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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
733 Results for "
blocking agents
" in MedChemExpress (MCE) Product Catalog:
Products (733)
733 Results for "blocking agents" in MCE Product Catalog:
Cat. No.: HY-B0937AR
CAS No.: 137-88-2
Research Areas:
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
Research Areas:
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 .
Target:
Potassium Channel Cholinesterase (ChE) TRP Channel NOD-like Receptor (NLR) Amyloid-β Tau Protein JNK NF-κB IKK
Research Areas:
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-W018798
CAS No.: 4005-51-0
1,3,4-Thiadiazol-2-amine is a 1,3,4-thiadiazole antitumor agent with the potential to penetrate the blood-brain barrier. 1,3,4-Thiadiazol-2-amine can induce hyperuricemia, and this effect is blocked by Nicotinamide (HY-B0150). 1,3,4-Thiadiazol-2-amine supports the simultaneous administration of Allopurinol (HY-B0219), and their combined use prevents hyperuricemia without reducing antitumor activity.\n1,3,4-Thiadiazol-2-amine is a condensation precursor for the synthesis of antibacterial Schiff bases and their Co/Cu/Ni/Zn (II) complexes. 1,3,4-Thiadiazol-2-amine is used in research related to tumors and bacterial infections .
Cat. No.: HY-W031757R
CAS No.: 117-78-2
Cat. No.: HY-W035399S
Cat. No.: HY-W035399S1
CAS No.: 2708340-91-2
Cat. No.: HY-Y1804S
CAS No.: 2714413-18-8
Cat. No.: HY-L153
5,267 compounds
Covalent inhibitors are small molecules that can bind specifically to target proteins through covalent bonds and inhibit their biological functions. Although for a long time, covalent targeting has been playing a subordinate role in drug discovery, with an increasing number of reports on successful clinical applications of such drugs, the potential of these agents is now being acknowledged. Currently, cysteine is the most common covalent amino acid residue in a variety of covalent drugs, and various warheads have been developed that can react with cysteine, providing the key building blocks for covalent drugs to form covalent bonds.
To meet the development needs of covalent inhibitors targeting cysteine, MCE has designed a unique collection of 5,267 compounds with different covalent warheads that target cysteine. The MCE Cysteine Targeted Covalent Library is designed using the following covalent warheads: Acrylamides, Propiolic acid ester, Dimethylamine functionalized acrylamides, Chloroacetamides, Acrylonitrile, 2-Cyanoacrylamide, Aziridine, Haloacetamide, etc.
Cat. No.: HY-118773R
CAS No.: 22816-60-0
Synonyms: A22 hydrochloride (Standard)
Target:
Research Areas:
MreB Perturbing Compound A22 hydrochloride (Standard) is the analytical standard for MreB Perturbing Compound A22 hydrochloride (HY-118773). This product is intended for research and analytical applications. MreB Perturbing Compound A22 hydrochloride (A22 hydrochloride) is a reversible MreB inhibitor and antimicrobial agent that exhibits bacteriostatic activity against Escherichia coli, with low activity against Gram-positive bacteria. MreB Perturbing Compound A22 hydrochloride rapidly and reversally delocalizes MreB from the helical/circular structures in cells, impairs MreB function, and reduces the binding of MreB to the chromosomal region proximal to the replication origin. MreB Perturbing Compound A22 hydrochloride alters the cell morphology of caulobacters to round/lemon-shaped, slows caulobacter growth, blocks their cell division, and induces the formation of spherical morphology, asymmetric division, and anucleate cells in Escherichia coli. MreB Perturbing Compound A22 hydrochloride is used for studies related to bacterial rod-shaped morphology determination, chromosome segregation, and cell division mechanisms .
Synonyms: 7-Desacetoxy-6,7-dehydrogedunin
Target:
PERK Prokineticin Receptor P2X Receptor Caspase NOD-like Receptor (NLR) Pyroptosis Tyrosinase
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology
7DG (7-Desacetoxy-6,7-dehydrogedunin) is a PKR inhibitor, P2X7 purinergic receptor inhibitor, and skin-lightening agent. 7DG binds outside the ATP-catalytic domain of PKR, blocks the kinase activity-independent protein-protein interactions of PKR, inhibits the phosphorylation and activity of PKR, disrupts ASC assembly and caspase-1 activation, and suppresses the activation of the NLRP1 inflammasome. 7DG inhibits pyroptosis, suppresses the ATP-P2X7 signaling pathway, and abolishes ATP-induced increases in the expression levels of MITF, tyrosinase, PMEL/gp100, and melanin content. 7DG exerts skin-lightening effects in cultured skin in vitro. 7DG can be used in research related to chronic obstructive pulmonary disease, gout, type 2 diabetes, Alzheimer's disease, and hyperpigmentary skin disorders .
Research Areas:
Chlorpromazine (Standard) is the analytical standard of Chlorpromazine (HY-12708). This product is intended for research and analytical applications. Chlorpromazine is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine also can inhibit clathrin-mediated endocytosis .
Research Areas:
16-Epiestriol (16-epi-Estriol; 16β,17β-Estriol) is a natural stereoisomer of estriol and an anti-inflammatory agent that targets UGT. The Ki values of 16-Epiestriol against human UGT1A10 and UGT2B7 are 98.1 μM and 162 μM, respectively. As a glucuronidation substrate, 16-Epiestriol can be modified at the 3-OH, 16-OH and 17-OH sites by various UGT enzymes; in liver microsomes, the modification mainly occurs at the 16-OH and 17-OH sites, while reactions take place at all three sites in intestinal microsomes. 16-Epiestriol acts on the phase II inflammatory process by blocking edema mediated by prostaglandins and leukocyte infiltration. It lacks glycogenic activity or any effect on blood glucose levels, and serves as an important candidate molecule in the research of inflammatory diseases .
Cat. No.: HY-B0407AR
CAS No.: 69-09-0
Research Areas:
Chlorpromazine (hydrochloride) (Standard) is the analytical standard of Chlorpromazine (hydrochloride). This product is intended for research and analytical applications. Chlorpromazine hydrochloride is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine hydrochloride exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine hydrochloride also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine hydrochloride also can inhibit clathrin-mediated endocytosis .
Cat. No.: HY-P10984
CAS No.: 206536-96-1
Target:
Research Areas:
Cat. No.: HY-W006886
CAS No.: 945212-26-0
Target:
Research Areas:
Cat. No.: HY-W041470R
CAS No.: 5349-62-2
Category:
Target:
Cat. No.: HY-L073
394 compounds
Hepatitis C virus (HCV) is a hepatotropic enveloped positive- strand RNA virus (family Flaviviridae) that infects the parenchymal cells of the liver. HCV infection is a significant public health burden. Globally, an estimated 71 million people have chronic hepatitis C virus infection. A significant number of those who are chronically infected will develop cirrhosis or liver cancer. To date, there is no vaccine against HCV, and combination pegylated alpha interferon (pIFN-) and ribavirin, the main standard-of-care treatment for HCV, is effective in only a subset of patients and is associated with a wide spectrum of toxic side effects and complications. More recently, new therapeutic approaches that target essential components of the HCV life cycle have been developed, including direct-acting antiviral (DAA) that specifically block a viral enzyme or functional protein and host-targeted agents (HTA) that block interactions between host proteins and viral components that are essential to the viral life cycle. However, the genetic diversity of HCV viruses and the stage of liver disease (i.e., cirrhosis) are revealing themselves as obstacles for effective, pan-genotypic treatments. There still exists a need for the discovery and development of new HCV inhibitors. In particular, since the future of HCV therapy will likely consist of a cocktail approach using multiple inhibitors that target different steps of infection, new antivirals targeting all steps of the viral infection cycle.
MCE offers a unique collection of 394 compounds with identified and potential anti-HCV activity. MCE Anti- Hepatitis C Virus Compound Library is a useful tool for discovery new anti-HCV drugs and other anti-infection research.
Cat. No.: HY-160906
CAS No.: 32607-79-7
Synonyms: GSSSG
Target:
Interleukin Related Tyrosinase ERK Microphthalmia Associated Transcription Factor (MITF) Reactive Oxygen Species (ROS) NF-κB
Research Areas:
Glutathione trisulfide (GSSSG) is an orally active, blood-brain barrier permeable neuroprotective agent. Glutathione trisulfide inactivates intracellular tyrosinase, regulates the expression of Cars2, Cbs, MITF and TYR, inhibits α-MSH (HY-P0252)-induced melanogenesis, and restores intracellular persulfide levels reduced by α-MSH. Glutathione trisulfide scavenges free radicals, quenches ROS, reduces Paclitaxel (HY-B0015)-induced superoxide production, upregulates the expression of antioxidant protein genes, and inhibits oxidative stress-induced cell death. Glutathione trisulfide promotes ERK1/2 activation, prevents NF-κB p65 activation, inhibits TAK1 phosphorylation, reduces pro-inflammatory cytokine expression, and blocks microglial activation. Glutathione trisulfide can be used in research related to dry age-related macular degeneration, inflammation-associated eye diseases, Alzheimer's disease, Parkinson's disease, etc.
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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
