p38 MAPK Inhibitor

PS-166276 is a highly potent and less cytotoxic inhibitor of p38. PS166276 has an IC₅₀ of 28 nM at p38 kinase and 170 nM in the THP-1 TNFα assay.

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.

p38α-IN-12 is an orally bioavailable p38α MAPK inhibitor, with an IC₅₀ of 0.11 nM and a K_i of 0.2 nM against human targets. p38α-IN-12 inhibits the production of TNFα in cellular systems and exerts in vivo efficacy in acute mouse models.

CK1δ-IN-9 (Compound 8) is the inhibitor for casein kinase 1 that inhibits CK1δ with IC₅₀ of 1.4 nM. CK1δ-IN-9 inhibits p38α and p38β with IC₅₀ of 0.25 μM and 0.78 μM. CK1δ-IN-9 exhibits pharmacokinetic characteristics with a good oral bioavailability (70%) and a moderate clearance.

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.

PD-254552 is a MEK inhibitor. PD-254552 exhibits hepatotoxicity and gastrointestinal toxicity in mice.

SH543 is a potent anti-osteoporosis agent. SH543 inhibits nuclear factor κB ligand (RANKL)-induced osteoclastogenesis with an IC₅₀ of 3.3 nM. SH543 directly binds to KEAP1, activates the Nrf2-HO-1 antioxidant pathway, reduces ROS levels, and inhibits PI3K-AKT and MAPK signaling pathways. SH543 attenuates pathological bone loss in ovariectomized mice. SH543 can be used for osteoporosis 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.

Eupalestin is an anti-inflammatory agent. Eupalestin reduces the levels of p-p65 NF-κB and p-p38 MAPK. Eupalestin inhibits MPO and adenosine deaminase. Eupalestin decreases the levels of pro-inflammatory cytokines including IL-17A, IL-6, TNF and IFN-γ. Eupalestin exerts anti-inflammatory activity in a carrageenan (HY-125474)-induced mouse pleurisy model.

Kaempferol 3-O-(2G-glucosylrutinoside)-7-O-glucoside is an anti-inflammatory agent. Kaempferol 3-O-(2G-glucosylrutinoside)-7-O-glucoside exerts significant anti-inflammatory effects in LPS (HY-D1056)-induced RAW 264.7 macrophages by inhibiting the NF-κB, MAPK and Akt signaling pathways, thereby reducing the production of inflammatory mediators (NO, PGE2) and pro-inflammatory cytokines (TNF-α, IL-1β, IL-6).

RIPK2-IN-6 (Compound 15a) is an inhibitor for RIPK, that inhibits the phosphorylation of RIPK2, and thus inhibits the NF-κB and MAPK signaling pathways. RIPK2-IN-6 exhibits anti-inflammatory and anti-fibrotic activities in Dextran sodium sulfate (HY-116282C)-induced mice colitis models.

Cyanidin 3,5-diglucoside (chloride) (Standard) is the analytical standard of Cyanidin 3,5-diglucoside (chloride) (HY-129138). This product is intended for research and analytical applications. Cyanidin 3,5-diglucoside chloride is an anthocyanin. Cyanidin 3,5-diglucoside chloride inhibits inflammatory cytokines (IL-1α, IL-1β, and IL-6) expression and NO production. Cyanidin 3,5-diglucoside chloride inhibits the phosphorylation of STAT3, IκB, ERK, p38, and AKT. Cyanidin 3,5-diglucoside chloride inhibits high pressure-induced decrease in GLAST. Cyanidin 3,5-diglucoside chloride exerts anti-inflammatory and skin barrier modulating effects. Cyanidin 3,5-diglucoside chloride can be used in retinal research.

3′-O-Demethyl-4′-N-demethyl-4′-N-acetyl-4′-epi-staurosporine (Compound 7) is an inhibitor of protein kinases, with IC₅₀s of 0.092, 0.26, 0.77 μM for PKC-α, ROCK, ASK1. 3′-O-Demethyl-4′-N-demethyl-4′-N-acetyl-4′-epi-staurosporine shows potent cytotoxicity against PC-3 cancer cells with an IC₅₀ value of 0.16 μM.

FKA-9i is an orally active anticancer agent. FKA-9i directly binds to and promotes the degradation of oncoproteins LRPPRC (k_d: 7.387 μM), YBX1 (k_d: 16.52 μM) and RPN1 (k_d: 26.82 μM). FKA-9i inhibits the MAPK signaling pathway and mitochondrial oxidative phosphorylation. FKA-9i also induces cancer cell cycle arrest, apoptosis, mitochondrial dysfunction and ROS accumulation. FKA-9i can be used in the research of tumors such as gastric cancer.

Emodic acid (NSC624610) is an anthraquinone compound isolated from A. microcarpus, which can inhibit the proliferation of cancer cells by inhibiting the activity of NF-κB. Emodic acid can also inhibit the phosphorylation of p38, ERK and JNK, the secretion of tumor-promoting cytokines IL-1β and IL-6, and the expression of VEGF and MMP, thereby inhibiting the invasion and migration potential of cancer cells.

MBL-1 is an orally active anti-inflammatory agent. MBL-1 can be isolated from the fermentation broth of Aspergillus sp. derived from gorgonians. MBL-1 inhibits the activity of the hCOX-2 protein with an IC₅₀ of 5.77 μM. MBL-1 reduces the production of key pro-inflammatory mediators such as NO, ROS, IL-1β and IL-18 by inhibiting the MAPK/NF-κB and NLRP3 signaling pathways. MBL-1 exerts a protective effect against DSS-induced colitis. MBL-1 can be used for the research of ulcerative colitis.

ASK1-IN-12 is an ASK1 inhibitor with an IC₅₀ of 6.3 nM. ASK1-IN-12 inhibits TNF-α-induced activation of the ASK1-p38/JNK pathway. ASK1-IN-12 can reduce free fatty acid-induced cholesterol increase, lipid droplet accumulation and improves hepatocellular steatosis. ASK1-IN-12 can be used for the research of non-alcoholic steatohepatitis (NASH).

Akt/NF-κB/MAPK-IN-1 (compound 2m) is a potent and orally active inhibitor against NO (IC₅₀=7.70 μM) with no significant toxicity. Akt/NF-κB/MAPK-IN-1 shows anti-inflammatory activity by inhibiting Akt/NF-κB and MAPK signaling pathways.

RANKL-IN-1 formate is a selective receptor activator of nuclear factor-κB ligand inhibitor ligand (RANKL) inhibitor with a K_D value of 7.6 μM. RANKL-IN-1 formate exhibits inhibitory activity and selectivity against osteoclastogenesis with an IC₅₀ value of 0.07 μM and SI of 82.57. RANKL-IN-1 formate binds directly to RANKL and blocks the RANKL-induced activation of the NF-κB and MAPK pathways. RANKL-IN-1 formate can be used for the research of metabolic disease, such as osteoporosis.

Losmapimod (GSK-AHAB; GW856553X) hydrochloride is an orally active p38α/β MAPK inhibitor, with pK_i values of 8.1 and 7.6 for p38α and p38β, respectively. Losmapimod hydrochloride reduces DUX4 expression, thus exerting efficacy in facioscapulohumeral muscular dystrophy. By inhibiting MAPK/NF-κB, Losmapimod hydrochloride reduces apoptosis of epileptiform hippocampal neurons, and exhibits anti-allodynia and anti-hyperalgesic activities. Losmapimod hydrochloride blocks the entry and fusion of Lassa fever virus (LASV). Losmapimod hydrochloride overcomes tyrosine kinase inhibitor resistance in non-small cell lung cancer (NSCLC). Losmapimod hydrochloride inhibits myocardial senescence and inflammation, and possesses cardioprotective activity against cardiotoxicity.