JNK Inhibitor

Multitarget AD-IN-8 is a blood-brain barrier-penetrant, orally active multitarget inhibitor. Multitarget AD-IN-8 inhibits abnormal Tau phosphorylation at Thr181 and Ser396 sites and attenuates NF-κB phosphorylation. Multitarget AD-IN-8 downregulates BACE1 expression to reduce Aβ production, inhibits the Bax/Bcl-2 pathway, and suppresses Caspase-1 activation. Multitarget AD-IN-8 attenuates p38, ERK1/2, and JNK phosphorylation and inhibits Aβ_25-35-induced Apoptosis. Multitarget AD-IN-8 exhibits neuroprotective effects against Aβ_25-35-induced injury, ameliorates learning and memory deficits in AD mouse models, and alleviates hippocampal neuronal pathological damage. Multitarget AD-IN-8 can be used for research on Alzheimer's disease.

NSC 90469 (Standard) is the analytical standard of NSC 90469. This product is intended for research and analytical applications. NSC 90469 (3,5-Diiodo-L-thyronine) is an orally active thyroid hormone derivative. NSC 90469 inhibits JNK phosphorylation and NF-κB acetylation, blocks SIRT1 protein expression, induces elevated PGC-1α levels, and stimulates COX activity. NSC 90469 enhances UCP1-mediated thermogenesis, increases hepatic Dio1 activity, inhibits TSH levels and hypothalamic-pituitary-thyroid axis function, enhances lipid metabolism, and regulates energy metabolism via the mitochondrial pathway. NSC 90469 prevents blood glucose reduction, reduces urinary albumin excretion, inhibits renal matrix expansion, decreases TGF-β1 expression, and reduces renal fibronectin and type Ⅳ collagen deposition. NSC 90469 also increases energy expenditure and prevents diet-induced overweight. NSC 90469 can be used in studies related to diabetic nephropathy, hypothyroidism, non-alcoholic fatty liver disease, and diet-induced obesity.

Saquinavir mesylate (Standard) (Ro 31-8959/003 (Standard)) is the analytical standard of Saquinavir mesylate (HY-17003). This product is intended for research and analytical applications. Saquinavir (Ro 31-8959) mesylate is an orally active HIV protease inhibitor that can be used in the research of AIDS. Saquinavir mesylate also has anti-inflammatory activity and can induce apoptosis of human red blood cells.

JNK3 inhibitor-8 is a potent, delective, orally active and cross the blood-brain barrier JNK3 inhibitor with IC₅₀ values of 21, 2203, >10000 nM for JNK3, JNK2, JNK1, respectively. JNK3 inhibitor-8 shows significant neuroprotective effects. JNK3 inhibitor-8 has the potential for the research of Alzheimer’s disease (AD).

Chalcomoracin is an orally active anticancer agent. Chalcomoracin exhibits anticancer, antibacterial, and α-glucosidase inhibitory activities, with an IC₅₀ of 14.23 µM against yeast α-glucosidase and an IC₅₀ of 5.5 μM against FabI of Staphylococcus aureus. Chalcomoracin reduces the phosphorylation levels of ERK, JNK, and P38; enhances the phosphorylation level of ERK1/2; regulates the MAPK, mTOR, AKT, and p53 signaling pathways; upregulates the expression of Chop, Bip, PINK1, GRP78, and GADD153; and downregulates the expression of Alix. Chalcomoracin induces apoptosis (apoptosis), endoplasmic reticulum stress (endoplasmic reticulum stress), paraptosis (paraptosis), ROS production, mitophagy (mitophagy), and autophagy (autophagy); it inhibits cancer cell viability, colony-forming ability, migration, invasion, proliferation, tumorigenesis, fatty acid synthesis, S. aureus growth, vitreous-stimulated retinal cell activity, and cell cycle progression at the G0/G1 phase. Chalcomoracin can be used in research related to hepatocellular carcinoma, non-small cell lung cancer, triple-negative breast cancer, prostate cancer, proliferative vitreoretinopathy, pancreatic cancer, diabetes, and bacterial infections.

MAP4K4-IN-6 (Compound 15f) is a MAP4K4 inhibitor (IC₅₀: 80 nM). MAP4K4-IN-6 reduces the c-Jun phosphorylation. MAP4K4-IN-6 has neuroprotective effects. MAP4K4-IN-6 increases the viability of motor neurons. MAP4K4-IN-6 can be used for research of Amyotrophic lateral sclerosis (ALS).

MR2938 is a potent AChE inhibitor, with an IC₅₀ of 5.04 μM. MR2938 also suppresses NO production obviously (IC₅₀ = 3.29 μM). MR2938 suppresses the neuroinflammation through blocking MAPK/JNK and NF-κB signaling pathways. MR2938 can be used for Alzheimer’s disease (AD) research.

JNK3 inhibitor-3 (compound 15g) is a selective, BBB permeable and orally active c-Jun N-terminal kinase 3 (JNK3) inhibitor. JNK3 inhibitor-3 has inhibitory activities to JNK1, JNK2 and JNK3 with IC₅₀ values of 147.8, 44.0 and 4.1 nM, respectively. JNK3 inhibitor-3 significantly improves the memory in mouse dementia model. JNK3 inhibitor-3 can be used for the research of Alzheimer’s disease.

BRAFV600E/JNK-IN-1 (Compound 14c) is an inhibitor of JNK1, JNK2, JNK3 and BRAFV600E, with IC₅₀ values of 0.51 μM, 0.53 μM, 1.02 μM and 0.009 μM, respectively. BRAFV600E/JNK-IN-1 can inhibit the phosphorylation of MEK1/2 and ERK1/2. In addition, BRAFV600E/JNK-IN-1 can inhibit tumor cell proliferation, NO release and PGE2 production, and has anti-tumor and anti-inflammatory activities.

CT1-3 is a potent anticancer agent. CT1-3 induces mitochondria-mediated apoptosis by regulating JNK/Bcl-2/Bax/XIAP pathway. CT1-3 suppresses the epithelial mesenchymal transition (EMT) potential of human cancer cells (HCCs) via regulating the E-cadherin/Snail axis, thus inhibits tumorigenesis. CT1-3 has a strong antitumor effect in mice model and exhibits no significant hepatic and renal toxicity.

MAPK-IN-6 is a blood-brain barrier-permeable MAPK inhibitor. MAPK-IN-6 inhibits oxidative stress-induced activation of the MAPK signaling cascade, including the phosphorylation of ERK1/2, p38 and JNK. MAPK-IN-6 eliminates intracellular reactive oxygen species (ROS) accumulation, stabilizes mitochondrial membrane potential and inhibits cell apoptosis. MAPK-IN-6 can be used for the research of ischemic stroke.

Evariquinone is an anthraquinone compound isolated from the endophytic fungus Colletotrichum sp. JS-0367 of mulberry. Evariquinone possesses direct antioxidant activity. It inhibits excessive phosphorylation of the JNK, ERK1/2 and p38 MAPK signaling pathways by suppressing ROS and Ca²⁺, thereby reducing neuronal apoptosis. Evariquinone can be used to study glutamate excitotoxicity-related neurological disorders (such as Alzheimer's disease, Parkinson's disease, cerebral ischemia, etc.).

N-Acetylgalactosaminyltransferase 4 (GALNT4) is a glycosyltransferase capable of inhibiting the activation of ASK1. By directly binding to ASK1, N-Acetylgalactosaminyltransferase 4 suppresses its N-terminal dimerization and subsequent phosphorylation, leading to robust inactivation of downstream JNK/p38 and NF-κB signals, and thereby improving the prognosis of liver surgery.

Silybin (Silibinin B) (Standard) is the analytical standard of Silybin B (HY-N7046). This product is intended for research and analytical applications. Silybin B (Silibinin B) is an orally active amyloid-β aggregation inhibitor and ATR pathway activator, that can cross the blood-brain barrier. Silybin B inhibits Aβ fibril formation and promotes amorphous aggregate formation, while activating the ATR-mediated DNA damage repair pathway and inhibiting JNK/p38 MAPK signaling. Silybin B can reduce Cisplatin (HY-17394)-induced neuronal DNA damage and apoptosis. Silybin B has anti-oxidative stress, cell cycle regulation and neuroprotective activities. Silybin B is mainly used in the study of Alzheimer's disease and Cisplatin chemotherapy-related neurotoxicity.

SP600125 (GMP) is SP600125 (HY-12041) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. SP600125 is an orally active, reversible, and ATP-competitive JNK inhibitor with IC₅₀s of 40, 40 and 90 nM for JNK1, JNK2 and JNK3, respectively. SP600125 is a potent ferroptosis inhibitor. SP600125 induces the transformation of bladder cancer cells from autophagy to apoptosis.

JNK2/3-IN-1 (Compound 56d) is an irreversible covalent inhibitor of c-Jun N-terminal kinases 2/3 (JNK2/3) with IC₅₀ values of 830 and 1909 nM, respectively. JNK2/3-IN-1 is promising for research of neurodegenerative diseases (e.g., Parkinson’s, Alzheimer’s) and fibrotic disorders.

JNK3-IN-10 is a blood-brain barrier-impermeable JNK3 inhibitor (IC₅₀=0.257 nM) with over 400-fold selectivity over JNK1. JNK3-IN-10 blocks the JNK3-mediated signaling pathway downstream of TGF-β₁, inhibits TGF-β₁-induced phosphorylation of c-Jun, reduces the expression of pro-fibrotic markers, and restores the expression of the epithelial protein E-cadherin. JNK3-IN-10 exhibits low cytotoxicity, anti-fibrotic, cytoprotective and renoprotective effects, and alleviates albuminuria, glomerulosclerosis and podocyte foot process fusion. JNK3-IN-10 can be used for the research of chronic kidney disease, glomerulosclerosis and adriamycin-induced nephropathy.

Viridicatol (Standard) is the analytical standard of Viridicatol (HY-116474). This product is intended for research and analytical applications. Viridicatol is a quinolone alkaloid with anti-inflammatory, antibacterial, antifungal, osteogenic and chondrogenic activities. Viridicatol reduces the phosphorylation levels of ERK, JNK, p38 and STAT6; inhibits MMP-2, MMP-9, NF-κB signaling pathway and PTP1B; downregulates genes related to mast cell activation; and binds to SHN3 to activate the Wnt/SHN3 signaling pathway. Viridicatol inhibits the expression of pro-inflammatory mediators and cytokines, and promotes osteogenic/chondrogenic differentiation. Viridicatol can be used in studies related to fibrosarcoma, allergy, bacterial infection, fungal infection and osteoporosis.

Tau Protein Phosphorylation-IN-1 is a tau protein phosphorylation inhibitor that potently protects PC12 cells against Aβ_25–35-induced cytotoxicity (EC₅₀ = 1.93 μM), and can penetrate the blood-brain barrier (BBB).Tau Protein Phosphorylation-IN-1 reverses the hyperphosphorylation of tau, significantly inhibits the expression of certain immune-related cytotoxic factors, suppresses the MAPK and NF-κB signaling pathways, and significantly inhibits the expression of RAGE and the apoptosis factors Bax/Bcl-2, both in vitro and in vivo. Tau Protein Phosphorylation-IN-1 relieves nerve damage, and improves learning and memory in an Alzheimer’s disease (AD) mouse model. Tau Protein Phosphorylation-IN-1 can be used for AD research.

Hydrostatin-TL1 (H-TL1), a nine-amino-acid peptide, is a TNF-α antagonist. Hydrostatin-TL1 can be isolated from the venom gland of sea snake Hydrophis cyanocinctus. H-TL1 competitively inhibits the interaction between TNF-α/TNFR1 and attenuates the cytotoxicity and inflammation of TNF-α. Hydrostatin-TL1 can be used for TNF-α-associated inflammatory diseases, such as rheumatoid arthritis, osteoporosis and inflammatory bowel disease (IBD) research.