IKK

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.

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.

7-Acetoxycoumarin (Acetylumbelliferone) is an anti-inflammatory inhibitor with antibacterial and amoebicidal activities. 7-Acetoxycoumarin reduces the phosphorylation levels of ERK, JNK, NF-κB and p38 MAPK. 7-Acetoxycoumarin downregulates the protein and mRNA expression levels of iNOS and COX-2. 7-Acetoxycoumarin inhibits the production of IL-1β, IL-6, TNF-α, NO and PG₂. 7-Acetoxycoumarin reduces the degradation of IκBα. 7-Acetoxycoumarin can be used in studies related to amoebiasis and Bacillus lentus infection.

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.

IMD-0560 (Standard) is the analytical standard of IMD-0560 (HY-105661). This product is intended for research and analytical applications. IMD-0560 is a novel IκB kinase β inhibitor.

BX795 (Standard) is the analytical standard of BX795 (HY-10514). This product is intended for research and analytical applications. BX795 is a potent and selective inhibitor of PDK1, with an IC₅₀ of 6 nM. BX795 is also a potent and relatively specific inhibitor of TBK1 and IKKε, with an IC₅₀ of 6 and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, and has lower selectivity over PKA, PKC, c-Kit, GSK3β etc. BX795 modulates autophagy.

Nomilin (Standard) is the analytical standard of Nomilin. This product is intended for research and analytical applications. Nomilin is a limonoid compound obtained from the extracts of citrus fruits. Nomilin is an anti-obesity and anti-hyperglycemic agent .

Wilforlide A (Standard) is the analytical standard of Wilforlide A. This product is intended for research and analytical applications. Wilforlide A is a bioactive triterpene isolated from Tripterygium wilfordii Hook f. Wilforlide A has anti-inflammatory and immune suppressive effects.

Dihydroparadol is a iNOS inhibitor with an IC₅₀ of 7.24 μM, and it is found in ginger. Dihydroparadol partially inhibits the catalytic activity of iNOS, blocks the nuclear translocation of NF-κB p65, reduces NF-κB activity, and attenuates lipopolysaccharide-induced degradation of IκB-α, thereby inhibiting NF-κB-mediated iNOS gene expression and protein production. Dihydroparadol inhibits lipopolysaccharide-induced nitric oxide production in macrophages and exhibits anti-inflammatory activity. Dihydroparadol increases ABCA1 protein abundance by elevating mRNA levels and reducing proteasomal degradation, and also increases ABCG1 protein abundance by enhancing protein stability. Dihydroparadol promotes cholesterol efflux from cholesterol-loaded macrophages via apolipoprotein A1-mediated and plasma-mediated pathways. Dihydroparadol inhibits PDGF-induced vascular smooth muscle cell proliferation, shows no cytotoxicity to vascular smooth muscle cells within the tested concentration range, and does not interfere with endothelial cell proliferation. Dihydroparadol can be used in the research of inflammatory diseases, atherosclerosis and cardiovascular diseases.

Pelubiprofen (Standard) is the analytical standard of Pelubiprofen. This product is intended for research and analytical applications. Pelubiprofen is an orally active anti-inflammatory agent that inhibits COX enzyme activity (with IC50 values of 10.66 and 2.88 μM for COX-1 and COX-2, respectively). Pelubiprofen has significant anti-inflammatory and analgesic effects.

Murrayafoline A (Standard) is the analytical standard of Murrayafoline A (HY-W100287). This product is intended for research and analytical applications. Murrayafoline A is a carbazole alkaloid that can be extracted from Murraya tetramera. Murrayafoline A directly targets Specificity protein 1 (Sp1), thereby inhibiting NF-κB and MAPK signaling pathways. Murrayafoline a induces a G0/G1-phase arrest in platelet-derived growth factor (PDGF)-stimulated vascular smooth muscle cells. Murrayafoline A attenuates the Wnt/β-catenin pathway by promoting the degradation of intracellular β-catenin proteins. Murrayafoline A enhances the contraction of rat ventricular myocytes and L-type calcium current by activating protein kinase C. Murrayafoline A inhibits LPS (HY-D1056)-induced neuroinflammation in vivo. Murrayafoline A can be used for the study of inflammation, vascular complications and colon cancer.

PS-1145 (Standard) is the analytical standard of PS-1145. This product is intended for research and analytical applications. PS-1145 is an IκB kinase (IKK) inhibitor with an IC50 of 88 nM.