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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
94 Results for "
threshold
" in MedChemExpress (MCE) Product Catalog:
Products (94)
94 Results for "threshold" in MCE Product Catalog:
Cat. No.: HY-183288
Target:
Research Areas:
COX-2-IN-66 is a cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 8.43 μM. COX-2-IN-66 reduces release of pro-inflammatory cytokines IL-6 and TNF-α. COX-2-IN-66 exhibits acceptable cellular tolerability, with cytokine-modulating concentrations remaining below its cytotoxic threshold. COX-2-IN-66 can be used for the research of inflammation .
Cat. No.: HY-184751
CAS No.: 58409-59-9
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Bucumolol is an orally active β-adrenergic receptor blocker. Bucumolol inhibits Renin release. Bucumolol exhibits activities including local anesthesia, antiarrhythmia, antihypertension, heart rate reduction, negative inotropy, cardiac action potential inhibition, and action potential duration shortening. Bucumolol does not increase cardiac electrical threshold, prolong atrial refractory period, or affect body weight in rodents. Bucumolol can be used in research related to arrhythmia and hypertension .
Cat. No.: HY-185967
CD19 mRNA (N1-methyl-pseudouridine) encodes the B cell surface antigen CD19, used in CAR-T cell research and immunological studies. CD19 plays two main functions in human B cells: as an aptamer protein, recruiting cytoplasmic signaling proteins to the cell membrane; and within the CD19/CD21 complex, lowering the activation threshold of B cell receptor signaling pathways.
Cat. No.: HY-W277805
CAS No.: 549-68-8
Target:
Cat. No.: HY-L0088V
50,240 compounds
Life Chemicals presents a number of exclusive Pre-Plated Diversity Sets composed of 50,240 novel compounds with optimal physicochemical properties selected from Life Chemicals collection of newly synthesized items by dissimilarity search with an average Tanimoto threshold of 82%. These Diverse Screening Sets are ideal starting points for customers looking for a wide range of dissimilarity to screen against a number of targets from different classes or where little information is available on targeted protein structure.
Cat. No.: HY-183652
CAS No.: 3091546-67-4
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5-HT2C-agonist-14 is a 5-HT2C receptor agonist with an EC50 of 2.9 μM against human receptors. It also acts as a voltage-gated sodium channel inhibitor with blood-brain barrier permeable. 5-HT2C-agonist-14 elevates seizure threshold, suppresses seizure progression and alleviates pain-related behaviors. It can be used in the research of epilepsy and pain-related diseases .
Cat. No.: HY-W087919R
CAS No.: 3857-25-8
Cat. No.: HY-119753
CAS No.: 68284-69-5
Synonyms: SC-31828
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Disobutamide (SC-31828) is an orally active, blood-brain barrier permeable cationic amphiphilic ditertiary amine piperidine ring compound with antiarrhythmic properties. Disobutamide induces lysosomal phospholipid accumulation, which triggers extensive cytoplasmic vacuolization and leads to cell death. Disobutamide prolongs multiple electrocardiographic intervals in canine hearts, induces cardiac arrest at high doses, and causes decreased retinal reflectivity. Disobutamide can be used in studies related to arrhythmias, and also serves as a model drug for investigating the storage mechanisms and toxicity thresholds of intracellular amphiphilic compounds .
Cat. No.: HY-W115674
CAS No.: 1668-99-1
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Quinidine hydrochloride is an orally active antiarrhythmic agent. Quinidine hydrochloride reduces the expression level of P-gp, inhibits P-gp-mediated efflux, increases the intracellular accumulation of P-gp substrates, induces PARP cleavage and Caspase-3 activation, and elevates the proportion of Apoptotic cells at the sub-G1 phase. Quinidine hydrochloride exerts sustained block and open-channel block effects on IK(f). Quinidine hydrochloride alters the urinary metabolic ratio of Amphetamine, modulates the Pentylenetetrazol-induced seizure threshold, and regulates the anticonvulsant effect of Dextromethorphan. Quinidine hydrochloride can be used in studies related to uterine sarcoma and seizures .
Cat. No.: HY-179684
CAS No.: 2921670-99-5
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PCC0105005 is a dual-target CGRP Receptor antagonist (IC50 = 1.01 nM) and a partial agonist of 5-HT1F Receptor (EC50 = 77.91 nM). PCC0105005 shows significant efficacy in the rat model of migraine. PCC0105005 significantly reduces the expression of CGRP and c-Fos proteins, and inhibits the phosphorylation levels of ERK and CREB. PCC0105005 can be used for research on migraine .
Cat. No.: HY-15080
CAS No.: 143691-37-6
Synonyms: LY 293606
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GYKI 53405 (LY 293606) is a non-competitive, orally active AMPA receptor antagonist. GYKI 53405 shows no significant binding affinity for GABAA, GABAB or benzodiazepine receptors. GYKI 53405 increases self-grooming behavior, induces wet dog-like shakes, reduces spontaneous activity, produces anxiolytic-like behavior, reverses the anxiogenic effect induced by mCPP, inhibits locomotor activity, suppresses sound-induced and maximal electroshock-induced seizures, prolongs survival in global cerebral ischemia models, and exhibits sustained anticonvulsant effects at doses below the sedation threshold. GYKI 53405 can be used in research related to absence epilepsy, anxiety disorders and global cerebral ischemia .
Cat. No.: HY-181482
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Research Areas:
A1480LS is a peripherally restricted, orally active covalent and irreversible inhibitor of DAGLα and DAGLβ, with IC50 values of 6 nM and 4 nM against human targets, respectively, and IC50 values ≤15 nM across mouse, rat, dog, monkey and human systems. A1480LS reduces the levels of 2-arachidonoylglycerol, arachidonic acid, and cyclooxygenase- and lipoxygenase-derived eicosanoids. A1480LS inhibits injury-induced production of 2-arachidonoylglycerol and arachidonic acid in the peripheral sciatic nerve, and suppresses the responses of high-threshold and wide-dynamic-range-like dorsal horn neurons to mechanical stimulation. A1480LS alleviates pain behaviors in rat models of inflammatory pain, neuropathic pain and chemotherapy-induced peripheral neuropathy .
Cat. No.: HY-L133
446 compounds
Copper is an important co-factor of all biological enzymes, but if the concentration exceeds the threshold of maintaining the homeostasis mechanism, copper will lead to cytotoxicity. This death mechanism has been named "Cuproptosis".
The mechanism of cuproptosis distinct from all other known mechanisms of regulated cell death, including apoptosis, pyroptosis, necroptosis, and ferroptosis.
Copper combine with the lipoylated components of the tricarboxylic acid cycle (TCA), leading to lipoylated protein aggregation and subsequent loss of iron-sulfur cluster proteins, ultimately resulting in protein toxicity stress and cell death. Studies have shown that the necessary factors for cuproptosis include the presence of glutathione, mitochondrial metabolism of galactose and pyruvate, and glutamine metabolism.
Targeted regulation of cuproptosis is a potential choice to treat cancer, rheumatoid arthritis, and other diseases. For example, up-regulation of LIPT1 may inhibit the occurrence and development of tumors by destroying TCA in mitochondria and then inducing cuproptosis.
MCE supplies a unique collection of 446 cuproptosis-related compounds, all of which act on the targets or signaling pathways related to cuproptosis and may have in inhibitory or activated effect on cuproptosis. MCE Cuproptosis Library is a useful tool for drug research related to cancer, rheumatoid arthritis, and other diseases.
Cat. No.: HY-L928
7,106 compounds
G protein-coupled receptors (GPCRs) are membrane proteins in humans and one of the most important targets in drug discovery. Approximately 35% of launched drugs are targeted GPCRs, making them a crucial class of targets in drug discovery.
The orthosteric site of a GPCR is its endogenous ligand’s (such as neurotransmitters or hormones) binding site. This site plays a central role in signal transduction. Small molecules binding to this site typically contain a protonatable amino group, enabling the formation of salt bridges or hydrogen bonds with acidic residues in the binding pocket. In contrast, the allosteric site does not directly initiate signaling but modulates the signal intensity of the GPCR by altering or stabilizing the conformation of the orthosteric site. Small molecules binding to the allosteric site often contain multiple aromatic rings to occupy hydrophobic pockets and achieve their functional effects.
MCE has collected over 7,106 reported bioactive molecules targeting GPCRs, covering Class A, B, and C GPCRs. These small molecules were subjected to AI representation to extract 2D and 3D features. Subsequently, we do screening by AI score based on similarity to identify molecules in diversity library highly similar to the reported bioactive molecules in both 2D and 3D, with a threshold greater than 0.7. Further screening based on cLogP was applied to select molecules with good lipophilicity, which facilitates the binding of small molecules to GPCRs. This diversity library can be widely applied to the discovery of compounds targeting GPCR proteins.
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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
