17 Results for "

normal endothelial cells

" in MedChemExpress (MCE) Product Catalog:
Products (17)

17 Results for "normal endothelial cells" in MCE Product Catalog:

7
7 Cited Publications
Cat. No.: HY-B0377
CAS No.: 76824-35-6
Synonyms: MK-208
Famotidine (MK-208) is an orally active and highly selective histamine H2 receptor antagonist. It inhibits gastric acid secretion by blocking the Gs signaling pathway, and regulates intracellular cAMP and ERK pathways. Famotidine inhibits TLR3-mediated inflammatory pathways, and reduces the expression of various inflammatory mediators and interferon-related genes. Famotidine scavenges DPPH and nitric oxide free radicals, alleviates oxidative stress damage in gastric tissue, inhibits proMMP-9, improves vascular endothelial permeability, and restores the normal physiological functions of neutrophils and eosinophils. Famotidine crosses intestinal epithelial cells via facilitated diffusion and passive diffusion, blocks paracellular cation transport, and increases intestinal transepithelial electrical resistance. Famotidine reduces serum levels of transaminases and alkaline phosphatase, exerts analgesic effects and gastric protective effects simultaneously. Famotidine can be used in studies related to COVID-19, liver injury and acute gastric ulcer .
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Cat. No.: HY-W707517
CAS No.: 2707433-64-3
Synonyms: MK-208-d4
Famotidine-d4 (MK-208-d4) is the deuterated-labeled Famotidine (HY-B0377). Famotidine (MK-208) is an orally active and highly selective histamine H2 receptor antagonist. It inhibits gastric acid secretion by blocking the Gs signaling pathway, and regulates intracellular cAMP and ERK pathways. Famotidine inhibits TLR3-mediated inflammatory pathways, and reduces the expression of various inflammatory mediators and interferon-related genes. Famotidine scavenges DPPH and nitric oxide free radicals, alleviates oxidative stress damage in gastric tissue, inhibits proMMP-9, improves vascular endothelial permeability, and restores the normal physiological functions of neutrophils and eosinophils. Famotidine crosses intestinal epithelial cells via facilitated diffusion and passive diffusion, blocks paracellular cation transport, and increases intestinal transepithelial electrical resistance. Famotidine reduces serum levels of transaminases and alkaline phosphatase, exerts analgesic effects and gastric protective effects simultaneously. Famotidine can be used in studies related to COVID-19, liver injury and acute gastric ulcer .
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Cat. No.: HY-B0377S
CAS No.: 2744683-81-4
Synonyms: MK-208-13C,d3
Famotidine- 13C,d3 (MK-208- 13C,d3) is the deuterated, 13C-labeled Famotidine (HY-B0377). Famotidine (MK-208) is an orally active and highly selective histamine H2 receptor antagonist. It inhibits gastric acid secretion by blocking the Gs signaling pathway, and regulates intracellular cAMP and ERK pathways. Famotidine inhibits TLR3-mediated inflammatory pathways, and reduces the expression of various inflammatory mediators and interferon-related genes. Famotidine scavenges DPPH and nitric oxide free radicals, alleviates oxidative stress damage in gastric tissue, inhibits proMMP-9, improves vascular endothelial permeability, and restores the normal physiological functions of neutrophils and eosinophils. Famotidine crosses intestinal epithelial cells via facilitated diffusion and passive diffusion, blocks paracellular cation transport, and increases intestinal transepithelial electrical resistance. Famotidine reduces serum levels of transaminases and alkaline phosphatase, exerts analgesic effects and gastric protective effects simultaneously. Famotidine can be used in studies related to COVID-19, liver injury and acute gastric ulcer .
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Cat. No.: HY-162815
Research Areas:  

Cancer

PROTAC SMARCA2/4 degrader-26 is a SMARCA2/4 PROTAC degrader with selective anti-tumor activity against lung cancer cells. PROTAC SMARCA2/4 degrader-26 degrades SMARCA2 and SMARCA4 via the PROTAC-mediated proteasomal pathway. It induces DNA damage and apoptosis in tumor cells, while inhibiting migration and colony formation of lung cancer cells; in addition, it damages normal vascular endothelial cells and exhibits significant off-target-related cytotoxicity. PROTAC SMARCA2/4 degrader-26 serves as the parent scaffold to construct the GSH-responsive prodrug PROTAC SMARCA2/4 degrader-25 (HY-162813), a derivative that shows drastically reduced cytotoxicity against normal cells. PROTAC SMARCA2/4 degrader-26 can be used in lung cancer-related research .
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Cat. No.: HY-B0377G
CAS No.: 76824-35-6
Synonyms: MK-208 (GMP)
Famotidine GMP (MK-208 GMP) is Famotidine (HY-B0377) produced in GMP guideline. Famotidine is an orally active and highly selective histamine H2 receptor antagonist. It inhibits gastric acid secretion by blocking the Gs signaling pathway, and regulates intracellular cAMP and ERK pathways. Famotidine inhibits TLR3-mediated inflammatory pathways, and reduces the expression of various inflammatory mediators and interferon-related genes. Famotidine scavenges DPPH and nitric oxide free radicals, alleviates oxidative stress damage in gastric tissue, inhibits proMMP-9, improves vascular endothelial permeability, and restores the normal physiological functions of neutrophils and eosinophils. Famotidine crosses intestinal epithelial cells via facilitated diffusion and passive diffusion, blocks paracellular cation transport, and increases intestinal transepithelial electrical resistance. Famotidine reduces serum levels of transaminases and alkaline phosphatase, exerts analgesic effects and gastric protective effects simultaneously. Famotidine can be used in studies related to COVID-19, liver injury and acute gastric ulcer .
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Cat. No.: HY-B0377R
CAS No.: 76824-35-6
Synonyms: MK-208 (Standard)
Famotidine (Standard) (MK-208 (Standard)) is the analytical standard of Famotidine (HY-B0377). This product is intended for research and analytical applications. Famotidine (MK-208) is an orally active and highly selective histamine H2 receptor antagonist. It inhibits gastric acid secretion by blocking the Gs signaling pathway, and regulates intracellular cAMP and ERK pathways. Famotidine inhibits TLR3-mediated inflammatory pathways, and reduces the expression of various inflammatory mediators and interferon-related genes. Famotidine scavenges DPPH and nitric oxide free radicals, alleviates oxidative stress damage in gastric tissue, inhibits proMMP-9, improves vascular endothelial permeability, and restores the normal physiological functions of neutrophils and eosinophils. Famotidine crosses intestinal epithelial cells via facilitated diffusion and passive diffusion, blocks paracellular cation transport, and increases intestinal transepithelial electrical resistance. Famotidine reduces serum levels of transaminases and alkaline phosphatase, exerts analgesic effects and gastric protective effects simultaneously. Famotidine can be used in studies related to COVID-19, liver injury and acute gastric ulcer .
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Cat. No.: HY-B0377S1
Synonyms: MK-208-13C
Famotidine- 13C (MK-208- 13C) is the 13C-labeled Famotidine (HY-B0377). Famotidine (MK-208) is an orally active and highly selective histamine H2 receptor antagonist. It inhibits gastric acid secretion by blocking the Gs signaling pathway, and regulates intracellular cAMP and ERK pathways. Famotidine inhibits TLR3-mediated inflammatory pathways, and reduces the expression of various inflammatory mediators and interferon-related genes. Famotidine scavenges DPPH and nitric oxide free radicals, alleviates oxidative stress damage in gastric tissue, inhibits proMMP-9, improves vascular endothelial permeability, and restores the normal physiological functions of neutrophils and eosinophils. Famotidine crosses intestinal epithelial cells via facilitated diffusion and passive diffusion, blocks paracellular cation transport, and increases intestinal transepithelial electrical resistance. Famotidine reduces serum levels of transaminases and alkaline phosphatase, exerts analgesic effects and gastric protective effects simultaneously. Famotidine can be used in studies related to COVID-19, liver injury and acute gastric ulcer .
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Cat. No.: HY-W777002
CAS No.: 1185241-48-8
Synonyms: MK-208-13C3
Famotidine- 13C3 (MK-208- 13C3) is the 13C3-labeled Famotidine (HY-B0377). Famotidine (MK-208) is an orally active and highly selective histamine H2 receptor antagonist. It inhibits gastric acid secretion by blocking the Gs signaling pathway, and regulates intracellular cAMP and ERK pathways. Famotidine inhibits TLR3-mediated inflammatory pathways, and reduces the expression of various inflammatory mediators and interferon-related genes. Famotidine scavenges DPPH and nitric oxide free radicals, alleviates oxidative stress damage in gastric tissue, inhibits proMMP-9, improves vascular endothelial permeability, and restores the normal physiological functions of neutrophils and eosinophils. Famotidine crosses intestinal epithelial cells via facilitated diffusion and passive diffusion, blocks paracellular cation transport, and increases intestinal transepithelial electrical resistance. Famotidine reduces serum levels of transaminases and alkaline phosphatase, exerts analgesic effects and gastric protective effects simultaneously. Famotidine can be used in studies related to COVID-19, liver injury and acute gastric ulcer .
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Cat. No.: HY-182274
CAS No.: 3106606-60-1
Target:  

Acyltransferase STAT

Research Areas:  

Others

DM245 is an EPAC1 activator and STAT3 phosphorylation inhibitor with a target pIC50 of 4.801. DM245 activates EPAC1 to increase Rap1-GTP levels, with no activation of EPAC2 or PKA. DM245 reduces IL-6/IL-6Rα-evoked STAT3 phosphorylation in endothelial cells. DM245 suppresses TGF-β1-induced fibroblast-to-myofibroblast transition, reducing αSMA and Collagen I levels. DM245 exhibits minimal cytotoxicity in normal human lung fibroblasts, with negligible loss of intact nuclei after 72 h exposure .
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Cat. No.: HY-136893
CAS No.: 1384170-58-4
Research Areas:  

Cancer

SP-6-27 is a tubulin depolymerizing agent that binds to the colchicine site of β-tubulin. SP-6-27 induces G2/M cell cycle arrest in ovarian cancer cells. SP-6-27 enhances intrinsic apoptosis in ovarian cancer cells through upregulation of Bax, Apaf-1, caspase-6, caspase-9, and caspase-3. SP-6-27 reduces ovarian cancer cell migration. SP-6-27 inhibits capillary tube formation by human umbilical vein endothelial cells. SP-6-27 shows minimum cytotoxicity to normal ovarian epithelia. SP-6-27 shows enhanced cytotoxicity in chemo-sensitive/resistant ovarian cancer cells when combined with Cisplatin (HY-17394). SP-6-27 can be used for the research of ovarian cancer .
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Cat. No.: HY-184159
AChE/BChE/MAO-A-IN-2 is an AChE, BChE, and MAO-A inhibitor with IC50 values of 104.28 nM, 23.04 nM, and 215.50 nM, respectively. AChE/BChE/MAO-A-IN-2 exhibits selective antiproliferative activity against cancer cells and low toxicity toward normal cells. AChE/BChE/MAO-A-IN-2 can be used for the research of alzheimer's disease, neuroblastoma .
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Cat. No.: HY-182273
CAS No.: 3106606-59-8
Target:  

STAT Acyltransferase

Research Areas:  

Others

DM243 is an EPAC1 activator and STAT3 modulator with an pIC50 of 4.769 for EPAC1. DM243 increases GTP-bound Rap1 levels in EPAC1-expressing cells. DM243 reduces IL-6/IL-6Rα-evoked STAT3 phosphorylation in endothelial cells. DM243 suppresses TGF-β1-induced fibroblast-to-myofibroblast transition, reducing α-smooth muscle actin and Collagen I levels in lung fibroblasts. DM243 exhibits minimal cytotoxicity in normal human lung fibroblasts .
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Cat. No.: HY-149035
PAA4 is a hypercoordinate carbon-centered tetranuclear gold (I) cluster prodrug . PAA4 releases active Au (I) ions upon triggering by GSH (HY-D0187), and this process is accelerated in the acidic microenvironment of bladder cancer cells with high GSH expression. PAA4 inhibits the activities of cytosolic TrxR1 and mitochondrial TrxR2, inducing ROS accumulation, lipid peroxidation, ferroptosis, loss of mitochondrial membrane potential and DNA damage. PAA4 can be used in bladder cancer-related research .
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Cat. No.: HY-176741
CAS No.: 2566503-77-1
MAPK ligand 1 is an apoptosis inducer and Bcl-xL/MAPK ligand that can be used to synthesize the Bcl-xL-targeted PROTAC degrader (HY-176740). MAPK ligand 1 triggers apoptosis through the mitochondrial pathway, MAPK pathway, reduction of mitochondrial membrane potential and elevation of reactive oxygen species levels. MAPK ligand 1 inhibits colony formation and migration of cancer cells, as well as angiogenesis of endothelial cells. MAPK ligand 1 can be used in the research of hepatocellular carcinoma .
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Cat. No.: HY-184307
Target:  

FAK CDK DNA/RNA Synthesis

Research Areas:  

Cancer

FAK1/2 Ligand-1 is a FAK1/FAK2 ligand with KD values of 2.9 μM and 2.5 μM for binding to FAK1 and FAK2, respectively. FAK1/2 Ligand-1 induces G2/M phase arrest, activates DNA damage-related signaling pathways, and reduces the phosphorylation level of CDK1. Antitumor agent-220 is applicable to the research of triple-negative breast cancer .
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Cat. No.: HY-182354
CAS No.: 861877-12-5
Research Areas:  

Cancer

VEGFR2-IN-84 is an orally active, multi-targeted tyrosine kinase inhibitor based on a naphthalene ring scaffold. VEGFR2-IN-84 inhibits VEGFR2 with sub-nanomolar affinity and broadly targets kinases including Kit, FGFR, PDGFR, and Ret. By competitively binding to the ATP-binding pocket, VEGFR2-IN-84 blocks the phosphorylation of VEGFR2 and its downstream AKT/ERK signaling pathway, thereby significantly inhibiting endothelial cell proliferation, migration, and tumor angiogenesis. VEGFR2-IN-84 exhibits broad-spectrum antiproliferative activity against various solid tumors such as liver cancer, lung cancer, and renal cancer, shows weak toxicity to normal cells, and has superior potency to Lenvatinib (HY-10981). VEGFR2-IN-84 possesses favorable pharmacokinetic properties and high safety (LD50>2000 mg/kg), and can be used in related studies of various malignant tumors .
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Cat. No.: HY-B0377A
CAS No.: 125193-62-6
Synonyms: MK-208 hydrochloride
Famotidine hydrochloride (MK-208 hydrochloride) is an orally active and highly selective histamine H2 receptor antagonist. It inhibits gastric acid secretion by blocking the Gs signaling pathway, and regulates intracellular cAMP and ERK pathways. Famotidine hydrochloride inhibits TLR3-mediated inflammatory pathways, and reduces the expression of various inflammatory mediators and interferon-related genes. Famotidine hydrochloride scavenges DPPH and nitric oxide free radicals, alleviates oxidative stress damage in gastric tissue, inhibits proMMP-9, improves vascular endothelial permeability, and restores the normal physiological functions of neutrophils and eosinophils. Famotidine hydrochloride crosses intestinal epithelial cells via facilitated diffusion and passive diffusion, blocks paracellular cation transport, and increases intestinal transepithelial electrical resistance. Famotidine hydrochloride reduces serum levels of transaminases and alkaline phosphatase, exerts analgesic effects and gastric protective effects simultaneously. Famotidine hydrochloride can be used in studies related to COVID-19, liver injury and acute gastric ulcer .
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