NF-κB Inhibitor

Diminazene is an antiparasitic agent widely used to treat parasitic diseases caused by hemoparasites (such as trypanosomes and babesia). Diminazene acts as an ACE2 activator and exerts cardiovascular protective effects by activating the ACE2/Ang-(1-7)/Mas receptor axis. By regulating gut microbiota-tryptophan metabolism, Diminazene inhibits the activation of core inflammatory signaling pathways including MAPK, STAT and NF-κB, increases central 5-HT levels, and suppresses splenic TNF-α production, thereby alleviating systemic inflammation.

Cloricromen (Cloricromene) hydrochloride is an orally active platelet inhibitor. Cloricromen hydrochloride inhibits thromboxane B₂ release, β-thromboglobulin, and thrombus formation. Cloricromen hydrochloride inhibits LPS (HY-D1056)-induced NF-κB activation, oxidative activity, and TNF-α expression. Cloricromen hydrochloride exhibits protective activity in animal models of shock and peripheral ischaemia. Cloricromen hydrochloride can be used for the research of myocardial ischaemia/reperfusion injury, and ischaemic cerebrovascular disease.

Taurodeoxycholate sodium salt (Standard) is a bile salt (Standard)-related anionic detergent. Taurodeoxycholate sodium salt (Standard) is formed in the liver by conjugation of deoxycholate with Taurine (HY-B0351). Taurodeoxycholate sodium salt (Standard) is used for isolation of membrane proteins including inner mitochondrial membrane proteins. Taurodeoxycholate (TDCA) exhibits anti-inflammatory and neuroprotective effects.

Cromolyn disodium (Standard) (Cromoglycate disodium (Standard)) is the analytical standard of Cromolyn disodium (HY-B0320A). This product is intended for research and analytical applications. Cromolyn (Cromoglycate) disodium is an orally active GSK-3β inhibitor with an IC₅₀ of 2.0 μM. Cromolyn disodium is also a mast cell stabilizer that can inhibit the release of mediators from mast cells, regulate reflex bronchoconstriction, and reduce non-specific bronchial hyperreactivity, and Cromolyn disodium can be used in the research of bronchial asthma. In addition, Cromolyn disodium has multiple activities such as anti-inflammatory, anti-allergic, anti-histamine, anti-cancer, and neuroprotective effects.

Grossamide is a natural product that can be isolated from fructus cannabis, the dried fruit of Cannabis sativa L.. Grossamide has anti-neuroinflammatory effects.

Gliquidone-d₆ (AR-DF 26-d₆) is the deuterated-labeled Gliquidone (HY-B1114). Gliquidone can bind to the pancreatic β-cells and increases insulin release to regulate blood glucose levels. Gliquidone significantly decreases LPS (HY-D1056)-induced proinflammatory responses and inhibits ERK/STAT3/NF-κB phosphorylation in BV2 microglial cells. Gliquidone can suppress microgliosis, microglial hypertrophy mediated by LPS, and proinflammatory cytokine COX-2 and IL-6 levels in murine model. Gliquidone also exhibits good anticancer activity in lung carcinoma cells. Gliquidone has antioxidant property. Gliquidone can be studied in research for type 2 diabetes and cancers.

Demethyleneberberine is a blood-brain barrier-permeable antioxidant. Demethyleneberberine exerts antioxidant effects by targeting mitochondria, activates the AMPK signaling pathway to regulate lipid metabolism, and inhibits inflammation-related pathways such as NF-κB and MAPK. Demethyleneberberine can be used in the research of inflammatory and other diseases.

Cupabimod is a decoy oligodeoxynucleotide for transcription factor NF-κB.

Azadirachtin (Standard) is the analytical standard of Azadirachtin. This product is intended for research and analytical applications. Azadirachtin, one of the most promising botanical insecticides, is widely used for pest control. Azadirachtin induces apoptosis in insect cell lines, including Sf9, SL-1 and BTI-Tn-5B1-4.

TIC10g is a dual inhibitor for toll-like receptor 7 and 9 (TLR7 and TLR9), which inhibits TLR7 and TLR9 mediated TNF-α release in mouse macrophages (IC₅₀ is 14.5 μM and 6.5 μM) and human B lymphocytes (IC₅₀ is 7.69 μM and 11.5 μM). TIC10g inhibits the activation of NF-κB and MAPK, and exhibits anti-inflammatory activity against systemic lupus erythematosus and rheumatoid arthritis .

Avarol is a sesquiterpene hydroquinone that can be isolated from Dysidea avara sponge. Avarol has the potential for the research of ehrlich carcinoma (EC) and cervical cancer (CC-5).

Z-Val-Arg-Pro-DL-Arg-Fluoromethylketone TFA is an irreversible MALT1 protein inhibitor. Z-Val-Arg-Pro-DL-Arg-Fluoromethylketone TFA inhibits the growth and invasion of diffuse large B-cell lymphoma by inhibiting MALT1-induced NF-κB activation and MMP expression.

Tryptanthrin (Standard) is the analytical standard of Tryptanthrin. This product is intended for research and analytical applications. Tryptanthrin is an indole quinazoline that could be an alkaloid from indigo-bearing plants. Tryptanthrin is a potent and orally active cellular Leukotriene (LT) biosynthesis inhibitor. Tryptanthrin has anticancer activity. Tryptanthrin suppresses the expression levels of NOS1, COX-2, and NF-κB and regulates the expression levels of IL-2, IL-10, and TNF-α.

Tamtuvetmab (AT-005) is a caninised blontuvetmab against CD52. Tamtuvetmab increases progression-free survival (PFS), exhibits in vivo efficacy in dogs with naïve T-cell lymphoma (LSA). Tamtuvetmab has been approved by veterinary.

Norbergenin is a polyphenolic isocoumarin derivative. Norbergenin acts as a non-competitive inhibitor of bovine adrenal tyrosine hydroxylase (TH) with a K_i value of 69.6 μM. Norbergenin inhibits lipopolysaccharide-induced inflammatory responses in macrophages by suppressing the activation of NF-κB, MAPK and STAT3, as well as blocking metabolic reprogramming. Norbergenin inhibits aluminum chloride-induced oxidative stress and apoptosis and restores neurocognitive parameters. Norbergenin scavenges ROS through multiple mechanisms and protects cell membranes from lipid peroxidation damage. Norbergenin can be used in research related to Alzheimer's disease, peptic ulcer and arthritis.

Arctiin (Standard) is the analytical standard of Arctiin. This product is intended for research and analytical applications. Arctiin is an orally active inhibitor of NF-κB. Arctiin suppresses cyclin D1 protein expression in human tumor cells. Arctiin also reduces malondialdehyde and pro-in?ammatory cytokines levels. Arctiin can used in study glomerulonephritis.

γ-Tocotrienol (Standard) is the analytical standard of γ-Tocotrienol. This product is intended for research and analytical applications. γ-Tocotrienol is an active form of vitamin E. γ-tocotrienol reverses the multidrug resistance (MDR) of breast cancer cells through the signaling pathway of NF-κB and P-gp. γ-Tocotrienol is also a novel radioprotector agent, can mitigate bone marrow radiation damage during targeted radionuclide treatment.

BIZ 114 (Example 11) is a fatty acid derivative and potent inhibits the TNF-α activated NF-κΒ pathway. BIZ 114 has the potential to prevent and / or treat ophthalmic disorders such as retinal degenerative disorders and ocular inflammatory diseases.

Lidocaine (GMP) is Lidocaine (HY-B0185) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Lidocaine inhibits sodium channels involving complex voltage and using dependence. Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative and has potential for the research of ventricular arrhythmia.

Herbimycin A is an antibiotic and protein tyrosine kinase inhibitor. Herbimycin A directly inhibits the autophosphorylation of p210 BCR-ABL with an IC₅₀ of approximately 5 μM, and reduces Src kinase activity. Herbimycin A also induces the degradation of receptor tyrosine kinases such as insulin-like growth factor 1 receptor (IGF-1R), insulin receptor (IR) and epidermal growth factor receptor (EGFR) via the ubiquitin-20S proteasome pathway. Herbimycin A directly modifies NF-κB p50, with the main target site involving Cys62, thereby blocking the DNA binding of p50 and NF-κB-driven gene expression. Herbimycin A can be used in studies related to tyrosine kinase signaling, chronic myeloid leukemia, NF-κB signaling, osteoclast function, apoptosis and cellular stress.