p38 MAPK Inhibitor

Isocucurbitacin B is a natural terpenoid compound found in Pedicellus Melo. Isocucurbitacin B can inhibit the PI3K/AKT, MAPK, and STAT3 signaling pathways and downregulate CAV1 expression. Isocucurbitacin B can inhbit cancer cell proliferation, migration and invision. Isocucurbitacin B can induce apoptosis and cause G2/M phase arrest. Isocucurbitacin B can decrease intracellular cholesterol and PH levels and increase intracellular calcium levels. Isocucurbitacin B can be used for the research of cancer, such as glioma^[1][2].

Bromuconazole is a triazole fungicide with oral efficacy and blood-brain barrier permeability. Bromuconazole protects crops from various fungal contaminations. Bromuconazole exhibits cytotoxicity against a variety of cancer cells, induces G0/G1 cell cycle arrest and inhibits DNA synthesis in cancer cells, and triggers cytoskeletal structural disorder, genotoxic damage, apoptotic (apoptosis) cell death, and mitochondrial membrane depolarization. Bromuconazole activates caspase-3, induces excessive production of ROS, p53 and Bax, lipid peroxidation, increased activities of SOD and CAT, and downregulates Bcl-2. By upregulating p-ERK1/2 and p-JNK, Bromuconazole disrupts the MAPK signaling pathway, impairs the cellular stress response of human trophoblast cells and endometrial cells, and damages the implantation process. Bromuconazole is applicable to research related to glioma, colon cancer, reproductive injury (implantation dysfunction), and cardiac dysfunction.

SB 242235 (Standard) is the analytical standard of SB 242235. This product is intended for research and analytical applications. SB-242235 is a potent and selective p38 MAP kinase inhibitor, with an IC50 of 1.0　μM in primary human chondrocytes.

p38 MAP Kinase-IN-4 is a p38α MAPK inhibitor with an IC₅₀ of 40.5 nM. p38 MAP Kinase-IN-4 is applicable to inflammation-related research.

Gamma-glutamylcysteine ammonium (γ-Glu-Cys ammonium) is an orally active, blood-brain barrier permeable dipeptide. Gamma-glutamylcysteine ammonium activates AMPK, SIRT1, IL-4/STAT6, AC/cAMP/PI3K, IGF-1R/IRS1/PI3K, and Nrf2 signaling pathways; it inhibits NF-κB, JAK1/STAT1/3, MAPKs, cadmium-induced p38 MAPK, JNK, and PI3K/Akt signaling pathways. Gamma-glutamylcysteine ammonium regulates macrophage polarization, modulates the trafficking of CD36 and GLUT4, induces glutathione synthesis, improves metabolic dysfunction, reduces lipid deposition, ameliorates glucose homeostasis, inhibits apoptosis (Apoptosis), stabilizes mitochondria, suppresses lipid peroxidation, iron accumulation and ferroptosis (Ferroptosis), reduces ds-HMGB1 levels, reverses mechanical hyperalgesia, and alleviates hepatic lipid droplet formation. Gamma-glutamylcysteine ammonium is applicable to research related to inflammatory bowel disease, type 2 diabetes, cadmium-induced neurotoxicity, Alzheimer's disease, cerebral ischemia/reperfusion injury, neuropathy, and alcoholic liver disease.

SKF-86002 (Standard) is the analytical standard of SKF-86002. This product is intended for research and analytical applications. SKF-86002 is an orally active p38 MAPK inhibitor, with anti-inflammatory, anti-arthritic and analgesic activities. SKF-86002 inhibits lipopolysaccharide (LPS)-stimulate human monocyte IL-1 and TNF-α production (IC50 = 1 μM). SKF-86002 inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid.

Hypaphorine is an indole found in Caragana korshinskii. Hypaphorine has neurological and glucose-lowering effects. Hypaphorine prevents Lipopolysaccharides (LPS) (HY-D1056)-mediated acute lung injury (ALI) and proinflammatory response via inactivating the p38/JNK signaling pathway by upregulating DUSP1.

PMK1-IN-1 (compound H17) is a potent PMK1 inhibitor. PMK1-IN-1 shows superior inhibitory effects against M. oryzae by targeting the pathogenicity MAPK MoPMk1, with an IC₅₀ of 0.42 μM. PMK1-IN-1 exhibits effects in vivo similar to those of Carbendazim (HY-13582). PMK1-IN-1 can be used for rice blast disease research.

RWJ-67657 (Standard) is the analytical standard of RWJ-67657. This product is intended for research and analytical applications. RWJ-67657 (JNJ 3026582) is an orally active and selective p38α and p38β MAPK inhibitor with IC50s of 1 and 11 μM, respectively. RWJ-67657 displays no activity at p38γ and p38δ, and exhibits cardio protective effect. Anti-inflammatory and anti-tumor activity.

WEIZ-WX-04-008 (Compound 1) is a covalent Lysine-targeting MKK7 inhibitor with IC₅₀ of 738 nM.

p38 MAPK-IN-11 is a CSBP (p38 MAPK) kinase inhibitor with IC₅₀ values of 0.15 μM (binding activity) and 0.21 μM (inhibitory activity). p38 MAPK-IN-11 shows weak inhibitory activity against PKCα kinase, with an IC₅₀ of 7.6 μM. p38 MAPK-IN-11 inhibits the production of IL-1. p38 MAPK-IN-11 also acts as a β-lactam antibiotic potentiator, but has no antibacterial activity itself.

p38 MAP Kinase-IN-1 (Compound 4) is the inhibitor for p38, and can be used for inflammation and auto-immune responses related research.

JH-I-25 is an orally active IRAK1 and IRAK4 inhibitor. JH-I-25 inhibits LPS-induced IRAK4 phosphorylation, IRAK1 degradation, MAPK activation, and the expression of proinflammatory cytokines TNF-α and IL-6 in lung tissues. JH-I-25 improves the survival rate of LPS-induced septic mice and serves as an IRAK4 recruiter in the design of proteolysis-targeting chimeric molecules. JH-I-25 can be used in research related to diffuse large B-cell lymphoma, Waldenström's macroglobulinemia, septic shock, rheumatoid arthritis, atherosclerosis, Alzheimer's disease, acute lung injury, sepsis, and psoriasis.

SKLB646 is an orally active multi-target kinase inhibitor. SKLB646 shows significant inhibitory effects on SRC and VEGFR2 with IC₅₀ values ??of 0.002 μmol/L and 0.012 μmol/L, respectively. SKLB646 also shows significant inhibitory effects on B-Raf and C-Raf with IC₅₀ values ??of 0.022 μmol/L and 0.019 μmol/L, respectively. SKLB646 inhibits the activation of the SRC signaling pathway and blocks the MAPK signaling pathway by inhibiting Raf kinase. In addition, SKLB646 can inhibit the proliferation, migration and invasion of human umbilical vein endothelial cells (HUVEC) to inhibit tumor-induced angiopoietic formation. SKLB646 shows significant anti-proliferative and anti-survival activities against triple-negative breast cancer (TNBC) cell lines.

7-Acetoxycoumarin (Acetylumbelliferone) is an anti-inflammatory inhibitor with antibacterial and amoebicidal activities. 7-Acetoxycoumarin reduces the phosphorylation levels of ERK, JNK, NF-κB and p38 MAPK. 7-Acetoxycoumarin downregulates the protein and mRNA expression levels of iNOS and COX-2. 7-Acetoxycoumarin inhibits the production of IL-1β, IL-6, TNF-α, NO and PG₂. 7-Acetoxycoumarin reduces the degradation of IκBα. 7-Acetoxycoumarin can be used in studies related to amoebiasis and Bacillus lentus infection.

Sorafenib (tosylate) (Standard) (Bay 43-9006 (tosylate) (Standard)) is the analytical standard of Sorafenib (tosylate) (HY-10201A). This product is intended for research and analytical applications. Sorafenib (Bay 43-9006) tosylate is a potent oral active multikinase inhibitor. Sorafenib blocks autophosphorylation and activity of receptor tyrosine kinases (VEGFR-2, VEGFR-3) and RAF family kinases, thereby suppressing the RAF/MEK/ERK and PI3K/Akt pathways, inhibiting STAT3 phosphorylation, and selectively inhibiting the MAPK pathway in cancer cells. Sorafenib tosylate induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib tosylate inhibits tumor growth and metastasis in mouse and rat models. Sorafenib tosylate can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma.

Gallic aldehyde (Standard) is an analytical standard of Gallic aldehyde (HY-W004486). This product is intended for research and analytical applications. Gallic aldehyde (3,4,5-Trihydroxybenzaldehyde) is a phenolic aldehyde. Gallic aldehyde can be isolated from Geum japonicum. Gallic aldehyde inhibits the gelatinolytic activity and expression of MMP-9. Gallic aldehyde also inhibits ERK1/2, p38, and JNK. Gallic aldehyde has potent anti-HSV-1 and antioxidant activities. Gallic aldehyde also exhibits antibacterial activity against Oenococcus oeni VF.

SX 011 (Standard) is the analytical standard of SX 011 (HY-108646). This product is intended for research and analytical applications. SX 011 is a p38 inhibitor with IC₅₀s of 9 nM and 90 nM against p38α and p38β, respectively. SX 011 also inhibits JNK-2 with an IC₅₀ of 100 nM. SX-011 is orally bioavailable.

Dihydrodaidzein (Standard) ((±)-Dihydrodaidzein (Standard)) is the analytical standard of Dihydrodaidzein (HY-N1461). This product is intended for research and analytical applications. Dihydrodaidzein is a dietary phytoestrogen. Dihydrodaidzein possesses functions including antioxidation, inhibition of DNA oxidative damage, regulation of lipid metabolism and maintenance of intestinal flora stability. Dihydrodaidzein induces apoptosis, regulates immune responses, modulates tumor-related factors, activates the Bmp-2 signaling pathway, inhibits NF-κB and MAPK, and exhibits anti-inflammatory activity. Dihydrodaidzein can be used in research related to cancer, cardiovascular diseases, osteoporosis and inflammatory diseases.

Neoandrographolide (Standard) is the analytical standard of Neoandrographolide. This product is intended for research and analytical applications. Neoandrographolide is a diterpenoid compound isolated from Andrographis paniculata. Neoandrographolide inhibits osteoclasts differentiation and bone resorption through inhibition of MAPK/NF-κB/PI3K/AKT/GSK3β/PPAR/CAMK signaling pathway. Neoandrographolide inhibits apoptosis in rat embryonic ventricular cardiomyocytes. Neoandrographolide inhibits iNOS and the generation of ROS, activates eNOS, exhibiting anti-inflammatory and hypolipidemic activity.