NF-κB

<p>IRAK4-IN-28 (compound 42), an orally-active IRAK4 inhibitor (IC50=8.9 nM), exhibits strong binding affinity with a Kd of 0.58 nM for the target enzyme.</p>

<p>NF-κB-IN-13 (compound 12) markedly suppresses LPS-induced NF-κB activation and NO synthesis in RAW264.7 macrophages, exhibiting anti-inflammatory properties [1</p>

<p>(Rac)-BAY-985 is a potent, ATP-competitive and selective inhibitor of TBK1(IC50 of 1.5 nM),with antitumor efficacy.</p>

<p>ACHP Hydrochloride (IKK-2 Inhibitor VIII) is a highly potent and selective IKK-β inhibitor with an IC50 of 8.5 nM.</p>

<p>RIPK2-IN-3 (FCG806791773) is a RIPK2 inhibitor with anti-inflammatory and anticancer activities, useful for research on immune diseases and cancer.</p>

<p>IR-Crizotinib is a conjugate of the near-infrared dye IR-786 and Crizotinib, an NF-κB-inducing kinase (NIK) inhibitor, with an IC50 of 3.381 μM for intracranial</p>

<p>Trovafloxacin: broad-spectrum fluoroquinolone, blocks DNA gyrase/topoisomerase IV and PANX1 channel (IC50=4μM).</p>

<p>IKK-IN-4 is a potent and selective inhibitor of IkappaB kinase 2 with IC 50 values of 45 and 650 nM against IKKβ and IKKα, respectively [1].</p>

<p>Bay 65-1942 R form is the less active R-form of Bay 65-1942. Bay 65-1942 is a selective and ATP-competitive IKKβ inhibitor.</p>

<p>GGTI 2147 decreased Rac1 activity, down-regulated p65 expression, and ameliorated OGD/R-induced neuronal apoptosis.</p>

<p>IKK-IN-1 is an inhibitor of IKK.</p>

<p>Glabrescone C exhibits strong anti-inflammatory properties through direct binding to IKKα/β.</p>

<p>Dimethoxycurcumin is a stable curcumin analog causing epigenetic shifts in leukemia cells, affecting gene expression.</p>

<p>Supercinnamaldehyde is a potent activator of transient receptor potential ankyrin 1 (TRPA1), exhibiting an EC50 of 0.8 μM, and induces activation of TRPA1 ion</p>

<p>Oditrasertib, a RIPK1 inhibitor characterized by an IC50 value below 100 nM, is employed in inflammation research.</p>

<p>LTβR-IN-1 is a potent and selective lymphin β receptor (LTβR) inhibitor.</p>

<p>RIPK1-IN-4 is a potent and selective type II kinase receptor interacting protein 1 (RIP1) kinase inhibitor and binds to a DLG-out inactive form of RIP1 (IC50s</p>

<p>MAY0132 is a potent and selective EPAC2 inhibitor with an IC50 of 0.4 μM. It significantly inhibits the replication of HMPV, AdV, and RSV, reduces cytokine/chemokine production induced by viral infections, and suppresses NF-κB activation. MAY0132 exhibits antiviral activity and can be used in respiratory virus infection research.</p>

<p>AS2690168 freebase is an orally active inhibitor of RANKL signaling, capable of suppressing RANKL-induced osteoclastogenesis in RAW264 cells. AS2690168 is applicable in research related to pathological bone resorption.</p>

<p>SBI-0640726, an eIF4G1 inhibitor, exhibits antiproliferative activity against melanoma. It disrupts the eIF4F translation initiation complex by inhibiting the AKT and NF-kB signaling pathways. Additionally, SBI-0640726 inhibits the growth of melanoma with NRAS and BRAF mutations in vitro.</p>

<p>TBK1/IKKε-IN-1 is a dual inhibitor of TBK1 and IKKε (IC50s of &lt;100 nM).</p>

<p>NIK-IN-2 (compound 1) is an effective inhibitor of NF-κB inducing kinase (NIK), exhibiting a pIC50 of 7.4. It plays a crucial role in cancer research.</p>

<p>GTCpFE, a compound synthesized from Dimethyl fumarate (DMF) and Aspirin (ASA), inhibits IKKα/β in the NF-κB pathway, exhibiting anti-inflammatory activity by preventing p65 from entering the nucleus. It selectively inhibits cancer stem cell (CSC) activity by reducing the growth of mammospheres and the expression of the CD44+CD24- immune phenotype. Furthermore, GTCpFE targets breast cancer stem cells, crucial in aggressive cancer phenotypes that depend on NFκB and PGE2.</p>

<p>K-14585 blocks PAR(2), reduces NFkappaB activity, and IL-8 response, but alone can boost IL-8.</p>

<p>NF-κB-IN-6 (Compound 3d) is an anti-inflammatory agent that works by reducing the protein expression of iNOS and COX-2 by suppressing the NF-κB signaling</p>

<p>Anti-inflammatory agent 6 blocks IKKα/β, IκBα, and NF-κB p65 phosphorylation, key to controlling inflammation.</p>

<p>DBMB is a spleen tyrosine kinase (Syk) inhibitor that significantly suppresses Syk enzyme activity. It possesses anti-inflammatory properties by inhibiting NF-κB signaling, thereby reducing the production of inflammatory mediators such as nitric oxide (NO) and prostaglandin E2 (PGE2). DBMB can be utilized in research on inflammatory diseases.</p>

<p>AS2690168 hydrochloride is an orally active inhibitor of RANKL signaling that can suppress RANKL-induced osteoclastogenesis in RAW264 cells. AS2690168 is applicable in research related to pathological bone resorption.</p>

<p>Ocadusertib is an effective inhibitor of the serine/threonine kinase receptor-interacting protein kinase 1 (RIPK1).</p>

<p>OxLig-1 (7-Ketocholesteryl-9-carboxynonanoate) constitutes a lipid component of oxidized low-density lipoprotein (oxLDL) and serves as a critical ligand for β-glycoprotein I (β(2)-GPI). It induces nuclear translocation by activating the NF-κB pathway. Additionally, oxLig-1 is utilized in the study of atherosclerosis (AS).</p>

<p>4-Octylphenol is an endocrine disruptor with gender-specific effects on male germ cells, significantly reducing the mitotic index and the number of spermatogonia. It also causes inflammatory damage in the gills of carp by activating the complement system through the C3a/C3a receptor (C3a/C3aR) axis and C5a/C5a receptor 1 (C5a/C5aR1) axis. Furthermore, 4-Octylphenol induces immune suppression by disrupting the balance between helper T (Th) cells 1/Th2 and regulatory T (Treg)/Th17 cells, and triggers inflammatory damage through the Toll-like receptor 7 (Toll-like Receptor (TLR))/inhibitor κBα/nuclear factor κB (TLR7/IκBα/NF-κB) pathway.</p>

<p>TLR4/NF-κB/MAPK-IN-1 is a novel antineuroinflammatory agent that functions by inhibiting the TLR4/NF-κB/MAPK pathways.</p>

<p>NLRP3-IN-78 (compound 21) is an NLRP3 inhibitor with a 46.72% inhibition rate of GSDMD-induced pyroptosis at 5 μM. It binds to the NLRP3 protein and prevents GSDMD-NT oligomerization. Additionally, NLRP3-IN-78 inhibits GSDMD cleavage and upstream NF-κB signaling, demonstrating anti-inflammatory activity.</p>

<p>RIPK1-IN-19 is a selective and potent RIPK1 inhibitor that protects against cell necrosis in the tnf α-induced SIRS model and IMQ-induced psoriasis model.</p>

<p>TNFα Activity Modulator 3 (example 6) is a molecule that regulates TNF activity by inhibiting TNFα-induced NF-κB activation, making it applicable for related research.</p>

<p>Antiproliferative agent-22 is an anticancer compound that shows antiproliferative activity on MCF-7, MDA-MB-231 and MDA-MB-468 cells.</p>

<p>HOIPIN-8 sodium is a LUBAC inhibitor for the study of inflammatory and immune diseases.</p>

<p>UBS109, a curcumin analog, is a DNA demethylating agent in pancreatic cancer that promotes osteoblast differentiation and mineralization.</p>

<p>Zharp1-211 is a RIPK3 inhibitor，reduces JAK/ stat1-mediated chemokines and MHC class II molecules in IECs, (GVHD) for gastrointestinal inflammation.</p>

<p>Tripeptide-41 (CG-Lipoxyn) is a bioactive peptide known for its ability to reduce fat accumulation.</p>

<p>2,3-Bis(3-indolylmethyl)indole exhibits a concentration-dependent inhibition of RANKL-induced osteoclastogenesis, actin ring formation, and bone resorption.</p>

<p>SEMBL, a novel inhibitor of DNA binding of NF-kappaB component p65 in vitro, inhibits NF-kappaB and cellular invasion in ovarian carcinoma ES-2 cells.</p>

<p>ALPK1-IN-2 is a potent inhibitor of ALPK1 (α-kinase 1) (IC50: 95 nM). ALPK1-IN-2 inhibits NF-κB (IC50: 1.31 μM).</p>

<p>ALPK1-IN-1 (A001) strongly inhibits ALPK1, key for innate immunity &amp; NF-κB signaling via TIFA/TRAF.</p>

<p>ALPK1-IN-3,serves as an ALPK1 inhibitor that dampens proinflammatory gene expression in the kidney and enhances survival in animal models of sepsis-induced</p>