NF-κB Modulator

α-MSH (11-13) (ACTH-(11-13)) is a C-terminal tripeptide of α-MSH that can cross the blood-brain barrier. α-MSH (11-13) exhibits antipyretic, anti-inflammatory, and antibacterial activities. α-MSH (11-13) also exerts neuroprotective effects after traumatic brain injury by inhibiting excessive activation of microglia and reducing neuronal apoptosis. α-MSH (11-13) can be used in research related to traumatic brain injury, fever, and bacterial infections.

IMD-catechol is a novel imidazoquinolinone-NF-κB immunomodulator dimer that improves efficacy in a CT26 mouse colon carcinoma tumor model while eliciting minimal adjuvant toxicity.

IMD-biphenylA is a novel imidazoquinolinone-NF-κB immunomodulator dimer that improves the adjuvanticity of small molecule immune potentiators.

IMD-biphenylB is a potent imidazoquinolinone-NF-κB immunomodulator dimer that inhibits tumor proliferation while induces low systemic inflammation and reduces adjuvant toxicity.

IMD-vanillin is a novel imidazoquinolinone-NF-κB immunomodulator dimers.

Nepetoidin B, an anti-inflammatory agent, inhibits inflammation by modulating the NF-κB and Nrf2/HO-1 signaling pathways. Nepetoidin B also has antifungal and antibacterial activity. Nepetoidin B is a natural product that can be obtained from Salvia plebeia R. Br. Nepetoidin B can be used in anti-inflammatory and anti-infectious research.

IKKβ-IN-6 is an antitumor agent. IKKβ-IN-6 inhibits IKKβ (IC₅₀: 18.24 μM), thereby suppressing the phosphorylation of p65 and IκBα, blocking the nuclear translocation of p65, and subsequently regulating genes controlled by NF-κB. IKKβ-IN-6 also targets topoisomerase I (Topo I), induces DNA damage, ROS accumulation, loss of mitochondrial membrane potential, and S-phase arrest. IKKβ-IN-6 is applicable to related research on colorectal cancer.

Cudraflavone B is a prenylated flavonoid with anti-inflammatory and anti-tumor properties. Cudraflavone B is also a dual inhibitor of COX-1 and COX-2. Cudraflavone B blocks the translocation of nuclear factor κB (NF-κB) from the cytoplasm to the nucleus in macrophages. Thus, Cudraflavone B inhibits tumor necrosis factor α (TNFα) gene expression and secretion. Cudraflavone B also triggers the mitochondrial apoptotic pathway, activates NF-κB, the MAPK p38, and ERK, and induced the expression of SIRT1. Thus Cudraflavone B inhibits the growth of human oral squamous cell carcinoma cells.

Beloranib (ZGN-440; CKD-732 free base) hemioxalate is a selective, irreversible inhibitor of methionine aminopeptidase MetAP2 that suppresses appetite and increases energy expenditure. Beloranib hemioxalate blocks the enzymatic cleavage of N-terminal methionine from nascent proteins by forming a covalent bond with MetAP2, thereby regulating fatty acid metabolism, adrenergic signaling, and hypothalamic NF-κB expression. Beloranib hemioxalate significantly reduces food intake, body weight, and fat accumulation, while improving glucose tolerance, insulin sensitivity, and lipid metabolism. Beloranib hemioxalate also elevates energy expenditure and fat oxidation levels, without affecting body temperature, spontaneous activity, or the inflammatory cytokine IL-1β. Beloranib hemioxalate can be used in research on obesity and hypothalamic obesity.

IMD-ferulic is a covalently linked NF-κB modulator that improves the adjuvanticity of small molecule immune potentiators.

TC-E 5003 (Standard) is the analytical standard of TC-E 5003 (HY-107574). This product is intended for research and analytical applications. TC-E 5003 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC₅₀ of 1.5 µM against hPRMT1. TC-E 5003 modulates the lipopolysaccharide (LPS) (HY-D1056)-induced AP-1 and NF-κB signaling pathways with anti-inflammatory properties. TC-E 5003 also upregulates the expression of Ucp1 and Fgf21, activates protein K_inase A signaling and lipolysis in primary subcutaneous adipocytes from both mouse and humans. TC-E 5003 is promising for research of obesity and associated metabolic disorders, oxidative stress, inflammation and cancers.

GQ-16 (Standard) is the analytical standard of GQ-16 (HY-111254). This product is intended for research and analytical applications. GQ-16 is an orally active PPARγ partial agonist with an IC₅₀ of 1.84 μM and a K_i of 160 nM against human PPARγ. GQ-16 inhibits Cdk5-mediated Ser-273 phosphorylation. GQ-16 improves insulin sensitivity and glucose tolerance in obese and diabetic mice. GQ-16 also exhibits certain cytotoxicity against tumor cells. GQ-16 can be used in research related to obesity, diabetes and cancer.

Benzylurea (Standard) is the analytical standard of Benzylurea (HY-W010253). This product is intended for research and analytical applications. Benzylurea is a benzylamide. Benzylurea is an anti-inflammatory agent. Benzylurea inhibits LPS (HY-D1056)-induced upregulation of MTCH2 expression and regulates pathways associated with mitochondrial function, inflammation and cell survival. Benzylurea alleviates LPS-induced proliferation inhibition and apoptosis of periodontal ligament fibroblasts, as well as the release of proinflammatory cytokines. Benzylurea can be used in studies related to periodontitis.

17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-docosapentaenoic acid (17-Oxo-DPA; 17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-DPA) is an electrophilic oxo-derivative (EFOX) of the docosahexaenoic acid (DHA) (HY-B2167). 17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-docosapentaenoic acid is generated during inflammation by COX-2-catalyzed mechanism in activated macrophages. 17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-docosapentaenoic acid acts as an agonist for PPARγ and a modulator for NF-κB signaling pathway, inhibits the production of pro-inflammatory cytokines and nitric oxide, and exhibits anti-inflammatory efficacy.