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.
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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.
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.
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.
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.
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.
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.
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.
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.
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.
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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