PS-1145 (dihydrochloride) is a potent IκB kinase-2 inhibitor with an IC50 value of 88 nM. PS-1145 (dihydrochloride) inhibits activity of NF-κB by blocking IκB kinase phosphorylation in tumor-bearing rats[1].
TPCA-1 is a potent and selective inhibitor of IKK-2 with IC50 of 17.9 nM.
4-Octyl Itaconate is a cell-permeable Itaconate derivative. Itaconate is an anti-inflammatory metabolite that activates Nrf2 via alkylation of KEAP1.
Methyl 3,4-dihydroxybenzoate (Protocatechuic acid methyl ester;Methyl protocatechuate) is a major metabolite of antioxidant polyphenols found in green tea. Antioxidant and anti-inflammatory effect[1].
Mepazine hydrochloride (Pecazine hydrochloride) is a potent and selective MALT1 protease inhibitor with IC50s of 0.83 and 0.42 μM for GSTMALT1 full length and GSTMALT1 325-760, respectively. Mepazine hydrochloride affects viability of ABC-DLBCL cells by enhancing apoptosis[1].
MLT-985 is a highly selective allosteric MALT1 inhibitor with an IC50 value of 3 nM.
LY2409881 is a selective IκB kinase β (IKK2) inhibitor with an IC50 of 30 nM.
HPN-01 is a potent and selective IKK inhibitor, with pIC50 values of 6.4, 7.0 and <4.8 for IKK-α, IKK-β and IKK-ε, respectively. HPN-01 displays greater 50-fold selectivity over a panel of more than 50 other kinases, including ALK5, CDK-2, EGFR, ErbB2, GSK3β, PLK1, Src, and VEGFR-2[1].
Dimethyl fumarate is a nuclear factor (erythroid-derived)-like 2 (Nrf2) pathway activator and induces upregulation of antioxidant gene expression.
Keap1-Nrf2-IN-3 is a KEAP1:NRF2 protein−protein interaction inhibitor, and with a Kd value of 2.5 nM for KEAP1 protein.
JSH-23 is an NF-κB inhibitor which inhibits NF-κB transcriptional activity with an IC50 of 7.1 μM.
Keap1-Nrf2-IN-13 is a Keap1-Nrf2 protein–protein interaction (PPI) inhibitor with an IC50 value of 0.15 μM. Keap1-Nrf2-IN-13 has strong binding affinities to the Keap1 protein by forming hydrogen bond with the key polar residues (Asn414, Arg415, Arg483, Gln530). Keap1-Nrf2-IN-13 can be used in the research of oxidative stress-related and inflammatory diseases, including pulmonary fibrosis, chronic obstructive pulmonary disorder (COPD) and cancers[1].
MALT1-IN-7 (compound 142b) is a potent MALT1 protease inhibitor. MALT1-IN-7 has the potential for cancer research[1].
ML385 is a specific nuclear factor erythroid 2-related factor 2 (NRF2) inhibitor with an IC50 of 1.9 μM.
A novel potent, selective TBK1 PROTAC with DC50 of 12 nM, selectively degrades TBK1 with excellent selectivity against a related kinase IKKε; a chemical tool to assess TBK1 as a target in mutant K-Ras cancer cells.
AZD3264 is a selective IkB-kinase IKK2 inhibitor.
(R)-MALT1-IN-7 (compound 142a) is a potent MALT1 protease inhibitor. (R)-MALT1-IN-7 has the potential for cancer research[1].
KI696 is a high affinity probe that disrupts the Keap1/NRF2 interaction.
Keap1-Nrf2-IN-16 is a biological active peptide. (KEAP1 binding activity)
R079 (compound 17) is a selective, orally active Nrf2 activator. R079 increases Nrf2 translocation activity (EC50 = 32.41 μM). R079 can neutralize excess levels of reactive oxygen species through activating Nrf2. R079 has anti-inflammatory properties and can be used in multiple sclerosis research [1].
Resveratrol (SRT 501), a natural polyphenol that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. It has a wide spectrum of targets including mTOR, JAK, β-amyloid.
PHA 408 (PHA-408) is a potent, selective and orally active IκB kinase-2 (IKK-2) inhibitor. PHA 408 is a powerful anti-inflammatory agent against lipopolysaccharide (LPS)- and cigarette smoke (CS)-mediated lung inflammation[1].
7-Deacetylgedunin is an activator of Keap1/Nrf2/HO-1. 7-Deacetylgedunin alleviates mice mortality induced by LPS. 7-Deacetylgedunin inhibits Keap1 expression and suppresses macrophage proliferation. 7-Deacetylgedunin suppresses inflammation in vivo and in vitro[1].
Val-Arg-Pro-DL-Arg-Fluoromethylketone is a potent MALT1 inhibitor. Val-Arg-Pro-DL-Arg-Fluoromethylketone inhibits cell proliferation and migration. Val-Arg-Pro-DL-Arg-Fluoromethylketone shows anticancer activity[1].
Antioxidant agent-5 (compound D-6) is a potent antioxidant agent. Antioxidant agent-5 can inhibit oxLDL (oxidized low-density lipoprotein)-induced apoptosis and the expression of ICAM-1 and VCAM-1 in VECs. Antioxidant agent-5 suppresses oxLDL-induced increase of ROS level and nuclear translocation of NF-κB. Antioxidant agent-5 protects against oxLDL-induced endothelial injury by activating Nrf2/HO-1 anti-oxidation pathway[1].
CDDO-Im (CDDO-imidazolide) is an activator of Nrf2 and PPAR, with Kis of 232 and 344 nM for PPARα and PPARγ.
5,7-Dihydroxychromone, the extract of Cudrania tricuspidata, activates Nrf2/ARE signal and exerts neuroprotective effects against 6-hydroxydopamine (6-OHDA)-induced oxidative stress and apoptosis. 5,7-Dihydroxychromone inhibits the expression of activated caspase-3 and caspase-9 and cleaved PARP in 6-OHDA-induced SH-SY5Y cells[1].
MSU38225 (MSU-38225) is a novel small molecule that inhibit the Nrf2 pathway, potentially inhibiting Nrf2 transcriptional activity and cancer cell growth;MSU38225 downregulates Nrf2 transcriptional activity and decreases the expression of Nrf2 downstream targets, including NQO1, GCLC, GCLM, AKR1C2, and UGT1A6.MSU38225 strikingly decreases the protein level of Nrf2, which can be blocked by the proteasome inhibitor MG132.Ubiquitination of Nrf2 is enhanced following treatment with MSU38225.By inhibiting production of antioxidants, MSU38225 increases the level of reactive oxygen species (ROS) when cells are stimulated with tert-butyl hydroperoxide (tBHP).MSU38225 also inhibits the growth of human lung cancer cells in both two-dimensional cell culture and soft agar.
4′-Hydroxywogonin (8-Methoxyapigenin), a flavonoid, could be isolated from a variety of plants including Scutellaria barbata and Verbena littoralis. 4′-Hydroxywogonin has anti-inflammatory activity via TAK1/IKK/NF-κB, MAPKs and PI3/AKT signaling pathways. 4′-Hydroxywogonin inhibits angiogenesis by disrupting PI3K/AKT signaling. 4′-Hydroxywogonin inhibits cell proliferation and induces apoptosis[1][2][3].
Bay 65-1942 hydrochloride is an ATP-competitive and selective IKKβ inhibitor.