p38 MAPK Inhibitor

p38-α MAPK-IN-9 (Compound 25a) is a p38-α MAPK inhibitor (K_i: 0.057 nM). p38-α MAPK-IN-9 inhibits LPS (HY-D1056) induced TNFα production in hPBMCs (IC₅₀: 18 nM).

Pexmetinib hydrochloride (ARRY-614 hydrochloride) is an orally active dual Tie-2 and p38 MAPK inhibitor. Pexmetinib hydrochloride binds to Tie-2 and p38 MAPK in a "DFG-out" conformation, attenuates the phosphorylation of p38, inhibits STAT3 activation, reduces the promoter-binding activity of NFATc1, and decreases the expression of MMPs. Pexmetinib hydrochloride inhibits leukemia cell proliferation, abrogates TNF-α-mediated myelosuppression of healthy hematopoietic stem cells, stimulates hematopoiesis in primary myelodysplastic syndrome (MDS) samples, inhibits RANKL-induced osteoclast formation and bone resorption, and suppresses migration, invasion and induced osteolysis of breast cancer cells. Pexmetinib hydrochloride can be used in research related to myelodysplastic syndrome, acute myeloid leukemia and breast cancer-induced osteolysis.

RANKL-IN-2 is an orally active RANKL inhibitor with K_d values of 3.21 μM and 4.625 μM in the SPR and MST assays, respectively. RANKL-IN-2 binds to RANKL to interfere with RANKL-RANK interaction. RANKL-IN-2 suppresses osteoclastogenesis by inhibiting ROS, MAPK and NF-κB pathways. RANKL-IN-2 inhibits osteoclastogenesis via inhibition of RANKL-induced osteoclast formation, bone resorption, and osteoclast-specific gene and protein expressions in vitro.RANKL-IN-2 prevents bone loss in ovariectomized osteoporosis mice.RANKL-IN-2 can be used for the research of osteoporosis.

Ceftiofur-d₃ sodium is deuterium labeled Ceftiofur sodium (HY-B0898). Ceftiofur sodium is a cell wall synthesis inhibitor that targets bacterial penicillin-binding proteins (PBPs) and has anti-inflammatory effects in endotoxemia. Ceftiofur sodium exerts bactericidal effects by inhibiting the synthesis of bacterial cell wall peptidoglycan, leading to bacterial cell lysis. Ceftiofur sodium also inhibits the activation of NF-κB and MAPKs, thereby reducing the secretion of pro-inflammatory cytokines such as TNF-α, IL-1β, and IL-6.

Tropisetron-d₅ (SDZ-ICS-930-d₅ (free base)) is deuterium labeled Tropisetron. Tropisetron (SDZ-ICS-930 free base) is an orally active anti-inflammatory and antiemetic agent. Tropisetron is 5-HT₃R antagonists with a K_i of 5.3 nM. Tropisetron is also a partial agonist of α7 nicotinic receptor (α7 nAChR) with an EC₅₀ of 1.3 μM. In addition, Tropisetron has antitumor and neuroprotective effects.

PH-797804 (Standard) is the analytical standard of PH-797804 (HY-10403). This product is intended for research and analytical applications. PH-797804 is a ATP-competitive, selective p38α/p38β inhibitor (IC₅₀=26 nM and Ki=5.8 nM for p38α; Ki=40 nM for p38β) and does not inhibit JNK2.

5-O-Methylvisammioside (4'-O-β-D-Glucosyl-5-O-methylvisamminol) (Standard) is the analytical standard of 5-O-Methylvisammioside. This product is intended for research and analytical applications. 5-O-Methylvisammioside is an orally active natural chromone glycoside and multiple biological activities. 5-O-Methylvisammioside inhibits ferroptosis by activating the Nrf2/HO-1 signaling axis. 5-O-Methylvisammioside alleviates intestinal barrier damage by inhibiting the ROS/NF-κB/NLRP3 pathway. 5-O-Methylvisammioside exerts a protective effect against acute liver injury by reducing ALT/AST, decreasing inflammatory infiltration, and inhibiting IκB-α phosphorylation and NF-κB nuclear translocation. 5-O-Methylvisammioside blocks the HMGB1/RAGE/MEK/ERK signaling axis to exert anti-tumor and anti-angiogenic effects. 5-O-Methylvisammioside improves depression-like behaviors by inhibiting Src kinase and the NF-κB pathway.

p38 MAP Kinase Inhibitor VI (compound c32) is a p38 MAPK inhibitor with an inhibition rate of 24%.

Cornuside (Standard) is the analytical standard of Cornuside (HY-N0631). This product is intended for research and analytical applications. Cornuside is an iridoid glycoside with anti-allergic, anti-inflammatory, and neuroprotective activities. Cornuside exerts anti-allergic activity by downregulating the p38 MAPK, JNK, and NF-κB signaling pathways, and inhibits IgE-mediated histamine release from mast cells. Cornuside improves cognitive impairment in mice by inhibiting BACE1 activity (IC₅₀ = 55.84 μg/mL) and enhancing ChAT activity. Cornuside inhibits LPS (HY-D1056)-induced inflammatory mediators, including iNOS, COX-2, PGE2, TNF-α, IL-6, and IL-1β, by suppressing NF-κB activation.

Tabersonine hydrochloride is a selective, orally active NLRP3 inhibitor. Tabersonine hydrochloride directly binds to the NACHT domain of NLRP3, inhibiting its ATPase activity and oligomerization, thereby blocking ASC spot formation and caspase-1 activation, and reducing the release of pro-inflammatory cytokines such as IL-1β. Tabersonine hydrochloride also inhibits K63-linked ubiquitination of TRAF6, blocking NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. Tabersonine hydrochloride can inhibit inflammatory responses, induce apoptosis of liver cancer cells through mitochondrial pathways and death receptor pathways, reduce mitochondrial membrane potential, promote cytochrome c release, and activate caspase proteins. Tabersonine hydrochloride is mainly used in the study of NLRP3-driven inflammatory diseases (such as acute lung injury, sepsis, peritonitis) and tumors such as liver cancer.

Acenocoumarol (Standard) is the analytical standard of Acenocoumarol. This product is intended for research and analytical applications. Acenocoumarol is an anticoagulant that functions as a Vitamin K antagonist. Acenocoumarol inhibits MAPK/ERK/JNK signaling pathway, reduces the nuclear translocation of NF-κB p65, activates Akt/GSK3β signaling pathway. Acenocoumarol induces apoptosis in cell A549, arrests cell cycle at S phase.

Vescalagin is a hexahydroxyphenol. Vescalagin is isolable from Camu-camu (Myrciaria dubia) and immature wax apple fruits. Vescalagin exhibits inhibitory activity against a variety of enzymes, with a K_i value of 5.87 nM against AChE, 3.89 nM against BChE, 11.75 nM against hCA I, 16.23 nM against hCA II, and 16.08 nM against α-glucosidase. Vescalagin inhibits hCA I, hCA II and α-glucosidase in a non-competitive manner. Vescalagin downregulates JNK/p38 MAPK to protect pancreatic β-cells and improve insulin secretion in methylglyoxal-treated rats. Vescalagin reduces hyperglycemia and hypertriglyceridemia in rats fed a high-fructose diet. Vescalagin possesses anti-inflammatory and antioxidant properties.

LasB-IN-1 (compound 5f) is a potent and orally active inhibitor of LasB (IC₅₀ = 8.7 μM). LasB-IN-1 effectively attenuates elastase production and biofilm formation by P. aeruginosa while alleviating the inflammatory response through downregulating MAPK and NF-κB pathways. LasB-IN-1 is potential to be a novel anti-infective candidate against drug-resistant infections.

Hederacoside C (Standard) is the analytical standard of Hederacoside C. This product is intended for research and analytical applications. Hederacoside C (Kalopanaxsaponin B) is an ingredient that can be obtained mainly from ivy leaves. Hederacoside C mediates inflammation by inhibiting activation of MAPK/NF-κB and its downstream signaling pathway. Hederacoside C has anti-inflammatory and antibacterial activity.

N-(p-Coumaroyl) Serotonin (Standard) is the analytical standard of N-(p-Coumaroyl) Serotonin (HY-129440). This product is intended for research and analytical applications. N-(p-Coumaroyl) Serotonin is an orally active polyphenol found in safflower seeds with potent anti-inflammatory, antioxidant, and antitumor activities. N-(p-Coumaroyl) Serotonin suppresses NF‑κB, TLR4/MyD88 and MAPK signaling, activates NQO1/HO‑1 pathways, and inhibits pro‑inflammatory cytokines, iNOS and COX‑2 and ROS production. N-(p-Coumaroyl) Serotonin induces S‑phase arrest and apoptosis in glioblastoma cells, reduces atherosclerotic lesions, and alleviates renal and vascular injuries. N-(p-Coumaroyl) Serotonin acts as a vasodilator, regulates calcium dynamics. N-(p-Coumaroyl) Serotonin can be used for the research of neurodegenerative diseases, atherosclerosis, glioblastoma, and acute renal failure.

Pamapimod-d₄ (Ro4402257-d₄) is the deuterium labeled Pamapimod. Pamapimod (Ro4402257) is a potent, selective and orally active p38 MAPK inhibitor with IC₅₀s of 14 nM and 480 nM and Kis of 1.3 nM and 120 nM for p38α and p38β, respectively. Pamapimod has no activity against p38δ or p38γ isoforms. Pamapimod has the potential for rheumatoid arthritis and other autoimmune diseases treatment.

Pulegone (Standard) is the analytical standard of Pulegone (HY-N1500). This product is intended for research and analytical applications. Pulegone is a monoterpene ketone compound widely present in the essential oils of many plants. Pulegone can also be used as a bird repellent. Pulegone has multiple activities such as anti-inflammatory, antibacterial, antifungal, and anti-hyperalgesic effects. Pulegone is particularly effective against bacteria of the Salmonella species.

LY456236 (Standard) is the analytical standard of LY456236 (HY-103566). This product is intended for research and analytical applications. LY456236 is a selective, non-competitive and orally active antagonist of glutamate receptor 1 (mGlu1), which can inhibit phosphatidylinositol hydrolysis with an IC₅₀ of 0.145 μM. LY456236 can also inhibit EGFR, with an IC₅₀ of 0.918 μM. LY456236 has anticonvulsant effects and blocks cell proliferation by inhibiting the MAPK pathway, reversing the anti-apoptotic effect of DHPG (HY-12598A). LY456236 can be used in epilepsy research.

Epimedin B (Standard) (Epmedin B (Standard)) is the analytical standard of Epimedin B (HY-N0259). This product is intended for research and analytical applications. Epimedin B (Epmedin B) is a flavonoid active component found in Epimedium, with oral activity, and exhibits anti-osteoporotic and neuroprotective effects. Epimedin B inhibits RANKL-induced osteoclast differentiation, F-actin ring formation, and mature osteoclast bone resorption, inhibits the phosphorylation of JNK, p38 MAPK, PI3K, and AKT, activates the AMPK-Nrf2 antioxidant pathway, and reduces cellular and mitochondrial ROS. Epimedin B acts on ESR1 and exerts its effects via GPER. Epimedin B alleviates bone loss and improves bone microstructure in vivo, and in Parkinson's models protects dopaminergic neurons and maintains striatal dopamine levels through anti-apoptotic and anti-endoplasmic reticulum stress effects. Epimedin B can be used for research related to osteoporosis, diabetic osteoporosis, and Parkinson's disease.

Multi-kinase-IN-11 (Compound 1a) is a DFG-out conformation-targeted multi-kinase inhibitor, including SRC, LCK, ABL, PYK2, CSK, HCK, P38 and C-KIT. Multi-kinase-IN-11 serves as a scaffold for the preparation of fluorescently labeled binding probes and affinity matrices.