IKK
IκB kinase; I kappa B kinase
IKK is a complex composed of three subunits: IKKα, IKKβ, and IKKγ (also called NEMO). The complex is the signal integration hub for NF-κB activation. It integrates signals from all NF-κB activating stimuli to catalyze the phosphorylation of various IκB and NF-κB proteins, as well as of other substrates. The human IKK family has four members, the IKKs IKK-alpha and IKK-beta, and the IKK-related kinases TBK1 and IKK-epsilon.
Two members, IKKα and IKKβ, the so-called canonical members, phosphoryate IκBα, leading to activation of the transcription factor NF-κB, which controls the expression of many immune and inflammatory genes. The IKK-related proteins TBK-1 and IKK-epsilon have a different substrate--IRF3--which regulates a different set of genes, the products of which include Type I interferons. IKKs are a therapeutic target due to their crucial roles in various biological processes, including the immune response, the stress response, and tumor development.
IKK Isoform Specific Products
All Product Categories
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IKK Related Products (215)
Related Products (215)
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Antibodies (15)
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IKK Isoform Comparison
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BAY 11-7082
0 ImagesSynonyms: BAY 11-7821BAY 11-7082 is an IκBα phosphorylation and NF-κB inhibitor. BAY 11-7082 selectively and irreversibly inhibits the TNF-α-induced phosphorylation of IκB-α, and decreases NF-κB and expression of adhesion molecules. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC50=0.19, 0.96 μM, respectively). BAY 11-7082 inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells.
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Resveratrol
0 ImagesResveratrol (trans-Resveratrol; SRT501) is a CNS-penetrant natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator. Resveratrol is a potent pregnane X receptor (PXR) inhibitor. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model. Resveratrol increases production of NO in endothelial cells.
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BX795
0 ImagesBX795 is a potent and selective inhibitor of PDK1, with an IC50 of 6 nM. BX795 is also a potent and relatively specific inhibitor of TBK1 and IKKε, with an IC50 of 6 and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, and has lower selectivity over PKA, PKC, c-Kit, GSK3β etc. BX795 modulates autophagy.
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CDDO-biotin
0 ImagesCat. No.: HY-186167CAS No.: 3110422-01-7CDDO-biotin is an IKKβ inhibitor with cancer cell inhibitory activity. CDDO-biotin directly interacts with and oxidizes Cys-179 in the activation loop of IKKβ, forming an adduct with wild-type IKKβ. CDDO-biotin can be used in the research of myeloid leukemia, osteosarcoma, multiple myeloma, lung cancer, breast cancer and pancreatic cancer.
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MAP3K14-IN-1
0 ImagesCat. No.: HY-124865CAS No.: 2113617-02-8MAP3K14-IN-1 (Compound 173) is a MAP3K14 (NIK kinase) inhibitor with an IC50 of 1.8 nM. MAP3K14-IN-1 inhibits the autophosphorylation of MAP3K14 kinase. MAP3K14-IN-1 reduces the level of phosphorylated IKKα in cancer cells. MAP3K14-IN-1 inhibits the proliferation of multiple myeloma cells. MAP3K14-IN-1 can be used in research related to multiple myeloma.
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STING-IN-19
0 ImagesCat. No.: HY-187227STING-IN-19 is a STING inhibitor with a Kd value of 2.31 μM for human STING. STING-IN-19 inhibits the activation of TBK1 and IRF3 by binding to STING, thereby suppressing the activation of downstream signaling pathways. STING-IN-19 reduces the levels of key inflammatory cytokines IL-1β, IL-6 and TNF-α in colonic tissues and serum of mice with ulcerative colitis. STING-IN-19 can be used in studies related to ulcerative colitis.
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Parthenolide
0 ImagesSynonyms: (-)-Parthenolide
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IKK 16
0 ImagesIKK 16 is an orally active IKK inhibitor. IKK 16 shows IC50s of 40 nM, 70 nM, 200 nM, and 50 nM for IKK2, IKK complex, IKK1, and LRRK 2, respectively. IKK 16 is also a pan-PKD inhibitor, inhibiting PKD1, PKD2, and PKD3 with IC50s of 153.9, 115, and 99.7 nM, respectively. IKK 16 is also an ABCB1 inhibitor, interfering with the binding of ABCB1 to its substrates. IKK 16 protects against LPS (HY-D1056)-induced multiple organ dysfunction by reducing the acute inflammatory response induced by endotoxin exposure. IKK 16 can restore renal function and alleviate fibrosis in acute kidney injury. IKK 16 attenuates cardiac dysfunction associated with polymicrobial sepsis in mice with type 2 diabetes mellitus (T2DM) by inhibiting the NF-κB pathway.
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Clemastine fumarate
0 ImagesSynonyms: HS-592 fumarate; Meclastine fumarateClemastine (HS-592; Meclastine) fumarate is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine fumarate also antagonizes muscarinic acetylcholine receptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine fumarate exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .
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β-1,3-Glucan
0 ImagesSynonyms: β Glucanβ-1,3-Glucan (β Glucan) is an orally active polysaccharide composed of glucose polymers. β-1,3-Glucan increase the activity of IKKβ kinase, enhances the production of nitric oxide. β-1,3-Glucan improves resistance to Vibrio harveyi infection. β-1,3-Glucan enhances immune response, promotes blood pressure recovery, reduces lung, kidney and liver damage, inhibits the growth of syngeneic tumors.
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Resveratrol (Standard)
0 ImagesSynonyms: trans-Resveratrol (Standard); SRT501 (Standard)Resveratrol (Standard) is the analytical standard of Resveratrol. This product is intended for research and analytical applications. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator. Resveratrol is a potent pregnane X receptor (PXR) inhibitor. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model. Resveratrol increases production of NO in endothelial cells.
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Vinpocetine
0 ImagesSynonyms: Ethyl apovincaminateVinpocetine (Ethyl apovincaminate) is a derivative of the alkaloid Vincamine that blocks voltage-gated Na+ channels. The IC50 value of Vinpocetine on direct IKK inhibition in the cell-free system is 17.17 μM. Vinpocetine is a phosphodiesterase (PDE) inhibitor and inhibits NF-κB-dependent inflammatory responses by directly targeting IκB kinase complex (IKK), and has been widely used for the treatment of cerebrovascular disorders.
