD3264

HY-19362

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.

Bay 65-1942 free base

HY-50949

Bay 65-1942 is an ATP-competitive inhibitor that selectively targets IKKβ kinase.

Bay 65-1942 hydrochloride

HY-50948

Bay 65-1942 Hcl is an ATP-competitive inhibitor that selectively targets IKKβ kinase.

Bay 65-1942 R form

HY-50949A

Bay 65-1942 (R form) is an ATP-competitive inhibitor that selectively targets IKKβ kinase.

BI605906

HY-13019

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

BMS-345541

HY-10518

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.

BMS-345541 free base

HY-10519

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.

IKK 16

HY-13687

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.

IKKε-IN-1

HY-12453

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.

IKK-3 Inhibitor

HY-14682

IKK-3 Inhibitor is a potent, selective, inhibitor of IKK-epsilon kinase with IC50 of 40 nM; inactive at IKK-α and IKK-β.

IMD-0354

HY-10172

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

LY2409881

HY-B0788

LY2409881 is a novel selective inhibitor of IKK2 with IC50 of 30 nM; IC50 for IKK1 and other common kinases is at least one log higher.

LY2409881 trihydrochloride

HY-B0788A

LY2409881 trihydrochloride is a novel selective inhibitor of IKK2 with IC50 of 30 nM; IC50 for IKK1 and other common kinases is at least one log higher.

MLN120B

HY-15473

MLN120B is a potent and effective IKKbeta inhibitor.

MRT67307

HY-13018

MRT67307 is a dual inhibitor of the IKKe and TBK-1.

PS-1145

HY-18008

PS-1145 is an IkappaB kinase (IKK) inhibitor with IC50 of 88 nM.

Resveratrol

HY-16561

Resveratrol(trans-Resveratrol) is a phenolic phytoalexin found in grape skin and other plants; trans-Resveratrol is also a selective inhibitor of cyclooxygenase-1 (COX-1), is also a TRIF inhibitor.