p38 MAPK Inhibitor

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.

PF-3644022 (Standard) is the analytical standard of PF-3644022 (HY-107427). This product is intended for research and analytical applications. PF-3644022 is a potent, selective, orally active and ATP-competitive MAPKAPK2 (MK2) inhibitor with an IC₅₀ of 5.2 nM and a K_i of 3 nM. PF-3644022 also inhibits MK3 and p38 regulated/activated K_inase (PRAK) with IC₅₀s of 53 nM and 5.0 nM, respectively. PF-3644022 potently inhibits TNFα production and has anti-inflammatory effect.

Pamapimod (Standard) is the analytical standard of Pamapimod. This product is intended for research and analytical applications. 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.

Artocarpesin is a flavonoid compound. Artocarpesin has inhibitory effects on methicillin-resistant Staphylococcus aureus (MRSA). Artocarpesin inhibits the production of NO, PGE₂ and ROS by inhibiting COX-2 and iNOS expression, and plays an anti-inflammatory role. In addition, Artocarpesin inhibits platelet aggregation by inhibiting cyclic nucleotides and MAPKs, which can be used in the study of cardiovascular diseases.

F16 (Standard) is the analytical standard of F16 (HY-100395). This product is intended for research and analytical applications. F16 is a mitochondrial permeability transition pore (PTP) modulator with an EC₅₀ of 30 μM in mice. F16 promotes PTP opening, accumulates in cancer cell mitochondria, and induces mitochondrial depolarization, swelling, cristae disruption, outer membrane rupture, ATP depletion, reactive oxygen species (ROS) production, cytochrome c release and mitochondrial uncoupling. F16 induces cell cycle arrest at the G1 (occasionally G2) phase, reduces the phosphotyrosine content of Neu, as well as the levels of phosphorylated PKB/Akt and phosphorylated MAP kinase, downregulates the protein expression levels of Neu and PKB, triggers apoptosis in cells with moderate Bcl-2 expression, and induces necrosis in cells with overexpressed Bcl-2. F16 can be used in research related to breast cancer and gastric cancer.

EO 1428 (Standard) is the analytical standard of EO 1428 (HY-108647). This product is intended for research and analytical applications. EO 1428 is a highly specific inhibitor of p38 of the aminobenzophenone class. EO 1428 (1 μM ) markedly attenuates LPS-induced tumor necrosis factor α-converting enzyme (TACE) activity up-regulation.

Hexamethylene bisacetamide (Standard) is the analytical standard of Hexamethylene bisacetamide. This product is intended for research and analytical applications. Hexamethylene bisacetamide (HMBA) is a differentiation inducer and selective bromine domain inhibitor that can differentiate across the blood-brain barrier. Hexamethylene bisacetamide can induce tumor cell differentiation and inhibit cell proliferation, showing antitumor activity. Hexamethylene bisacetamide induces apoptosis by Notch1, Bcl-2 and p53 signaling pathways. In addition, Hexamethylene bisacetamide improves the obesity phenotype of mice.

Hispidin (Standard) is the analytical standard of Hispidin. This product is intended for research and analytical applications. Hispidin, a PKC inhibitor and a phenolic compound can be found in Phellinus linteus, has been shown to possess strong anti-oxidant, anti-cancer, anti-diabetic, and anti-dementia properties[1][2][3][4][5][6][7].

Aspartyl-alanyl-diketopiperazine (DA-DKP) (Standard) is the analytical standard of Aspartyl-alanyl-diketopiperazine (HY-107091). This product is intended for research and analytical applications. Aspartyl-alanyl-diketopiperazine is an immunomodulatory molecule and anti-inflammatory agent. Aspartyl-alanyl-diketopiperazine increases the level of active Rap1 in activated human T lymphocytes and reduces the phosphorylation levels of Ras, ATF-2, c-jun, MEK1, MEKK1, ERK1, JNK1,2,3, p38MAPK and MEF-2. Aspartyl-alanyl-diketopiperazine inhibits the production of pro-inflammatory cytokines, including the levels of IFN-γ and TNF-α. Aspartyl-alanyl-diketopiperazine can be used in studies of inflammatory immune responses.

Acenocoumarol-d₅ is the deuterium labeled Acenocoumarol (HY-B1014). 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.

SD-169 is an orally active ATP-competitive inhibitor of p38α MAPK, with an IC50 of 3.2 nM. SD-169 also weakly inhibits p38β MAPK with an IC50 of 122 nM. SD-169 prevents the development and progression of diabetes by inhibiting T cell infiltration and activation.

Roburic acid (Standard) is the analytical standard of Roburic acid. This product is intended for research and analytical applications. Roburic acid acts as an anti-inflammatory, anti-tumor and osteoclastogenesis inhibitor, with a K_i of 7.066 μM against human TNF, an IC₅₀ of 9 μM against human COX-2, and an IC₅₀ of 5 μM against ovine COX-1. Roburic acid reduces the production of inflammatory mediators such as NO and IL-6 in macrophages by inhibiting the NF-κB and MAPK (p38/JNK) pathways. By competitively inhibiting the TNF-TNF-R1 interaction, Roburic acid blocks the downstream NF-κB signaling pathway, thereby inducing cell cycle arrest and apoptosis in cancer cells. Roburic acid specifically inhibits osteoclastogenesis and bone resorption by suppressing the RANKL/TRAF6/NF-κB/NFATc1 axis. Roburic acid can be used in research related to osteolytic diseases such as osteoporosis, colorectal cancer and inflammatory diseases.

SB 202190 (hydrochloride) (Standard) is the analytical standard of SB 202190 (hydrochloride). This product is intended for research and analytical applications. SB 202190 hydrochloride is a selective p38 MAP kinase inhibitor with IC50s of 50 nM and 100 nM for p38α and p38β2, respectively. SB 202190 hydrochloride binds to the ATP pocket of the active recombinant human p38 kinase with a Kd of 38 nM. SB 202190 hydrochloride has anti-cancer activity. SB202190 hydrochloride induces autophagy.

Curcumenol (Standard) ((+)-Curcumenol (Standard)) is the analytical standard of Curcumenol (HY-N2259). This product is intended for research and analytical applications. Curcumenol ((+)-Curcumenol) is a natural compound with oral efficacy, exhibiting an IC₅₀ of 12.6 μM and a K_i of 10.8 μM against human CYP3A4. Curcumenol inhibits TNFα-induced phosphorylation/degradation of IκBα, phosphorylation/nuclear translocation of NF-κB p65, as well as the upregulation of MMP3, MMP9, MMP13, TRAF3, IL1RL1, TNFα and IL-1β. Curcumenol suppresses LPS-induced phosphorylation of Akt and p38 MAPK, as well as the production of pro-inflammatory mediators/proteins, and downregulates the SLC7A11/NF-κB/TGF-β pathway. Curcumenol binds to and inhibits the activation of Fyn and Lyn, blocks the function of downstream FcεRI signaling components, and reduces the release of allergic mediators/cytokines. Curcumenol upregulates the expression of KDM6B, and promotes chondrocyte proliferation and cartilage repair. Curcumenol induces ferroptosis and apoptosis, regulates the EMT process, and inhibits tumor growth and metastasis of triple-negative breast cancer. Curcumenol possesses anti-inflammatory, neuroprotective, antioxidant, antitumor, antiviral and hepatoprotective activities. Curcumenol can be used in research related to intervertebral disc degeneration, cancer, inflammation, central nervous system neurodegenerative diseases, allergic reactions and knee osteoarthritis.

RPR203494 is a potent inhibitor against CYP isozymes. RPR203494 shows inhibition against p38 kinase with an IC₅₀ value of 9 nM and an EC₅₀ value of 60 nM. RPR203494 demonstrates an inhibition of hepatic Cytochrome P450. RPR203494 is promising for research of rheumatoid arthritis (RA).