IKK Inhibitor

NF-κB-IN-21 is a NF-κB signaling pathway inhibitor. NF-κB-IN-21 reduces the phosphorylation levels of IκBα and p65, and inhibits the nuclear translocation of p65. NF-κB-IN-21 downregulates the expression of iNOS, inhibits nitric oxide production, and decreases the levels of pro-inflammatory cytokines TNF-α and IL-6. NF-κB-IN-21 is used in the research of inflammatory diseases.

Isophysalin A is a physalin with alpha and beta unsaturated ketone components. Isophysalin A binds to GSH and targets multiple cysteine residues on IKKβ. Isophysalin A also inhibits inducible NO synthase (iNOS) and nitric oxide (NO) production, showing anti-inflammatory activity.

UM-203 is a reversible covalent STING antagonist. UM-203 is effective against both mouse and human STING, and in particular, it inhibits the most common human STING R232 variant. UM-203 can inhibit STING oligomerization and reduce phosphorylation of downstream TBK1 and IRF3, thereby blocking the IRF3 and NF-κB-mediated signaling pathways and inhibiting IFNβ and IL-6 secretion. UM-203 can be used for the research of inflammation and immunology, such as systemic lupus erythematosus.

MRT67307 dihydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC₅₀s of 160 and 19 nM, respectively. MRT67307 dihydrochloride also inhibits ULK1 and ULK2 with IC₅₀s of 45 and 38 nM, respectively. MRT67307 dihydrochloride also blocks autophagy in cells.

IKKβ-IN-5 is an orally active and selective IKKβ inhibitor with an IC₅₀ of 7.5 nM. IKKβ-IN-5 directly inhibits IKKβ phosphorylation and attenuates NF κB mediated inflammatory and survival signals while promoting autophagy flux. IKKβ-IN-5 exhibits a 6-fold selectivity forIKKβ over the homologous kinase IKKα. IKKβ-IN-5 exerts robust antiproliferative effects through a dual mechanism involving G₂/M phase cell cycle arrest and autophagy activation, even under inflammatory stimulation in vitro. IKKβ-IN-5 demonstrates favorable pharmacokinetics and suppresses tumor growth in vivo. IKKβ-IN-5 can be used for colorectal cancer and potentially other inflammation driven malignancies research.

Tizoxanide (Standard) is the analytical standard of Tizoxanide. This product is intended for research and analytical applications. Tizoxanide (TIZ) is the active metabolite of Nitazoxanide, which is a thiazolide anti-infective compound against anaerobic bacteria, protozoa, and a range of viruses. Tizoxanide (TIZ) has anti-HIV-1 activities and potent inhibition of both HBV and HCV replication with values EC₅₀ of 0.46μM and 0.15 μM, respectively. Tizoxanide also exerts anti-inflammatory effects by inhibiting the production of pro-inflammatory cytokines and suppressing of the activation of the NF-κB and the MAPK signaling pathways in LPS-treated macrophage cells.

SAR113945 is a highly selective IKK-β inhibitor with an IC₅₀ value of 0.4 nM. SAR113945 blocks the canonical NFκB signaling pathway. SAR113945 alleviates hyperalgesia to heat and mechanical stimuli, and exerts effects in a zymosan-induced knee joint inflammation model. SAR113945 is applicable to research related to symptomatic knee osteoarthritis.

ITA-5 is a TBK1 inhibitor based on the structure of itaconic acid. can significantly inhibit the secretion of IFN-β. ITA-5 can inhibit the phosphorylation of TBK1, IRF3, and STAT1. ITA-5 can be used for research on autoimmune diseases and excessive inflammation.

IKKε-IN-1 is a IKKε inhibitor. IKKε-IN-1 reduces cell viability, inhibits colony formation and cell migration. IKKε-IN-1 induces autophagy (Autophagy) in cancer cells. IKKε-IN-1 can be used in the research of cancers including colorectal cancer, hepatocellular carcinoma, bladder cancer, breast cancer, lung cancer, and cervical cancer.

Lucidone, an anti-inflammatory agent that can be isolated from the fruit of Lindera erythrocarpa Makino. Lucidone inhibits LPS-induced NO and PGE₂ production in RAW 264.7 mouse macrophages. Lucidone also decreases TNF-α secretion, iNOS and COX-2 expression. Lucidone prevents NF-κB translocation and inhibits JNK and p38MAPK signals. Lucidone also has inhibitory activity against Dengue virus (DENV) (EC₅₀=25 μM).

Anti-inflammatory agent 116 is an anti-inflammatory agent. Anti-inflammatory agent 116 inhibits the abnormal activation of the NF-κB/MAPK signaling pathway. Anti-inflammatory agent 116 binds to the p50 subunit and impairs the DNA-binding ability of the p65-p50 heterodimer. Anti-inflammatory agent 116 inhibits LPS-induced production of NO and MtROS, secretion of IL-1β and TNF-α, expression of iNOS and COX-2, phosphorylation of IKK, IκB, p65, p38, ERK and JNK, as well as nuclear translocation of p65. Anti-inflammatory agent 116 alleviates sepsis-associated acute liver injury in mice. Anti-inflammatory agent 116 can be used for the research of sepsis-associated acute liver injury.

Resveratrol analog 2 is an analog of Resveratrol (HY-16561). Resveratrol is a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties.

HIF-1α-IN-8 is an orally active HIF-1α inhibitor, with an IC₅₀ of 2.02 μM. HIF-1α-IN-8 significantly suppresses the expression of inflammation factors of IL-6 and NO, reduces hypoxia-induced ROS production and apoptosis in C8-D1A cells. HIF-1α-IN-8 inhibits HIF-1α/IKKα/NF-κB signaling pathway and reduces the expression of blood-brain barrier permeability-related proteins. HIF-1α-IN-8 reduces brain water content and oxidative stress level in mice with high altitude cerebral edema (HACE) model. HIF-1α-IN-8 can be used for the study of high altitude cerebral edema (HACE).

DMX-129 is an ΙΚΚε and TBK-1 inhibitor with IC₅₀ values of <30 nM for both TBK1 and IKKε.

Oxaprozin (Standard) is the analytical standard of Oxaprozin. This product is intended for research and analytical applications. Oxaprozin is an orally active and potent COX inhibitor, with IC₅₀ values of 2.2 μM for human platelet COX-1 and and 36 μM for IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin also inhibits the activation of NF-κB. Oxaprozin induces cell apoptosis. Oxaprozin shows anti-inflammatory activity. Oxaprozin-mediated inhibition of the Akt/IKK/NF-κB pathway contributes to its anti-inflammatory properties.

(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.

Vinpocetine-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.

DN203316 (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.

Vitedoamine 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.

SAR113945 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.