IKK Inhibitor

LLVK TFA is a selective IκB phosphorylation inhibitor. LLVK TFA reduces LPS-induced pro-inflammatory cytokines (IL-1β, IL-6, TNF-α). LLVK TFA is promising for research of inflammatory bowel disease and rheumatoid arthritis.

Lucidenic acid B is a triterpenoid compound. Lucidenic acid B inhibits the activities of ERK1/2, AP-1, NF-kB, and IKK, suppresses PMA (Phorbol 12-myristate 13-acetate) (HY-18739)-induced MMP-9 expression and cell invasion, and induces apoptosis in leukemia cells via the mitochondrial pathway. Lucidenic acid B inhibits the growth of various cancer cell lines without affecting normal lymphocytes and does not induce G1 phase arrest or necrosis. Lucidenic acid B can be used in research on hepatocellular carcinoma, human acute promyelocytic leukemia, and skin tumor promotion.

5-(3',4'-Dihydroxyphenyl)-γ-valerolactone is an intestinal microbiota metabolite of (-)-Epicatechin (HY-N0001). 5-(3',4'-Dihydroxyphenyl)-γ-valerolactone downregulates TNF-α-stimulated phosphorylation of IKK and IκBα, inhibits the transcriptional activation of NF-κB, and suppresses the expression of adhesion molecules and chemokines. 5-(3',4'-Dihydroxyphenyl)-γ-valerolactone promotes autophagy, alleviates oxidative stress, maintains osteoblast differentiation, induces G₁ phase arrest, inhibits adipogenesis, and scavenges ABTS free radicals. 5-(3',4'-Dihydroxyphenyl)-γ-valerolactone inhibits the adhesion of uropathogenic Escherichia coli to bladder epithelial cells; when used in combination with Curcumin (HY-N0005), it downregulates the NLRP3 and NOX2/Nrf2 signaling pathways, thereby reducing microglial activation. 5-(3',4'-Dihydroxyphenyl)-γ-valerolactone can be used in research related to diabetes, atherosclerosis, osteoporosis, obesity, neurodegenerative diseases involving microglial activation, and urinary tract infections.

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.

MLN120B dihydrochloride (ML120B dihydrochloride) is a potent, ATP competitive, and orally active inhibitor of IKKβ with an IC₅₀ of 60 nM. MLN120B inhibits multiple myeloma cell growth in vitro and in vivo and also can be used for the research of rheumatoid arthritis.

Vinpocetine (Standard) is the analytical standard of Vinpocetine. This product is intended for research and analytical applications. 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.

IKK-IN-1 is an inhibitor of IKK extracted from patent WO2002024679A1, compound example 18-13.

Tat-IKIP (46-60) TFA is the trifluoroacetic acid of Tat-IKIP (46-60) (HY-P10966). Tat-IKIP (46-60) is a IκB kinase (IKK)-targeting membrane-penetrating peptide. Tat-IKIP (46-60) inhibits IKK activation and NF-κB targeted gene expression by disrupting the IKKβ/NEMO complex. Tat-IKIP (46-60) significantly reduces DSS (HY-116282)-induced acute inflammation in inflammatory bowel disease (IBD) mice model and attenuates Zymosan-induced acute arthritis in acute arthritis model (AAM). Tat-IKIP (46-60) can be used for inflammatory diseases research, such as IBD, pancreatitis and rheumatoid arthritis.

Bay 65-1942 R form is the less active R-form of Bay 65-1942. Bay 65-1942 is an ATP-competitive and selective IKKβ inhibitor.

Amlexanox (Standard) is the analytical standard of Amlexanox. This product is intended for research and analytical applications. Amlexanox (AA673; Amoxanox; CHX3673) is a specific inhibitor of IKKε and TBK1, and inhibits the IKKε and TBK1 activity determined by MBP phosphorylation with an IC₅₀ of approximately 1-2 μM.

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.

Oxaprozin potassium 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 potassium also inhibits the activation of NF-κB. Oxaprozin potassium induces cell apoptosis. Oxaprozin potassium shows anti-inflammatory activity. Oxaprozin potassium-mediated inhibition of the Akt/IKK/NF-κB pathway contributes to its anti-inflammatory properties.

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).

Multi-target Pt (IV), an antitumor agent, suppresses the IKKβ phosphorylation, IκBα phosphorylation and NF-κB p65 phosphorylation and nuclear translocation, leading to blocked the NF-kB signal pathway.

IKK-IN-4 is a potent and selective IkappaB kinase 2 (IKKβ orIKK2) inhibitor, with IC₅₀s of 45 and 650 nM for IKKβ and IKKα, respectively.

TBK1 ligand 2-C-O-C4-O-C3-O-C-amide is a conjugate of TBK1 ligand and linker, which can be used in the synthesis of PROTAC TBK1 degrader-2 (HY-112557).

Tat-IKIP (46-60) is a IκB kinase (IKK)-targeting membrane-penetrating peptide. Tat-IKIP (46-60) inhibits IKK activation and NF-κB targeted gene expression by disrupting the IKKβ/NEMO complex. Tat-IKIP (46-60) significantly reduces DSS (HY-116282)-induced acute inflammation in inflammatory bowel disease (IBD) mice model and attenuates Zymosan-induced acute arthritis in acute arthritis model (AAM). Tat-IKIP (46-60) can be used for inflammatory diseases research, such as IBD, pancreatitis and rheumatoid arthritis.

CS12192 is a compound improving survival and weight gain. CS12192 has the potential for the research of graft-versus-host disease (GVHD) (extracted from the patent CN112773802A).

TBK1/IKKε-IN-6 (example 110) is a TBK1 and IKKε inhibitor, with IC₅₀ values of <100 nM for both TBK1 and IKKε.

(Rac)-Mefloquine ((Rac)-Mefloquin) is an orally active NF-κB inhibitor. (Rac)-Mefloquine inhibits the NF-κB and IKK signaling pathways, suppresses NF-κB-Luc luciferase activity, blocks the activation of p65 and IκBα, and reduces the expression of downstream target genes of NF-κB. (Rac)-Mefloquine activates apoptosis-related factors and induces apoptosis in tumor cells. (Rac)-Mefloquine functions as a tumor cell inhibitor. (Rac)-Mefloquine can be used for the research of colorectal cancer.