NF-kB (Nuclear factor kappa-light-chain-enhancer of activated B cells) is a protein complex that controls transcription of DNA. NF-kB is found in almost all animal cell types and is involved in cellular responses to stimuli such as stress, cytokines, free radicals, ultraviolet irradiation, oxidized LDL, and bacterial or viral antigens. NF-kB plays a key role in regulating the immune response to infection. Incorrect regulation of NF-kB has been linked to cancer, inflammatory, and autoimmune diseases, septic shock, viral infection, and improper immune development. NF-kB has also been implicated in processes of synaptic plasticity and memory. There are five proteins in the mammalian NF-kB family: NF-kB1, NF-kB2, RelA, RelB, c-Rel.
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BAY 11-7082 a NF-κB inhibitor that selectively and irreversibly inhibits the TNF-α-inducible phosphorylation of IκBα (IC50=10 uM), also inhibits ubiquitin-specific protease USP7 and USP21 with IC50 of 0.19 uM and 0.96 uM, respectively; induces apoptosis of HTLV-I-infected T-cell lines but only negligible apoptosis of HTLV-I-negative T cells, rapidly and efficiently reduces the DNA binding of NF-κB in HTLV-I-infected T-cell lines and down-regulates the expression of the antiapoptotic gene, Bcl-xL, regulated by NF-κB; selectively inhibits Tax-induced NF-κB activity in a human T-cell line.
NDMC101 is a small molecule that inhibits NFATc1 and NF-κB activity, inhibits RANKL-induced osteoclastogenesis in vivo; markedly inhibits RANKL-induced formation of TRAP+ multinucleated cells in RAW264.7 and bone marrow macrophage cells (BMMs); significantly reduces the bone-resorbing activity of mature osteoclasts; reduces arthritic index and mitigated bone erosion in CIA mice.
SR12343 (SR-12343) is a novel NF-κB essential modulator (NEMO)-binding domain (NBD) mimetic for inhibiting IKK/NF-κB activation, inhibits TNF-α-mediated NF-κB activation with IC50 of 11.34 uM in luciferase assays; inhibits lipopolysaccharide (LPS)-induced NF-κB activation by blocking the interaction between IKKβ and NEMO, significantly inhibits COX-2, IL-6, and iNOS expression at 50 uM in cellular assays; suppresses LPS-induced acute pulmonary inflammation, alleviates necrosis and muscle degeneration in mdx mice without overt liver toxicity.
SR12460 (SR-12460) is a novel NF-κB essential modulator (NEMO)-binding domain (NBD) mimetic for inhibiting IKK/NF-κB activation, inhibits TNF-α-mediated NF-κB activation with IC50 of 20.24 uM; inhibits lipopolysaccharide (LPS)-induced NF-κB activation by blocking the interaction between IKKβ and NEMO and suppressed LPS-induced acute pulmonary inflammation in mice without overt liver toxicity.
A ribonucleotide reductase inhibitor; overcomes Bcl-2 mediated radiation resistance in PC-3 cells; induces apoptosis and inhibits DNA repair in multiple myeloma cells by downregulation of bcl family proteins including bcl-2, bcl(xl), and XIAP; (150 mg/kg daily) significantly protects the cardiomyocyte membrane integrity and decreases the intra-cardiac oxidative stress induced by DOX treatment (15 mg/kg) in mice.
An enantiomer of Ibuprofen that is generally not considered a COX inhibitor and is instead thought to be involved in pathways of lipid metabolism as it is incorporated into triglycerides along with fatty acids; inhibits NF-κB activation (IC50=121.8 uM) in response to T-cell stimulation as well as block superoxide formation, β-glucuronidase release, and LTB4 generation by stimulated neutrophils (IC50 =40-100 uM).
IT-901 is a novel potent, small molecule inhibitor of NF-κB subunit c-Rel, inhibits DNA binding of c-Rel and NF-κB activity with IC50 of 3 uM; reduces stimulation of the oxidative stress response gene heme oxygenase-1, inhibits c-Rel/NF-κB both in vitro and in vivo.
BAY 11-7085 is an inhibitor of the expression of ICAM-1, VCAM-1, and E-selectin in human endothelial cells (IC50=5-10 uM); acts by selectively inhibiting TNFα-induced phosphorylation of IκB-α without affecting the constitutive IκB-α phosphorylation; prevents PMA-induced NF-kappaB nuclear translocation; reduces swelling in both the rat carrageenan paw edema assay and in a rat adjuvant arthritis model.
ABD328 (ABD-328) is an orally active, small molecule inhibitor of RANKL and TNF signalling that inhibits inflammation in vivo; inhibits TNF-induced activation of the NF-κB pathway, ERK, JNK and MAPKs in osteoclasts and macrophages, suppresses inflammatory arthritis, inhibits joint destruction and prevented systemic bone loss in mice model of rheumatoid arthritis.
ABD345(ABD-345;ABD 345) is a small molecule inhibitor of RANKL signalling, inhibits TNF-induced NF-κB and MAPK activation and inflammation; inhibits osteoclast formation in mouse bone marrow cultures (IC50=1.7 uM) without any effects on bone marrow macrophage viability; inhibits RANKL-induced phosphorylation of IκB and ERK in M-CSF-dependent bone marrow macrophage cultures; inhibits both RANKL- and TNF-induced NF-κB and MAPK signalling in osteoclasts and macrophages, and inflammation and bone destruction in mouse model of rheumatoid arthritis.
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