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You are here:Home-Inhibitors & Agonists-NF-κB Pathway-IκB kinase (IKK)

Request The Product List ofIκB kinase (IKK) IκB kinase (IKK)

IKK (IkB kinase) 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-kB 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.

Cat. No. Product Name CAS No. Information
GY03930

TPCA-1

507475-17-4

A potent, selective and orally bioavailable IKK-2 inhibitor with IC50 of 63 nM, TNF cell IC50 of 0.4 uM; displays >100-fold selectivity over IKK-1.

GY10152

PIAA

851814-28-3

PIAA is a TBK1/IKKε inhibitor with IC50 of 0.40/1.07 uM, selectively accelerates proliferation of β-cells; downregulates polyinosine:polycytidylic acid (poly I:C)-stimulated phosphorylation of interferon responsive factor-3 (IRF3), a substrate of TBK1/IKKε; augments β-cell-specific proliferation by increasing cAMP levels and mTOR activity via PDE3, improves glucose control and β-cell mass in the STZ-induced diabetic mouse model.

GY10062

BAY-985

2409479-29-2

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.

GY04291

WS3

1421227-52-2

WS3 is a small molecule that can induce proliferation of β cells with EC50 of 74 nM; modulates the activity of Erb3 binding protein-1 and the IκB kinase pathway; can reversibly proliferates primary RPE cells isolated from fetal and adult human donors.

GY04290

WS6

1421227-53-3

WS6 is a small molecule that can induce proliferation of β cells with EC50 of 0.28 uM; promotes β cell growth in vivo, increasing β cell mass and normalizing blood glucose in the RIP-DTA mouse model of β cell ablation; acts by inhibiting IKKε and blocking the ability of EBP1 to suppress E2F-medtiated transcription; also stimulates α cell proliferation in human pancreatic islets.

GY03361

BMS-345541

547757-23-3

BMS-345541 is a potent and selective IKK-2 inhibitor with IC50 of 0.3 uM; less potent for IKK-1 (IC40=4 uM) and no activity against IKK-ε; inhibits LPS-stimulated TNFα, IL-1β, IL-8, and IL-6 in THP-1 cells with IC50 of1-5 uM; has excellent pharmacokinetics in mice.

GY07386

GSK8612

2361659-62-1

GSK8612 is a highly selective and potent Tank-binding Kinase-1 (TBK1) inhibitor, with a pIC50 of 6.8 for recombinant TBK1.GSK8612 inhibits toll-like receptor (TLR)3-induced IRF3 phosphorylation in Ramos cells and type I IFN secretion in primary human mononuclear cells. In THP1 cells, GSK8612 is able to inhibit secretion of IFNβ in response to dsDNA and cGAMP, the natural ligand for STING.

GY01777

PS-1145

431898-65-6

PS-1145 is a specific IκB kinase (IKK) inhibitor with IC50 of 88 nM; shows no activity for JNK2, c-Src, p38α, IRAK, Lck, etc.; blocks TNFα-induced NF-κB activation in MM cells through inhibition of IκBα phosphorylation and degradation of IκBα, respectively; blocks the protective effect of IL-6 against Dex-induced apotosis, inhibits both IL-6 secretion from BMSCs triggered by MM cell adhesion and proliferation of MM cells adherent to BMSCs.

GY01532

IMD-0354

978-62-1

IMD-0354 is a potent, selective IKKβ inhibitor that inhibits NF-κB activity both in vitro and in vivo; suppresses neoplastic proliferation of human mast cells with constitutively activated c-kit receptors; also suppresses the growth of human breast cancer cells, MDA-MB-231, HMC1-8, and MCF-7, by arresting cell cycle and inducing apoptosis.

GY06382

AS602868

219773-55-4

AS602868 (AS 602868;SPC 839) is a potent, selective and ATP-competitive inhibitor of IKK2 with IC50 of 60 nM and Ki of 20 nM, also interfers directly with FLT3 kinase activation; displays no significant inhibitory activity for IKK1 and a large panel of recombinant kinases; prevents TNF-α induction of the antiapoptotic genes coding for c-IAP-2, Bclx, Bfl-1/A1 and Traf-1, induces cell death in Jurkat leukemic T cells.

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