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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
6698 Results for "
Blockers
" in MedChemExpress (MCE) Product Catalog:
Products (6698)
6698 Results for "Blockers" in MCE Product Catalog:
Cat. No.: HY-184736
Domaines de recherche:
STAT3/NF-κB-IN-3 is an orally active STAT3/NF-κB inhibitor with anti-inflammatory and antioxidant activities, which specifically blocks the phosphorylation of NF-κB and STAT3 proteins. STAT3/NF-κB-IN-3 downregulates the expression of iNOS and NOX-2 in macrophages, reduces intracellular levels of ROS and MDA, and upregulates the expression of antioxidant genes at the same time. In a mouse model of acute liver failure induced by LPS/D-GalN, STAT3/NF-κB-IN-3 alleviates liver necrosis and inflammatory cell infiltration, and reduces the release of pro-inflammatory cytokines such as IL-6 and IL-12 via the TLR4 pathway. STAT3/NF-κB-IN-3 can be used in studies related to acute liver failure .
Cat. No.: HY-184964
CAS No.: 3041997-77-4
Domaines de recherche:
NF-κB-IN-22 is an inhibitor targeting IKKβ, IκBα and NF-κB p65. NF-κB-IN-22 selectively inhibits the proliferation, migration and invasion of various cancer cells, arrests the cell cycle, and suppresses tumor growth in vivo, while exhibiting low toxicity to normal cells. NF-κB-IN-22 induces DNA damage, ROS production and apoptosis through endoplasmic reticulum stress and mitochondrial apoptotic pathways. NF-κB-IN-22 inhibits the phosphorylation of IKKβ, IκBα and NF-κB p65, blocks the NF-κB signaling pathway, and suppresses the nuclear translocation of NF-κB p65. NF-κB-IN-22 reverses the resistance to cisplatin (HY-17394). NF-κB-IN-22 can be used in research related to lung cancer, gastric cancer and liver cancer .
Cat. No.: HY-18542
CAS No.: 1402612-58-1
Target:
Domaines de recherche:
Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
KT195 is a serine hydrolase inhibitor that targets ABHD6 (IC50 = 10 nM) and ABHD2, with no significant activity against DAGLβ. KT195 inhibits endoplasmic reticulum calcium release and mitochondrial calcium uptake by targeting ABHD2, thereby blocking A23187 (HY-N6687) and H2O2-induced necrotic cell death and apoptosis. By inhibiting ABHD6 activity, KT195 significantly induces 2-AG accumulation in Neuro2A cells and reduces IL-1β secretion in lipopolysaccharide-treated macrophages. KT195 has been used as a negative control probe for DAGLβ and can be applied in studies of ABHD6 and ABHD2 in calcium signaling, lipid metabolism, neuronal function, and inflammatory .
Cat. No.: HY-187473
Domaines de recherche:
PARP1-IN-58 is a ROS-responsive prodrug constructed based on a natural stilbene scaffold, and its active parent nucleus 24c acts as a selective PARP-1 inhibitor. PARP1-IN-58 only hydrolyzes to release the active parent compound in the high-ROS microenvironment of tumors; the active parent compound competitively binds to PARP-1 and blocks DNA single-strand damage repair, upregulates intracellular ROS levels, reduces mitochondrial membrane potential, and thereby induces cell cycle arrest and mitochondria-dependent apoptosis. PARP1-IN-58 exerts potent proliferation-inhibiting effects on BRCA-deficient breast cancer cells under simulated tumor oxidative stress conditions, and exhibits tumor growth inhibitory activity in breast cancer xenograft models. PARP1-IN-58 can be used in cancer-related research .
Cat. No.: HY-189068
CAS No.: 1240895-94-6
GL-4512 is an orally active LILRB4/ILT3 inhibitor with an IC50 of 37 nM against human targets, and human Kd values of 18.1 nM and 39.2 nM, respectively. GL-4512 directly binds to the extracellular pockets of LILRB4/ILT3 that accommodate their ligands, blocks the LILRB4-SCG2 signaling pathway, and inhibits the downstream SHP1/SHP2 and STAT3 signaling pathways. GL-4512 restores anti-tumor immune activity, promotes the production of IFN-γ and IL-2, enhances the activation of cytotoxic T cells, reduces tumor cell viability, inhibits tumor growth, and strengthens intratumoral immune activation. GL-4512 can be used in research related to colorectal cancer and acute myeloid leukemia .
Cat. No.: HY-189470
Domaines de recherche:
Nav1.2-IN-4 is a blood-brain barrier-penetrant NaV1.2 inhibitor (IC50 = 31.21 μM). Nav1.2-IN-4 preferentially blocks the inactivated state of the neuronal voltage-gated sodium channel NaV1.2, inhibiting persistent and resurgent sodium currents associated with epileptogenesis. Nav1.2-IN-4 restores the GABA-glutamate balance by enhancing GABA and reducing glutamate. Nav1.2-IN-4 reduces oxidative stress in brain tissue by increasing GSH and decreasing MDA. Nav1.2-IN-4 protects mice against MES-induced tonic hindlimb extensor seizures and attenuates hippocampal neuronal degeneration in the PTZ kindling model. Nav1.2-IN-4 can be used for research on epilepsy .
Cat. No.: HY-B0426A
CAS No.: 140462-76-6
Synonyms: ALO4943A; KW4679
Target:
Domaines de recherche:
Infection Neurological Disease Metabolic Disease Inflammation/Immunology
Olopatadine hydrochloride (ALO4943A; KW4679) is an orally active histamine H1 receptor antagonist and mast cell stabilizer. Olopatadine hydrochloride exerts antiallergic effects by blocking histamine H1 receptor-mediated activities. Olopatadine hydrochloride inhibits exocytosis, chemokine release, F-actin polymerization, CXCL10-induced calcium influx, and T cell chemotactic activity. Olopatadine hydrochloride also reduces the expression levels of CXCR3 on the surface of CD4 + and CD8 + T cells. Olopatadine hydrochloride inhibits scratching behavior, improves dermatitis scores, and suppresses intraepidermal neurite outgrowth. Olopatadine hydrochloride simultaneously decreases the levels of inflammatory markers, growth factors, histamine, and specific IgE, while increasing the expression of ErbB3A/HER3A. Olopatadine hydrochloride can be used in research related to seasonal pollinosis, chronic rhinitis, urticaria, allergic conjunctivitis, alopecia areata, and atopic dermatitis .
Cat. No.: HY-B0937AR
CAS No.: 137-88-2
Domaines de recherche:
Amprolium (hydrochloride) (Standard) is the analytical standard of Amprolium (hydrochloride) (HY-B0937A). This product is intended for research and analytical applications. Amprolium hydrochloride is a thiamine transporter inhibitor and antiparasitic agent with oral activity and blood-brain barrier penetration. Amprolium hydrochloride blocks thiamine transport at the blood-brain barrier and intestine, and competitively inhibits thiamine pyrophosphokinase, inducing thiamine pyrophosphate deficiency and impairing carbohydrate synthesis. Amprolium hydrochloride induces oxidative stress, alters antioxidant enzyme activity, and inhibits acetylcholinesterase (AchE) activity. Amprolium hydrochloride disrupts reproductive organs and gametogenesis, and causes histopathological and ultrastructural damage to multiple organs. Amprolium hydrochloride induces thiamine deficiency, reduces body weight gain in mice, and causes psychomotor behavioral changes and nephropathy. Amprolium hydrochloride exhibits molluscicidal activity against the terrestrial snail Eobania vermiculata, and reduces the shedding of Eimeria meleagrimitis oocysts in feces and litter. Amprolium hydrochloride can be used for research on thiamine deficiency and coccidiosis .
Cat. No.: HY-B0937S
Domaines de recherche:
Amprolium-d7 (bromide hydrobromide) is the deuterated-labeled Amprolium (HY-B0937). Amprolium is a thiamine transporter inhibitor and antiparasitic agent with oral activity and blood-brain barrier penetration. Amprolium blocks thiamine transport at the blood-brain barrier and intestine, and competitively inhibits thiamine pyrophosphokinase, inducing thiamine pyrophosphate deficiency and impairing carbohydrate synthesis. Amprolium induces oxidative stress, alters antioxidant enzyme activity, and inhibits acetylcholinesterase (AchE) activity. Amprolium disrupts reproductive organs and gametogenesis, and causes histopathological and ultrastructural damage to multiple organs. Amprolium induces thiamine deficiency, reduces body weight gain in mice, and causes psychomotor behavioral changes and nephropathy. Amprolium exhibits molluscicidal activity against the terrestrial snail Eobania vermiculata, and reduces the shedding of Eimeria meleagrimitis oocysts in feces and litter. Amprolium can be used for research on thiamine deficiency and coccidiosis .
Cat. No.: HY-B1067AR
CAS No.: 91-75-8
Synonyms: Phenazoline (Standard)
Domaines de recherche:
Antazoline (Phenazoline) (Standard) is the analytical standard of Antazoline. This product is intended for research and analytical applications. Antazoline is a histamine H1 receptor antagonist with anticholinergic and antiviral properties. Antazoline can prevent histamine from acting on target cells through a reversible competition effect on histamine receptor sites of these cells. Antazoline can exert an antiallegic effect and prevent the occurrence of physiological reactions from the effect of blocking as well as inhibiting H1 receptor. Antazoline can effectively reduce HBV DNA in the extracellular supernatant in a dose-dependent manner, with EC50 of 2.910 μmol/L in HepAD38 cells. Antazoline also has a significant inhibitory effect on HBV DNA in the extracellular supernatant of Huh7 cells (EC50 = 2.349 μmol/L). Antazoline has anti-arrhythmic effect in acute myocardial infarctions. Antazoline can be studied in research for cardiovascular diseases, and HBV .
Cat. No.: HY-B1067BR
CAS No.: 154-68-7
Synonyms: Phenazoline phosphate (Standard)
Domaines de recherche:
Antazoline (phosphate) (Standard) is the analytical standard of Antazoline (phosphate). This product is intended for research and analytical applications. Antazoline phosphate is a histamine H1 receptor antagonist with anticholinergic and antiviral properties. Antazoline phosphate can prevent histamine from acting on target cells through a reversible competition effect on histamine receptor sites of these cells. Antazoline phosphate can exert an antiallegic effect and prevent the occurrence of physiological reactions from the effect of blocking as well as inhibiting H1 receptor. Antazoline phosphate can effectively reduce HBV DNA in the extracellular supernatant in a dose-dependent manner, with EC50 of 2.910 μmol/L in HepAD38 cells. Antazoline phosphate also has a significant inhibitory effect on HBV DNA in the extracellular supernatant of Huh7 cells (EC50 = 2.349 μmol/L). Antazoline phosphate has anti-arrhythmic effect in acute myocardial infarctions. Antazoline phosphate can be studied in research for cardiovascular diseases, and HBV .
Target:
Domaines de recherche:
Antazoline (hydrochloride) (Standard) is the analytical standard of Antazoline (hydrochloride). This product is intended for research and analytical applications. Antazoline hydrochloride is a histamine H1 receptor antagonist with anticholinergic and antiviral properties. Antazoline hydrochloride can prevent histamine from acting on target cells through a reversible competition effect on histamine receptor sites of these cells. Antazoline hydrochloride can exert an antiallegic effect and prevent the occurrence of physiological reactions from the effect of blocking as well as inhibiting H1 receptor. Antazoline hydrochloride can effectively reduce HBV DNA in the extracellular supernatant in a dose-dependent manner, with EC50 of 2.910 μmol/L in HepAD38 cells. Antazoline hydrochloride also has a significant inhibitory effect on HBV DNA in the extracellular supernatant of Huh7 cells (EC50 = 2.349 μmol/L). Antazoline hydrochloride has anti-arrhythmic effect in acute myocardial infarctions. Antazoline hydrochloride can be studied in research for cardiovascular diseases, and HBV .
Domaines de recherche:
Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Fludrocortisone (9α-Fludrocortisone) is an orally active mineralocorticoid and glucocorticoid receptor agonist. Fludrocortisone suppresses pro-inflammatory cytokine expression, reduces CCL2, IL-6, IL-8 levels, upregulates mineralocorticoid receptor (MR) expression, induces PI3K/Akt, GSK-3β, CREB, ERK1/2, mTOR phosphorylation, blocks Tau hyperphosphorylation, prevents apoptosis, promotes survival and proliferation, enhances renal sodium and water transport, increases plasma volume and blood pressure, reduces plasma potassium and renin activity, stimulates erythropoietin expression, modulates uterine receptivity genes, and reverses PP242-induced MUC1 upregulation. Fludrocortisone can be used for the research of congenital adrenal hyperplasia, postural hypotension, and adrenal insufficiency .
Target:
Potassium Channel Cholinesterase (ChE) TRP Channel NOD-like Receptor (NLR) Amyloid-β Tau Protein JNK NF-κB IKK
Domaines de recherche:
Neurological Disease Metabolic Disease Inflammation/Immunology
Drofenine (Cycloadiphene; Hexahydroadiphenine) is an brain-penetrant antispasmodic agent. Drofenine is a Kv2.1 channel inhibitor with human IC50 of 9.53 μM. Drofenine is a butyrylcholinesterase (BChE) inhibitor with Ki of 0.003 mM, and is a TRPV3 activator. Drofenine blocks Kv2.1-dependent potassium efflux, inhibits Kv2.1/JNK/NF-κB and IkBa/NF-kB signaling, suppresses Kv2.1 mRNA/protein expression. Drofenine suppresses oligomeric Aβ-induced microglial NLRP3 inflammasome activation and neuronal Tau hyperphosphorylation, improves cognitive impairment, promotes neurite outgrowth. Drofenine induces calcium influx in keratinocytes and exert cytotoxicity against keratinocytes. Drofenine ameliorates diabetic peripheral neuropathy -like pathology. Drofenine can be used for the researches of Alzheimer's disease, diabetic peripheral neuropathy and smooth muscle spasm .
Cat. No.: HY-D2984
CAS No.: 1308789-62-9
Synonyms: SNAP-PEG-NH2
Target:
Domaines de recherche:
BG-PEG-NH2 (SNAP-PEG-NH2) is an amino-terminal fluorescent probe building block and a precursor for site-specific labeling of SNAP-tag fusion proteins. BG-PEG-NH2 undergoes one-step coupling with activated carboxyl esters to form customized SNAP-tag substrates, which covalently bind to SNAP tags via a thioether bond formed at the Cys145 site. After coupling with a caged carboxyfluorescein, BG-PEG-NH2 forms a probe with Ex/Em = 500/524 nm following ultraviolet uncaging. Coupling of BG-PEG-NH2 with SeTau-647-NHS enables visualization of GPCR signal transduction. BG-PEG-NH2 is suitable for coupling reactions in aqueous phases or buffers, conjugation of labels, and labeling of intracellular or cell-surface proteins .
Cat. No.: HY-DY1081
CAS No.: 28718-90-3
Synonyms: 4',6-Diamidino-2-phenylindole dihydrochloride (solution)
Solvent and concentration: ddH2O: 5 mg/mL
Cat. No.: HY-N11846
CAS No.: 68978-09-6
Cat. No.: HY-N2600
CAS No.: 76472-87-2
Cat. No.: HY-N4246
CAS No.: 382148-47-2
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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
