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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
707 Results for "
time
" in MedChemExpress (MCE) Product Catalog:
Products (707)
707 Results for "time" in MCE Product Catalog:
Cat. No.: HY-114118S3
Purity: 96.04%
Target:
Isotope-Labeled Compounds GLP Receptor Insulin Receptor α-synuclein Apoptosis p38 MAPK Autophagy Bcl-2 Family
Research Areas:
Semaglutide- 13C6, 15N TFA is the 13C- and 15N-labeled Semaglutide TFA (HY-114118A). Semaglutide TFA is a long-acting, selective, competitive GLP-1R agonist that can penetrate the blood-brain barrier. After activating GLP-1R, Semaglutide TFA promotes insulin secretion, inhibits gastric emptying and appetite, and at the same time enhances autophagy, inhibits oxidative stress and apoptosis. Semaglutide TFA also regulates mitochondrial function and lipid metabolism (such as reducing de novo lipogenesis in the liver). Semaglutide TFA has activities such as lowering blood sugar, reducing weight, neuroprotection (such as improving motor function in Parkinson's disease models, reducing α-synuclein aggregation) and improving hepatic steatosis. Semaglutide TFA can be used for the study of neurodegenerative diseases and liver diseases such as type 2 diabetes, obesity, Parkinson's disease, metabolic associated fatty liver disease (MASLD), and cancer .
Cat. No.: HY-N3097
CAS No.: 18836-52-7
Cat. No.: HY-N3097R
CAS No.: 18836-52-7
Cat. No.: HY-L154
3,728 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 3,728 fragments with different covalent warheads that target cysteine. The MCE Cysteine Targeted Covalent Fragment Library is designed using the following covalent warheads: Acrylamides, Propiolic acid ester, Dimethylamine functionalized acrylamides, Chloroacetamides, Acrylonitrile, 2-Cyanoacrylamide, Aziridine, Haloacetamide, etc. All fragments are pre-filtered with the Rule of Three restrictions which can be used for fragment-based covalent drug development.
Cat. No.: HY-L053
1,534 compounds
From target identification to clinical research, traditional drug discovery and development is a time-consuming and costly process, which also bears high risk. Compared with traditional drug discovery, drug repositioning or repurposing, also known as old drugs for new uses can greatly shorten the development cycle and reduce development cost, which has become a new trend of drug development. After undergoing clinical trials, approved drugs have identified bioactivities, good pharmacokinetic characteristics and safety, which can greatly improve the success rate of drug discovery. A number of successes have been achieved, such as metformin for type 2 diabetes and thalidomide for leprosy and multiple myeloma, etc.
MCE provides a unique collection of 1,534 China NMPA (National Medical Products Administration) approved compounds, which have undergone extensive preclinical and clinical studies and have well-characterized bioactivities, safety and bioavailability properties. MCE NMPA-Approved Drug Library is a good tool for drug repurposing which could dramatically accelerate drug development.
Cat. No.: HY-L021M
20,566 compounds
From the discovery of traditional Chinese medicine to modern antibiotics, natural products have played an important role in the drug development process. A review of all FDA-approved drugs shows that natural products and natural product-like compounds account for more than one-third of all approved drugs. Nearly half of that came from mammals, a quarter from microbes, and a quarter from plants. Over time, the proportion of microbial natural products and natural product derivatives in approved drugs has increased. Natural products have natural advantages in drug development and can be used as lead compounds in drug discovery for drug identification and mechanism research.
MCE provides a unique collection of 20,566 natural compounds and natural product-like compounds that contain saccharides and glycosides, phenylpropanoids, quinones, flavonoids, terpenoids and glycosides, steroids, alkaloid, phenols, acids and aldehydes. Natural product and natural product-like compounds library is a useful tool for drug discovery that can be used for high-throughput screening (HTS) and high-content screening (HCS).
Cat. No.: HY-103117
CAS No.: 847871-78-7
Target:
Research Areas:
S 32212 hydrochloride is an inverse agonist of 5-HT receptors 5-HT2(CINI) and 5-HT2(CVSV) (Kis=6.6, 8.9 nM) and an antagonist of 5-HT2A and α2β-adrenergic receptors (Ki=5.8, 5.8 nM). S 32212 hydrochloride can reduce the binding of GTPγS to Gαq, and reduce the activity of phospholipase C (PLC) in HEK293 cells expressing 5-HT2(CINI) receptor and CHO cells expressing 5-HT2(CVSV) receptor (EC50=38 and 18.6 nM, respectively). S 32212 hydrochloride (2.5 mg/kg) reduces 5-HT receptor agonist-induced head twitches and penile erections in mice and rats. S 32212 hydrochloride (10, 40 mg/kg) reduces immobility time in the forced swim test and marble burying behavior in mice and rats, exerting antidepressant and anxiolytic activities.
Cat. No.: HY-112624B
CAS No.: 9004-54-0
Synonyms: Dextran 70; Dextran D70; Dextran T70(MW 64000-76000)
Cat. No.: HY-187390
Research Areas:
BRD4 RIMTAC-1 is a BRD4 PROTAC degrader based on the RIPK1-mediated targeted chimera (RIMTAC) technology. It hijacks the endogenous RIPK1-VHL complex via the RIPK1 inhibitor moiety to indirectly recruit the VHL E3 ligase, forming a BRD4-Compound 10-RIPK1-VHL quaternary complex, and degrades BRD4 through the ubiquitin-proteasome system (UPS). BRD4 RIMTAC-1 exhibits selectivity over other BET proteins, induces concentration- and time-dependent, reversible post-translational degradation of BRD4 without altering the target mRNA level. BRD4 RIMTAC-1 potently induces endogenous BRD4 degradation in RAW264.7 and HEK-293T cells, with DC50 values of 179.1 nM and 54.12 nM, respectively. BRD4 RIMTAC-1 can be used for the research of cancer and inflammation-related diseases .
Cat. No.: HY-P990175
Target:
Research Areas:
Cat. No.: HY-L136
1,525 compounds
Coagulation, also known as clotting, is the process in which blood changes from a liquid to a solid gel to form a blood clot. Thrombin, which is accurately and evenly generated in the injured part of blood vessels, is a key effector enzyme of the blood coagulation system and participates in many important biological processes, such as platelet activation, fibrinogen conversion to fibrin network, coagulation feedback amplification, etc. At the same time, to avoid the accidental formation of thrombus in the body, there is also an anticoagulant mechanism that inhibits blood coagulation.
Normal coagulation mechanism represents a balance between the pro-coagulant pathway in the injured site and anti-coagulant pathway beyond it. The blood coagulation system may be out of balance during the perioperative period or critical illness, which may lead to thrombosis or excessive bleeding. Therefore, the physiological study of coagulation balance is an important basis for clinical diagnosis and treatment of the abnormal coagulation process.
MCE supplies a unique collection of 1,525 compounds targeting key proteins in coagulation and anti-coagulation system. MCE Coagulation and Anti-coagulation Compound Library is a useful tool for study the mechanism of coagulation and anticoagulation.
Cat. No.: HY-L260
82 compounds
KRAS (Kirsten Rat Sarcoma Viral Oncogene Homolog) is one of the most important oncogenic driver genes in oncology, with high mutation frequencies in pancreatic cancer, non‑small cell lung cancer, and colorectal cancer. For a long time, KRAS was considered "undruggable" due to the lack of suitable small‑molecule binding pockets on its protein surface. In recent years, with the discovery of the switch‑II pocket and the successful approval of KRAS G12C inhibitors, KRAS‑targeted research has achieved groundbreaking progress, which has also spurred a wave of development targeting non‑G12C mutants such as G12D and G12V, as well as upstream and downstream regulatory factors including SOS1 and SHP2.
MCE KRAS Targeted Compound Library contains 82 small‑molecule compounds targeting the KRAS, serving as high‑quality research tools for mechanistic studies of KRAS‑mutant tumors, combination therapy development, resistance mechanism exploration, and high‑throughput drug screening, thereby providing robust support for KRAS‑targeted drug discovery.
Cat. No.: HY-134096
CAS No.: 78323-98-5
Synonyms: DNS-M
Target:
Research Areas:
Dansyl-morpholine (DNS-M) is a Fluorescent probe for lipid droplet imaging, cancer cell discrimination, and real-time tracking of lipid droplet dynamics. As a solvatochromic probe with a donor-π-acceptor structure, it relies on hydrophobic interaction for its mechanism of action: its good lipophilicity, confirmed by an oil-water partition coefficient LogP = 2.35, allows it to rapidly penetrate cell membranes, and it specifically localizes to the hydrophobic core of lipid droplets; its fluorescence is strongly enhanced in the nonpolar environment of lipid droplets, while it emits very weak fluorescence in polar environments like PBS buffer, and it exhibits a bathochromic shift in emission wavelength with increasing solvent polarity. It has negligible cytotoxicity, with cell viability remaining over 95% after 24-hour incubation with 100 μM of the probe, and it possesses excellent photostability, retaining over 97% of initial fluorescence intensity after 60 continuous laser scans. For cell imaging applications, its excitation/emission wavelengths for lipid droplet labeling are Ex/Em = 405/480−540 nm, and in a simulative lipid environment O/W emulsion, it has an excitation wavelength of ~346 nm and emission wavelength of ~500 nm, giving a Stokes shift of 154 nm[1].
Cat. No.: HY-13443S
Synonyms: Exenatide (Leu-13C6,15N) TFA
Exendin-4 (Leu- 13C6, 15N) TFA (Exenatide (Leu- 13C6, 15N) TFA) is the 13C, 15N-labeled Exendin-4 (HY-13443). Exendin‑4 (Exenatide) is an orally active, blood-brain barrier-permeable glucagon-like peptide-1 receptor (GLP‑1 receptor) agonist that resists degradation mediated by dipeptidyl peptidase IV. Exendin‑4 mediates multiple glucose-regulating effects, including stimulation of glucose-dependent insulin secretion, inhibition of glucagon production, increase in β-cell mass, delay of gastric emptying, reduction of food intake, improvement of peripheral insulin sensitivity, and restoration of normal islet structure. Exendin‑4 inhibits oxidative stress, alleviates inflammatory responses, and reduces neuronal apoptosis. Exendin‑4 reduces the aggregation level of mutant huntingtin, improves motor function, prolongs survival time, and regulates the expression levels of leptin and ghrelin. Exendin‑4 can be used in research related to type 2 diabetes, acute ischemic stroke, and Huntington's disease .
Cat. No.: HY-141439
CAS No.: 936475-62-6
Research Areas:
TBE 31 is an orally active Keap1/Nrf2 pathway activator and NQO1 inducer with a Dm value of 1.1 nM for NQO1. TBE 31 binds to cysteine residues of Keap1, inhibits ubiquitination and degradation of Nrf2, thereby activating the expression of ARE-dependent genes. TBE 31 induces cytoprotective enzymes including NQO1 and GST isoforms, promotes Nrf2 accumulation, and upregulates Nrf2-regulated genes related to antioxidation and lipid metabolism. TBE 31 inhibits pro-inflammatory responses, formation of AFB1-DNA adducts, endoplasmic reticulum stress, cell apoptosis (apoptosis), hepatic fibrosis, oxidative stress, and the expression of ChREBP. TBE 31 reduces the number of tumors in a mouse model of ultraviolet-induced skin carcinogenesis. TBE 31 enhances nerve growth factor-induced neurite outgrowth. TBE 31 attenuates LPS-induced serum TNF-α levels and immobility time in mice. TBE 31 can be used in research related to liver cancer, skin cancer, inflammation-related depression, and non-alcoholic steatohepatitis .
Cat. No.: HY-173309
Research Areas:
P53/TLR2 modulator-1 (Compound Z9) is a modulator that targets both the P53 pathway and TLR2 simultaneously, exhibiting anti-radiation activity. P53/TLR2 modulator-1 reduces apoptosis by inhibiting the radiation-induced expression of P53 and Bax. At the same time, it activates the TLR2 pathway, upregulates the expression of downstream proteins MyD88 and P65, and promotes the secretion of cytokines such as IL-6, thus exerting an anti-radiation effect. P53/TLR2 modulator-1 shows significant anti-radiation activity against both AHH-1 cells and HUVECs. It can also increase the survival rate of C57BL/6J mice irradiated with a lethal dose of radiation and reduce the damage to their hematopoietic system, the villous structure of the small intestine, and the spleen caused by radiation. P53/TLR2 modulator-1 can be used in the research of radiation injury-related diseases .
Cat. No.: HY-D2465
Target:
Research Areas:
CY5-Dextran (MW60-80k) is a fluorescent probe formed by covalent conjugation of the cyanine dye Cy5 to dextran. It is a pH-insensitive fluid-phase endocytosis tracer (the pH of endosomal lumen is precisely quantified by the fluorescence ratio of FITC/Cy5). CY5-Dextran (MW60-80k) is internalized by cells via a clathrin-independent fluid-phase pinocytosis pathway, and is sequentially evidenced by early endosomes, late endosomes are transported to lysosomes. CY5-D I cannot pass through the limited pore size formed by uncoating of human rhinovirus type 2 (HRV2), but can be released into the neutral cytoplasm upon adenovirus-mediated endosomal rupture, thus distinguishing between the two viral modes of "pore-forming escape" and "lysis escape". CY5-Dextran (MW60) -80k) has an excitation wavelength of 635 nm, and it can also be used for time-lapse imaging of endocytosis dynamics of stromal cells in tissues such as rat salivary glands under in vivo two-photon microscopy .
Cat. No.: HY-D3440
Target:
Research Areas:
CDPP-2PF6 is a dicationic aggregation-induced emission (AIE) fluorescent probe used for imaging of cell membranes, migrasomes, and PIP2 lipid vesicles, as well as for long-term imaging of cell membranes and migrasomes. CDPP-2PF6 relies on electrostatic and hydrophobic interactions to achieve dual-mode membrane anchoring, with the PF6 - counterion enhancing lipophilicity and generating fluorescence through restriction of intramolecular motion (RIM). When CDPP-2PF6 accumulates in phosphoinositide-rich membrane regions, RIM suppresses non-radiative decay pathways. Due to the electrostatic interaction between the positively charged core of CDPP-2PF6 and the high negative charge density of PIP2, CDPP-2PF6 exhibits a strong preferential affinity for phosphatidylinositol 4,5-bisphosphate (PIP2). The fluorescence localization of CDPP-2PF6 depends on intact lipid microdomain structures and enables real-time tracking of membrane remodeling processes (Ex/Em = 450/760 nm) .
Cat. No.: HY-L039
3,231 compounds
Techniques for reprogramming somatic cells create new opportunities for drug screening, disease modeling, artificial organ development, and cell therapy. The development of reprogramming techniques has grown exponentially since Yamanaka reprogrammed somatic cells to become induced pluripotent stem cells (iPSCs) using four transcription factors, OCT4, SOX2, KLF4, and c-MYC in 2006. Despite the development of efficient reprogramming methods, most methods are inappropriate for clinical applications because they carry the risk of integrating exogenous genetic factors or use oncogenes. Alternative approaches, such as those based on miRNA, non-viral genes, non-integrative vectors, and small molecules, have been studied as possible solutions to the problems. Among these alternatives, small molecules are attractive options for clinical applications. Reprogramming using small molecules is inexpensive and easy to control in a concentration- and time-dependent manner. It offers a high level of cell permeability, ease of synthesis and standardization, and it is appropriate for mass-producing cells.
MCE Reprogramming Compound Library contains a unique collection of 3,231 compounds that act on reprogramming signaling pathways. These compounds are potential stimulators for reprogramming. This library is a useful tool for researching reprogramming and regenerative medicine.
Cat. No.: HY-L251
93 compounds
Ionizable lipids are a class of specialized, functional lipid molecules with pH-sensitive charge characteristics. They are primarily divided into two major categories: ionizable cationic lipids and ionizable anionic lipids, though the term typically specifies ionizable cationic lipids within the biomedical field. Structurally, these lipids consist of an ionizable hydrophilic headgroup, a biodegradable linker, and hydrophobic tails. Their primary application is serving as the key delivery vehicle in lipid nanoparticles (LNPs) to encapsulate negatively charged nucleic acid macromolecules, such as mRNA vaccines, siRNA therapeutics, and CRISPR gene-editing components. In a physiological, neutral environment, they remain electrically neutral to minimize systemic toxicity and prolong circulation time. Upon entering the acidic microenvironment of cellular endosomes, however, they undergo protonation to become positively charged, thereby inducing membrane fusion and enabling the highly efficient intracellular release of the nucleic acid cargo. Consequently, they serve as the technological cornerstone for bringing nucleic acid therapies into clinical application.
To accelerate the translational process of cutting-edge nucleic acid drugs, MCE has meticulously constructed an ionizable lipid compound library containing 93 high-performance molecules, aiming to provide researchers and pharmaceutical professionals with a high-throughput, multi-dimensional lipid screening platform.
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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
