p38 MAPK

p38-α MAPK-IN-8 (Compound 13) is a lipophilic cationic derivative. p38-α MAPK-IN-8 is cytotoxic to various tumor cells, and can induce cell cycle arrest, apoptosis, increase reactive oxygen species (ROS) production, and induce mitochondrial membrane potential depolarization. The antitumor activity of p38-α MAPK-IN-8 may be related to p38α MAPK pathway, which can be used in the study of cancer.

Hordenine sulfate (Ordenina sulfate; Peyocactine sulfate) is a multifunctional alkaloid with oral activity and blood-brain barrier penetration. Hordenine sulfate inhibits LPS-induced phosphorylation of p38, JNK, ERK1/2, p65, IκB, and AKT, prevents p65 nuclear translocation, and suppresses inflammatory cytokines and mediators. Hordenine sulfate promotes M2 macrophage polarization, restores blood-milk barrier integrity, alleviates oxidative stress by reducing ROS and MDA, and attenuates LPS-induced lung injury and pulmonary edema. Hordenine sulfate inhibits cAMP production, CREB phosphorylation, and MITF expression, thereby suppressing melanin synthesis in melanocytes and reconstructed epidermis. Hordenine sulfate activates the Wnt/β-catenin signaling pathway, promotes dermal papilla cell proliferation and hair shaft elongation, and accelerates hair regeneration. Hordenine sulfate activates DRD2, acts as a D3R partial agonist, α2A-AR full agonist, and 5-HT2A-R antagonist, and inhibits SERT and DAT. Hordenine sulfate inhibits α-synuclein accumulation and ameliorates motor deficits in Parkinson's disease models. Hordenine sulfate limits alcohol intake, reduces relapse drinking behavior, and modulates alcohol-induced conditioned place preference. Hordenine sulfate can be used for research on mastitis, skin pigmentation, acute lung injury, foodborne diseases, hair loss, Parkinson's disease, bacterial infections, and alcohol use disorder.

Anti-inflammatory agent 74 (B5) is an anti-inflammatory agent that can inhibit NO, IL-6, and TNF-α, with IC₅₀ values of 10.88 μM and 4.93 μM for NO and IL-6, respectively. Anti-inflammatory agent 74 alleviates acute lung injury (ALI) by regulating inflammatory mediators and inhibiting the MAPK and NF-κB signaling pathways.

JNK3 inhibitor-5 (Compound 22b) is a potent and selective JNK3 inhibitor with an IC₅₀ of 0.379 nM. JNK3 inhibitor-5 effectively protects the neuronal cells against amyloid beta-induced apoptosis. JNK3 inhibitor-5 has a high cell permeability and is predicted as BBB permeable.

Anti-inflammatory agent 102 (Compound 11a) is an orally active anti-inflammatory agent. Anti-inflammatory agent 102 exerts its anti-inflammatory effect by blocking the activation of the ASK1/p38 MAPKs/NF-κB signaling pathway. Anti-inflammatory agent 102 has significant anti-inflammatory activity and can inhibit the release of NO, ROS, and inflammatory factors (such as IL-6, TNF-α, IL-1β). Anti-inflammatory agent 102 can be used in the study of inflammatory diseases such as ulcerative colitis (UC).

P38-α MAPK-IN-11 (Compound 4C) is a selective inhibitor of P38α MAPK that can cross the blood-brain barrier with an IC₅₀ value of 43 nM. P38-α MAPK-IN-11 has extremely low inhibitory activity against other MAPK subtypes, namely p38β, p38γ, and p38δ, with IC₅₀ values of > 100 nM, > 100 nM, and 48.6 mM respectively. P38-α MAPK-IN-11 exhibits outstanding neuroprotective effects and anti-neuroinflammatory effects in Alzheimer's disease-like rat models. P38-α MAPK-IN-11 can be used for the study of Alzheimer's disease.

KAI-11101 is the inhibitor for dual leucine zipper kinase (DLK, MAP3K12) with a K_i of 0.7 nM. KAI-11101 inhibits Paclitaxel (HY-B0015)-induced cJun phosphorylation (IC₅₀=95 nM) and thus inhibits the activation of MAPK pathway. KAI-11101 is blood brain barrier penetrable and can be further investigated for its neuroprotective property.

p38 MAP Kinase-IN-3 is a p38 MAP kinase inhibitor (IC₅₀ = 0.09 µM). p38 MAP Kinase-IN-3 can be used for research on metabolic conditions.

Vacquinol-1 (NSC13316) is a MKK4-specific activator that activates the MAPK pathway. Vacquinol-1 inhibits the growth, migration and colony formation, and induces apoptosis of cancer cells. Vacquinol-1 is applicable to research related to cancers such as hepatocellular carcinoma.

LC-SF-14 is a selective dual inhibitor of SHP2 and FGFR (IC₅₀ values are 71.6 and 8.9 nM, respectively). LC-SF-14 inhibits FGFR2-FRS2α-SHP2-MAPK signaling and ERK phosphorylation. LC-SF-14 inhibits the proliferation of KATOIII cancer cells (IC₅₀: 9.2 nM). LC-SF-14 has antitumor activity in the SNU-16 xenograft mouse model. LC-SF-14 can be used in FGFR2-driven gastric cancer research.

Macranthoin G is an inhibitor of p38 MAPK. Macranthoin G protects the cytotoxicity induced by Aβ or hydrogen peroxide in neuronal cells by downregulating p38 MAPK. Macranthoin G can used in study Alzheimer’s Disease.

Kukoamine B (Standard) is the analytical standard of Kukoamine B. This product is intended for research and analytical applications. Kukoamine B, a spermine alkaloid, is a potent dual LPS and CpG DNA inhibitor with K_d values of 1.23 µM and 0.66 µM, respectively. Kukoamine B exerts anti-inflammatory, anti-diabetic, anti-oxidant, anti-osteoporotic and neuroprotective effects. Kukoamine B has the potential for the study of sepsis.

Lumichrome (Standard) is the analytical standard of Lumichrome. This product is intended for research and analytical applications. Lumichrome, a photodegradation product of Riboflavin, is an endogenous compound in humans. Lumichrome inhibits human lung cancer cell growth and induces apoptosis via a p53-dependent mechanism. Lumichrom is the inhibitor for AKT/β-catenin signaling pathway. Lumichrom is the inhibitor for AKT/β-catenin signaling pathway.

p38 MAPK-IN-8 (Compound 8) is an orally active, potent and selective p38 mitogen-activated protein kinase (p38 MAPK) inhibitor. p38 MAPK-IN-8 is promising for research of inflammatory responses, autoimmune diseases, and cancer.

Methylcarbamyl PAF C-8 is resistant to the degradation function of platelet-activating factor acetylhydrolase (PAF-AH). It has a half-life of more than 100 minutes in platelet-poor plasma and possesses the activity of inducing platelet aggregation. In NRK-49 cells overexpressing the PAF receptor, Methylcarbamyl PAF C-8 can induce the expression of c-myc and c-fos, and activate mitogen-activated protein kinase (MAPK). Additionally, Methylcarbamyl PAF C-8 can induce cell cycle arrest in the G1 phase. Methylcarbamyl PAF C-8 holds promise for research in the fields of cardiovascular diseases and anti-cancer therapy.

The mitogen-activated protein kinase kinase 6 (MKK6) is one of the upstream activators of p38 MAPK. MKK6 activates myocardial cell NF-κB and inhibits apoptosis in a p38 MAPK-dependent manner. MKK6 SDTD is a mutant of MKK6. MKK6 SDTD Recombinant Human Active Protein Kinase is a recombinant MKK6 SDTD protein that can be used to study MKK6 SDTD-related functions.

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.

Zaltoprofen sulfoxide (Compound M2) is the main metabolite of Zaltoprofen (HY-B0619). Zaltoprofen sulfoxide is an efficient and selective COX-2 inhibitor (IC₅₀ = 45.38 nM) and a PPAR-γ activator. Zaltoprofen sulfoxide effectively inhibits NF-κB and MAPK inflammatory signaling pathways and alleviates acute lung injury induced by LPS (HY-D1056B3). Zaltoprofen sulfoxide can be used for the study of acute lung injury.

LC-MG-10 is a selective molecular glue degrader targeting FGFR2, with a DC₅₀ of 230.2 nM in KATO III cells. LC-MG-10 induces proteasomal degradation of FGFR2 via a covalent molecular glue mechanism. LC-MG-10 inhibits cancer cell proliferation. LC-MG-10 suppresses FGFR2-mediated PI3K/AKT and MAPK/ERK signaling pathways. LC-MG-10 can be used in studies related to gastric cancer.