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 (220)
Related Products (220)
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Antibodies (15)
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IKK Isoform Comparison
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(Rac)-PF-184
0 ImagesCat. No.: HY-107591CAS No.: 1187460-81-6(Rac)-PF-184 is a potent inhibitory factor-κB kinase 2 (IKK-2) inhibitor with an IC50 of 37 nM. (Rac)-PF-184 has anti-inflammatory effects.
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Vinpocetine-d5
0 ImagesCat. No.: HY-13295SCAS No.: 2734920-39-7Vinpocetine-d5 is the deuterium labeled Vinpocetine. Vinpocetine (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.
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DN203316
0 ImagesCat. No.: HY-162963CAS No.: 2982696-04-6Synonyms: PPARδ agonist 11DN203316 (PPARδ agonist 11) is a potent, selective, orally active PPARδ agonist (EC50 = 20 nM) with high selectivity over PPARα and PPARγ. DN203316 suppresses NF-κB-mediated inflammatory signaling, inhibits ferroptosis by upregulating xCT and GPX4, and attenuates STING-TBK1-IRF3-driven fibrogenic responses. DN203316 is useful for research on inflammatory disorders, metabolic dysfunction-associated steatohepatitis (MASH), and liver fibrosis.
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Vitedoamine A
0 ImagesCat. No.: HY-N17353CAS No.: 819861-41-1Vitedoamine A is a Phenylnaphthalene-type lignan alkaloid. Vitedoamine A can be isolated from Vitex negundo. Vitedoamine A inhibits the activity of IKKβ with an IC50 value of 39 μM. Vitedoamine A could inhibit the transcriptional activity of NF-κB, and suppress the production of NO and reduce the expressions of inflammatory cytokines (IL-1β, IL-6, and TNF-α). Vitedoamine A inhibits the phosphorylation of IKKα/β and p65, and prevents the degradation of IκBα. Vitedoamine A possesses anti-rheumatoid arthritis capacity.
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SAR113945 monopotassium
0 ImagesCat. No.: HY-111970BCAS No.: 899418-65-6SAR113945 monopotassium is a highly selective IKK-β inhibitor with an IC50 value of 0.4 nM. SAR113945 monopotassium blocks the canonical NFκB signaling pathway. SAR113945 monopotassium alleviates hyperalgesia to heat and mechanical stimuli, and exerts effects in a zymosan-induced knee joint inflammation model. SAR113945 monopotassium is applicable to research related to symptomatic knee osteoarthritis.
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LLVK
0 ImagesCat. No.: HY-P11296CAS No.: 798540-36-0LLVK is a selective IκB phosphorylation inhibitor. LLVK reduces LPS-induced pro-inflammatory cytokines (IL-1β, IL-6, TNF-α). LLVK is promising for research of inflammatory bowel disease and rheumatoid arthritis.
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1-Dehydro-[10]-gingerdione
![1-Dehydro-[10]-gingerdione](https://file.medchemexpress.com/product_pic/hy-n10768.gif "Click to View 1-Dehydro-[10]-gingerdione Product Detail")
0 ImagesCat. No.: HY-N10768CAS No.: 136826-50-11-Dehydro-[10]-gingerdione directly inhibits IKKβ activity by targeting the activation loop of IKKβ, thus disrupting IKKβ-catalysed IκBα phosphorylation in macrophages stimulated with agonists. 1-Dehydro-[10]-gingerdione inhibits LPS (HY-D1056)-induced NF-κB transcriptional activity. 1-Dehydro-[10]-gingerdione has the potential for NF-κB-associated inflammation and autoimmune disorders research.
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KSI-028
0 ImagesCat. No.: HY-183537KSI-028 is a STING inhibitor. KSI-028 disrupts STING-mediated signal transduction, reduces IFN-β and pro-inflammatory cytokine (IL-6, IL-1β and TNF-α) production. KSI-028 inhibits the phosphorylation of STING, TBK1, IRF3, and STAT1. KSI-028 attenuates renal and hepatic injury in a Cisplatin (HY-17394)-induced acute kidney injury mouse model.
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Resveratrol (GMP)
0 ImagesResveratrol (GMP) is Resveratrol (HY-16561) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. 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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NLRP3-IN-32
0 ImagesCat. No.: HY-161329NLRP3-IN-32 (compound 7a), a 3, 4-dihydronaphthalene-1(2H)-one derivative, is a potential NLRP3 inflammatory vesicles inhibitor. NLRP3-IN-32 can block the assembly and activation of NLRP3 inflammasome by down-regulating the expression of NLPR3 and apoptosis-associated speck-like protein containing a CARD (ASC), and inhibiting the production of reactive oxygen species (ROS) and other inflammatory mediators. NLRP3-IN-32 inhibits the phosphorylation of IκBα and NF-κB/p65 and the nuclear translocation of p65, thereby inhibiting NF-κB signaling.
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IKKβ-IN-6
0 ImagesCat. No.: HY-181836CAS No.: 3117527-91-7IKKβ-IN-6 is an antitumor agent. IKKβ-IN-6 inhibits IKKβ (IC50: 18.24 μM), thereby suppressing the phosphorylation of p65 and IκBα, blocking the nuclear translocation of p65, and subsequently regulating genes controlled by NF-κB. IKKβ-IN-6 also targets topoisomerase I (Topo I), induces DNA damage, ROS accumulation, loss of mitochondrial membrane potential, and S-phase arrest. IKKβ-IN-6 is applicable to related research on colorectal cancer.
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Drofenine
0 ImagesDrofenine (Cycloadiphene; Hexahydroadiphenine) is an brain-penetrant antispasmodic agent. Drofenine is a Kv2.1 channel inhibitor with human IC50 of 9.53 μM. Drofenine is a butyrylcholinesterase (BChE) inhibitor with Ki of 0.003 mM, and is a TRPV3 activator. Drofenine blocks Kv2.1-dependent potassium efflux, inhibits Kv2.1/JNK/NF-κB and IkBa/NF-kB signaling, suppresses Kv2.1 mRNA/protein expression. Drofenine suppresses oligomeric Aβ-induced microglial NLRP3 inflammasome activation and neuronal Tau hyperphosphorylation, improves cognitive impairment, promotes neurite outgrowth. Drofenine induces calcium influx in keratinocytes and exert cytotoxicity against keratinocytes. Drofenine ameliorates diabetic peripheral neuropathy -like pathology. Drofenine can be used for the researches of Alzheimer's disease, diabetic peripheral neuropathy and smooth muscle spasm.
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HDAC6-IN-71
0 ImagesCat. No.: HY-180829CAS No.: 3062867-16-4HDAC6-IN-71 (Compound 24) is a HDAC6 inhibitor with IC50 values for HDAC6 and HDAC1 of 13.68 and 443.12 nM respectively. HDAC6-IN-71 effectively inhibits the production of NO by mouse macrophages, with its IC50 being 2.31 μM. HDAC6-IN-71 inhibits the HDAC6-NF-κB signaling pathway, reduces the levels of phosphorylated IκB-α and IKK-α/β, and suppresses the expression of downstream inflammatory proteins COX-2 and iNOS. HDAC6-IN-71 significantly alleviates ulcerative colitis in mice.
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Butrin
0 ImagesButrin is a compound found in Butea monosperma flowers. Butrin reduces expression of SIRT1, AURKB, cyclin D1, pAKT, GSK-3β, β-catenin, and TGF-3β expression, enhances apoptosis and ROS production in cancer cells. Butrin downregulates Wnt and NF-κB signaling, mitigates oxidative stress, reduces proinflammatory cytokine (TNF-α, IL-6 and IL-8) production and suppresses neuroinflammation. Butrin inhibits IKK enzyme activity. Butrin can be used for the researches of colorectal cancer, Alzheimer’s disease, and rheumatoid arthritis.
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Triptolidenol
0 ImagesCat. No.: HY-N11784CAS No.: 99694-86-7Triptolidenol, a traditional Chinese medicine, is an epoxy diterpene lactone that can be isolated from Tripterygium wilfordii. Triptolidenol has anti-inflammatory and anticancer activities. Triptolidenol significantly inhibits tumor cell proliferation and migration, arrests cell cycle arrest at S phase and induces apoptosis by activating the cytochrome c/caspase cascade signaling pathway. Triptolidenol disrupts NF-κB/COX-2 pathway by inhibiting IKKβ at ATP-binding sites. Triptolidenol can be used for chronic nephritis and kidney cancer like clear cell renal cell carcinoma (ccRCC) research.
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Malachite green hemioxalate (Standard)
0 ImagesMalachite green hemioxalate (Standard) is the analytical standard of Malachite green hemioxalate (HY-D0162). This product is intended for research and analytical applications. Malachite green hemioxalate is a triphenylmethane dye which can be used to detect the release of phosphate in enzymatic reactions. Malachite green hemioxalate has antimicrobial activity, which is attributed to inhibition of intracellular enzymes, intercalation into DNA, and/or interaction with cellular membranes. Malachite green hemioxalate is also a potent and selective inhibitor of IKBKE, and inhibits its downstream targets such as IκBα, p65 and IRF3. Malachite green hemioxalate exhibits antitumor activity in vitro and in vivo.
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3,4-Dihydroxyphenylglycol (Standard)
0 ImagesCat. No.: HY-W010066RCAS No.: 28822-73-33,4-Dihydroxyphenylglycol (Standard) is the analytical standard of 3,4-Dihydroxyphenylglycol (HY-W010066). This product is intended for research and analytical applications. 3,4-Dihydroxyphenylglycol is a phenolic compound and antioxidant. 3,4-Dihydroxyphenylglycol can be extracted from olive oil. 3,4-Dihydroxyphenylglycol downregulates the expression of proinflammatory enzymes (iNOS, COX-2) and prevents the degradation of IκBα. 3,4-Dihydroxyphenylglycol has antioxidant properties. 3,4-Dihydroxyphenylglycol has shown positive effects on frozen-thawed ram sperm. 3,4-Dihydroxyphenylglycol can be used in the study of inflammatory-related diseases (such as ulcerative colitis) and reproductive health (sperm cryopreservation).
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LIB3S0280
0 ImagesCat. No.: HY-172620Purity: 99.89%LIB3S0280 is a potent TBK1 inhibitor with an IC50 value of 493.9 nM. LIB3S0280 exhibits better anticancer effects in pancreatic cancer cell lines with high TBK1 expression. LIB3S0280 inhibits TBK1 downstream signaling pathways, including PI3K/AKT and NF-κB. LIB3S0280 induces G2/M arrest, apoptosis and cellular senescence. LIB3S0280 can be used for pancreatic ductal adenocarcinoma (PDAC) research.
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SMU-L11-R
0 ImagesCat. No.: HY-179047CAS No.: 3040320-18-8SMU-L11-R is a selective TLR7 agonist with an EC50 of 0.012 μM for human TLR7. SMU-L11-R specifically activates TLR7, recruits MyD88, and triggers MAPK/NF-κB pathways, leading to TNF-α/IL-1β/IL-6 secretion in both mouse and human peripheral blood mononuclear cells. SMU-L11-R promotes M1-like macrophage polarization. SMU-L11-R exhibits excellent synergistic anti-tumor effects with PD-L1 inhibitors by upregulating CD8+T cells. SMU-L11-R shows potential in colorectal cancer studies.
