2412 Results for "

decrease

" in MedChemExpress (MCE) Product Catalog:
Products (2412)

2412 Results for "decrease" in MCE Product Catalog:

4
4 Cited Publications
Art. -Nr.: HY-16346
CAS. Nr.: 290297-26-6
Synonyms: CID 6451149
Target:  

Neurokinin Receptor

Forschungsgebiete:  

Neurological Disease Endocrinology

Netupitant (CID 6451149) is a blood-brain barrier penetrable, orally active NK1 receptor inhibitor with a Ki of 0.95 nM (CHO cells) against the human receptor. Netupitant antagonizes the effects induced by Substance P, inhibits the maximal response of Substance P with a long-lasting action, and suppresses NK1 agonist-induced behaviors in mice and gerbils. Netupitant reduces the frequency of bladder contractions, prolongs contraction intervals, decreases basal pressure at high doses, and acts on the afferent branch of the micturition reflex. Netupitant can be used in research related to overactive bladder, chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, anxiety disorders, and depression .
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4
4 Cited Publications
Art. -Nr.: HY-N2445
CAS. Nr.: 37308-75-1
Flavokawain C is an orally active natural chalcone. Flavokawain C inhibits the proliferation of various cancer cells. Flavokawain C upregulates GADD153 in cancer cells, inhibits the phosphorylation of Akt and JNK, suppresses early ERK phosphorylation, activates late ERK phosphorylation, activates caspase related subtypes, induces PARP-1 cleavage, causes upregulation of p21 and p27, downregulation of mutant p53 and anti-apoptotic IAP proteins, elevates intracellular ROS levels, reduces SOD activity, and induces apoptosis. Flavokawain C downregulates FABP4, induces autophagy in cancer cells, and activates the AMPK/mTOR pathway . Flavokawain C decreases the expression of glycolysis-related proteins GLUT1 and HK2, and inhibits glycolysis in nasopharyngeal carcinoma cells. Flavokawain C inhibits the activation of the EGFR/PI3K/Akt/mTOR signaling pathway and reduces the expression of HSP90B1. Flavokawain C inhibits angiogenesis by decreasing the expression of angiogenic proteins Ang-1 and VEGF in human umbilical vein endothelial cells. Flavokawain C increases γ-H2AX levels in cells, inhibits the phosphorylation of FAK, PI3K and AKT in cells, and induces DNA damage in cells. Flavokawain C exerts anti-tumor activity in multiple tumor xenograft mouse models. Flavokawain C is applicable to research related to colorectal cancer, colon adenocarcinoma, nephroblastoma, nasopharyngeal carcinoma and liver cancer .
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4
4 Cited Publications
Art. -Nr.: HY-101126
CAS. Nr.: 1361951-15-6
Reinheit:  99.96%
Synonyms: TP-3654
Forschungsgebiete:  

Cancer

Nuvisertib (TP-3654) is an orally active second-generation pan-PIM kinase inhibitor with Ki values of 5 nM, 239 nM, and 42 nM against PIM-1, PIM-2, and PIM-3, respectively. Nuvisertib inhibits JAK-independent inflammatory and survival signaling pathways, reduces the production of proinflammatory cytokines, restores apoptotic sensitivity, inhibits mTORC1, MYC, and TGF-β signaling pathways, and decreases the expression of fibrosis markers. Nuvisertib selectively impairs the transport function of ABCG2, resensitizes multidrug-resistant cancer cells to cytotoxic drugs, and overcomes JAK2 inhibitor resistance. Nuvisertib can be used in research related to myelofibrosis, renal cell carcinoma, multidrug-resistant cancer, advanced solid tumors, urothelial carcinoma, and prostate adenocarcinoma .
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4
4 Cited Publications
Art. -Nr.: HY-18071A
CAS. Nr.: 1422252-46-7
Forschungsgebiete:  

Cardiovascular Disease

BI-9627 hydrochloride is a potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor (IC50 = 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays). BI-9627 hydrochloride displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 hydrochloride decreases autophagy in HTR-8/SVneo cells. BI-9627 hydrochloride can significantly reduce the pHi of human sperm and partially reverse the effect of DMA. BI-9627 hydrochloride prolongs Ca 2+ recovery time in KO hiPSC-CMs. BI-9627 hydrochloride shows low DDI (agent-agent interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury .
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4
4 Cited Publications
Art. -Nr.: HY-18071
CAS. Nr.: 1204329-34-9
Forschungsgebiete:  

Cardiovascular Disease

BI-9627, a chemical probe, is a potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor (IC50 = 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays). BI-9627 displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 decreases autophagy in HTR-8/SVneo cells. BI-9627 can significantly reduce the pHi of human sperm and partially reverse the effect of DMA. BI-9627 prolongs Ca 2+ recovery time in KO hiPSC-CMs. BI-9627 shows low DDI (agent-agent interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury .
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4
4 Cited Publications
Art. -Nr.: HY-N2609
CAS. Nr.: 2196-14-7
7,4'-Dihydroxyflavone (7,4'-DHF) is a flavonoid, which can be isolated from Glycyrrhiza uralensis. 7,4'-Dihydroxyflavone is eotaxin/CCL11 inhibitor and CBR1 inhibitor (IC50=0.28 μM). 7,4'-Dihydroxyflavone has the ability to consistently suppress eotaxin production and prevent dexamethasone (Dex)‐paradoxical adverse effects on eotaxin production . 7,4'-Dihydroxyflavone (7,4'-DHF) inhibits MUC5AC gene expression, mucus production and secretion via regulation of NF-κB, STAT6 and HDAC2.7,4'-Dihydroxyflavone (7,4'-DHF) decreases phorbol 12-myristate 13-acetate (PMA) stimulated NCI-H292 human airway epithelial cell MUC5AC gene expression and mucus production with IC50 value of 1.4 µM .
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3
3 Cited Publications
Art. -Nr.: HY-W017692
CAS. Nr.: 1416354-35-2
Forschungsgebiete:  

Metabolic Disease

2-Aminoindan-2-phosphonic acid hydrochloride is a competitive phenylalanine ammonia lyase (PAL) inhibitor that significantly decreases the levels of total phenolic compounds and PheGs in plant cultured cells .
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3
3 Cited Publications
Art. -Nr.: HY-14896
CAS. Nr.: 923287-50-7
Reinheit:  99.06%
Synonyms: BIA 9-1067
Target:  

COMT

Forschungsgebiete:  

Neurological Disease

Opicapone (BIA 9-1067) is a potent third-generation catechol-O-methyltransferase (COMT) inhibitor for the research of Parkinson's disease and motor fluctuations. Opicapone decreases the ATP content of the cells with an IC50 of 98 μM .
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3
3 Cited Publications
Art. -Nr.: HY-N1940
CAS. Nr.: 38226-86-7
Synonyms: Cycloicaritin
β-Anhydroicaritin is isolated from Boswellia carterii Birdware, has important biological and pharmacological effects, such as antiosteoporosis, estrogen regulation and antitumor properties . β-Anhydroicaritin ameliorates the degradation of periodontal tissue and inhibits the synthesis and secretion of TNF-α and MMP-3 in diabetic rats . β-Anhydroicaritin decreases the overproduction of NO, IL-10, TNF-α, MCP-1 and IL-6 in inperitonitis mice. β-Anhydroicaritin inhibits the elevation of intracellular Ca 2+, and markedly decreases iNOS protein expression .
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3
3 Cited Publications
Art. -Nr.: HY-128971
CAS. Nr.: 170111-28-1
Reinheit:  98.03%
Target:  

Cathepsin Parasite

Forschungsgebiete:  

Infection Neurological Disease

LHVS is a potent, non-selective, irreversible, cell-permeable cysteine protease and cathepsin inhibitor. LHVS decreases actin ring formation. LHVS inhibits T. gondii invasion with an IC50 of 10 μM .
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3
3 Cited Publications
Art. -Nr.: HY-N2497
CAS. Nr.: 120926-46-7
Isoliquiritin apioside significantly decreases PMA-induced increases in MMP9 activities and suppresses PMA-induced activation of MAPK and NF-κB. Isoliquiritin apioside auppresseses invasiveness and angiogenesis of cancer cells and endothelial cells .
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3
3 Cited Publications
Art. -Nr.: HY-113486
CAS. Nr.: 80-99-9
Reinheit:  98.09%
Lathosterol is a plant sterol and cholesterol-like molecule. Lathosterol increases antioxidant enzymes (such as SOD, CAT, and GSH) and decreases LDH. Lathosterol has a hepatoprotective effect on mice with acetaminophen (HY-66005)-induced liver injury [1] .
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3
3 Cited Publications
Art. -Nr.: HY-112902
CAS. Nr.: 350997-39-6
Reinheit:  99.60%
Target:  

DNA Glycosylase

Forschungsgebiete:  

Inflammation/Immunology

OGG1-IN-08 is a potent 8-oxoguanine DNA glycosylase-1 (OGG1) inhibitor with an IC50 value of 0.22 μM. OGG1-IN-08 decreases both the glycosylase and lyase activities of OGG1 .
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3
3 Cited Publications
Art. -Nr.: HY-15297
CAS. Nr.: 81840-15-5
Reinheit:  98.58%
Synonyms: OPC-8212
Forschungsgebiete:  

Infection Cardiovascular Disease

Vesnarinone (OPC-8212) is an orally active phosphodiesterase 3 (PDE3) inhibitor. Vesnarinone can increase in calcium flux and decrease in potassium flux. Vesnarinone shows dose-dependent positive inotropic activity. Vesnarinone can be used in heart failure research .
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3
3 Cited Publications
Art. -Nr.: HY-B2099A
CAS. Nr.: 1190-53-0
Synonyms: 1-Butylbiguanide hydrochloride
Target:  

AMPK

Forschungsgebiete:  

Cancer

Buformin hydrochloride (1-Butylbiguanide hydrochloride), a potent AMPK activator, acts as an orally active biguanide antidiabetic agent. Buformin hydrochloride decreases hepatic gluconeogenesis and lowers blood glucose production in vivo. Buformin hydrochloride also has anti-cancer activities and is applied in cancer study (such as, cervical cancer and breast cancer, et al) .
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3
3 Cited Publications
Art. -Nr.: HY-12025
CAS. Nr.: 881202-45-5
Reinheit:  99.56%
Synonyms: JNJ-26854165
Forschungsgebiete:  

Cancer

Serdemetan (JNJ-26854165) is a potent anticancer agent with radiosensitizing activity. Serdemetan exhibits antiproliferative activity in various p53 wild-type tumor cells. Serdemetan also antagonizes the Mdm2-HIF1α axis leading to decreased levels of glycolytic enzymes .
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3
3 Cited Publications
Art. -Nr.: HY-W013274
CAS. Nr.: 357649-93-5
Forschungsgebiete:  

Cancer

CPTH2 is a potent histone acetyltransferase (HAT) inhibitor. CPTH2 selectively inhibits the acetylation of histone H3 by Gcn5. CPTH2 induces apoptosis and decreases the invasiveness of a clear cell renal carcinoma (ccRCC) cell line through the inhibition of acetyltransferase p300 (KAT3B) .
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3
3 Cited Publications
Art. -Nr.: HY-112726
CAS. Nr.: 1478364-68-9
Reinheit:  98.79%
Synonyms: BI-1467335
Target:  

VAP-1 MMP

Forschungsgebiete:  

Infection Inflammation/Immunology

PXS-4728A is an orally active, selective VAP-1/SSAO inhibitor with an IC50 of 5 nM and a Ki of 175 nM. PXS-4728A inhibits the expression of MMP-9. It reduces cell rolling, adhesion and migration, decreases cell infiltration levels, pro-inflammatory cytokines, chemokines and collagen deposition, and improves pulmonary function. PXS-4728A reduces the formation and progression of atherosclerotic plaques, and decreases blood lipid and blood glucose levels as well as body weight gain. PXS-4728A can be used in research related to chronic obstructive pulmonary disease, cystic fibrosis, acute pulmonary inflammation, acute lung injury, bronchiolitis obliterans syndrome, rhinovirus-exacerbated asthma, sepsis, Klebsiella pneumoniae pulmonary infection and atherosclerosis .
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3
3 Cited Publications
Art. -Nr.: HY-16688
CAS. Nr.: 66611-26-5
Target:  

5-HT Receptor

Forschungsgebiete:  

Neurological Disease

RU 24969 is a preferential 5-HT1B agonist, with a Ki of 0.38 nM, but also displays appreciable affinity for the 5-HT1A receptor (Ki=2.5 nM), and has low affinity for other receptor sites in the brain. RU 24969 could decrease fluid consumption and increase forward locomotion .
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3
3 Cited Publications
Art. -Nr.: HY-B0523
CAS. Nr.: 68475-42-3
Forschungsgebiete:  

Cardiovascular Disease Cancer

Anagrelide is a potent inhibitor of phosphodiesterase type III (PDE3) (IC50=36 nM). Anagrelide, an imidazoquinazoline derivative, acts as an inhibitor of platelet aggregation. Anagrelide inhibits bone marrow megakaryocytopoiesis. Anagrelide decreases gastrointestinal stromal tumor (GIST) cell proliferation and promotes their apoptosis in vitro. Anagrelide is a platelet-lowering agent and plays in the antithrombopoietic action .
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