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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
703 Results for "
Noncompetitive
" in MedChemExpress (MCE) Product Catalog:
Products (703)
703 Results for "Noncompetitive" in MCE Product Catalog:
Cat. No.: HY-N2735
CAS No.: 1111897-60-9
Target:
Cat. No.: HY-U00134R
CAS No.: 2179-37-5
Synonyms: Bencyclane (Standard); Benzcyclan (Standard)
Target:
Research Areas:
Benzcyclane (Standard) is the analytical standard of Benzcyclane (HY-U00134). This product is intended for research and analytical applications. Benzcyclane (Bencyclane; Benzcyclan) is a vasodilator with serotonin receptor antagonism. Benzcyclane exerts atypical serotonin antagonistic effects in rabbit superior mesenteric arteries. Benzcyclane relaxes high K +-induced contractions in rabbit basilar arteries and superior mesenteric arteries, and selectively inhibits sympathetic nerve stimulation-induced contractions in rabbit pulmonary arteries. Benzcyclane exerts non-competitive norepinephrine antagonistic effects in rabbit superior mesenteric arteries, and slightly reduces the maximum contractile response induced by histamine. Benzcyclane relaxes smooth muscles, induces transient hypotension, inhibits thrombosis, and accelerates blood fibrinolytic activity. Benzcyclane increases cerebral glucose content/uptake, enhances hypoxia tolerance in mice, and increases cerebral blood supply in dogs. Benzcyclane is applicable to studies related to cerebral vascular circulation .
Cat. No.: HY-W683756
CAS No.: 16625-69-7
Target:
Telomerase Gap Junction Protein P2X Receptor Calcium Channel Reactive Oxygen Species (ROS) NF-κB SGK TNF Receptor
Research Areas:
Boldine hydrochloride is an aporphine alkaloid telomerase (telomerase) inhibitor (IC50 of 0.17 μM for TERT) and a pannexin/connexin hemichannel blocker, with oral activity and blood-brain barrier permeability. Boldine hydrochloride inhibits telomerase activity through direct interaction with the telomerase ribonucleoprotein and non-competitive binding near the TERT active site, and downregulates hTERT mRNA while shifting alternative splicing toward non-functional transcripts. Boldine hydrochloride blocks Panx1, Cx43, Cx26, and Cx30 hemichannels as well as P2X7 receptor-mediated calcium influx. Boldine hydrochloride exhibits antioxidant, anti-inflammatory, antiproliferative, and cytotoxic activities by scavenging ROS, inhibiting NFκB, dephosphorylating SGK1, and reducing TNF-alpha levels. Boldine hydrochloride can be used in research on breast cancer, Alzheimer's disease, glioblastoma, diabetes, and spinal cord injury .
Cat. No.: HY-103430B
CAS No.: 164265-49-0
Research Areas:
SKF-83566 hydrochloride is an orally active, blood-brain barrier-permeable D1/D5 dopamine receptor antagonist with a Ki value of approximately 0.4-0.56 nM.
SKF-83566 hydrochloride modulates locomotor behavior and spatial memory by blocking D1 receptors and inhibits glioblastoma progression by targeting the DRD1/c-Myc/UHRF1 pathway.
SKF-83566 hydrochloride acts as an inhibitor of the dopamine transporter (DAT) and adenylyl cyclase 2 (AC2).
SKF-83566 hydrochloride competitively binds to DAT to inhibit dopamine reuptake and non-competitively inhibits AC2 activity, thereby reducing cAMP accumulation.
SKF-83566 hydrochloride is used in research areas such as dopaminergic system mechanisms, learning and memory, targeted intervention for glioblastoma, AC2 pathophysiology, antiparasitic drug screening, and synaptic plasticity (the "gating effect") .
Cat. No.: HY-113416AS
Purity: 98.00%
Synonyms: DHEA sulfate-d6 sodium dihydrate; Prasterone sulfate-d6 sodium dihydrate
Cat. No.: HY-114849R
CAS No.: 27314-13-2
Synonyms: SAN 9789 (Standard)
Research Areas:
Norflurazon (Standard) (SAN 9789 (Standard)) is the analytical standard of Norflurazon (HY-114849). This product is intended for research and analytical applications. Norflurazon (SAN 9789) is a pre-emergence Herbicide. Norflurazon non-competitively inhibits phytoene desaturase by competing with the enzyme cofactor and disrupts carotenoid biosynthesis, thereby leading to chlorophyll photodegradation and chlorosis. Norflurazon inhibits MGDG synthase, CDP-choline phosphotransferase, Omega-3 FAD7 desaturase, and PG delta-3-trans desaturase, and activates LysoPC-acyltransferase and Omega-3 FAD3 desaturase. Norflurazon inhibits photosynthetic membrane organization, mitochondrial respiration, ATP production, PI3K signaling, and ERK1/2 phosphorylation. Norflurazon activates MAPK P38 phosphorylation and ER stress signaling. Norflurazon induces morphological malformations and cardiovascular effects in zebrafish embryos .
Synonyms: R-40244
Target:
Environmental Pollutants Apoptosis Bcl-2 Family Herbicide HSP PERK Eukaryotic Initiation Factor (eIF) Akt GSK-3 Reactive Oxygen Species (ROS)
Research Areas:
Flurochloridone (R-40244) is an orally active herbicide and an inducer of ER stress, apoptosis, and cytotoxicity. Flurochloridone upregulates GRP78 and activates the PERK-eIF2α-ATF4 UPR axis, ATF6, CHOP, Bax, and Bim. Flurochloridone decreases Akt, p-Akt, GSK3β, and p-GSK3β levels, and induces ROS, oxidative stress, γ-glutamyl cycle activation, and GSH accumulation. Flurochloridone inhibits mitochondrial respiration and ATP production while enhancing glycolysis and cell viability inhibition. Flurochloridone inhibits spermatogonial proliferation, spermatocyte meiosis, and sperm mitochondrial membrane potential, and induces Sertoli cell apoptosis and mitochondrial damage. Flurochloridone non-competitively binds phytoene desaturase, blocking phytoene desaturation and carotenoid synthesis, leading to leaf bleaching and phytotoxicity. Flurochloridone can be used for research on male reproductive toxicity, hepatotoxicity, and as a herbicide .
Target:
TRP Channel Aldehyde Dehydrogenase (ALDH) Cholinesterase (ChE) Keap1-Nrf2 Amyloid-β Fungal Apoptosis
Research Areas:
Infection Neurological Disease Inflammation/Immunology Cancer
Dyclonine (Dyclocaine) is an orally active, blood-brain barrier-permeable piperidine phenylacetone small molecule commonly used as a local anesthetic. Dyclonine acts as a highly selective allosteric antagonist of TRPV3; it also reversibly inhibits G9a, ALDH2 and ALDH3A1, non-competitively blocks AChE. Dyclonine activates the Nrf2/ARE pathway, relieves the epigenetic silencing of FXN, blocks Aβ42 aggregation, and promotes remyelination and reparative polarization of microglia. Dyclonine alleviates pruritus via TRPV3 inhibition; it is used in studies of neurodegenerative disease models based on its AChE inhibitory, antioxidant and remyelinating effects; it sensitizes drug-resistant tumors through ALDH inhibition, and combined use with protease inhibitors induces more tumor cell apoptosis; it inhibits Candida albicans in vitro. Dyclonine can be used for research on multiple diseases including neurodegenerative diseases, cancer and pruritic dermatitis .
Cat. No.: HY-P11313
Synonyms: Rat chromogranin A367–387
Research Areas:
Cat. No.: HY-103430
CAS No.: 108179-91-5
Research Areas:
SKF-83566 hydrobromide is an orally active, blood-brain barrier-permeable D1/D5 dopamine receptor antagonist with a Ki value of approximately 0.4-0.56 nM.
SKF-83566 hydrobromide modulates locomotor behavior and spatial memory by blocking D1 receptors and inhibits glioblastoma progression by targeting the DRD1/c-Myc/UHRF1 pathway.
SKF-83566 hydrobromide acts as an inhibitor of the dopamine transporter (DAT) and adenylyl cyclase 2 (AC2).
SKF-83566 hydrobromide competitively binds to DAT to inhibit dopamine reuptake and non-competitively inhibits AC2 activity, thereby reducing cAMP accumulation.
SKF-83566 hydrobromide is used in research areas such as dopaminergic system mechanisms, learning and memory, targeted intervention for glioblastoma, AC2 pathophysiology, antiparasitic drug screening, and synaptic plasticity (the "gating effect") .
Synonyms: DHEA sulfate sodium-d6; Prasterone sulfate sodium-d6
Cat. No.: HY-180155
CAS No.: 3105470-83-2
Target:
Keap1-Nrf2 Cholinesterase (ChE) Interleukin Related TNF Receptor Reactive Oxygen Species (ROS) Heme Oxygenase (HO) Quinone Reductase
Research Areas:
Keap1/Nrf2/ARE activator 2 is an activator of Keap1/Nrf2/ARE pathway and non-competitively inhibits AChE with an IC50 of 14.79 μM and a Ki of 1.35 μM. Keap1/Nrf2/ARE activator 2 promotes Nrf2 nuclear translocation, leading to antioxidant gene upregulation and enhanced cellular defense against oxidative stress. Keap1/Nrf2/ARE activator exhibits robust neuroprotection against both H2O2- and Scopolamine (SCA) (HY-N0296)-induced injury in PC12 cells. Keap1/Nrf2/ARE activator 2 ameliorates memory impairment and the neuro-inflammation associated with SCA-initiated cognitive dysfunction in a zebrafish model. Keap1/Nrf2/ARE activator 2 can be used for the research of Alzheimer's disease .
Synonyms: DHEA sulfate sodium (Standard); Prasterone sulfate sodium (Standard)
Category:
Cat. No.: HY-W778236
CAS No.: 1346603-47-1
Synonyms: SAN 9789-13C,d3
Research Areas:
Norflurazon- 13C,d3 (SAN 9789- 13C,d3) is the d3, 13C-labeled Norflurazon (HY-114849). Norflurazon (SAN 9789) is a pre-emergence Herbicide. Norflurazon non-competitively inhibits phytoene desaturase by competing with the enzyme cofactor and disrupts carotenoid biosynthesis, thereby leading to chlorophyll photodegradation and chlorosis. Norflurazon inhibits MGDG synthase, CDP-choline phosphotransferase, Omega-3 FAD7 desaturase, and PG delta-3-trans desaturase, and activates LysoPC-acyltransferase and Omega-3 FAD3 desaturase. Norflurazon inhibits photosynthetic membrane organization, mitochondrial respiration, ATP production, PI3K signaling, and ERK1/2 phosphorylation. Norflurazon activates MAPK P38 phosphorylation and ER stress signaling. Norflurazon induces morphological malformations and cardiovascular effects in zebrafish embryos .
Cat. No.: HY-103430AR
CAS No.: 99295-33-7
SKF-83566 (Standard) is the analytical standard of SKF-83566 (HY-103430A). This product is intended for research and analytical applications. SKF-83566 is an orally active, blood-brain barrier-permeable D1/D5 dopamine receptor antagonist with a Ki value of approximately 0.4-0.56 nM.
SKF-83566 modulates locomotor behavior and spatial memory by blocking D1 receptors and inhibits glioblastoma progression by targeting the DRD1/c-Myc/UHRF1 pathway.
SKF-83566 acts as an inhibitor of the dopamine transporter (DAT) and adenylyl cyclase 2 (AC2).
SKF-83566 competitively binds to DAT to inhibit dopamine reuptake and non-competitively inhibits AC2 activity, thereby reducing cAMP accumulation.
SKF-83566 is used in research areas such as dopaminergic system mechanisms, learning and memory, targeted intervention for glioblastoma, AC2 pathophysiology, antiparasitic drug screening, and synaptic plasticity (the "gating effect") .
Cat. No.: HY-121337R
CAS No.: 61213-25-0
Synonyms: R-40244 (Standard)
Target:
Reference Standards Environmental Pollutants Apoptosis Bcl-2 Family Herbicide HSP PERK Eukaryotic Initiation Factor (eIF) Akt GSK-3 Reactive Oxygen Species (ROS)
Research Areas:
Flurochloridone (Standard) (R-40244 (Standard)) is the analytical standard of Flurochloridone (HY-121337). This product is intended for research and analytical applications. Flurochloridone (R-40244) is an orally active herbicide and an inducer of ER stress, apoptosis, and cytotoxicity. Flurochloridone upregulates GRP78 and activates the PERK-eIF2α-ATF4 UPR axis, ATF6, CHOP, Bax, and Bim. Flurochloridone decreases Akt, p-Akt, GSK3β, and p-GSK3β levels, and induces ROS, oxidative stress, γ-glutamyl cycle activation, and GSH accumulation. Flurochloridone inhibits mitochondrial respiration and ATP production while enhancing glycolysis and cell viability inhibition. Flurochloridone inhibits spermatogonial proliferation, spermatocyte meiosis, and sperm mitochondrial membrane potential, and induces Sertoli cell apoptosis and mitochondrial damage. Flurochloridone non-competitively binds phytoene desaturase, blocking phytoene desaturation and carotenoid synthesis, leading to leaf bleaching and phytotoxicity. Flurochloridone can be used for research on male reproductive toxicity, hepatotoxicity, and as a herbicide .
Cat. No.: HY-B0364AR
CAS No.: 536-43-6
Synonyms: Dyclocaine hydrochloride (Standard)
Dyclonine hydrochloride (Standard) (Dyclocaine hydrochloride (Standard)) is the analytical standard of Dyclonine hydrochloride (HY-B0364A). This product is intended for research and analytical applications. Dyclonine hydrochloride (Dyclocaine hydrochloride) is an orally active, blood-brain barrier-permeable piperidine phenylacetone small molecule commonly used as a local anesthetic. Dyclonine hydrochloride acts as a highly selective allosteric antagonist of TRPV3; it also reversibly inhibits G9a, ALDH2 and ALDH3A1, non-competitively blocks AChE. Dyclonine hydrochloride activates the Nrf2/ARE pathway, relieves the epigenetic silencing of FXN, blocks Aβ42 aggregation, and promotes remyelination and reparative polarization of microglia. Dyclonine hydrochloride alleviates pruritus via TRPV3 inhibition; it is used in studies of neurodegenerative disease models based on its AChE inhibitory, antioxidant and remyelinating effects; it sensitizes drug-resistant tumors through ALDH inhibition, and combined use with protease inhibitors induces more tumor cell apoptosis; it inhibits Candida albicans in vitro. Dyclonine hydrochloride can be used for research on multiple diseases including neurodegenerative diseases, cancer and pruritic dermatitis .
Cat. No.: HY-B0364AS
Synonyms: Dyclocaine-d9 hydrochloride
Cat. No.: HY-W015490R
CAS No.: 130-15-4
Research Areas:
1,4-Naphthoquinone is an inhibitor with broad-spectrum inhibitory activity targeting DNA polymerase, NF-κB and monoamine oxidase (MAO-A/B), with antibacterial and anti-biofilm efficacy. 1,4-Naphthoquinone is a competitive inhibitor of MAO-B (Ki=1.4 μM) and a non-competitive inhibitor of MAO-A (Ki=7.7 μM). 1,4-Naphthoquinone inhibits DNA polymerase pol α, β, γ, δ, ε, λ with IC50 ranging from 5.57-128 μM. 1,4-Naphthoquinone inhibits tumor cell proliferation, induces apoptosis and necrosis, and has anti-angiogenic and anti-inflammatory activities by inducing oxidative stress, depleting glutathione (GSH), inhibiting DNA polymerase-mediated DNA synthesis and blocking NF-κB nuclear translocation. 1,4-Naphthoquinone can be used in anti-bacterial , anti-tumor and anti-inflammatory studies, including inhibition of melanoma and colon cancer cell growth and endothelial cell function, as well as LPS-induced inflammation models .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
