IKK Inhibitor

DCLK1-IN-6 (Compound 12n) is a Doublecortin-like kinase 1 (DCLK1) inhibitor with an IC₅₀ of 58 nM. DCLK1-IN-6 significantly inhibits DCLK1 enzyme activity and its mediated inflammatory pathway. DCLK1-IN-6 has remarkable anti-inflammatory activity and significantly alleviates symptoms in acute lung injury (ALI) and sepsis mouse models. DCLK1-IN-6 can be used for acute inflammation diseases research.

ITA-9 is a TBK1 inhibitor based on the structure of itaconic acid. ITA-9 can inhibit the IFN-I signaling pathway. ITA-9 can inhibit the phosphorylation of TBK1, IRF3, and STAT1. ITA-9 can be used for research on inflammatory reactions and tissue damage.

CGA-JK3 is CGA-JK3 is an ATP-competitive inhibitor of IKKβ-catalyzed kinase activity. CGA-JK3 inhibits IκBα phosphorylation in LPS (HY-D1056) - induced RAW 264.7 cells.

Desmethoxyyangonin (Standard) is one of the six major kavalactones found in the Piper methysticum (kava) plant. Desmethoxyyangonin (Standard) is a selective inhibitor of monoamine oxidase-B (MAO-B) (IC₅₀: 0.123  µM). Desmethoxyyangonin (Standard) exerts anti-inflammatory effects by inhibiting Jak2/STAT3 and IKK signaling pathways. Desmethoxyyangonin (Standard) induces CYP3A23 expression and leads to skeletal muscle relaxation.

BAY 11-7082 (Standard) is the analytical standard of BAY 11-7082 (HY-13453). This product is intended for research and analytical applications. BAY 11-7082 is an IκBα phosphorylation and NF-κB inhibitor. BAY 11-7082 selectively and irreversibly inhibits the TNF-α-induced phosphorylation of IκB-α, and decreases NF-κB and expression of adhesion molecules. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC₅₀=0.19, 0.96 μM, respectively). BAY 11-7082 inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells.

2'-Acetylacteoside (Standard) is the analytical standard of 2'-Acetylacteoside (2'-AA) (HY-N0026). This product is intended for research and analytical applications. 2'-Acetylacteoside is a natural compound with oral activity and blood-brain barrier permeability. 2'-Acetylacteosideexhibits MAO‑B inhibitory activity (IC₅₀ = 17.71 μM, K_i = 13.81 μM). 2'-Acetylacteoside downregulates the expression of RANK, TRAF6, NF‑κB, NFATc1 and IKKβ, disrupts the RANKL/RANK interaction, blocks downstream signaling pathways, and increases the level of phosphorylated Akt. 2'-Acetylacteoside possesses potent anti-osteoclastogenic, anti-bone resorptive, pro-neurogenic, neuroprotective and antioxidant activities. 2'-Acetylacteoside can be used in the research of osteoporosis, ischemic stroke and Parkinson's disease.

GTCpFE inhibits IKKα/β in the NF-κB pathway with anti-inflammatory activities and blocks p65 nuclear entry, which consists of Dimethyl fumarate (DMF) (HY-17363) linked to Aspirin (ASA) (HY-14654). GTCpFE exhibits selective anti-cancer stem-like cell (CSC) activity by reducing mammosphere growth and the CD44⁺ CD24^- immunophenotype. GTCpFE inhibits breast cancer stem cells, an important NFκB- and PGE2-dependent phenotype in aggressive cancers.

TBK1/IKKε-IN-1 is a dual TBK1 and IKKε inhibitor extracted from patent US20160376283 A1, Compound 274 in Example 60, has IC₅₀s of <100 nM.

GSK8612 (Standard) is the analytical standard of GSK8612 (HY-111941). This product is intended for research and analytical applications. GSK8612 is a highly selective and potent Tank-binding K_inase-1 (TBK1) inhibitor, with a pIC₅₀ of 6.8 for recombinant TBK1.

TPCA-1 (Standard) is the analytical standard of TPCA-1 (HY-10074). This product is intended for research and analytical applications. TPCA-1 is a potent and selective inhibitor of IKK-2 with IC50 of 17.9 nM. TPCA-1 is an effective inhibitor of STAT3 phosphorylation, DNA binding, and transactivation.

H-Val-Tyr-OH is an endogenous metabolite.

IKK 16 (Standard) is the analytical standard of IKK 16. This product is intended for research and analytical applications. IKK 16 hydrochloride is an orally active IKK inhibitor. IKK 16 hydrochloride shows IC₅₀s of 40 nM, 70 nM, 200 nM, and 50 nM for IKK2, IKK complex, IKK1, and LRRK 2, respectively. IKK 16 hydrochloride is also a pan-PKD inhibitor, inhibiting PKD1, PKD2, and PKD3 with IC₅₀s of 153.9, 115, and 99.7 nM, respectively. IKK 16 hydrochloride is also an ABCB1 inhibitor, interfering with the binding of ABCB1 to its substrates. IKK 16 hydrochloride protects against LPS (HY-D1056)-induced multiple organ dysfunction by reducing the acute inflammatory response induced by endotoxin exposure. IKK 16 hydrochloride can restore renal function and alleviate fibrosis in acute kidney injury. IKK 16 hydrochloride attenuates cardiac dysfunction associated with polymicrobial sepsis in mice with type 2 diabetes mellitus (T2DM) by inhibiting the NF-κB pathway.

BMS-345541 (Standard) is the analytical standard of BMS-345541 (HY-10519). This product is intended for research and analytical applications. BMS-345541 is a selective inhibitor of the catalytic subunits of IKK (IKK-2 IC₅₀=0.3 μM, IKK-1 IC₅₀=4 μM). BMS-345541 binds at an allosteric site of IKK.

BMS-345541 hydrochloride (Standard) is the analytical standard of BMS-345541 hydrochloride (HY-10518). This product is intended for research and analytical applications. BMS-345541 hydrochloride is a selective inhibitor of the catalytic subunits of IKK (IKK-2 IC₅₀=0.3 μM, IKK-1 IC₅₀=4 μM). BMS-345541 binds at an allosteric site of IKK.

Ruberythric acid is a natural product found in madder (Rubia tinctorum). Acid treatment induces hydrolysis of Ruberythric acid, producing pentose-containing sugar residues and alizarin. Ruberythric acid inhibits stimulus-induced phosphorylation of IKK, IκBα and p65 in the NF-κB pathway, regulates tight junction integrity, suppresses stimulus-induced MLCK activation and myosin light chain phosphorylation, reduces tight junction disruption associated with cytoskeletal contraction, alleviates stimulus-induced increase in intestinal permeability, and prevents stimulus-induced redistribution of tight junction proteins. Ruberythric acid forms red salts when dissolved in alkali and can be used as a dye. Ruberythric acid is applicable to research related to inflammatory bowel disease.

NF-κB-IN-22 is an inhibitor targeting IKKβ, IκBα and NF-κB p65. NF-κB-IN-22 selectively inhibits the proliferation, migration and invasion of various cancer cells, arrests the cell cycle, and suppresses tumor growth in vivo, while exhibiting low toxicity to normal cells. NF-κB-IN-22 induces DNA damage, ROS production and apoptosis through endoplasmic reticulum stress and mitochondrial apoptotic pathways. NF-κB-IN-22 inhibits the phosphorylation of IKKβ, IκBα and NF-κB p65, blocks the NF-κB signaling pathway, and suppresses the nuclear translocation of NF-κB p65. NF-κB-IN-22 reverses the resistance to cisplatin (HY-17394). NF-κB-IN-22 can be used in research related to lung cancer, gastric cancer and liver cancer.

GS143 (Standard) is the analytical standard of GS143 (HY-110261). This product is intended for research and analytical applications. GS143 is a selec-tive IκBα ubiquitination inhibitor with an IC₅₀ of 5.2 μM for SCFβTrCP1-mediated IκBα ubiquitylation. GS143 sup-presses NF-κB acti-va-tion and tran-scrip-tion of tar-get genes and does not inhibit proteasome activity. GS143 has anti-asthma effect.

LASSBio-1829 hydrochloride is an orally active IKK2 inhibitor with an IC₅₀ of 3.8 μM against the human target (Sf21 cells). LASSBio-1829 hydrochloride blocks signal transduction of the inflammation-associated NF-κB activation pathway. LASSBio-1829 hydrochloride reduces leukocyte migration, TNF-α biosynthesis, ROS production and NO production. LASSBio-1829 hydrochloride exhibits anti-inflammatory activity in a carrageenan-induced subcutaneous air pouch mouse model. LASSBio-1829 hydrochloride alleviates licking behavior during the inflammatory phase of the mouse formalin test. LASSBio-1829 hydrochloride can be used in inflammation-related research.

IMD-0354 (Standard) is the analytical standard of IMD-0354. This product is intended for research and analytical applications. IMD-0354 (IKK2 Inhibitor V) is a selective IKKβ inhibitor which inhibits NF-κB activity. IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC50 of 1.2 uM.

SC-514 (Standard) is the analytical standard of SC-514. This product is intended for research and analytical applications. SC-514 is a selective IKK-2 inhibitor (IC50=11.2 μM), which does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases.