p38 MAPK

Neflamapimod (Standard) is the analytical standard of Neflamapimod (HY-10328). This product is intended for research and analytical applications. Neflamapimod (VX-745) is a potent, blood-brain barrier penetrant, highly selective inhibitor of p38α inhibitor with an IC₅₀ for p38α of 10 nM and for p38β of 220 nM. Neflamapimod (VX-745) possesses anti-inflammatory activity.

(E/Z)-Afatinib (Standard) is the analytical standard of (E/Z)-Afatinib. This product is intended for research and analytical applications. (E/Z)-Afatinib ((E/Z)-BIBW 2992) is the mixture of (E)-Afatinib and (Z)-Afatinib. Afatinib (HY-10261) is an irreversible inhibitor of EGFR, by irreversibly binding to their ATP binding site to block activation of EGFR, HER2, HER4, and EGFRvIII. Afatinib used in co-administration with Temozolomide (HY-17364), potently targeting to EGFRvIII-cMet signaling in glioblastoma cells.

Buloxibutid (AT2 receptor agonist C21) (Standard) is the analytical standard of Buloxibutid (HY-100113). This product is intended for research and analytical applications. Buloxibutid is an orally active, selective angiotensin II type 2 receptor (AT2R) agonist, with a K_i value of 0.4 nM for porcine AT2R. Buloxibutid exerts effects such as vasodilation, anti-inflammation, anti-fibrosis (promoting the expression of collagenase MMP-13) and tissue repair mainly by activating the NO/cGMP pathway, inhibiting the pro-proliferative MAPK signaling, and suppressing the pro-fibrotic TGF-β/Smad pathway as well as the inflammatory NF-κB pathway. Buloxibutid can be used in research related to idiopathic pulmonary fibrosis, hypertension, and systemic sclerosis.

GNE-140 racemate (Standard) is the analytical standard of GNE-140 racemate (HY-100742). This product is intended for research and analytical applications. GNE-140 racemate is a racemic mixture of (R)-GNE-140 (HY-100742A) and (S)-GNE-140 (HY-100742B), and also a tautomer of GNE-140 (HY-118241). GNE-140 racemate is an orally active lactate dehydrogenase inhibitor, with an IC₅₀ of 3 nM against human LDHA and an IC₅₀ of 5 nM against LDHB. GNE-140 racemate reduces the phosphorylation level and total protein expression of p38 MAPK, and inhibits EGF-induced AKT phosphorylation. GNE-140 racemate decreases lactate production, regulates glycolysis, the pentose phosphate pathway and nucleotide biosynthesis, increases extracellular pH, inhibits cell proliferation, migration and invasion, and induces caspase-3 activation and ROS accumulation. GNE-140 racemate can be used in research related to breast cancer, cystic fibrosis and pancreatic cancer.

Anti-osteoporosis agent-11 (compound 3k) is an anti-osteoporosis compound targeting osteoclasts. Anti-osteoporosis agent-11 has the most significant inhibitory effect on osteoclast differentiation, with an IC₅₀ value of 0.36 μM. In addition, Anti-osteoporosis agent-11 inhibits osteoclast formation, bone resorption, and the expression of osteoclast-specific genes by blocking rankl-induced mitogen-activated protein kinase (MAPK) and NF-κB signaling pathways.

Fumaric acid disodium (Standard) is the analytical standard of Fumaric acid disodium (HY-W015883A). This product is intended for research and analytical applications. Fumaric acid disodium is an unsaturated dicarbonic acid, an intermediate product of the citric acid cycle that provides intracellular energy in the form of ATP. Fumaric acid disodium exerts anti-inflammatory effects by inhibiting the NF-κB signaling pathway dependent on p38 MAPK. Fumaric acid disodium can be used in the study of pregnancy-induced hypertension.

Indoprofen (Standard) is the analytical standard of Indoprofen. This product is intended for research and analytical applications. Indoprofen activates AKT-AMPK signaling pathway, inhibits NF-κB/MAPK signaling pathway. Indoprofen exhibits anti-inflammatory and immunomodulatory activities. Indoprofen is orally active.

Pectolinarigenin (Standard) is the analytical standard of Pectolinarigenin. This product is intended for research and analytical applications. Pectolinarigenin is an orally active dual inhibitor of COX-2/5-LOX with anti-inflammatory, antioxidant, antitumor and neuroprotective activities. Pectolinarigenin exerts neuroprotective and anti-inflammatory effects on astrocyte inflammation via the NFκB and MAPK pathways. Pectolinarigenin inhibits LPS-induced phosphorylation of ERK1/2, N-FκB and p38MAPK, directly inhibits the enzymatic activity or binding of COX-2, 5-LOX and HIF-1α, and reduces the level of XIAP. Pectolinarigenin modifies Keap1 to promote nuclear accumulation of Nrf2, induces ARE-mediated antioxidant enzyme expression, and possesses direct free radical scavenging activity. Pectolinarigenin reduces the release of NO, proinflammatory mediators and leukotrienes, and increases the level of IL-10. Pectolinarigenin induces G₂/M cell cycle arrest, apoptosis (Apoptosis) and autophagy (Autophagy) via the PI3K/AKT/mTOR signaling pathway. Pectolinarigenin reduces renal crystal deposition and inhibits melanin synthesis. Pectolinarigenin inhibits inflammation and alleviates allergy in mouse models of inflammation. Pectolinarigenin alleviates renal injury, inflammation and oxidative stress in mice by inhibiting HIF-1α activity. Pectolinarigenin can be used for the research of neurodegenerative diseases, inflammatory/allergic diseases, calcium oxalate nephrocalcinosis, gastric cancer, melasma, post-inflammatory diseases and chloasma.

Malabaricone C is an orally active and noncompetitive sphingomyelin synthase (SMS) inhibitor with IC50 values of 3 μM and 1.5 μM for SMS 1 and SMS 2, respectively. Malabaricone C reduces body weight gain, improves glucose tolerance, and decreases lipid accumulation in the liver, showing significant prevention of high fat diet-induced fatty liver in mice. Malabaricone C has anti-inflammatory effects, which is found in the fruits of Myristica cinnamomea King. Malabaricone C is promising for research of obesity and immunological disorders caused due to hyper-activation of T-cells.

CK1-IN-1 (Standard) is the analytical standard of CK1-IN-1 (HY-111820). This product is intended for research and analytical applications. CK1-IN-1 (Compound 1c) is a casein K_inase 1 (CK1) inhibitor with IC₅₀ values of 15 nM and 16 nM for CK1δ and CK1ε, respectively. CK1-IN-1 inhibits p38α MAPK with an IC₅₀ of 73 nM. CK1-IN-1 can be used to study cardiomyogenesis.

AZD7624 (Standard) is the analytical standard of AZD7624 (HY-103672). This product is intended for research and analytical applications. AZD7624 is an inhaled p38 inhibitor, with potent anti-inflammatory activity.

Balanophonin is an anti-inflammatory and anti-cancer agent. Balanophonin inhibits microglial activation and neurodegeneration via inhibiting activated microglia-induced apoptosis.

Olprinone (Loprinone) Hydrochloride Standard is the analytical standard of Olprinone (Hydrochloride) (HY-14254). This product is intended for research and analytical applications. Olprinone (Loprinone) Hydrochloride is a potent and selective phosphodiesterase 3 (PDE3) inhibitor, with IC₅₀ values of 150, 100, 0.35, and 14 μM against PDE1, PDE2, PDE3, and PDE4, respectively. Olprinone Hydrochloride exerts comprehensive protective effects including anti-inflammatory, antioxidant, and anti-apoptotic activities by elevating intracellular cAMP levels and inhibiting the NF-κB and MAPK signaling pathways. Olprinone Hydrochloride can be used in studies related to lung injury, spinal cord injury, heart failure, myocardial ischemia-reperfusion injury, and cerebral ischemic injury.

CGH 2466 dihydrochloride is an orally active adenosine A1, A2B and A3 receptor antagonist with the IC₅₀ values of 19 nM, 21 nM, and 80 nM respectively. CGH 2466 dihydrochloride inhibits p38 MAPK (IC₅₀ = 187~ 400 nM) and phosphodiesterase type 4D (IC₅₀ = 22 nM). CGH 2466 dihydrochloride displays potent anti-inflammatory effects both in vitro and in vivo, and can be used for research on asthma and chronic obstructive pulmonary disease (COPD).

Saquinavir-¹³C₆ (Ro 31-8959-¹³C₆) is ¹³C labeled Saquinavir (HY-17007). Saquinavir (Ro 31-8959) is an orally active HIV protease inhibitor that can be used in the research of AIDS. Saquinavir also has anti-inflammatory activity and can induce apoptosis of human red blood cells.

Umckalin (Standard) is the analytical standard of Umckalin (HY-N8712). Umckalin is Coumarin (HY-N0709) derivative that exhibits anti-inflammatory properties. Umckalin reduces phosphorylation of p38 MAPK, JNK, and ERK, lowers TNF-α, IL-6, IL-1β, NO, and PGE₂ production. Umckalin can be used for the research of chronic inflammatory diseases.

Nalmefene (Standard) is the analytical standard of Nalmefene. This product is intended for research and analytical applications. Nalmefene is a long acting opioid (MOR and DOR antagonist), and a partial KOR agonist. Nalmefene is used for opioid overdose and alcohol dependence.

Benzyl salicylate (Standard) (NSC 6647 (Standard)) is the analytical standard of Benzyl salicylate (HY-B1556). This product is intended for research and analytical applications. Benzyl salicylate (NSC 6647)?is a salicylic acid benzyl ester. It can be used as a fragrance additive or UV light absorber.

Linderane (Standard) is the analytical standard of Linderane (HY-N0688). This product is intended for research and analytical applications. Linderane is an orally active natural sesquiterpene lactone with blood-brain barrier permeability. Linderane indirectly activates PDE3 by activating ERK/STAT3, thereby inhibiting the cAMP/PKA/CREB signaling pathway and hepatic gluconeogenesis. Linderane protects pancreatic β cells against oxidative damage by inhibiting the activation of the p38 MAPK pathway and activating the Nrf2 pathway. Linderane inhibits cell apoptosis and ameliorates intestinal mucosal inflammation by suppressing the IL-6/JAK/STAT3 signaling pathway. Linderane reduces pain sensitivity and alleviates anxiety-like behaviors by activating cannabinoid receptor 2 (CB2R). Linderane can be used in studies related to type 2 diabetes, ulcerative colitis, and chronic inflammatory pain with anxiety.

p38 Kinase inhibitor 8 (Compound CCLXXVIII) is the orally active inhibitor for p38β and JNK2α2 with IC₅₀s of 6.3 nM and 53.6 nM. p38 Kinase inhibitor 8 exhibits anti-inflammatory effect in rats collagen-induced arthritis models.