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SARS-CoV-2 contains four main structural proteins: spike (S), membrane (M), envelope (E), and nucleocapsid (N) proteins. All the proteins and subcellular structures of CoVs are promising targets for SARS-CoV-2 research.
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Organoids represent an important bridge between 2D cultures and in vivo mouse/human models. The organoid technology exerts enormous potential in evaluation of efficacy and toxicity of drugs, regenerative medicine, and precision medicine.In this article, we will briefly introduce organoid technology.
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Development of Intestinal Organoid
2022-07-28
3D organoid is one of the revolutionary developments in biomedical field during the past 10 years. The establishment of intestinal organoids is an important milestone in the development of organoid technology. -
RNA therapeutics have changed the landscape of drug development, which possess broader spectrum of drug targets, simplicity and efficiency in development and manufacturing.In this article, we will discuss the underlying mechanisms of RNA-based drugs on the market or in clinical stages.
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Tsvetkov et al. published in Science and demonstrated a copper-induced programmed cell death — Cuproptosis. As a novel programmed cell death, excess copper triggers abnormal aggregation of lipoylated proteins in TCA cycle and clearance of Fe-S cluster proteins, ultimately leading to cell death.
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A comprehensive explanation of ferroptosis
2022-09-15
Ferroptosis is a new type of RCD that depends on iron and characterized by the accumulation of lipid peroxides. In this article, we will pay our attention on ferroptosis and briefly discusses its mechanism. -
It's has been proved that p53, as a tumor suppressor gene and immune guardian, may become a destroyer through its own mutation. Moreover, the mechanism of p53 was found to be related to ferroptosis. This article mainly explores the mechanism between p53 and ferroptosis in detail.
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Organoids have great potential in research of organ development, disease modeling, drug screening and, precision and regenerative medicin. In this article, we will expalin the origin of the organoids. Adult stem cells (ASCs) or pluripotent stem cells (PSCs) , which is the better choice.
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Autophagy, derived from the Greek meaning "eating of self", plays an indispensable role in maintaining homeostasis. p27 is an inhibitor of cyclin CDKs, but how p27 regulates autophagy remains unknown. This article will cover the mechanism of autophagy and p27-related cell cycle regulation.
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AlphaFold2 can predict disease-related protein structures at low cost, and then find potential drugs for these diseases through drug repositioning, virtual screening, and other methods. ZINC is a public database summarizing information about billions of compounds. AlphaFold2 + ZINC20 speeds up the virtual screening process and improves the computing speed.
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CMA (chaperone-mediated autophagy) plays an essential role in maintaining neuronal protein stability and preventing neurodegeneration. In this article, we will comprehensively clarify the role of CMA in the occurrence and development of neurodegenerative diseases.
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TME (Tumor microenvironment) is considered as a complex integrated system, composed of cellular components such as tumor cells and immune cells, as well as non-cellular components such as ECM and cytokines. According to the spatial distribution of immune cells in TME, "hot" and "cold" TME will be explained in this article.
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As powerful pain relievers, the opioids morphine and fentanyl have been "checked" by their side effects (listed as controlled substances). How to reduce its side effects? What is its mechanism? This research will explore its mechanism.
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Efferocytosis is the process in which phagocytes remove programmed dead cells. It prevents secondary necrosis of dying cells from releasing harmful cell contents (such as oxides and proteases) that may cause inflammation. Here, we will introduce three stages of efferocytosis: Find, Eat, Digest.
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Understanding the mechanism of aging not only has guiding significance for prolonging human life but also has important clinical significance for the prevention and treatment of diseases in the elderly population , thus, improving their life quality and well-being.
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Mammalian cells can also photosynthesize like plants! Photosynthesis can improve cell anabolism and exhibit good clinical effect in degenerative diseases (osteoarthritis).
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The latest study of Cell magazine "Neural mechanism underlying depressive-like state associated with social status loss" considers social factors as a breakthrough point. It has been found that the downward transition of social status induces depression-like behavior in mice whereas improves the depressive state by restoring their social environment.
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Necroptosis, also known as necroptosis, is a form of regulated necrotizing cell death mediated by RIP1 and RIP3 kinases. Necroptosis is a process that prevents the self-destruction of activated cells that are blocked by apoptosis. Necroptosis plays a tumor suppressor role in most cases. It may provide benefits in the researches of a variety of human diseases involving immune inflammation and cell death.
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Stem cell classification and its application
2023-05-18
Stem cells (SCs) have the unique ability to self-renew and differentiate into different cell types. SCs can differentiate into various types of tissue cells under specific conditions. Additionally, they can be further cultured to form different tissues and organs in the human body. Stem cells have numerous applications in various fields, including cell therapy, organ transplantation, neurodegenerative disease modeling, and drug screening. -
Mitophagy:Mechanisms and Detection
2023-05-25
About 60 years ago, Christian de Duve first used the term "autophagy" to describe his observation of the degradation of mitochondria and other intracellular structures in lysosomes of rat liver. Over the years, autophagy has remained a beloved topic of research by the National Natural Science Foundation of China (NSFC).Today, let's talk about mitochondrial autophagy. -
Structure of Lipid Droplets
2023-06-15
Huh? Lipid droplets? Organelles? In the past, biological data usually only show the traditional organelles, such as mitochondria, Golgi apparatus, endoplasmic reticulum, etc., lipid droplets are often not mentioned by people. Today, we will make a systematic explanation of lipid droplets, so that everyone has a clear understanding! -
HLA-E, A Novel Immune Checkpoint
2023-06-29
Immune checkpoints have immunosuppressive functions. It can be used in the research of tumor immunotherapy. In this article, we introduce a new paper entitled "Immune checkpoint HLA-E: CD94 - NKG2Amediates evasion of circulating tumor cells from NK cell surveillance "research paper. -
How to Perform Western Blot?
2023-07-13
Western blot is one of the most frequently performed experiments in molecular biology, biochemistry and immunology. This article describes in detail how to do WB. -
Organoid Culture: Questions & Answers
2023-07-26
In the last issue, we conducted a live lecture on the theme of organoid culture. Today, we have a special topic to solve your doubts in the last live class! -
WHO's Q2 drug list has been updated. Let's take you through the list of the most noteworthy small molecule drugs that we should pay attention to.
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FDA Approved Drug List!
2023-09-14
In the first half of 2023 (as of June 27), the FDA approved 26 new drugs, let's take you learn about it through the article. -
IHC is an indispensable technique for studying tissue morphology and in situ antigen expression, but usually only one or two antigens in tissues can be stained for analysis. It cannot judge the results more intuitively. Today, Little M will introduce you to the upgraded version mlHC.
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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 of diseases such as cancer, infectious diseases, and rare diseases.
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FDA Annual Review | Record-breaking number of new drug approvals in 2023!
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Are frozen cells always damaged? Is the survival rate of revived cells low? When is it appropriate to freeze cells? What should be considered when reviving them? Today, we're sharing a guide to avoid pitfalls in cell freezing and revival!
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KRAS, a gene we've heard so much about, has quickly risen to fame after shedding its "undruggable" label. After reading numerous articles, it's easy to feel overwhelmed and wonder: What exactly should we know about this often-discussed but previously "undruggable" target KRAS?
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Compound Screening Guide!
2024-03-15
How to use compound library? How to design an experiment if you buy a compound library? Want a specific experimental protocol? This article will introduce popular experimental techniques and provide new ideas for publishing high level literature. -
Wnt/β-catenin and tumor EMT
2024-03-18
Epithelial-Mesenchymal Transition (EMT) is closely related to the plasticity of tumor cells and is a necessary process for tumor metastasis. Wnt/β-catenin is one of the main actors involved in the EMT process. Today, we’re here to popularize the tumor EMT and Wnt/β-catenin pathway~ -
The 2024 AACR meeting concluded successfully in California, USA. Which antitumor drugs stole the show at this conference?
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Katalin Karikó and Drew Weissman were awarded the Nobel Prize in Physiology or Medicine in 2023 for their groundbreaking work in nucleoside modification, which paved the way for the creation of successful mRNA vaccines to fight against COVID-19. Let's now delve into the complete process of mRNA vaccine development.
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SPR, which stands for Surface Plasmon Resonance, essentially works by detecting the interaction between ligands and analytes on a biosensor chip. This in turn allows us to probe the properties and structure of substances. With this technology, we can analyze molecules, proteins, DNA, and various organic and inorganic substances in samples in real-time with precision.
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Common Questions and Solutions for WB
2024-05-09
Come to understand the common problems and solutions of WB, and better complete the experiment! -
Still struggling to find the preparation methods for various solutions? Save your time! Here comes a nanny-level tutorial!
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STZ Induced Diabetes Models
2024-06-13
Spotlight: How can STZ Help Diabetes Research? -
How important is the compound library? It connects to drug screening on one end and leads to lead compound modifications on the other, serving as one of the sources of new drug development.
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Antibodies!
2024-07-26
Today, We introduce antibodies for everyone! -
Streptavidin-Biotin System
2024-08-03
Streptavidin strongly binding small molecule biotin is one of the most popular non-covalent coupling methods. Streptavidin can be coupled to various carriers such as magnetic beads and agarose matrix, and become a highly specific affinity medium to capture various biotin-labeled ligands. -
What Are Popular Anti-tumor Drug Targets?
2024-08-20
The rapid development of targeted anti-cancer drugs has spurred diverse research across various modalities. These include small molecules, monoclonal antibodies (mAbs), cell immunotherapies, antibody-drug conjugates (ADCs), and PROTACs (proteolysis targeting chimeras). -
Cuproptosis, How much do you know?
2024-08-22
Cells die in a variety of ways, including apoptosis, pyroptosis, necrosis, and ferroptosis......And, of course, cuproptosis. So, how much do you know about cuproptosis? -
Virtual Screening and New Uses for Old Drugs
2024-09-17
With the advancement of medical science, drug screening against various disease targets has become the fundamental strategy for drug development. Currently, computer-based virtual screening techniques are emerging in the field of new drug research due to their efficiency and low cost. Let's explore it today! -
Recently, Mol Cell reported the discovery of the first ferroptosis marker, Hyperoxidized PRDX3! Let’s take a look together~
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Cuproptosis's Knowledge Points!
2024-09-25
With the establishment of the cuproptosis mechanism related research has attracted more and more attention from major journals. Expect to use the sharp sword of cuproptosis to stab the tumor cells. -
2024 Nobel Prize Announcements! Curious about the details? Click to dive into the exciting developments!
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How they used PKH 26 for cellular studies?
2024-10-21
We are thrilled to highlight our client study using PKH 26 (MedChemExpress) , a red fluorescent dye that has proven invaluable for in vitro cell labeling and tracing. This innovative research, published in the Journal of Nanobiotechnology. -
Delve into the intricate networks that govern mitochondrial quality control. By examining key mechanisms such as biogenesis, mitochondrial dynamics (fission and fusion), proteolysis, and mitophagy.
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A New Form of Cell Death: PANoptosis!
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We are thrilled to share the latest advancements in AI technology as highlighted in this insightful article. From groundbreaking innovations to transformative applications, the future of AI is brighter than ever!
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Advancing Chronic Kidney Disease Research with GJ103 and Lamin B1 Antibody!
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In early January 2025, MIT Tech Review unveiled its annual list of top 10 breakthrough technologies poised to redefine the future. Among these, stem cell therapy stood out for its potential to treat diverse diseases—including neurodegenerative disorders, diabetes, cancer, and heart failure. This groundbreaking approach uses stem cells to replace damaged cells, offering hope for millions worldwide.
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When you hear "inflammation" and "DNA damage," you might immediately think of disease or injury. However, in brains, these two processes are key steps in forming long-term memories, particularly related to specialized cells in our brain called hippocampal neurons.
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Autophagy is a fundamental process that degrades various components within the cell.
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This article will tell you about the common methods of modeling liver disease in animal models.
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This article introduces some common cardiovascular disease models, inducers, modeling protocols and successful modeling cases in the research.
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Do you feel confused when you start culturing cells? This article will show you the basic methods and steps of cell culture!
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As a pivotal branch in the post - genomic era, proteomics is committed to comprehensively elucidating the types, abundances, structures, functions, and interactions of all proteins within living organisms. This article will tell you the key steps of proteomics sample preparation based on mass spectrometry. This article will tell you the key steps of proteomics sample preparation based on mass spectrometry.
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Cell Migration vs. Invasion: Differences Revealed by Scratch Assays and Transwell Experiments
2025-05-30
In scientific research, cell migration and invasion are crucial for understanding many important biological processes. This article delves into commonly used detection methods: the scratch assay and Transwell migration/invasion assay. -
Western blotting is a crucial and fundamental technique in life science research. It plays a significant role in exploring protein expression and function. The following article will comprehensively and thoroughly elaborate on the specific procedures and detailed key points of this experiment.
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How should drug screening experiments be conducted? How can we ensure the accuracy of the lead compounds identified? This article will take you through how MCE's clients conduct drug screening experiments.
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In this issue, we will conduct an in-depth interpretation from the dimensions of nanoparticle design, mechanism of action, in vivo and in vitro efficacy, and immune regulation, revealing how this research brings new hope for the treatment of invasive tumors through interdisciplinary innovation!
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In protein biology, Co-IP is a powerful tool to uncover protein "social networks." But poorly performed, it easily becomes an awkward lab "meet-and-greet." Today, we discuss making Co-IP experiments elegant and efficient—so you pull down target proteins with confidence and precision.
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IHC, ICC, IF Techniques: A Practical Guide
2025-07-25
Confused About IHC/ICC/IF? Why Does Immunostaining Seem So Complicated? Read This Now! Master Immunostaining with Confidence! -
Chromatin Immunoprecipitation (ChIP) Demystified: A Complete Guide to Epigenetic Analysis
2025-08-05
In this issue, we introduce a powerful technique for detecting interactions between epigenetic regulatory factors and DNA—Chromatin Immunoprecipitation (ChIP)! -
HTS Breakthroughs Powered by MCE Libraries
2025-08-13
Key High-Throughput Screening Breakthroughs of 2024 Featuring MCE -
The article introduces the mechanisms of ROS generation and the methods for their detection.
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Encountering challenges with the high costs and long timelines of drug screening? Have a defined target but remain uncertain how to efficiently identify active molecules? Unsure how to validate hits generated from virtual screening? The ‘Winning Combination’ of drug screening offers a powerful solution to address these critical obstacles.
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Generating Stable Cell Lines with Lentivirus
2025-09-16
A step-by-step protocol of establishing stable cell lines using lentivirus -
A groundbreaking study in Nature Communications reveals the key mechanism behind Idiopathic Pulmonary Fibrosis and identifies an existing drug with the potential to counter it.
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This detailed guide outlines the standardized experimental protocols for multiplex immunohistochemistry (mIHC), systematically summarizes common technical issues encountered during sample preparation, staining and imaging processes, and provides practical troubleshooting solutions to ensure reliable and reproducible results in biomedical research and clinical sample analysis.
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For all the protein research folks out there, techniques like IP and Co-IP are no stranger, right? And of course, there's a faster and more convenient go-to tool—Protein A/G magnetic beads! In this article, let's chat about how these beads work their magic in classic experiments like IP and Co-IP.
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Microglia– the only immune cells within the brain parenchyma. With advancements in imaging technologies, people’s understanding of microglia has shifted from being viewed as 'resting' cells to 'highly active' cells, particularly due to their dynamic processes that seem to be probing surrounding tissues and monitoring neuronal activity. This has made microglia a focal point of research in the field of neuroscience.
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Efficient Generation of Mouse Small Intestinal Organoids: A Complete Experimental Protocol Guide
2025-12-10
How to successfully create mouse small intestine organoids? A detailed, hands-on guide to the entire process, all in one article! -
A November 2025 Cell study discovers Mitoxyperilysis, a new mTOR-regulated, caspase-independent cell death pathway driven by innate immune and metabolic dysregulation via mitochondrial-plasma membrane contact and oxidative damage, and verifies its potential to induce tumor necrosis for cancer therapy with key regulators including BAX, BAK1 and BID.
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This paper elaborates on cytokines for culturing major immune cells, their regulatory roles, recombinant cytokines' merits and MCE’s related high-quality products.
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Essential for High-Impact Papers: Present Your CCK-8 Experimental Results in a More Outstanding Way!
2026-03-18
CCK-8 is a widely used WST‑8‑based reagent for cell proliferation and cytotoxicity assays. It features high sensitivity, reliable results and easy operation, and is applicable to cell viability analysis, drug screening and growth inhibition testing. -
FISH is a molecular technique using fluorescent probes to detect specific nucleic acids in cells, with high sensitivity and diverse biomedical applications.
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This article walks you through the experimental design and workflow of flow cytometry, delivering a clear, dynamic, and professional overview to elevate your research.
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This review introduces the major forms of programmed cell death, with a focus on the molecular mechanisms of ferroptosis and the methods used for its detection.
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This review critically examines the role of the JAK-STAT pathway in immunity and autoimmune diseases, reviews current clinical applications of targeted therapies, and highlights emerging trends in autoimmune drug development.
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This review summarizes the mechanisms of DSS-induced colitis, commonly used modeling approaches, and key considerations related to DSS molecular weight.
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This review discusses β-cell dysfunction driven by mitochondrial impairment, outlines mitochondrial quality control networks, and summarizes strategies to restore mitochondrial function.
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This review provides a practical guide to the fundamental mechanisms, regulatory pathways, and detection methods of pyroptosis.
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Review mitophagy regulation, disease mechanisms, and therapeutic advances to guide future research and drug development.
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Review the mechanisms, mitochondrial regulation, disease relevance, and translational opportunities of the NLRP3–STING axis in neuroinflammation.
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Explore the mechanisms driving immune tolerance breakdown in autoimmune diseases and emerging tolerance-restoring strategies, with a focus on IL-2-based immune modulation.
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Explore how mitochondrial quality control, inflammatory signaling, and metabolic–epigenetic reprogramming regulate cellular senescence and the SASP, along with strategies to restore mitochondrial homeostasis.
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EC0489, a SMDC for Cancer Therapy
2019-03-25
EC0489, a conjugate of folic acid and desacetyl vinblastine hydrazide, is a SMDC under development for the treatment of solid tumours. -
Role of PRMT7 Probe SGC3027 in Cancer
2019-03-27
SGC3027 is the first potent, selective and cell active chemical probe for PRMT7. SGC3027 is also a pro-drug, which converts to the active compound SGC8158 -
AZD5991, a macrocyclic molecule with high selectivity for Mcl-1, reduces Mcl-1 protein in AZD5991-sensitive but not in AZD5991-resistant MM cell lines.
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A Novel and Efficacious RAF Inhibitor RAF709
2019-03-30
RAF709, a novel and efficacious RAF inhibitor, activates the MAPK pathway and shows antitumor activity in tumor cells harboring BRAF or RAS mutations. -
CF53 is a highly potent, selective and orally active inhibitor of BET protein, with anti-tumor activity in acute leukemia and breast cancer cell lines.
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HJB97 is a BET PROTAC inhibitor with good anti-tumor activity, and effectively blocks the degradation of BRD2, BRD3, and BRD4 proteins induced by BETd-260.
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CCB02 is an tubulin binder and has potential in the therapy of cancer cells with extra centrosomes. CCB02 also activates spindle assembly checkpoint.
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H3B-5942 is a selective and irreversible estrogen receptor covalent antagonist, inactivates both ERαWT and ERα mutation.
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AZD3229 is a Potent Pan-KIT Mutant Inhibitor
2019-04-04
AZD3229 is a potent, pan-KIT mutant inhibitor with potent single digit nM growth inhibition against a diverse panel of mutant KIT driven Ba/F3 cell lines. -
A Lead PROTAC BRD9 Chemical Degrader
2019-04-06
PROTAC BRD9 Degrader-1 is a lead PROTAC BRD9 chemical degrader and a selective probe useful for the study of BAF complex biology. -
SGC-GAK-1 is a potent, selective, and cell-active GAK inhibitor and shows potent anti-proliferative activity in LNCaP and 22Rv1 cells.
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COH000 is an allosteric, covalent and irreversible inhibitor of SUMO-activating enzyme, with an IC50 of 0.2 μM for SUMOylation in vitro.
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HS-1371 is a Small Molecule RIP3 Inhibitor
2019-04-09
HS-1371 is a novel kinase inhibitor of RIP3-mediated necroptosis, showing an inhibitory effect on S227 auto-phosphorylation of RIP3 at the basal level. -
Nevanimibe is a selective and potent ACAT1 inhibitor. An excellent drug candidate in the treatment of adrenocortical cancer.
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PhiKan 083 is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a Kd of 167 μM.
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AZ304, a Dual BRAF Inhibitor Against Cancer
2019-04-12
AZ304 is a potent BRAF inhibitor, blocks both wild type BRAF and V600E mutant BRAF activity, with IC50s in the nanomolar range. -
Novel Greatwall Kinase Inhibitor GKI-1
2019-04-13
GKI-1, a GWL inhibitor, robustly inhibited ROCK1 with an IC50 of ~11 μM, but only weakly affected PKA and had no observable inhibition towards CDK2. -
IITZ-01 is a potent lysosomotropic autophagy inhibitor with single-agent antitumor activity, with an IC50 of 2.62 μM for PI3Kγ.
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SSE15206 is a microtubule polymerization inhibitor, with a GI50 of 197 nM in HCT116 cells. Causes aberrant mitosis resulting in G2/M arrest.
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Erteberel is a Selective ERβ Agonist
2019-04-16
Erteberel (LY500307) is a synthetic, nonsteroidal estrogen which acts as a selective ERβ agonist and under development for the treatment of schizophrenia. -
MBQ-167 is a dual Rac/Cdc42 inhibitor in in metastatic cancer, with IC50s of 103 nM for Rac 1/2/3 and 78 nM for Cdc42 in MDA-MB-231 cells, respectively.
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PRN1008 is a Reversible Covalent and Oral Active Inhibitor of Bruton’s Tyrosine Kinase (BTK)
2019-04-18
PRN1008 is a selective, reversible covalent and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 1.3 nM. -
Multiple Tyrosine Kinases Inhibitor TAS-115
2019-04-19
TAS-115 is a potent VEGFR and c-Met/HGFR-targeted kinase inhibitor with IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively. -
Y06036 is a potent and selective BET inhibitor for potential treatment of castration-resistant prostate cancer. With nanomolar inhibition.
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JNJ-64619178 is a selective and pseudo-irreversible PRMT5 inhibitor with an IC50 of 0.14 nM. Has potent Activity In Lung Cancer.
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(E)-AG 99 is an EGFR inhibitor and shows a growth-inhibition on not only serum-starved cells but also normally grown cells. Treatment for Bladder cancer.
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Cevipabulin is a microtubule-active compound and inhibits the binding of [3H] vinblastine to tubulin, with an IC50 of 18-40 nM for in human tumor cell line.
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BTR-1 potently inhibits cell growth. It induces S phase arrest, affects DNA replication. Dose-dependently induces cytotoxicity in leukemic cell lines.
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TAK-828F is a potent, selective and orally active retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist. TAK-828F inhibits IL-17A cytokine expression and reduces symptoms of autoimmune encephalomyelitis mice.
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Y06137 is a potent and selective BET inhibitor, which binds to the BRD4(1) bromodomain with a Kd of 81 nM. Antitumor activity.
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Borussertib is a covalent-allosteric and first-in-class inhibitor of protein kinase Akt, with an IC50 of 0.8 nM and a Ki of 2.2 nM for Akt-wt.
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TD-428 is a Highly Specific BRD4 Degrader
2019-04-29
TD-428, a immunomodulatory drug analog, is a highly specific BRD4 degrader with a DC50 of 0.32 nM. TD-428 reduces c-Myc levels more efficiently than JQ1. -
SLLN-15 is an oral activ enhancer of autophagy that activates cytostatic macroautophagy/autophagy in triple-negative breast cancer (TNBC).
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CB-6644 is a selective non-ATP-competitive inhibitor of the RUVBL1/2 complex. CB-6644 significantly reduces tumor growth without obvious toxicity.
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A1874 is a nutlin-based and BRD4-degrading PROTAC with a DC50 of 32 nM. Effective in inhibiting many cancer cell lines proliferation
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NSC 228155 is a activator of EGFR and a potent inhibitor of KIX-KID interaction. NSC 228155 shows excellent anti-tumor activity.
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BSJ-03-123, a Degrader with Proteome-wide Selectivity for CDK6 (PROTAC). Induces a G1 cell-cycle arrest without a measurable increase in apoptosis.
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FT671 is a potent, non-covalent and selective USP7 inhibitor with an IC50 of 52 nM and binds to the USP7 catalytic domain with a Kd of 65 nM.
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BSc5371 is a potent and irreversible FLT3 inhibitor. BSc5371 is cytotoxic to FLT3-dependent cell line. BSc5371 has potential to treat Acute Leukemia.
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MRTX-1257 is a selective, irreversible, covalent and oral active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation.
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SJ572403 (SJ403) is an inhibitor of disordered protein p27 (Kip1). p27 (Kip1) is a regulator of the CDKs that control eukaryotic cell division.
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ZM223 is a non-sulfamide NEDD8 activating enzyme (NAE) inhibitor, with IC50 value of 100 nM in cells. ZM223 has potential to treat colon cancer.
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JR-AB2-011 inhibits mTORC2 activity by blocking Rictor-mTOR association. JR-AB2-011 has anti-glioblastoma multiforme (GBM) properties.
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CHMFL-ABL-039 is a Type II native and drug-resistant mutant BCR-ABL inhibitor for chronic myeloid leukemia. The IC50s are 7.9 nM and 27.9 nM, respectively.
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MM-589 is an inhibitor of WDR5 and MLL protein-protein interaction. Binds to WDR5 (IC50=0.90 nM) and inhibits the MLL H3K4 methyltransferase activity.
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GNE-955 is a potent and orally active pan Pim kinase inhibitor with Kis of 0.018, 0.11, 0.08 nM for Pim1, Pim2, Pim3, respectively.
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STL127705 is a Ku 70/80 heterodimer protein inhibitor, inhibits Ku70/80-DNA interaction (IC50 of 3.5 μM) and Ku-dependent activation of DNA-PKCS kinase.
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SRT 1460, a Sirtuin-1 Activator, Negatively Regulate Pancreatic Cancer Cell Growth and Viability
2019-05-18
SRT 1460, a selective SIRT1 activator with an EC1.5 value of 2.9 μM, is more potent than Resveratrol and the closest sirtuin homologues. -
MS4077 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) with a Kd of 37 nM for binding affinity to ALK. Efficacy for breast cancer and lung cancer.
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A Potent and Specific Tankyrase Inhibitor RK-287107, Blocks Colorectal Cancer Cell Growth
2019-05-20
RK-287107 is a specific tankyrase inhibitor with IC50s of 14.3 and 10.6 nM for tankyrase-1 and tankyrase-2, respectively. -
JI051 is a stabilizer for the Hes1-PHB2 interaction, induces cell-cycle arrest by inhibiting the Notch downstream effector gene Hes1.
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ORIC-101 is a highly potent and selective glucocorticoid receptor antagonist, with an EC50 of 5.6 nM. ORIC-101 has anti-cancer activity.
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BGT226 is a Dual PI3K/mTOR Inhibitor
2019-05-25
BGT226 (NVP-BGT226) is a PI3K (with IC50s of 4 nM, 63 nM and 38 nM for PI3Kα, PI3Kβ and PI3Kγ)/mTOR dual inhibitor. -
SNIPER(TACC3)-1 targets the TACC3 protein for degradation via the ubiquitin-proteasome pathway. SNIPER(TACC3)-1 induces cancer cell death.
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MDL-800 is an allosteric and selective SIRT6 activator. MDL-800 increases SIRT6 deacetylation activity with an EC50 of 10.3 µM
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TAS-114 is a dual dUTPase/dihydropyrimidine dehydrogenase (DPD) inhibitor, can improving the therapeutic efficacy of fluoropyrimidine.
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CFI-402257 is a highly selective and oral active TTK/Mps1 inhibitor with an IC50 of 1.7 nM for TTK. CFI-402257 has potential to treat ovary cancer and TNBC.
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RIPGBM is a selective inducer of apoptosis in glioblastoma multiforme (GBM) cancer stem cells (CSCs) with an EC50 less than 500 nM.
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GGTI-2418 is a selective GGTase I inhibitor. GGTI-2418 inhibits GGTase I and FTase activities with IC50s of 9.5 nM and 53 μM, respectively.
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TX1-85-1, a ATP-competitive ligand of Her3, covalent modification of Her3 to inhibit Her3 signaling
2019-06-01
TX1-85-1 is a Her3 (ErbB3) inhibitor with an IC50 of 23 nM. TX1-85-1 induces partial degradation of Her3 protein and attenuates Her3-dependent signaling. -
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PF-06821497 (compound 23a) is an orally active EZH2 inhibitor, with a Ki value <0.1 nM against mutant Y641N EZH2. Exhibits robust tumor growth inhibition.
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OTS186935 is a methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 reveales significant inhibition of tumor growth in animal models.
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GSK3145095 is a RIP1 kinase inhibitor with an IC50 of 6.3 nM. Potently blocks the TNF response and RIP1-dependent inflammatory cytokine MIP-1β production.
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IZCZ-3 is a potent c-MYC transcription inhibitor with antitumor activity. IZCZ-3 induces an apparent accumulation of cells in the G0/G1 phase.
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PF-06465469 is a Covalent Inhibitor of ITK
2019-06-08
PF-06465469 is a potent and covalent inhibitor of ITK with an IC50 of 2 nM. PF-06465469 inhibits MEK1/2 or AKT phosphorylation. -
Riviciclib is a Potent CDKs Inhibitor
2019-06-09
Riviciclib P276-00 free base) is a potent CDK inhibitor, which inhibits CDK9-cyclinT1, CDK4-cyclin D1, and CDK1-cyclinB with IC50s of 20 nM, 63 nM, and 79 nM, respectively -
Olutasidenib is a highly potent, selective inhibitor of mutant IDH1 that could be used in the treatment of AML or myelodysplastic syndrome (MDS).
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SJFδ, a 10-atom Linker PROTAC, Degrades p38δ
2019-06-11
SJFδ, a 10-atom Linker PROTAC, Degrades p38δ, degrades p38δwith strong capacity. SJFδ degrades p38δ with a DC50 of 46.17±9.85 nM and a Dmax of 99.41±3.31%. -
Gboxin is an oxidative phosphorylation inhibitor that targets glioblastoma. Gboxin inhibits the activity of F0F1 ATP synthase and shows antitumour activity.
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CBS9106, a Reversible Oral CRM1 Inhibitor, Causes Arrest of the Cell Cycle and Induces Apoptosis
2019-06-14
CBS9106 (SL-801) is a reversible oral CRM1 inhibitor antitumor activities. CBS9106 causes arrest of the cell cycle and induces apoptosis. -
Ralimetinib (LY2228820) is a selective and ATP-competitive inhibitor of p38 MAPK α/β, with IC50s of 5.3 and 3.2 nM, respectively. Anti-tumor activity.
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BAY-11-7082 inhibits the proliferation and induces the apoptosis of U266 cells through inhibiting NF-κB pathway. BAY 11-7082 ameliorates experimental diabetic neuropathy by modulating neuroinflammation and improving antioxidant defence.
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NU6140 is a selective CDK2-cyclin A inhibitor (IC50, 0.41 μM). NU6140 also potently inhibits Aurora A and Aurora B, with IC50s of 67 and 35 nM, respectively
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ASP5878 is an oral active inhibitor of FGFR 1, 2, 3, and 4, with IC50 values of 0.47 nM, 0.6 nM, 0.74 nM and 3.5 nM for FGFR 1, 2, 3, and 4 kinase activity.
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SPP-86 is a selective inhibitor of RET tyrosine kinase, with an IC50 of 8 nM. SPP-86 inhibits RET-induced PI3K/Akt and MAPK signaling.
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S130, Targeting ATG4B, Inhibits Autophagy and Activates Apoptosis in Colorectal Colon Cancer
2019-06-19
S130 is a high affinity, selective inhibitor of ATG4B (a major cysteine protease) with an IC50 of 3.24 µM. S130 suppresses autophagy flux. -
BI8622 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC50 of 3.1 μM. BI8622 suppresses colony formation of Ls174T cells.
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RO-5963 is a dual p53-MDM2 and p53-MDMX inhibitor with IC50s of ~17 nM and ~24 nM, respectively. Potently shows apoptotic activity.
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S18-000003 is a potent, selective and orally active inhibitor of retinoic acid receptor-related orphan receptor-gamma-t (RORγt). S18-000003 ameliorates psoriasis-like lesions in vivo. S18-000003 can be used for the research of skin inflammatory diseases.
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TH34, an HDAC6/8/10 inhibitor with IC50s of 4.6 μM, 1.9 μM, and 7.7 μM respectively, shows high selectivity over HDAC1/2/3.
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Alisertib (MLN 8237) is an oral active and selective Aurora A kinase inhibitor with an IC50 of 1.2 nM. To treat hematologic malignancies and solid tumors.
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MA242 is a Dual Inhibitor of MDM2 and NFAT1
2019-06-24
MA242 is a dual inhibitor of murine double minute 2 (MDM2) and nuclear factor of activated T cells 1 (NFAT1) for Pancreatic Cancer Therapy. -
PTC299 is a dual and orally active DHODH and VEGF inhibitor, has broad and potent activity against hematological cancer cells.
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NG25, a Dual Inhibitor of TAK1 and MAP4K2, Enhances Doxorubicin-mediated Apoptosis in Breast Cancer
2019-06-26
NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with IC50s of 149 nM and 21.7 nM, respectively. NG25 enhances Dox-mediated apoptosis in breast cancer. -
GW7604 is an antiestrogen. GW7604 is the metabolite of GW5638, which is a high affinity estrogen receptor (ER) antagonist
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TAS4464 is a highly potent and selective inhibitor of NEDD8 activating enzyme (NAE), with an IC50 of 0.955 nM. TAS4464 shows antitumor activity.
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DK419 is an orally active Wnt/β-catenin inhibitor, with an IC50 of 0.19 μM. DK419 reduces Axin2, β-catenin, c-Myc, Cyclin D1 and Survivin expression.
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AZ82 is a selective kinesin-like protein KIFC1 (HSET/KIFC1) inhibitor, with a Ki of 43 nM and an IC50 of 300 nM for KIFC1.
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CH-223191 is a Specific Antagonist of Aryl Hydrocarbon Receptor (AhR) with Anti-Tumor Activity
2019-07-02
CH-223191 is a potent and specific antagonist of aryl hydrocarbon receptor (AhR). CH-223191 blocks the binding of TCDD to AhR with an IC50 of 0.03 µM. -
MRT67307, a dual IKKε/TBK1 inhibitor, inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 blocks mTOR-dependent autophagy.
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NSC 95397 inhibits MKP-1 and suppresses proliferation and induces apoptosis in colon cancer cells through MKP-1 and ERK1/2 pathway.
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PTC-028 is an orally bioavailable inhibitor of stem cell factor BMI-1 in ovarian cancer. Depletion of BMI-1 by PTC-028 induces caspase-mediated apoptosis
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DS21360717 is a potent and orally active FER tyrosine kinase inhibitor, with an IC50 of 0.49 nM. DS21360717 has anti-cancer activity.
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LY3295668 is a potent, orally active and highly specific Aurora-A kinase inhibitor, with Ki values of 0.8 nM and 1038 nM for AurA and AurB, respectively.
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BAY1238097 is a selective inhibitor of BET binding to histones and has strong anti-proliferative activity through down-regulation of c-Myc levels.
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CCT020312, the G1/S checkpoint activator, is a selective EIF2AK3/PERK activator. CCT020312 elicits EIF2A phosphorylation in cells.
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MRT-83, a Potent Smoothened Antagonist, has Potential to Treat Hh-pathway Related Diseases
2019-07-10
MRT-83 is a potent antagonist of Smo, with an IC50 in the nanomolar range. MRT-83 antagonizes the up-regulation of Ptc transcription. -
MS023 is a selective inhibitor of human type I PRMTs inhibitor, with IC50s of 30, 119, 83, 4 and 5 nM for PRMT1, 3, 4, 6, and 8, respectively.
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S55746 (BLC201) is an orally active and selective BCL-2 inhibitor, with a Ki of 1.3 nM.. S55746 (BLC201) has antitumor activity with low toxicity.
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WYC-209 is a retinoic acid receptor (RAR) agonist. WYC-209 induces apoptosis primarily via the caspase 3 pathway (IC50 = 0.19 μM for mTRCs).
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SBI-0206965 is a selective and cell permeable autophagy kinase ULK1 inhibitor with IC50s of 108 nM for ULK1 and 711 nM for the highly related kinase ULK2 .
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TPCA-1, a Direct Dual Inhibitor of STAT3 and NF-κB, Regresses Mutant EGFR-Associated NSCLC
2019-07-15
TPCA-1 is a potent and selective inhibitor of IKK-2 with IC50 of 17.9 nM. TPCA-1 is an effective inhibitor of STAT3 phosphorylation, DNA binding. -
NMS-P515 is a potent, orally active and stereospecific PARP-1 inhibitor, with a Kd of 16 nM and an IC50 of 27 nM (in Hela cells). Anti-tumor activity.
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ERD-308 is a highly potent PROTAC degrader of ER for ER+ breast cancer treatment. ERD-308 induces >95% of ER degradation at concentrations as low as 5 nM.
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JG-98, an Hsp70 inhibitor, binds tightly to a conserved site on Hsp70 and disrupts the Hsp70-Bag3 interaction. JG-98 shows anti-cancer activities.
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ARS-853 is a Selective KRAS (G12C) Inhibitor
2019-07-19
ARS-853 is a selective, covalent KRAS (G12C) inhibitor, with an IC50 of 2.5 μM. ARS-853 treatment also induces apoptosis in four KRASG12C mutant cell lines. -
ARS-1620 is an atropisomeric selective KRAS G12C inhibitor for KRAS-mutant cancer with desirable pharmacokinetics. A promising clinical candidate.
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MZP-55 is a selective PROTAC degrader of BRD3/4, shows no obvious effect on BRD2. MZP-55 exhibits excellent activity in cancer research.
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dBET6 is a potent PROTAC degrader of BET, shows high affinity to BRD4(1), and possess good efficacy in T cell acute lymphoblastic leukemia activity.
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SAR-260301 is a selective PI3Kβ inhibitor with an IC50 of 23 nM. SAR-260301 is a potent and highly selective PI3Kβ inhibitor for melanoma.
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FGTI-2734 is a dual farnesyl and geranylgeranyl transferase-1 inhibitor. FGTI-2734 prevents membrane localization of KRAS and mutant KRAS pancreatic tumors.
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GSK2643943A is a Novel DUB Inhibitor
2019-07-25
GSK2643943A is a novel deubiquitylating enzyme (DUB) inhibitor. GSK2643943A targets USP20/Ub-Rho and shows an IC50 of 160 nM. -
M-89 is a specific menin inhibitor, with a Kd of 1.4 nM. M-89 inhibits the Menin-MLL protein-protein interaction and has potential to treat MLL leukemia.
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APG-115 is an orally active MDM2 protein inhibitor binding to MDM2 protein. APG-115 blocks the interaction of MDM2 and p53 and induces apoptosis.
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MBM-55 is a potent, selective Nek2 inhibitor with an IC50 of 1 nM. MBM-55 shows antitumor activities and induces cell cycle arrest and apoptosis.
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GSK3368715 is an orally active and SAM uncompetitive type I PRMT inhibitor that produces a shift in arginine methylation states.
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MT-802 is a potent BTK degrader based on PROTAC technology, with a DC50 of 1 nM. MT-802 has potential to treat C481S mutant chronic lymphocytic leukemia.
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Alobresib is an Orally Active BET Bromodomain Inhibitor for Uterine Serous Carcinoma Treatment
2019-07-31
Alobresib is a novel and potent BET bromodomain inhibitor for recurrent/chemotherapy resistant uterine serous carcinoma overexpressing c-Myc. -
GNE-207 is an orally bioavailable inhibitor of the bromodomain of CBP, with an IC50 of 1 nM, exhibits a selectively index of >2500-fold against BRD4 (1).
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BI-0252 is an orally active, selective MDM2-p53 inhibitor with an IC50 of 4 nM and can induce tumor regressions in all animals of a mouse SJSA-1 xenograft.
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ML367 is an ATAD5 Stabilization Inhibitor
2019-08-03
ML367 is a potent inhibitor of ATAD5 stabilization. It blocks DNA repair pathways, and suppresses phosphorylation of RPA32 and CHK1. -
DW14800 is a potent PRMT5 inhibitor, exhibits anti-cancer activity. DW14800 reduces H4R3me2s and H3R8me2s, and reduces symmetric dimethylarginine.
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LSN 3213128 is a selective, nonclassical, orally bioavailable antifolate with anti-cancer activity. LSN 3213128 potently and specifically inhibits AICARFT.
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CA-5f is a potent late-stage macroautophagy (autophagy) inhibitor via inhibiting autophagosome-lysosome fusion. CA-5f increases LC3B-II and SQSTM1 protein.
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ACBI1 is a PROTAC Degrader of BAF Complex
2019-08-07
ACBI1 is a potent PROTAC degrader of BAF ATPase subunits SMARCA2, SMARCA4 and PBRM1, with DC50s of 6 nM, 11 nM and 32 nM in MV-4-11 cells, respectively. -
TAK-659 is a highly potent, selective, reversible and orally available inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3).
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dMCL1-2 is a potent and selective degrader of myeloid cell leukemia 1 (MCL1) based on PROTAC, which binds to MCL1 with a KD of 30 nM.
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VERU-111 (ABI-231) is a potent and orally bioavailable α and β tubulin inhibitor, which displays strong antiproliferative activity.
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JH-RE-06, a potent REV1-REV7 interface inhibitor (IC50=0.78 μM; Kd=0.42 μM), targets REV1 that interacts with the REV7 subunit of POLζ.
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BI-882370 is a potent RAF kinase inhibitor with IC50s of 0.4, 0.8, and 0.6 nM for oncogenic BRAFV600E-mutant, the WT BRAF and CRAF kinases , respectively.
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BDP9066 is a potent and selective myotonic dystrophy-related Cdc42-binding kinase MRCK inhibitor with an IC50 of 64 nM for MRCKβ in SCC12 cells.
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TTT-28 Antagonizes Multidrug Resistance by Selectively Inhibiting the Efflux Activity of ABCB1
2019-08-15
TTT-28 is a novel selective inhibitor of ABCB1 (P-gp/MDR1) with high efficacy and low toxicity, which selectively blocks the efflux function of ABCB1. -
MPT0B392 Induces Apoptosis via Inhibiting Tubulin Polymerization and Inducing c-JNK Activation
2019-08-16
MPT0B392 is a novel microtubule depolymerizing agent that triggers induction of the mitotic arrest and induces JNK activation, leading to apoptosis. -
ZT-12-037-01 is a ATP-competitive and specific STK19 inhibitor and inhibits oncogenic NRAS-driven melanocyte malignant transformation.
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NXT629 is a potent, selective, and competitive PPAR-α antagonist and shows high selectivity over other nuclear hormone receptor.
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GNA002 is a highly potent, specific and covalent EZH2 inhibitor, which efficiently reduces EZH2-mediated H3K27 trimethylation.
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BJE6-106 is a selective PKCδ inhibitor with an IC50 of 0.05 μM and targets selectivity over PKCα. BJE6-106 induces caspase-dependent apoptosis.
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PT2977 is an orally active and selective HIF-2α inhibitor with an IC50 of 9 nM. PT2977 is a potential treatment for ccRCC and VHL disease.
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BI-2852 is a potent KRAS inhibitor with nanomolar affinity and reduces pERK and pAKT levels in a dose-dependent manner in a KRAS mutant cell line NCI-H358.
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BI-4924 is a Selective PHGDH Inhibitor
2019-08-23
BI-4924 is a lipophilic and highly plasma protein bound selective phosphoglycerate dehydrogenase (PHGDH) inhibitor (IC50=3 nM) with excellent microsomal. -
MS31 is a highly selective spindlin 1 inhibitor, which inhibits the interactions between SPIN1 and H3K4me3. MS31 is not toxic to nontumorigenic cells.
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CP-10 is a Specific PROTAC Degrader of CDK6
2019-08-25
CP-10 is a PROTAC with highly selective, specific, and remarkable CDK6 degradation (DC50=2.1 nM), which has anti-cancer activity. -
AAPK-25 is a potent and selective Aurora kinases and Polo-like Kinases (PLK) dual inhibitor, which shows anti-tumor activity.
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AMG 232 is a potent, selective and orally available inhibitor of p53-MDM2 interaction, with an IC50 of 0.6 nM. AMG 232 binds to MDM2 with a Kd of 0.045 nM.
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RG7112 is a potent, selective, first clinical and orally active MDM2-p53 inhibitor, with a KD of 11 nM for binding to MDM2.
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ARV-825 is a PROTAC, and acts as a potent BRD4 degrader, with Kds of 90 and 28 nM for BRD4 BD1 and BRD4 BD2, respectively.
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GMB-475 is a PROTAC BCR-ABL1 degrader, overcomes BCR-ABL1-dependent drug resistance, targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel Lindau.
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BAY-293 is a potent inhibitor of Son of Sevenless 1 (SOS1) and blocks RAS activation via disruption of the KRAS-SOS1 interaction with an IC50 of 21 nM.
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MI-773 is a potent MDM2 inhibitor (Ki, 0.88 nM), blocks p53-MDM2 interaction, and and leads to p53 accumulation, with anti-cancer activity.
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CITCO is a selective agonist of constitutive androstane receptor, with an EC50 of 49 nM, with potent activity against brain tumor stem cells.
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RRx-001 is a hypoxia-selective epigenetic agent, triggers apoptosis and overcomes drug resistance in multi myeloma cells.
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MI-1061 is an Orally Active MDM2 Inhibitor
2019-09-04
MI-1061 is an orally bioavailable MDM2 inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53, induces apoptosis, and has anti-tumor activity -
dBET57 is a potent and selective degrader of BRD4BD1 based on the PROTAC technology and mediates recruitment to the CRL4CRBN E3 ubiquitin ligase.
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FT113 is a potent and orally active fatty acid synthase inhibitor, with an IC50 of 213 nM for full-length recombinant human FAS, with anti-tumor activity.
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SGC-iMLLT is a potent, selective MLLT1/3-histone interactions inhibitor and shows high binding activity towards MLLT1 YEATS domain and MLLT3 YD.
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YUKA1 is a potent, selective and cell permeable KDM5A inhibitor, with an IC50 of 2.66 μM. YUKA1 exhibits anti-cancer activity.
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MD-224 is a human MDM2 degrader based on the PROTAC concept. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells.
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BAY 61-3606 is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor and sensitizes apoptosis by in breast cancer.
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E3330, an APE1 Redox Inhibitor, Modulates Cell Migration and Invasion in Metastatic Cancer
2019-09-13
E3330 is a direct, orally active AP endonuclease 1 (APE1) inhibitor, which suppresses NF-κB DNA-binding activity. E3330 shows good anticancer properties. -
AOH1160, an Orally Active PCNA Inhibitor, Exhibits Efferctive Anti-cancer Activity with Low Toxicity
2019-09-14
AOH1160 is a potent, first-in-class, orally available PCNA inhibitor and exhibits broad-spectrum anti-cancer activity without causing unacceptable toxicity. -
WJ460 is a potent myoferlin (MYOF) inhibitor, which exerts anti-metastatic activity in the nanomolar range in breast cancer cells.
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UPGL00004 is a allosteric glutaminase C inhibitor which strongly inhibits the proliferation of highly aggressive triple-negative breast cancer cell lines.
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TL02-59 is a selective Src-family kinase Fgr inhibitor with an IC50 of 0.03 nM. TL02-59 also inhibits Lyn and Hck. TL02-59 suppresses AML cell growth.
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IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1) R132 mutations.
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DVD-445 is a potent peptidomimetic covalent TrxR1 inhibitor with an IC50 of 0.60 μM for rat TrxR1. DVD-445 has good anticancer application.
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MPT0E028 is an orally active and selective histone deacetylase (HDAC) inhibitor with IC50s of 53.0 nM, 106.2 nM, 29.5 nM for HDAC1, HDAC2 and HDAC6.
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VU0155069 is a selective phospholipase D1 inhibitor with an IC50 of 46 nM, which strongly inhibits the invasive migration of several cancer cell lines.
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KPT-6566 is a Selective PIN1 Inhibitor
2019-09-23
KPT-6566 is a potent prolyl isomerase PIN1 inhibitor, covalently binds to the catalytic site of PIN1, selectively inhibits and degrades PIN1. -
BY27 is a potent, selective BET BD2 inhibitor, shows high BD1/BD2 selectivity for BRD2, BRD3, BRD4, and BRDT. BY27 has anti-cancer activity.
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AZD0424 is a selective Src/Abl kinase inhibitor with potential antineoplastic activity. AZD0424 induces apoptosis and cell cycle arrest in lymphoma cells
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SS-208 is a selective HDAC6 inhibitor, with an IC50 of 12 nM. SS-208 (25 mg/kg, ip) significantly reduces the tumor growth in melanoma murine model.
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PTC596, an orally active and selective BMI-1 inhibitor, induces p53-independent mitochondrial apoptosis in acute myeloid leukemia progenitor cells.
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CSRM617 is a selective inhibitor of ONECUT2 (OC2). CSRM617 induces apoptosis. Well tolerated in the prostate cancer mouse model.
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BPK-29 disrupts the NR0B1 protein-protein interactions and impairs the anchorage-independent growth of KEAP1-mutant cancer cells.
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LDN-192960 is a potent Haspin and DYRK2 dual inhibitor. LDN-192960 may have potential therapeutic utility in treating cancer.
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SCH772984 is a highly selective and ATP-competitive ERK inhibitor. SCH772984 shows robust efficacy in RAS- or BRAF-mutant cancer cells.
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LY3214996 is a highly potent and selective ERK1 and ERK2 inhibitor and shows potent antitumor activities in cancer models with MAPK pathway alterations.
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Ravoxertinib (GDC-0994) is an orally bioavailable ERK kinase inhibitor with an IC50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively.
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FR 180204 is an ATP-competitive and selective ERK inhibitor and inhibits ERK1 and ERK2 with IC50s of 0.51 μM and 0.33 μM, respectively.
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CGS 15943 is an orally bioavailable adenosine receptor antagonist with low nanomolar range Ki values for human A1, A2A, A2B, and A3 adenosine receptors.
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CG-200745 is a potent and pan HDAC inhibitor. CG200745 inhibits the deacetylation of histone H3 and tubulin, inducing p53 accumulation.
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NV03 is a potent and selective antagonist of UHRF1-H3K9me3 interaction by binding to UHRF1 TTD with a Kd of 2.4 μM and has anticancer activity.
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CD161 is a potent and orally bioavailable bromodomain and extra-terminal bromodomain inhibitor with an IC50 of 28.2 nM and a Ki of 8.2 nM for BRD4 BD1.
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sAJM589 is a Myc inhibitor which potently disrupts the Myc-Max heterodimer in a dose dependent manner with an IC50 of 1.8 μM.
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Tasisulam is an anticancer agent and induces apoptosis, which also inhibits mitotic progression and induces vascular normalization.
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BI-167107 is a high affinity, full agonist that binds to the β2 adrenergic receptor (β2AR) with a dissociation constant Kd of 84 pM.
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JTE-013 is a potent and specific S1P2 antagonist and increases the excitability of sensory neurons independently of the receptor.
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OTS964 is an orally active, high affinity and selective TOPK inhibitor and is also a potent inhibitor of the cyclin-dependent kinase CDK11.
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IPR-803 is a potent inhibitor of the uPAR•uPA protein-protein interaction, and binds directly to uPAR with sub-micromolar affinity.
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FTI-2153 is a potent and highly selectiveof farnesyltransferase (FTase) inhibitor and a highly potent antagonist of oncogenic H-Ras signaling.
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TVB-3166 is an orally-available, reversible, and selective FASN inhibitor and it induces apoptosis, and inhibits in-vivo xenograft tumor growth.
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Vorolanib is an orally active, multikinase VEGF/PDGF receptor inhibitor with antitumor activity and is expected to disrupt tumor angiogenesis.
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CCG-222740 is a potent and selective MRTF pathway inhibitor. It effectively reduces fibrosis in the skin and blocks melanoma metastasis.
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ASLAN003 is an orally active and potent inhibitor of hDHODH with antitumor activity, and it has the potential to be a first-in-class drug candidate in AML.
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MN58b, a selective choline kinase α (CHKα) inhibitor, results in inhibition of phosphocholine synthesis, induces of apoptosis, and has antitumoral activity.
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JNJ-10198409 is an orally active PDGF-RTK inhibitor (IC50=2 nM). It also has potent activity against PDGFR-β (IC50=4.2 nM) and PDGFR-α kinase (IC50=45 nM).
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SU16f is a selective PDGFRβ inhibitor and significantly decreases the enhanced migratory ability of SGC-7901 cells by GC-MSC.
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IACS-8803 is a highly potent cyclic dinucleotide stimulator of interferon genes (STING) agonist with robust systemic antitumor efficacy.
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MRTX849 is a potent, orally-available, and mutation-selective covalent inhibitor of KRASG12C with potential antineoplastic activity.
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AG-825 is a selective and ATP-competitive ErbB2 inhibitor and leads to a decrease in ErbB2–nucleolin interaction, which suppresses tyrosine phosphorylation.
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CP5V is a Specific PROTAC Degrader of Cdc20
2019-11-20
CP5V is a PROTAC, which specifically degrades Cdc20 by linking Cdc20 to the VHL/VBC complex for ubiquitination followed by proteasomal degradation. -
DS18561882 is a highly potent, sozyme-selective methylenetetrahydrofolate dehydrogenase 2 (MTHFD2) inhibitor with a good oral pharmacokinetic profile.
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AC-73 is a first specific, orally active the cluster of differentiation 147 (CD147) inhibitor and specifically disrupts CD147 dimerization.
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S516 is a potent tubulin polymerization inhibitor with an IC50 of 4.29 μM and has marked antitumor activity against murine and human solid tumors.
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GNE-618 is a Orally Active NAMPT Inhibitor
2019-11-28
GNE-618 is an orally active NAMPT inhibitor and reduces tumor growth. GNE-618 depletes NAD levels and induces tumor cell death. -
MS645, a bivalent BET BrD inhibitor, affords a sustained repression of BRD4 transcriptional activity in solid-tumor cells.
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PK11007 is a Mild Alkylating Agent with Anticancer Activity and induces mutant p53 cancer cell death by increasing reactive oxygen species (ROS) levels.
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PI-273 can be used to treat breast cancer. PI-273 is a first reversibly and specific PI4KIIα inhibitor (IC50 = 0.47 μM) and induce cell apoptosis.
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SD-36 is a Selective PROTAC STAT3 Degrader
2019-12-06
SD-36 is a potent, efficacious and selective PROTAC STAT3 degrader (Kd=50 nM) and achieves complete tumor regression in vivo. -
SR-4835 is a potent, highly selective and ATP competitive dual inhibitor of CDK12/CDK13.SR-4835 can provoke triple-negative breast cancer (TNBC) cell death.
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SI-109 is a potent STAT3 SH2 domain inhibitor and effectively inhibits the transcriptional activity of STAT3. SI-109 is the ligand of PROTAC degrader SD-36.
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CMLD010509 is a Highly Specific Inhibitor of the Oncogenic MYC-Driven Translation Program
2019-12-10
CMLD010509 (SDS-1-021) is a highly specific inhibitor of the oncogenic translation program supporting multiple myeloma (MM)-including key oncoproteins. -
BI-4020 is an orally active, and non-covalent EGFR tyrosine kinase inhibitor. It inhibits BaF3 and EGFR wt cell lines with low IC50 values.
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Sotorasib, a first-in-class, selective KRAS G12C covalent inhibitor, irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state.
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Telaglenastat is a first-in-class, reversible, orally bioavailable glutaminase 1 splice variants (KGA and GAC) inhibitor. It shows antitumor activity.
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Alpelisib is a potent, selective, and orally active PI3Kα inhibitor (IC50=5 nM, 250 nM, 290 nM and 1200 nM for p110α, p110γ, p110δ, and p110β).
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Niraparib is an Orally Active PARP Inhibitor
2019-12-18
Niraparib is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor. Niraparib has potent anti-cancer activity. -
MG-277 works as a PROTAC molecular glue, inducing degradation of a translation termination factor, GSPT1 to achieve its potent anticancer activity.
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TK216 is a potent ETS inhibitor. TK216 blocks the binding between EWS-FLI1 and RNA helicase A. TK216 has anticancer activity.
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DRF-1042 is an orally active derivative of Camptothecin and acts to inhibit DNA topoisomerase I with good anticancer activity.
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UK 356618 is a Selective MMP-3 Inhibitor
2019-12-25
UK 356618 is a selective and potent inhibitor of MMP-3. UK 356618 exhibits potent anti-inflammatory and anti-cancer activity. -
MS432 is a first-in-class and highly selective PD0325901-based VHL-recruiting PROTAC degrader for MEK1 and MEK2 with good anti-cancer activity.
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PI-828 is a dual PI3K and casein kinase 2 (CK2) inhibitor with good anti-cancer activity. PI-828 mitigated radiation-induced apoptosis in NCCIT cells.
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FPA-124 is a cell-permeable copper complex and a selective Akt inhibitor. FPA-124 induces apoptosis in multiple human cancer cells.
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KB02-JQ1 is a highly potent and selective PROTAC BRD4 degrader that degrades nuclear proteins by engaging CUL4-DDB1 E3 ubiquitin ligases DCAF16.
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CH6953755 is a potent, orally active and selective YES1 kinase inhibitor leading to antitumor activity against YES1 Gene -amplified cancers.
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CA-4948 is a Selective and Orally Bioavailable IRAK4 Kinase Inhibitor for Lymphoma Treatment
2020-01-05
CA-4948 is a potent, selective and orally bioavailable IRAK4 kinase inhibitor. CA-4948 can be used for the treatment of lymphoma. -
D-I03 is a Selective RAD52 Inhibitor
2020-01-08
D-I03 is a selective RAD52 inhibitor, which specifically inhibits RAD52-dependent single-strand annealing (SSA) and D-loop formation. -
CWP232228, a highly potent selective Wnt/β-catenin signaling inhibitor, antagonizes binding of β-catenin to T-cell factor (TCF) in the nucleus.
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CKI-7 is a potent CK1 and Cdc7 kinase inhibitor, which induces cytotoxicity of established leukemia and lymphoma cell lines.
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GPP78 is a potent Nampt inhibitor. GPP78 is cytotoxic to neuroblastoma cell line SH-SY5Y cells. GPP78 has anti-cancer and anti-tumor activity.
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CC-223 is an orally bioavailable mTOR kinase inhibitor and demonstrates mTORC1/2 and growth inhibitory activity across a variety of tumor cell types.
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COTI-2 is an orally available third generation activator of p53 mutant forms by inhibiting the PI3K/AKT/mTOR pathway. COTI-2 has has anti-cancer activity.
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PI-103 is a Potent PI3K and mTOR Inhibitor
2020-01-17
PI-103 is a potent PI3K and mTOR inhibitor, it also inhibits DNA-PK. PI-103 exhibits antiproliferative properties in a panel of human cancer cell lines. -
CGP52411 (DAPH) is a high selective, potent, orally active and ATP-competitive EGFR inhibitor with good anticancer activity.
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AZD4547 is a Potent FGFR Family Inhibitor
2020-01-21
AZD4547 potently inhibits the FGFR family with low IC50s. AZD4547 inhibits FGF/FGFR downstream signaling through FRS2, PLCγ, and MAPK at the cellular level. -
A-366 is a potent G9a-inhibitor without affect other histone methyltransferases. A-366 significantly results in tumor growth inhibition in leukemia.
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PF-573228 is a potent and selective FAK inhibitor and serves as a useful tool to dissect the functions of FAK in normal and cancer cells.
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BCI-215 is a potent and tumor cell-selective DUSP-MKP inhibitor without affecting normal cells. Anti-migratory and proapoptotic activities in cancer cells.
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PKI-166 is an orally active EGFR tyrosine kinase inhibitor and inhibits pancreatic cancers. Combined with Gemcitabine produces a decrease in tumor growth.
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BAY-474 is a tyrosine-protein kinase c-Met inhibitor. BAY-474 is a structural genomics consortium (SGC) epigenetics probe.
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SAR439859 is an orally active and selective estrogen receptor degrader. SAR439859 is a potent ER antagonist, with an EC50 of 0.2 nM for ERα degradation.
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M8891 is an orally active, reversible and brain penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor with antiangiogenic and antitumoral activity.
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BRD7389 is a specific RSK family kinase inhibitor and is a small-molecule inducer of insulin expression in pancreatic α-cells.
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MRT199665 is a potent, ATP-competitive, and selective MARK/SIK/AMPK inhibitor, and causes apoptosis in MEF2C-activated human AML cells.
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AKOS-22, a VDAC1 Oligomerization and Apoptosis Inhibitor, Protects Against Mitochondrial Dysfunction
2020-02-15
AKOS-22 is a potent mitochondrial protein VDAC1 and apoptosis inhibitor. AKOS-22 protects against Mitochondrial Dysfunction. -
SB-218078, a Chk1 inhibitor, inhibits Chk1 phosphorylation of cdc25C with an IC50 of 15 nM, causeing apoptosis by DNA damage and cell cycle arrest.
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HKI-357 is an irreversible EGFR and ERBB2 inhibitor and is effective in the treatment of EGFR-mutant non-small cell lung cancers resistant to Gefitinib.
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BAY-985 is an orally active and selective ATP-competitive dual inhibitor of TBK1 and IKKε with IC50s of 2/30 and 2 nM for TBK1 and IKKε, respectively.
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DS-437 is a Dual PRMT5/7 Inhibitor
2020-02-25
DS-437 is a dualPRMT5/7 inhibitor, and is selective for PRMT5 and PRMT7 over 29 other human protein-, DNA-, and RNA-methyltransferases. -
CNX-500 is a probe consisting of a covalent Btk inhibitor (CC-292) chemically linked to biotin, and retains inhibitory activity against Btk.
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ADH-503 is an orally active and allosteric CD11b agonist and leads to the repolarization of tumor-associated macrophages.
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6RK73 is a covalent irreversible and specific UCHL1 inhibitor,which specifically inhibits UCHL1 activity in breast cancer.
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AGN194204 is an orally active and selective RXR agonist. AGN194204 is inactive against RAR and has anti-inflammatory and anticarcinogenic actions.
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BI-9321 is a potent, selective and cellular active NSD3-PWWP1 domain antagonist, and specifically disrupts histone interactions of the NSD3-PWWP1 domain.
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BPI-9016M is a dual c-Met and AXL tyrosine kinases inhibitor. BPI-9016M suppresses lung cancer cell lines growth, migration, and invasion.
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MSN-125, a potent Bax and Bak oligomerization inhibitor, efficiently prevents mitochondrial outer membrane permeabilization.
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F1324 is a potent and high-affinity peptidic inhibitor of BCL6 with anti-cancer activity. F1324 has strong inhibition activity against BCL6 PPI.
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BTSA1 is a high affinity and orally active BAX activator and induces conformational changes to BAX leading to BAX-mediated apoptosis.
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ZLDI-8 is an ADAM-17 inhibitor that makes tumor cells susceptible to anti-tumor agents and therefore overcoming the HCC multi-drug resistance process.
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ZCL278 is a potent and selective Cdc42 inhibitor with anticancer and antiviral activity. ZCL278 targets Cdc42-ITSN interaction.
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CID2950007 is an allosteric inhibitor that binds the guanine nucleotide-associated Cdc42 and induces ligand dissociation.
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CID-1067700 is a pan GTPase inhibitor, and competitively inhibits Rab7. CID-1067700 is a competitive guanine nucleotide binding inhibitor.
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Ro 90-7501, an Aβ42 fibril assembly inhibitor, inhibits PP5 in a TPR-dependent manner and has radiosensitizing effects on cervical cancer cells.
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CM-272, a first-in-class, selective, substrate-competitive and reversible dual G9a/DNMTs inhibitor, inhibits cell proliferation and promotes apoptosis.
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CCT367766, a PROTAC-based Pirin-targeting PDP, exhibits a moderate affinity for the CRBN-DDB1 complex and reveals a good affinity for Pirin and CRBN.
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PS315 is an allosteric PKC inhibitor by binding to the PIF-pocket of aPKC and inducing a displacement of the active site residue Lys111.
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JBJ-04-125-02 is a mutant-selective, allosteric and orally active EGFR inhibitor. JBJ-04-125-02 inhibits cancer cell proliferation.
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DB1976 is a selenophene analog of DB270 and a potent and fully efficacious transcription factor PU.1 inhibitor with apoptosis-inducing effect.
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CM10 is a potent and selective aldehyde dehydrogenase 1A family inhibitor and regulates metabolism and has anti-cancer activity.
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E64FC26 is a highly potent pan-style inhibitor of the protein disulfide isomerase (PDI) family with anti-myeloma activities.
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EB-3D, a selective ChoKα1 inhibitor, induces deregulation of the AMPK-mTOR pathway and apoptosis in leukemia T-cells, and shows antiproliferative activity.
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NU1025 is a potent PARP inhibitor and potentiates the cytotoxicity of ionizing radiation drug. NU1025 has anti-cancer and neuroprotective activity.
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Mobocertinib is a potent epidermal growth factor receptor (EGFR, ErbB1) inhibitor, which displays antineoplastic activity.
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Mepazine is an effective MALT1 inhibitor. Antipsychotic and tranquilizing agent. Mepazine affects viability of ABC-DLBCL cells by enhancing apoptosis.
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LBW242, a Smac mimetic, is a potent and orally active proapoptotic IAP inhibitor. LBW242 shows effects on mutant FLT3-expressing cells.
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LCH-7749944 is a potent PAK4 inhibitor and effectively suppresses the proliferation of human gastric cancer cells and induces apoptosis.
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TL13-112 is a PROTAC Degrader of ALK
2020-04-15
TL13-112 is a selective ALK-PROTAC degrader and inhibits ALK activity. TL13-112 is comprised of the conjugation of Ceritinib and the ligand pomalidomide . -
CCT365623, an Orally Active LOX Inhibitor, Supresses EGFR (pY1068) and AKT Phosphorylation
2020-04-16
CCT365623 is an orally active LOX inhibitor, suppresses EGFR (pY1068) and AKT phosphorylation driven by EGF. CCT365623 has good pharmacokinetic properties. -
TP3011 is a potent DNA topoisomerase I inhibitor. Antitumor activities.Active metabolite of TP3076. TP3011 inhibits cancer cell proliferative activities.
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TL13-12 is a Selective ALK-PROTAC Degrader
2020-04-21
TL13-12 can induce receptor tyrosine kinase anaplastic lymphoma kinase degradation in non small cell lung cancer cells. PROTAC ALK degrader. -
DC-5163 is a potent GAPDH inhibitor, can inhibit glycolysis pathway partially. DC-5163 selectively inhibits cancer cell proliferation and induces apoptosis.
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BAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor, which is highly effective in inhibiting Pten-null prostate cancer growth.
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M2698 is an orally active, ATP competitive, selective p70S6K and Akt dual-inhibitor with anti-cancer activity. M2698 can cross the blood-brain barrier.
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ARCC-4 is a low-nanomolar AR degrader, and effectively degrades clinically relevant AR mutants associated with antiandrogen therapy.
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TAK-683 is a Potent Metastin/GPR54 Agonist
2020-04-29
TAK-683 is a full KISS1R agonist (IC50=170 pM) with improved metabolic stability. It has the potential for the study of hormone-dependent prostate cancer. -
AMG 511 is a potent and selective class I PI3K inhibitor. Suppresses PI3K signaling. Decreases in phosphorylated AKT at Ser473 in a dose-dependent manner.
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PIK-75 is a reversible DNA-PK and p110α selective inhibitor. Impairs cell proliferation, survival, and tumor growth. Induce apoptosis.
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BO-264, an orally active TACC3 inhibitor, specifically blocks the function of FGFR3-TACC3 fusion protein and has broad-spectrum antitumor activity.
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MK-2206 is an orally active, highly potent and selective allosteric AKT inhibitor, with IC50s in the nanomolar range and antitumor activity.
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CPTH2 is a potent histone acetyltransferase (HAT) inhibitor and selectively inhibits the acetylation of histone H3 by recombinant human Gcn5.
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ONO-7475 is a selective and orally active novel Anexelekto (AXL) inhibitor. It sensitizes AXL-overexpressing EGFR-mutant NSCLC cells to the EGFR-TKIs.
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iFSP1 is a potent, selective FSP1inhibitor that induces ferroptosis in GPX4-knockout cells which overexpressed FSP1.
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SB-633825 is a potent and ATP-competitive inhibitor of TIE2, LOK (STK10) and BRK. SB-633825 can inhibit cancer cell growth and angiogenesis.
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Zotatifin is a potent and selective eIF4A inhibitor. Zotatifin effectively reduces viral infectivity by inhibiting SARS-CoV-2 NP protein biogenesis.
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SNDX-5613 is a potent, selective, small molecule inhibitor of the Menin-MLL binding interaction for targeted therapy in MLL-rearranged leukemias.
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OTS514 is a TOPK inhibitor induces complete tumor regression in xenograft models of human cancer through inhibition of cytokinesis.
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BAY1082439, an orally bioavailable, selective PI3K inhibitor, inhibits mutated forms of PIK3CA and is effective in treating prostate cancer with PTEN-loss.
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RBN-2397 is an orally active accross species NAD+ competitive inhibitor of PARP7. RBN-2397 binds to PARP7 and restores interferon (Type I) signaling.
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TNO155 is an allosteric inhibitor of wild-type SHP2. TNO155 has the potential for the study of RTK-dependent malignancies, especially advanced solid tumors.
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UT-34 is a potent, selective and orally active second-generation pan-androgen receptor (AR) antagonist and degrader with anti-prostate cancer efficacy.
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MYCMI-6 is a selective MYC:MAX protein interactions inhibitor, which blocks MYC-driven transcription and binds selectively to the MYC bHLHZip domain.
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AKN-028 is an Orally Active FLT3 Inhibitor
2020-05-28
AKN-028 is an orally active and potent FLT3 tyrosine kinase inhibitor and causes dose-dependent inhibition of FLT3 autophosphorylation. -
CGP77675 is an orally active and potent inhibitor of Src family kinases with anticancer activity. CGP77675 inhibits Src, EGFR, KDR, v-Abl, and Lck.
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HSD1590 is potent ROCK inhibitor, with IC50s of 1.22 and 0.51 nM for ROCK1 and ROCK2, respectively. HSD1590 displays low cytotoxicity.
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PD-161570 is a potent inhibitor of FGF-1R, PDGFR, EGFR, c-Src tyrosine kinases and inhibits PDGF-stimulated autophosphorylation and FGF-1R phosphorylation.
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OT-82 is a selective inhibitor of NAMPT. Selectively toxic to cells of hematopoietic origin. OT-82 is a promising antineoplastic agent.
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PD-089828 is an competitive inhibitor of FGFR-1/PDGFR-β/EGFR, and a noncompetitive inhibitor of c-Src tyrosine kinase with a long-lasting cellular activity.
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TED-347 is a potent, irreversible, covalent and allosteric inhibitor at YAP-TEAD protein-protein interaction with antitumor activity.
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THZ-P1-2 is a Selective PI5P4K Inhibitor
2020-06-10
THZ-P1-2 is a potent and selective PI5P4K inhibitor and covalently targets PI5P4Kα/β/γ. THZ-P1-2 causes autophagy disruption and upregulates TFEB signaling. -
ZINC69391, a Rac1 inhibitor, interferes with Rac1-GEF interaction. ZINC69391 induces apoptosis, and shows antiproliferative and antimetastatic effects.
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CID44216842 is a potent Cdc42 selective guanine nucleotide binding lead inhibitor. Cdc42 plays important roles in cell cycle progression.
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AZA1, a potent dual inhibitor of Rac1 and Cdc42, induces apoptosis and inhibits prostate cancer cells proliferation, migration and invasion.
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HM03 is a potent and selective HSPA5 inhibitor with anticancer activity. HSPA5 plays a key role in monitoring protein transport through the cell.
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XZ739 is a PROTAC BCL-XL Degrader
2020-06-18
XZ739 is a PROTAC BCL-XL Degrader. XZ739 is potent against various cancer cell lines. PROTAC is an emerging therapeutic modality. -
TNP-351, an Antifolate, is a Dihydrofolate Reductase (DHFR) Inhibitor. Antifolates serve medical science well in neoplastic and non-neoplastic diseases.
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ASP4132 is an Orally Active AMPK Activator
2020-06-23
ASP4132 is an orally active, potent AMPK activator with anti-cancer activity and makes tumor regression in breast cancer xenograft mouse models. -
JCN037 is a potent, non-covalent, and brain-penetrant EGFR tyrosine kinase inhibitor. JCN037 has potent anti-cancer activity.
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DI-82 is a potent deoxycytidine kinase (dCK) inhibitor. DI-82 is potent against hematological malignancies and other cancers.
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MYLS22 is a first-in-class and selective optic atrophy 1 (OPA1) inhibitor with anti-angiogenesis and anti-cancer activity.
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RA-9 is a potent and selective proteasome-associated DUBs inhibitor with favorable toxicity profile and anticancer activity.
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DI-87, an orally active and selective dCK inhibitor, has antitumor activity and is used in combination therapy against tumors expressing dCK.
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XMU-MP-3, a noncovalent inhibitor that suppresses BTK kinase activity both in vitro and in vivo.
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HLI373 represents a potential drug-able lead for the development of therapeutically efficacious inhibitors of Hdm2. Hdm2 is an ubiquitin protein ligase.
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GSK143 is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor. GSK143 reduces inflammation in the intestinal muscularis in mice.
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GSK621 is a potent and specific AMPK activator and induces autophagy and apoptosis in acute myeloid leukemia (AML) cells.
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Targapremir-210 binds miR-210’s Dicer processing site and modulates the miR-210 hypoxic circuit in triple-negative breast cancer cells and a mouse xenograft model.
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LQZ-7I orally and effectively inhibits xenograft tumor growth and induces survivin loss in tumors.
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M-808 is a highly potent and efficacious covalent Menin-MLL interaction inhibitor. M-808 has a binding IC50 value of 2.6 nM.
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S2116 is a potent lysine-specific demethylase 1 (LSD1) inhibitor and increases H3K9 methylation, reciprocal H3K27 deacetylation at super-enhancer regions.
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HJC0416 is a potent and orally active STAT3 inhibitor with an enhanced anticancer profile. HJC0416 is a promising anti-cancer agent for breast cancer study.
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TH1834 is a specific Tip60 (KAT5) histone acetyltransferase (HAT) inhibitor. TH1834 induces apoptosis and increases DNA damage in breast cancer.
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RA375, a RPN13 inhibitor, inhibits proteasome function in muscle. RA375 is highly active against cell lines of multiple myeloma and diverse solid cancers.
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MRK-740 is a selective PRDM9 inhibitor. MRK-740 is more selective for PRDM9 than other histone methyltransferases and other non-epigenetic targets.
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TAI-1 is an orally active and highly potent first-in-class Hec1 (Ndc80) inhibitor and disrupts Hec1-Nek2 protein interaction, leads to Nek2 degradation.
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SR7826 is a potent, selective and orally active LIM kinase (LIMK) inhibitor. SR7826 is highly efficient in inhibiting cell-invasion/migration in PC-3 cells.
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EW-7195 is a potent and selective ALK5 inhibitor, and efficiently inhibits TGF-β1-induced Smad signaling, EMT and breast tumour metastasis to the lung.
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AMG-458 is a potent, selective and orally bioavailable c-Met inhibitor with potent anti-tumor activity in the NIH3T3/TPR-Met and U-87 MG xenograft models.
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GSK778 is a potent and selective inhibitor of bromodomain (BRD) BD1 and offers a super survival advantage in the aggressive MLL-AF9 AML model.
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JX06 is a potent, selective and covalent inhibitor of PDK via covalently binding to a cysteine residue in an irreversible manner.
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DM-01 is a EZH2 inhibitor with anticancer activity. DM-01 has significant ability to reduce the cellular H3K27me3 level in K562 cells.
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MS117 is a potent, selective, and cell-active PRMT6 inhibitor. MS117 is an invaluable tool for testing biological and therapeutic hypotheses.
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MCP110 is an inhibitor of Ras/Raf-1 interaction in human cancer cells. The Ras family GTPases play a central role in the growth factor signaling.
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KCC-07 prevents binding of MBD2 to methylated DNA and activates BAI1 inducing anti-proliferative BAI1/p53/p21 signaling. Anticancer activity.
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CYH33 is an orally active, highly selective PI3Kα inhibitor and inhibits phosphorylation of Akt, ERK with potent activity against solid tumors.
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UC2288 is an Orally Active p21 Attenuator
2020-08-12
UC2288 is a cell-permeable p21 attenuator. UC2288 decreases p21 mRNA expression independently of p53, and attenuates p21 protein levels. -
SKI-178 is a potent SphK1 and SphK2 inhibitor and is cytotoxic in both drug sensitive and multi-drug resistant cancer cell lines.
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SC-43 is a potent and orally active SHP-1 (PTPN6) agonist. SC-43 inhibits the phosphorylation of STAT3 and induces cell apoptosis.
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ATH686 is a potent, selective, and ATP-competitive FLT3 inhibitor with an antileukemic effect. ATH686 induces apoptosis and inhibits cell cycle.
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SP-146 is a potent Aurora B inhibitor (IC50=0.316 nM), and shows >2000 fold selectivity against FLT3 and KIT. SP-146 is used for the research of TNBC.
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SBP-0636457 is a smac mimetic and small-molecule IAP antagonist. Act as potent TRAIL-sensitizing agents in a variety of cancer cell lines.
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BM-1197 is a potent and specific Bcl-2/Bcl-xL inhibitor inducing complete and long-lasting tumor regression in vivo. Antitumor activity.
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JH295 is a potent, irreversible and selective Nek2 inhibitor. JH295 is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1.
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YKL-5-124 is a potent, selective, irreversible and covalent CDK7 inhibitor and induces a strong cell-cycle arrest, inhibits E2F-driven gene expression.
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BRD9500 is an Orally Active Phosphodiesterases 3 (PDE3) Inhibitor with Antitumor Activity
2020-08-27
BRD9500 is an orally active phosphodiesterases 3 (PDE3) inhibitor. BRD9500 is active in an SK-MEL-3 xenograft model of cancer. -
ZZW-115, a NUPR1 Inhibitor, Possesses Anticancer Activity via Inducing Necroptosis and Apoptosis
2020-08-29
ZZW-115 is a potent NUPR1 inhibitor, with a Kd of 2.1 μM. ZZW-115 induces tumor cell death by necroptosis and apoptosis. ZZW-115 exerts anticancer activity. -
SM1-71, a potent TAK1 inhibitor. it is also a multi-targeted kinase inhibitor and has the potential to be a useful tool to for cancer research.
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IPI-9119 is an orally active, selective and irreversible FASN inhibitor with potent anti-cancer activity. IPI-9119 induces cell cycle arrest, apoptosis.
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CAY10404 is a potent and highly selective COX-2 inhibitor. CAY10404 is a potent inhibitor of PKB/Akt and MAPK signalling pathways.
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RJW100 is a Potent LRH-1 and SF-1 Agonist
2020-09-05
RJW100 is a potent LRH-1 and SF-1 agonist. RJW100 also causes strong activation of the miR-200c promoter and downregulates ZEB1 and ZEB2 proteins. -
Z-LEHD-FMK, an irreversible, selective caspase-9 inhibitor, protects some human cancer cell lines from TRAIL-induced apoptosis
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CRT0044876 is a potent and selective APE1 inhibitor. CRT0044876 inhibits the AP endonuclease, 3′-phosphodiesterase and 3′-phosphatase activities of APE1.
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EPI-001 is a selective inhibitor of Androgen Receptor (AR) and can inhibit transactivation of the AR amino-terminal domain (NTD).
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MSA-2 is an orally available non-nucleotide STING agonist. MSA-2 shows antitumor activity and stimulates interferon-β secretion in tumors.
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MPT0G211, an orally active and selective HDAC6 inhibitor, ameliorates tau phosphorylation, and cognitive deficits in an Alzheimer’s disease model.
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SC99 is an orally active, selective STAT3 inhibitor targeting JAK2-STAT3 pathway. SC99 displays potent anti-myeloma, anti-thrombotic activity.
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PU02, a derivative of 6-MP, is an allosteric antagonist of 5-HT3 receptor. PU02 possesses anti-cancer cativity by inducing aopotosis.
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SP-8356, an orally active CD147inhibitor, exerts anti-breast cancer effects by inhibiting NF-κB signaling. Anti-atherosclerotic effects.
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AZD-9833 is a potent and orally active ER antagonist. AZD-9833 has the potential for the study of ER+ HER2-advanced breast cancer.
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RapaLink-1, a third-generation bivalent mTOR inhibitor, potently blocking cancer-derived, activating mutants of mTOR. It can cross the blood-brain barrier.
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CMLD012073, an Amidino-Rocaglates, is a Potent eIF4A Inhibitor. Amidino- and amino-rocaglates act as potent translation inhibitors and anti-cancer agents.
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SJF620 is a Potent PROTAC BTK Degrader
2020-09-26
SJF620 is a potent PROTAC BTK degrader with improved pharmacokinetic properties. Contains a Lenalidomide analog for recruiting CRBN. -
Ilorasertib is a potent inhibitor of Aurora A, B, and C, FLT-3,and the VEGF and PDGF receptor kinases. Activity in acute myeloid leukemia.
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EEDi-5285 is an exceptionally potent and orally active embryonic ectoderm development (EED) inhibitor with potent anti-cancer activity.
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CB-1158, a potent and orally bioavailable inhibitor of arginase, blocks myeloid cell-mediated immune suppression in the tumor microenvironment.
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AG-494 is a potent and selective EGFR tyrosine kinase inhibitor. AG-494 inhibits the autophosphorylation of EGFR, ErbB2, HER1-2 and PDGFR.
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SRX3207 is an orally active and first-in-class dual Syk/PI3K inhibitor. SRX3207 possesses effective anti-tumor activity in vitro and in vivo.
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A 419259 is a Potent Src Inhibitor
2020-10-08
A 419259 is a Src family kinases inhibitor with IC50s of 9 nM, 3 nM and 3 nM for Src, Lck and Lyn, respectively. A 419259 is used for cancer research. -
CMLD012612 is a potent eIF4A inhibitor. CMLD012612 inhibits cell translation and is cytotoxic to NIH/3T3 cells with an IC50 value of 2 nM.
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D-3263 is an enteric-coated, orally bioavailable (transient receptor potential melastatin member 8) TRPM8 agonist with antineoplastic activity.
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Giredestrant is an orally active and selective estrogen receptor (ER) antagonist with anti-tumor activity. Giredestrant is a non-steroidal ER ligand.
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NEO2734 (EP31670) is an orally active p300/CBP and BET bromodomain selective inhibitor, with IC50 values of <30 nM for both p300/CBP and BET bromodomains.
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Mavelertinib is a high-affinity irreversible inhibitor targeting oncogenic EGFR mutants with selectivity over wild-type EGFR.
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Verucopeptin inhibits v-ATPase activity by directly targeting the v-ATPase ATP6V1G subunit but not ATP1V1B2 or ATP6V1D. Also a potent HIF-1 inhibitor.
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BRD3731 is a Selective GSK3β Inhibitor
2020-10-21
BRD3731 is a selective GSK3β inhibitor. BRD3731 can be used for the research of a mood disorder, diabetes, and neurodegenerative disorder, etc. -
Telomestatin is a potent telomerase inhibitor and selectively facilitates the formation of intramolecular G-quadruplexes. ADC cytotoxin for cancer research.
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BSJ-04-132 is a potent and selective Ribociclib-based CDK4 degrader (PROTAC) and does not induce CDK6 and IKZF1/3 degradation with anti-cancer activity.
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BC-LI-0186 is a selective inhibitor of LeuRS and RagD interaction (IC50=46.11 nM). BC-LI-0186 suppresses the activity of cancer-associated MTOR mutants.
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BSJ-03-204 is a potent and selective Palbociclib-based CDK4/6 dual degrader (PROTAC) and does not induce IKZF1/3 degradation with anti-cancer activity.
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MSAB, a strongest and selective inhibitor of Wnt/β-catenin signaling activity, represents an effective strategy for cancers.
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APS6-45 is an orally active tumor-calibrated inhibitor. A highly efficacious lead. Inhibits RAS/MAPK signaling and exhibits antitumor activity.
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CCT369260 is an Orally Avtive B-cell Lymphoma 6 (BCL6) Inhibitor with Anti-Tumor Activity
2020-11-03
CCT369260 is an orally avtive B-cell lymphoma 6 (BCL6) inhibitor with anti-tumor activity. CCT369260 exhibits an IC50 of 520 nM. -
KB02-SLF is a PROTAC-based nuclear FKBP12 degrader. KB02-SLF promotes nuclear FKBP12 degradation by covalently modifying DCAF16 (E3 ligase).
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E7820, sulfonamide derivative, is a unique angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium.
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Cyclo(-RGDfK) is a selective inhibitor of the αvβ3 integrin. Cyclo(-RGDfK) potently targets cancer cells through binding to the cell surface αvβ3 integrin.
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Cilengitide is a compound targeting angiogenesis, the cornerstone of tumor growth and metastasis. ανβ3 and ανβ5 are the target of Cilengitide.
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Tetrac inhibits the cellular actions of thyroid hormone initiated at the hormone receptor on plasma membrane integrin alphavbeta3.
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DT2216 is a potent and selective BCL-XL degrader based on PROTAC technology. DT2216 inhibits leukemia and has potent anti-cancer activity.
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dTRIM24 will be a useful tool to further probe the function of TRIM24 by rapid chemical depletion in hematopoietic cancers and other biological contexts.
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ZXH-3-26 is a Selective PROTAC BRD4 Degrader
2020-11-17
ZXH-3-26 is a Selective PROTAC BRD4 Degrader and allows pharmacologic targeting of BRD4 without significant inhibition or degradation of BRD2/3. -
BETd-260 is a Potent PROTAC BET Degrader
2020-11-18
BETd-260 is a highly potent, efficacious, and promising BET degrader. -
SIAIS178 is a potent and selective BCR-ABL degrader based on PROTAC technology by recruiting VHL E3 ubiquitin ligase. SIAIS178 has anticancer activity.
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GNE-987, a potent chimeric BET degrader, exhibits picomolar cell BRD4 degradation activity. GNE-987 can be used in PROTAC-Antibody Conjugate (PAC).
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BI-3663 is a highly selective PTK2/FAK PROTAC (DC50=30 nM), with cereblon ligands to hijack E3 ligases for PTK2 degradation.
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dFKBP-1 induces potent and dose-dependent degradation of FKBP12 in 293FT-WT cells. A facile and general new strategy to control target protein stability.
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UNC6852 is a chemical degrader that targets polycomb repressive complex 2 (PRC2). Anti-proliferative in diffuse large B cell lymphoma cell lines.
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VZ185 is a highly selective, potent, and rapid dual degrader with a slight preference for BRD9 over BRD7.
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PQR530 is a potent, ATP-competitive, orally bioavailable and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor. Antitumor activity.
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MZP-54 is a Selective BRD3/4 PROTAC Degrader
2020-12-02
MZP-54 is a PROTAC that would link together specific VHL ligand and BET bromodomain ligand. MZP-54 induces degradation of BRD3/4. -
H3B-6545 is a selective estrogen receptor covalent antagonist and prevents bone loss in ovariectomized Sprague-Dawley rats.
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ADPM06 is a Novel Nonporphyrin Photodynamic Therapeutic (PDT) Sensitizer and Induces Apoptosis
2020-12-05
ADPM06 is a nonporphyrin PDT agent. ADPM06 exhibits IC50 values in the micro-molar range in human tumor cells and induces apoptosis. -
CC-90010 is a reversible and orally active BET inhibitor. CC-90010 is applied in the study for advanced solid tumors and non-Hodgkin's lymphoma.
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GNE-371, a Chemical Probe for the Second Bromodomains of TFIID Subunit 1 and TFIID Subunit 1-Like
2020-12-09
GNE-371 is a selective chemical probe for the second bromodomains of human transcription-initiation-factor TFIID subunit 1 and TFIID subunit 1-like. -
VERU-111 inhibits the expression of tubulin βIII and βIV over other isotypes, which supports the ability of VERU-111 to surmount drug resistance.
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BMS-P5 is an Orally Active PAD4 Inhibitor
2020-12-12
BMS-P5 is an orally active PAD4 inhibitor. BMS-P5 blocks MM-induced NET formation and delays progression of MM in a syngeneic mouse model -
ML132, a potent and selective caspase 1 inhibitor with a unique selectivity pattern, is responsible for the proteolytic activation of IL-1β and IL-18.
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CHDI-390576, a potent and CNS penetrant class IIa HDAC inhibitor, show selectivity over class I HDACs, HDAC8 and the class IIb HDAC6 isoform.
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SAR-020106 is an ATP-competitive CHK1 inhibitor with an IC50 of 13.3 nM for hCHK1. SAR-020106 can enhance antitumor activity with selected anticancer drugs.
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EMI56 is a Superior Mutant EGFR Inhibitor
2020-12-19
EMI56 is a Superior Mutant EGFR InhibitorLung Cancer, Non-Small Cell Lung Cancer A drug discovery platform to identify compounds that inhibit EGFR triple mutants. -
CTPI-2 is a SLC25A1 inhibitor. CTPI-2 inhibits glycolysis, PPARγ, and its downstream target the glucose transporter GLUT4. Antitumor activity.
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BI-3802, a BCL6 degrader, inhibits the BCL6 BTB domain. BI-3802 induces the polymerization of BCL6 and promotes BCL6 degration depended on E3 ligase SIAH1.
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DMU-212 Possesses Antimitotic, Anti-Proliferative, Antioxidant and Apoptosis Promoting Activities
2020-12-24
Activation of ERK1/2 is required for the antimitotic activity of the Resveratrol analogue DMU‐212 in human melanoma cells. -
PND-1186 is a FAK inhibitor and selectively promotes tumor cell apoptosis in three-dimensional environments. Acts as an anti-cancer therapy.
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AZ9482 is a Triple PARP1/2/6 Inhibitor
2021-01-05
AZ9482 is a triple PARP1, PPAR2 and PPAR6 inhibitor, with IC50 values of 1 nM, 1 nM and 640 nM for PARP1, PARP2 and PARP6, respectively. -
CPL304110 is a potent, orally active and selective inhibitor of fibroblast growth factor receptors FGFR (1-3), respectively.
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APG-1387 is a bivalent SMAC mimetic and an IAP antagonist. APG-1387 induces apoptosis with anti-cancer activity.
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WL47, a high-affinity cavolin-1 (CAV1) ligand (Kd=23 nM), act as a potent and selective disrupter of CAV1 oligomers.
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NHWD-870 is a potent, orally active and selective BET family bromodomain inhibitor with potent tumor suppressive efficacies.
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CJ-2360 is an ALK inhibitor with IC50s of 2.2-8.9 nM against wild-type ALK and F1197M, G1269A, L1196M, and S1206Y ALK mutants, respectively.
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NSC 80467, a potent DNA damaging agent, selectively inhibits survivin, and preferentially inhibits DNA synthesis.
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G5-7, an orally active and allosteric JAK2 inhibitor. G5-7 induces cell cycle arrest, apoptosis and possesses antiangiogenic effect.
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R59949 is a pan DGK inhibitor with an IC50 of 300 nM. R59949 activates PKC by enhancing the levels of the endogenous ligand diacyl glycerol.
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ML786 is an orally bioavailable Raf inhibitor, inhibits V600EΔB-Raf, wt B-Raf, and C-Raf. It also inhibits Abl-1, DDR2, EPHA2, KDR, and RET.
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NSC-105808, a potent, specific DNA2 nuclease inhibitor, inhibits HR repair, DSB end resection and suppresses proliferation of cancer cells.
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Afatinib is an irreversible EGFR family inhibitor and shows potent activity against wild-type and mutant forms of EGFR and HER2.
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Senaparib, a selective and orally active PARP1/2 inhibitor, has great potential as a monotherapy as well as in combination with other agents.
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CMLD-2 is Inhibits HuR and Induces Apoptosis
2021-01-20
CMLD-2, a HuR -ARE interaction inhibitor, competitively binds HuR protein and induces apoptosis. CMLD-2 has potent anti-cancer activity. -
NU6102 is a Potent CDK1 and CDK2 Inhibitor
2021-01-21
NU6102 is a potent CDK1 and CDK2 inhibitor with IC50s of 9.5 nM and 5.4 nM for CDK1/cyclinB and CDK2/cyclinA3, respectively. -
JH-XI-10-02, a highly Potent CDK8 Degrader, modulates the CDK8 protein levels. A viable therapeutic strategy in cancer.
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ICCB280, a inducer of C/EBPα, exhibits anti-leukemic properties including terminal differentiation, proliferation arrest, and apoptosis.
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NVS-CECR2-1, a non-BET family Bromodomain (BRD) inhibitor, is a potent and selective CECR2 inhibitor with potent anti-cancer activity.
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BI99179 is a Selective Type I FASN Inhibitor
2021-01-28
FASN is a key enzyme for lipogenesis and highly expressed in lipogenic tissues. BI99179 is a Selective Type I FASN Inhibitor. -
The retinoic acid receptor antagonist, BMS453, inhibits normal breast cell growth by inducing active TGFβ and causing cell cycle arrest
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Triciferol combines VDR agonism and HDAC inhibition to enhance the cytostatic and cytotoxic activities of 1,25D.
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Fasentin inhibits GLUT-1 and GLUT-4 transporters. Fasentin blocks glucose uptake in cancer cell lines and has anti-angiogenic activity.
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PINT87aa, a Potential Tumor-Suppressive Peptide, Directly Interacts with the PAF1 Complex
2021-02-04
PINT87aa, a potential tumor-suppressive peptide, directly interacts with the PAF1 complex and inhibits mRNA transcriptional elongation. -
KS15 is an inhibitor of the cryptochromes and clockbmal1 heterodimer interaction.
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dCBP-1 is a potent and selective degrader of p300/CBP based on PROTAC. dCBP-1 is exceptionally potent at killing multiple myeloma cells.
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Tuxobertinib (BDTX-189) is a small molecule ATP-competitive inhibitor against a family of allosteric EGFR and HER2 mutations.
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Piclidenoson (IB-MECA) is an A3 adenosine receptor (A3AR) agonist. Piclidenoson is used for the research of cancer, inflammatory diseases and COVID-19.
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PF 477736 (PF 00477736) is a Chk1 inhibitor. Breaching the DNA damage checkpoint. PF-00477736 combines with Gemcitabine to abrogates cell cycle arrest.
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CXD101 is a selective and orally active class I HDAC inhibitor for advanced cancer.
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AKI603 is a potent Aurora kinase inhibitor. AKI603 attenuates breast tumor-initiating cells and overcomes drug resistance.
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NSC 33994 is a Selective JAK2 Inhibitor
2021-02-18
NSC 33994 (G6) is a selective JAK2 inhibitor. NSC 33994 reduces the levels of pJAK2 in both a dose- and time-dependent manner. -
PR-619 is a Broad-Range DUB Inhibitor
2021-02-20
PR-619, a broad-spectrum deubiquitinating enzyme (DUB) inhibitor, induces ER stress and ER-stress related apoptosis. -
Barasertib (AZD1152), a Pro-Drug of Barasertib-hQPA, is a Highly Selective Aurora B Inhibitor
2021-02-23
Barasertib (AZD1152) is a pro-drug of Barasertib-hQPA. A selective Aurora B kinase inhibitor. Provides a potential treatment for multiple myeloma. -
ML390 is a Potent DHODH Inhibitor
2021-02-24
ML390 is a potent dihydroorotate dehydrogenase (DHODH) inhibitor and is an inducer of myeloid differentiation. -
PF-06843195 is a Selective PI3Kα Inhibitor
2021-02-25
PF-06843195 is a selective PI3Kα inhibitor. The Kis of PF-06843195 for PI3Kα and PI3Kδ are less than 0.018 nM and 0.28 nM, respectively. -
TAS-119 is an orally active, selective inhibitor of Aurora kinase A. A clinical candidate for efficacy testing in combination with taxanes.
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AES-135 is a Potent HDAC Inhibitor
2021-03-03
AES-135, a potent HDAC inhibitor, demonstrates high cytotoxicity in a variety of cancer cell lines, most notably in pancreatic tumor lines. -
NAZ2329 is an allosteric, noncompetitive and reversible inhibitor of R5 RPTP subfamily and PTPRZ/PTPRG with anti-cancer activity.
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GW806742X, an ATP mimetic and a potent MLKL inhibitor, retards MLKL membrane translocation and inhibits necroptosis.
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ENMD-1198 is an orally active microtubule-targeting agent with antiproliferative and antiangiogenic activity.
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DTHIB is a Direct and Selective Heat Shock Factor 1 (HSF1) Inhibitor. Selectively accelerates the degradation of nuclear HSF1.
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CC-90001 is a potent, selective, and orally active inhibitor of JNK. CC-90001 can be used for the research of idiopathic pulmonary fibrosis (IPF).
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BrBzGCp2 is a Glyoxalase 1 (GLO1) inhibitor for a variety of disorders. Possesses antitumor and neuroprotective activity.
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IACS-13909 is a Selective and Orally Active SHP2 Inhibitor. Overcomes tumor resistance to Osimertinib. Targeting SHP2. Therapeutic strategy.
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IMT1 is a first-in-class specific and noncompetitive human POLRMT inhibitor for mitochondrial transcription disorders related diseases.
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Z-LE(OMe)TD(OMe)-FMK is a Selective Caspase-8 Inhibitor. Caspase-8 is a cysteine protease for Fas-induced apoptosis and lymphocyte activation.
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BIM-23190, a somatostatin analog, is a selective SSTR2 and SSTR5 agonist. BIM-23190 can be used in the study for cancer and acromegaly.
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Conglobatin inhibits proliferation and induces apoptosis by binding to N-terminus of Hsp90 and disrupting Hsp90-Cdc37 complex formation.
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TPP-1 is a potent inhibitor of the PD-1/PD-L1 interaction. TPP-1 binds specifically to PD-L1 with a high affinity (KD=95 nM).
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YUM70 inhibits GRP78. Induces endoplasmic reticulum stress-mediated apoptosis. Pancreatic cancer. Acts as a novel anticancer agent.
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DBPR112 is an orally active furanopyrimidine-based EGFR (WT and L858R/T790M) inhibitor with significant antitumor efficacy.
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UZH1a is a Selective METTL3 Inhibitor
2021-03-25
UZH1a, a potent and selective METTL3 inhibitor can be used for epitranscriptomic modulation of cellular processes with antitumor activity. -
Olafertinib is a Third-Generation EGFR TKI
2021-03-27
Olafertinib acts as a promising third-generation EGFR inhibitor. Olafertinib has the potential for NSCLC research. -
Elimusertib is a potent, orally available and selective ATR inhibitor. Elimusertib has potent anti-tumor activity.
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FLTX1, a Fluorescent Tamoxifen Derivative, Specifically Labels Intracellular Binding Sites (ER)
2021-03-31
FLTX1 is a fluorescent Tamoxifen (Tx) derivative that specifically labels intracellular Tx-binding sites (estrogen receptors). -
Rineterkib, an orally active RAF and ERK1/2 inhibitor, has activity in multiple MAPK activated cancer cells and xenograft models.
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DC_AC50 is a dual inhibitor of Atox1 and CCS (copper chaperones). DC_AC50 can be used for cancer research.
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LC-2 is a potent and first-in-class PROTAC capable of degrading endogenous KRAS G12C, with DC50s between 0.25 and 0.76 μM.
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PF-06260414 is an orally active and nonsteroidal selective androgen receptor modulator (SARM) and has the potential for muscle weakening.
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Stafib-1 is the First Selective Inhibitor of STAT5b SH2 Domain. Anticancer agent. STAT5b acts as a target for tumor therapy.
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LDN193189 is a selective BMP type I receptor inhibitor, which efficiently inhibits ALK2 and ALK3, with weaker effects on ALK4, ALK5 and ALK7.
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Retro-2 is an inhibitor of retrograde protein trafficking at the endosome-trans-Golgi network interface. Retro-2 induces cell autophagy
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APS-2-79 is a MEK inhibitor. Stabilization of the KSR inactive state. An effective strategy to target other pseudokinases.
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BMS-354825 is a dual Src and Abl kinase inhibitor. Antitumor activity. Orally active in the chronic myelogenous leukemia.
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Miransertib is an orally active, selective and allosteric Akt inhibitor. Miransertib is also a potent the AKT1-E17K mutant protein inhibitor.
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L-Moses is the first potent, selective, and cell-active PCAF Brd inhibitor. L-Moses disrupts PCAF-Brd histone H3.3 interaction.
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MS049 is a potent, selective dual inhibitor of PRMT4 and PRMT6. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells.
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LYN-1604 is a Potent ULK1 Activator
2021-04-24
LYN-1604, a potent ULK1 activator, induces cell death involved in ATF3, RAD21, and caspase3, accompanied by autophagy and apoptosis. -
SB-332235 is a potent, orally active nonpeptide CXCR2 antagonist. SB-332235 inhibits acute and chronic models of arthritis in the rabbit.
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AZD1208 is a potent, selective, ATP-competitive, and orally active pan-Pim kinase inhibitor. AZD1208 inhibits acute myeloid leukaemia.
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ML-00253764 is a brain penetrant nonpeptidic melanocortin receptor 4 (MC4R) antagonist with a Ki/IC50 of 0.16 µM/0.103 µM, respectively.
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Rosabulin is a Potent Microtubule Inhibitor
2021-05-01
Rosabulin is a small molecule vascular disrupting agent, with potential antimitotic and antineoplastic activities. -
BMSpep-57 is a potent and competitive macrocyclic peptide inhibitor of PD-1/PD-L1 interaction. It induces high levels of IL-2.
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A-674563 is an orally active and selective Akt1 inhibitor. A-674563 induces G2 cell cycle arrest and apoptosis in STS cells.
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Pirtobrutinib, a highly selective and non-covalent next generation BTK inhibitor, inhibits diverse BTK C481 substitution mutations.
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SHP394 acts as a Potent, Selective, and Orally Efficacious SHP2 Inhibitor. SHP2 is a multifunctional therapeutic target.
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MR837 is an Inhibitor of NSD2-PWWP1
2021-05-11
MR837 is a potent inhibitor of NSD2 (WHSC1)-PWWP1 protein-protein interaction. MR837 can bind with human NSD2. -
ML339 is a Selective CXCR6 Antagonist
2021-05-12
ML339 is a small molecule antagonist would block Prostate cancer cell trafficking; hence mediate a metastatic event and disease progression. -
SIS3 is a selective Smad3 phosphorylation inhibitor and inhibits the myofibroblast differentiation of fibroblasts by TGF-β1.
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PROTAC MDM2 degrader MD-222 is highly potent and effective in inducing degradation of MDM2 and in activating wild-type p53 in cells.
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BI-3406 is a selective, orally bioavailable SOS1 inhibitor that binds to the catalytic domain of SOS1, preventing the interaction with KRAS.
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GSK973, a selective, orally bioavailable inhibitor of the BD2s of the BET family, shows good potency against BRD2 BD2, BRD3 BD2 and BRDT BD2.
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DT-061 is an Orally Active PP2A Activator
2021-05-21
DT-061 is an Orally Active PP2A Activator. PP2A inhibition is a druggable MEK inhibitor resistance mechanism. -
Lonafarnib is a potent and orally active farnesyl transferase inhibitor, and it inhibits the activities of H-ras, K-ras and N-ras.
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FTI-277 is a farnesyl transferase inhibitor, selectively blocks oncogenic Ras signaling. It inhibits hepatitis delta virus infection.
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PHT-7.3 is a Selective Inhibitor of Connector Enhancer of Kinase Suppressor of Ras 1 (Cnk1)
2021-05-27
PHT-7.3 is a selective inhibitor of Cnk1 pleckstrin homology (PH) domain. PHT 7.3 blocks the growth of mutant KRAS cells and tumors. -
Lenalidomide, a CRBN ligand, is an orally active immunomodulator that effective treatment for myelodysplastic syndrome and multiple myeloma.
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Trilaciclib is a CDK4/6 inhibitor with IC50s of 1 nM/4 nM for CDK4/6, respectively. Use for chemotherapy-induced myelosuppression in vivo.
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SMAP-2 is an orally active PP2A activator. SMAP-2 reduces cell viability of pancreatic ductal adenocarcinoma (PDA) cell lines.
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LJI308 inhibits the phosphorylation of RSK and YB-1 after irradiation, treatment with EGF, and in cells expressing a KRAS mutation.
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Sitravatinib (MGCD516) is an Orally Bioavailable RTK Inhibitor with PD-1 Blockade Activity
2021-06-03
Sitravatinib, a small molecule RTK inhibitor, shows potent anti-tumor activity in preclinical models of sarcoma. -
CC-90011 is a potent, selective, reversible and orally active LSD1 inhibitor that induces AML and SCLC cells differentiation.
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Elacestrant is an orally available selective estrogen receptor degrader (SERD). Elacestrant is an effective breast cancer cell antagonist.
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PTC-209, a specific BMI-1 inhibitor, irreversibly impairs colorectal cancer-initiating cells (CICs) and impairs the tumor microenvironment.
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AUTAC4 is a mitochondria-targeting autophagy-targeting chimera, which can be used for the study of mitochondrial dysfunction.
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NU9056 is a selective Tip60 (KAT5) histone acetyltransferase inhibitor. NU9056 shows >16-fold selectivity for Tip60 over PCAF, p300 and GCN5.
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DGY-06-116 is an irreversible covalent, selective Src inhibitor with an IC50 of 3nM. DGY-06-116 inhibits FGFR1 with an IC50 of 8340 nM.
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Acolbifene is a 4th generation SERM with potent and pure anticarcinogenic properties in the mammary gland and uterus.
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ARV-110 is an orally active, specific androgen receptor (AR) PROTAC degrader. ARV-110 can be used for the research of prostate cancer.
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CCI-007, a selective MLL-r leukemia cell lines inhibitor, and inhibits the viability of CALM-AF10 and SET-NUP214 leukemia.
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NCGC00378430 is a potent SIX1/EYA2 interaction inhibitor and inhibits SIX1-mediated breast cancer metastasis.
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Golvatinib (E-7050) is an inhibitor of c-Met and VEGFR2 kinases with IC50s of 14 and 16 nM, respectively. Can be used for cancer research.
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Vorasidenib is an orally available, brain penetrant second-generation dual mutant isocitrate dehydrogenases 1 and 2 (mIDH1/2) inhibitor.
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Motesanib (AMG 706) is an orally active VEGFR inhibitor. Potently inhibits angiogenesis and induces regression in tumor xenografts.
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Rociletinib is a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC.
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Venadaparib is a selective and orally active PARP1/2 inhibitor with significant in vitro and in vivo activities in multiple cancer models.
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LP-261 is a potent and orally active anti-mitotic agent and shows an inhibition of in vitro tubulin polymerization with an EC50 of 3.2 μM.
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Capivasertib is an orally active AKT inhibitor with pharmacodynamic activity in multiple solid and hematologic tumors.
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Proxalutamide (GT0918) is an orally active potent androgen receptor (AR) antagonist. And Proxalutamide (GT0918) plays important roles in the study of prostate cancer and COVID-19.
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SG3199, an ADC Cytotoxin, is a Cytotoxic DNA Minor Groove Interstrand Crosslinking PDB Dimer
2021-07-12
SG3199, a PBD dimer, is a warhead in next-generation ADCs with potently cytotoxic and a very short half-life. -
BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC). BSJ-4-116 exhibits potent antiproliferative effects.
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GL0388 activates Bax and induces Bax-mediated apoptosis. GL0388 suppresses breast cancer xenograft tumor growth in vivo.
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Lumiracoxib is a COX-2 inhibitor. Lumiracoxib acts as nonselective NSAID with anti-inflammatory, analgesic and antipyretic activities.
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SJ6986 is a selective and orally active GSPT1/GSPT2 degrader, displaying selectivity over classical IMiD neosubstrates, such as IKZF1/3
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DP-C-4 is a CRBN-Based dual PROTAC for EGFR and PARP could provide an effective study for cancer diseases.
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ABBV-744 is a first-in-class, orally active and selective BET BDII inhibitor could provide an effective study for prostate cancer.
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Inupadenant is an orally active, highly selective A2A receptor antagonist with potent anti-tumor activity.
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GGTI-2154 is a potent and selective inhibitor of GGTase I and has the potential for the research of cancer.
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XY028-140 is a potent and selective PROTAC-based CDK4/6 degrader, which can inhibit RB-E2F signaling and reduce CDK4 and CDK6 protein levels.
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Nimotuzumab is a humanized IgG1 monoclonal antibody targeting EGFR. Nimotuzumab is a strong antitumor drug.
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Pelcitoclax (APG-1252) is a Bcl-2/Bcl-xl Inhibitor with Antineoplastic and Pro-Apoptotic Effects
2021-07-28
Pelcitoclax has potent anti-tumor effects through ntrinsic mitochondrial pathway of apoptosis in cancer cells. -
UK122 is a potent and selective urokinase-type plasminogen activator (uPA) inhibitor with anti-cancer activity.
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DCH36_06 is a Selective p300/CBP Inhibitor
2021-07-31
DCH36_06 is a potent and selective p300/CBP inhibitor with strong anti-tumor activities both in vivo and in vitro. -
Aderbasib is a potent and orally active inhibitor of ADAM10 and ADAM17. Aderbasib exhibits robust antineoplastic activity in vivo.
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NRX-2663 is a potent enhancer of the interaction between β-catenin SCFβ-TrCP, potentiates the ubiquitylation of mutant β-Catenin by β-TrCP.
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M3258 is an orally bioavailable, potent, reversible, and highly selective immunoproteasome subunit LMP7 (β5i) inhibitor.
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MRTX9768 is an Orally Active PRMT5 Inhibitor
2021-08-07
MRTX9768 is an orally active PRMT5 inhibitor and designed to bind the PRMT5-MTA complex and selectively target MTAP/CDKN2A-deleted tumors. -
E67-2 is a Selective KIAA1718 Jumonji Domain Inhibitor with Low toxicity and is a potent compound of cancer research.
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SIM1 is a PROTAC Based BET Family Degrader
2021-08-11
SIM1 is a potent von Hippel-Lindau (VHL)-based trivalent PROTAC capable of degradation for all BET family members. -
AC-4-130 is a potent STAT5 SH2 domain inhibitor. AC-4-130 induces cell cycle arrest and apoptosis with anti-cancer activity.
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PHPS1 is a Selective Shp2 Inhibitor
2021-08-14
PHPS1 is a potent and selective Shp2 inhibitor. PHPS1 reveals a significant decrease in atherosclerotic plaque size. -
UMB298 is a selective CBP/P300 bromodomain inhibitor and could provide an effective study for acute myeloid leukemia.
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VT-107 is a potent and pan-TEAD auto-palmitoylation inhibitor. VT-107 can inhibit the proliferation of NF2-deficient mesothelioma cells.
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IV-361 is an orally active, potent, and selective CDK7 inhibitor. IV-361 exhibits excellent anti-tumor activity.
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HS-131, a near infrared dye tethered Hsp90 inhibitor, is able to detect oncogene-driven many breast cancers.
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Z-VAD-FMK is a cell-permeant, irreversible pan-caspase inhibitor, which prevents apoptosis in many different cell types.
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Rapamycin is a Specific mTOR Inhibitor
2021-08-25
Rapamycin is a specific inhibitor of mTOR, an autophagy activator, an immunosuppressant, with anti-inflammatory and anti-tumor activities. -
Staurosporine is an ATP-competitive protein kinases inhibitor and is a potent compound of cancer research.
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LY294002, a broad-spectrum inhibitor of PI3K (IC50s ranging 0.5-0.97 μM for PI3Kα, PI3Kδ, and PI3Kβ), is an apoptosis inducer.
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Trichostatin A (TSA) is a potent and specific inhibitor of HDAC class I/II. Trichostatin A exhibits anti-tumor activity.
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Fulvestrant is a pure antiestrogen and a potent estrogen receptor (ER) antagonist. Fulvestrant induces autophagy and has antitumor efficacy.
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Iberdomide (CC-220) is an orally active cereblon (CRBN) E3 ligase modulator (CELMoD) with antitumor and immunostimulatory activities。
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Ruxolitinib is a potent and selective JAK1/2 inhibitor and has 130-fold selectivity for JAK1/2 over JAK3. Ruxolitinib induces autophagy.
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Everolimus (RAD001), a Rapamycin Derivative, is a Selective and Orally Active mTOR1 Inhibitor
2021-09-07
Everolimus (RAD001), a Rapamycin derivative, is a selective and orally active mTOR1 inhibitor with anticancer activities. -
SN-38 (NK012) is an active metabolite of the Topoisomerase I inhibitor Irinotecan and inhibits DNA and RNA synthesis.
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Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor with good anticancer activity.
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Sorafenib (Bay 43-9006) is an orally active Raf inhibitor and induces autophagy and apoptosis with anti-tumor activity.
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ARQ 531 is a potent, ATP-competitive, reversible non-covalent and orally active BTK inhibitor, with anti-tumor activities.
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Wortmannin is a potent, selective, irreversible and orally active PI3K inhibitor, with anticancer effects.
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Birinapant (TL32711), a bivalent Smac mimetic, is a potent antagonist for XIAP and cIAP1 and induces apoptosis.
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GSK2606414 is an orally available PERK inhibitor and is a potent compound of cancer and neurological diseases.
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AZD4635 is a potent, selective and orally active antagonist of A2AR that reverses adenosine-mediated immune suppression.
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IACS-010759 is an orally active, potent mitochondrial complex I of oxidative phosphorylation (OXPHOS) inhibitor with antitumor activity.
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Infigratinib is a potent inhibitor of the FGFR family, with IC50s of 0.9 nM, 1.4 nM, 1 nM, and 60 nM for FGFR1/2/3/4, respectively.
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Sapanisertib is an orally available, potent, and highly selective mTORC1/2 inhibitor demonstrating promise in numerous malignancies.
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Elesclomol is an oxidative stress inducer that induces cancer cell apoptosis. Elesclomol is a reactive oxygen species (ROS) inducer.
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Ganetespib (STA-9090) is a HSP90 Inhibitor
2021-10-14
Ganetespib is a unique Hsp90 inhibitor that exhibits potent and sustained antitumor effects in a broad range of malignancies. -
Atuveciclib (BAY-1143572) is a highly selective, oral PTEFb/CDK9 inhibitor with potent antitumor activity.
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Cytochalasin B is a cell-permeable mycotoxin binding to the barbed end of actin filaments, disrupting the formation of actin polymers.
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Saracatinib is a potent Src inhibitor (IC50s of 2.7 to 11 nM for c-Src, Lck, c-YES, Lyn, Fyn, Fgr, and Blk) and has anti-invasive activities.
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Quizartinib (AC220) is an Orally Active and Highly Selective FLT3 Tyrosine Kinase Inhibitor
2021-10-24
Quizartinib (AC220) is an orally active, highly selective, and potent second-generation type II FLT3 tyrosine kinase inhibitor. -
Brusatol (NSC 172924) is a Nrf2 Inhibitor
2021-10-26
Brusatol inhibits the Nrf2 signaling pathway by reducing the protein level of Nrf2, with anticancer activities. -
SB 258719 is a selective 5-HT7 receptor antagonist and can be used for the research of cancer and neurological disease.
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CX-5461 is a potent and orally bioavailable inhibitor of Pol I-mediated rRNA synthesis with potent antitumor activity.
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Daunorubicin is a topoisomerase II inhibitor with a wide spectrum of anticancer activity and anti-HBV effect.
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MB710 is a stabilizer of oncogenic p53 mutation Y220C. MB710 binds to the Y220C pocket and stabilizes p53-Y220C, with a Kd of 4.1 μM.
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Nintedanib a potent and orally active triple vascular kinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β.
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IMD-0354 is a Selective IKKβ Inhibitor
2021-11-09
IMD-0354 is a selective IKKβ inhibitor and potently inhibits NF-κB activity. IMD0354 has antitumor activity. -
Anisomycin is a potent protein synthesis inhibitor which interferes with protein and DNA synthesis. Anisomycin is a JNK activator.
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Crizotinib is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Anti-tumor activity.
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Oltipraz is a Nrf2 Inhibitor
2021-11-18
Oltipraz is a potent Nrf2 activator. Oltipraz has an inhibitory effect on HIF-1α activation in a time-dependent manner, the IC50 is 10 μM. -
Cyclopamine is a potent Hedgehog (Hh) pathway antagonist and a selective Smo inhibitor with antitumor activity.
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A 83-01 is an inhibitor of ALK5/4/7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5/4/7, respectively.
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PR-104A is a hypoxia-selective DNA cross-linking agent/DNA-damaging agent and cytotoxin. Antitumor Activity. Leukemia (T-ALL).
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Axitinib is a multi-targeted tyrosine kinase inhibitor and potently inhibitor VEGFR1, VEGFR2, VEGFR3 and PDGFRβ.
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Fadrozole is a potent, selective, and nonsteroidal inhibitor of aromatase with an IC50 of 6.4 nM. Can be used for cancer research.
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Troglitazone is a potent PPARγ agonist with antitumor activies. Troglitazone has the potential for the research of the pancreatic cancer.
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Spautin-1 is a specific and potent autophagy inhibitor which inhibits ubiquitin-specific peptidases, USP10 and USP13.
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Flavopiridol is a broad spectrum and competitive inhibitor of CDKs, inhibiting CDK1, CDK2, CDK4 with IC50s of 30, 170, 100 nM, respectively.
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Lonidamine, an antitumor agent and an indazole derivative, interferes with energy-yielding processes in cancer cells.
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CBL0137 is an inhibitor of the histone chaperone, FACT. CBL0137 activates p53 and inhibits NF-κB with EC50s of 0.37 and 0.47 µM, respectively.
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AZD1390 is a potent, highly selective, orally bioavailable, brain-penetrant ATM inhibitor with an IC50 of 0.78 nM.
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MRTX1133, a selective, first-in-class inhibitor of KRAS G12D, selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells.
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Zebularine is a potent DNA methyltransferase inhibitor with anti-tumor activity. Zebularine also inhibits cytidine deaminase.
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MS4322 is a first-in-class PRMT5 degrader and a valuable chemical tool for exploring the PRMT5 functions in vitro and in vivo.
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Apitolisib is a potent Class I PI3 kinase and mTORC1/2 inhibitor with IC50s of 5 nM/27 nM/7 nM/14 nM for PI3Kα/β/δ/γ, respectively.
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Almonertinib is an orally available, third-generation EGFR TKI with selectivity for EGFR-sensitizing and T790M resistance mutations.
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ABT-737, a BH3 mimetic, is a potent Bcl-2, Bcl-xL and Bcl-w inhibitor and has the potential for acute myeloid leukemia (AML) research.
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Alda-1 is a potent ALDH2 Agonist
2021-12-30
Alda-1 ameliorates H2O2-induced Achilles tendinopathy. Alda-1 could be used for preventing Achilles tendinopathy. -
Bestatin is a broad-spectrum and competitive aminopeptidase and leukotriene A4 hydrolase inhibitor, with anticancer effects.
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Repotrectinib is a potent ROS1 (IC50=0.07 nM) and TRK (IC50=0.83/0.05/0.1 nM for TRKA/B/C) inhibitor. Repotrectinib has anti-cancer activity.
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Deguelin acts as a chemopreventive agent by blocking multiple pathways like PI3K-Akt, IKK-NF-κB, and MAPK-mTOR-survivin-mediated apoptosis.
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XL092 is a potent inhibitor of the activity of Axl, Mer and C-Met kinase with IC50s of <10 nM, respectively. Anti-tumor Activity.
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Dovitinib is a multi-targeted tyrosine kinase inhibitor. Dovitinib inhibits cell proliferation and has potent antitumor activity.
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Rucaparib is a PARP Inhibitor
2022-01-13
Rucaparib is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3). Rucaparib has the potential for CRPC research. -
β-Lapachone, a topoisomerase I inhibitor, induces apoptosis by inhibiting cell cycle progression. β-Lapachone has anti-inflammatory effect.
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Tirabrutinib is a Selective BTK Inhibitor
2022-01-18
Tirabrutinib is a selective and novel inhibitor of BTK, Tirabrutinib prevents B-cell receptor signaling and impeding B-cell development. -
SD-1029 is a JAK2/STAT3 Activation Inhibitor
2022-01-22
SD-1029, a JAK2/STAT3 activation inhibitor, can inhibit STAT3 nuclear translocation and JAK2 phosphorylation. -
VU0359595 is a Selective PLD1 Inhibitor
2022-01-26
VU0359595 is a potent and selective PLD1 inhibitor, and VU0359595 shows >1700-fold selective for PLD1 over PLD2. -
CL097 is a TLR7/8 agonist. CL097 induces pro-nflammatory cytokines. CL097 induces NADPH oxidase priming and efficient diabetogenic cytotoxic T lymphocyte (CTL) function in NOD mice.
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Zingerone is a natural orally active nontoxic methoxyphenol potent anti-inflammatory, antidiabetic, antioxidize, and anti-tumor properties.
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ML-099 is a pan Ras-related GTPases activator. ML-099 can activate Rac1, cell division cycle 42, Ras, Rab7, and Rab-2A.
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IACS-15414, a potent and orally active SHP2 inhibitor, exhibits significant anti-tumor efficacy in mouse xenograft model.
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GS-493 is a selective SHP2 inhibitor and blocks cellular motility and growth of cancer cells in vitro and in vivo.
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HM43239 is a potent, selective, and orally active FLT3 inhibitor and shows effectiveness in AML with FLT3 mutations.
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PFM39 is a potent and selective MRE11 exonuclease inhibitor, and does not inhibit endonuclease, nuclease activity.
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Hesperadin, an ATP competitive inhibitor of Aurora A/B, inhibits Aurora B with an IC50 of 250 nM. A broad-spectrum influenza antiviral.
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VAL-083 is an alkylating agent that creates N7 methylation on DNA, VAL-083 exhibits antitumor activity in vitro and in vivo.
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Lomeguatrib is a highly potent MGMT inactivator, improves the therapeutic effect of alkylating agents in a number of tumour models.
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Indoximod, an immunometabolic adjuvant, is an orally active IDO pathway inhibitor. Indoximod acts as a Trp mimetic in regulating mTOR.
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MS170 is a PROTAC AKT Degrader
2022-02-27
MS170 is a CRBN-recruiting degrader, the AKT proteolysis targeting chimera (PROTAC) degrader. -
Avitinib is a potent, irreversible and orally active inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase.
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Rigosertib (ON-01910), a multi-kinase inhibitor, inhibits PLK1 (IC50=9 nM), and induces G2/M arrest in cell cycle and apoptosis.
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PX-12 is an irreversible inhibitor of Trx-1 and inhibits the growth, migration, and invasion of colorectal cancer cell lines.
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Chelerythrine is a potent inhibitor pf protein kinase C with anti-cancer activity.
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Tanomastat is an orally active, non-peptidic biphenyl MMPs inhibitor, with antiangiogenic, anti-invasive and antimetastatic activities.
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Linzagolix is a potent, non-peptide, and orally active GnRH antagonist used for the research of endometriosis and uterine myomas.
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BM213 is a selective C5aR1 agonist. It’s a useful research tool to study C5aR1 function
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Mirin is a potent MRN complex inhibitor. Mirin prevents MRN-dependent activation of ATM without affecting ATM protein kinase activity.
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Monastrol, a potent and cell-permeable inhibitor of the mitotic kinesin Eg5, has potential for cancer research.
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FH535 is a potent inhibitor of Wnt/β-catenin and PPAR.
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GNE-149 is an orally bioavailable full antagonist of estrogen receptor α. GNE-149 has potent antitumor activity.
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Bafetinib is an orally active dual Abl/Lyn tyrosine kinase inhibitor. Bafetinib suppresses the growth of Ph+ leukemia cells.
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Pirarubicin, an anthracycline antibiotics, is a topoisomerase II Inhibitor.
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WAY 316606 is an inhibitor of the secreted protein sFRP-1.
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Ulixertinib is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases.
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Nimbolide, a triterpene derived from the leaves and flowers of neem, induces apoptosis through inactivation of NF-κB.
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Telatinib is an orally active inhibitor of VEGFR2, VEGFR3, PDGFα, and c-Kit.
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Reversine is a potent, ATP-competitive Aurora kinases inhibitor. Reversine is a potential anticancer agent for ALL.
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Tivantinib is a selective and orally active inhibitor of c-MET. Tivantinib can be used for the research of cancer.
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Oprozomib (PR-047) is an orally active peptide epoxyketone proteasome inhibitor.
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Embelin is a Nonpeptidic XIAP Inhibitor
2022-05-05
Embelin is a potent inhibitor of nonpeptidic XIAP. -
Splitomicin is a cell-permeable, potent inhibitor of SIR2. Splitomicin inhibits the aggregation of human platelets.
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Bisantrene is topoisomerase II poisons and DNA intercalators. Bisantrene intercalates with and disrupts the configuration of DNA.
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Epothilone B is a Microtubule Stabilizer
2022-05-10
Epothilone B, a non-taxane-related and nonneurotoxic microtubule stabilizer, can be used for the research of breast cancer. -
Pimasertib is a highly selective, ATP non-competitive allosteric orally available MEK1/2 inhibitor with antitumor activies.
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5-Azacytidine is a DNMT inhibitor. 5-Azacytidine can be used for the research of myelodysplastic syndrome.
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Epoxomicin is an epoxyketone-containing natural product and a selective and irreversible proteasome inhibitor. Cross the blood-brain barrier.
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Vistusertib is an ATP competitive mTOR inhibitor with an IC50 of 2.81 nM. AZD2014 inhibits both mTORC1 and mTORC2 complexes.
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Seliciclib, a potent, selective and orally active CDKs inhibitor, preferentially inhibits CDK2, CDK7 and CDK9.
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Temoporfin, a photosensitizer agent, can be used for the research of squamous cell carcinoma of the head and neck.
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Namodenoson (CF-102) is a selective A3 adenosine receptor (A3AR) agonist.
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Marimastat (BB2516) is a broad spectrum and orally bioavailable inhibitor of MMPs (Matrix metalloproteinases).
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Ascochlorin Mediates Anti-tumor Effects through the Suppression of STAT3 Signaling Cascade
2022-06-05
Ascochlorin, an isoprenoid antibiotic, mediates its anti-tumor effects predominantly through the suppression of STAT3 signaling cascade. -
Gardiquimod is a TLR7/8 agonist and can inhibit HIV-1 infection.
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Vatalanib is an inhibitor of VEGFR2/KDR. Vatalanib induces inhibition of the angiogenic response to VEGF and PDGF.
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β-Amanitin is a cyclic peptide toxin, inhibits eukaryotic RNA polymerase II and III. It inhibits DNA transcription, and protein synthesis.
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LTX-315 is an oncolytic peptide with potent anticancer activity.
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Actinomycin D (Dactinomycin) is an autophagy activator inhibiting DNA repair with an IC50 of 0.42 μM.
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Pitstop 2 is a clathrin inhibitor which inhibits clathrin-mediated endocytosis (CME) by associating with the terminal domain of clathrin.
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DS17701585 is a highly selective and orally active EP300 and CBP inhibitor and DS17701585 can be used for cancer research.
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Rebeccamycin, an antitumor antibiotic, inhibits DNA topoisomerase I. Rebeccamycin can be used for leukemia research.
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Lapatinib is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively.
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CQ211 is a selective RIOK2 inhibitor (Kd=6.1 nM). CQ211 exhibits anti-proliferation inhibition activity against multiple cancer cell lines.
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FPDT is an anti-glioblastoma agent. Besides, FPDT shows anti-proliferative activity for GBM cells and astrocytes.
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SBI-581 is an orally active and selective serine-threonine kinase TAO3 inhibitor with potent antitumor activity.
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AZD7254 is a potent and orally active Smoothened (SMO) inhibitor, against sonic Hh protein (shh), with strong anti-cancer effects.
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Toceranib is a selective and orally active inhibitor of RTK and has the potential for the research of canine mast cell tumors.
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RKI-1313 is a Potent ROCK1/2 inhibitor
2022-07-09
RKI-1313 is a potent ROCK inhibitor and shows little effect on the phosphorylation levels of ROCK substrates, migration, invasion. -
LDN-211904 oxalate is a potent and selective EphB3 inhibitor and combines with cetuximab can overcome cetuximab resistance.
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Pulrodemstat is a potent, selective, reversible and orally active LSD1 inhibitor, with anticancer effects.
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Tiragolumab is an immune checkpoint inhibitor binding to TIGIT. Tiragolumab is effective against multiple solid malignancies.
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PSB-SB-487 is a Potent GPR55 Antagonist
2022-07-21
PSB-SB-487, a Coumarin derivative, is a potent GPR55 antagonist, and is also a partial CB2 receptor agonist. -
Henatinib is an orally active small-molecule multikinase inhibitor that has demonstrated broad and potent antitumor activities.
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Panobinostat, a potent and orally active non-selective HDAC inhibitor, exhibits antineoplastic activities.
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DD1, a proteasome inhibitor, targets Bax activation and P70S6K degradation during acute myeloid leukemia (AML) apoptosis.
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Rucaparib (AG014699) is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with IC50s <5 nM , possessing anticancer activity.
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ML-097 is a pan Ras-related GTPases activator that can activate Rac1, cell division cycle 42, Ras, and Rab7.
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KGP94 is a selective inhibitor of cathepsin L. KGP94 has antitumor activity and improves survival of bone metastases bearing mice.
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PU-H54 is a potent purine-based (PU) Grp94-selective inhibitor. PU-H54 has the potential for the research of breast cancer.
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Vamotinib is a novel, potent and selective BCR-ABL tyrosine kinase inhibitor that can induce apoptosis in chronic myelogenous leukemia cells.
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BI-1622 is an orally active, potent and highly selective HER2 inhibitor, and shows antiproliferative and anti-tumor activity.
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BNS-22 is a potent and selective inhibitor of TOP2α and TOP2β that exhibits anti-proliferative activities.
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Pelecopan is a potent, selective, and orally active complement factor D inhibitor, possessing the potential to study paroxysmal nocturnal hemoglobinuria (PNH).
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FL118 is a survivin inhibitor and a camptothecin analogue. FL118 has the potential for the research of cancer.
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BM-1074 is a potent and specific Bcl-2 and Bcl-xL inhibitor and shows antiproliferative and anti-tumor activity.
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MS159 is a frist-In-class nuclear receptor binding SET NSD2 PROTAC degrader for multiple myeloma research.
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DC-S239 is a potent and selective SET7 Inhibitor, and DC-S239 shows antiproliferative activity for some cancer cells.
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Certepetide is a Tumor-penetrating Enhancer via RGD Motif Interaction with Alphav-integrins
2022-09-01
Certepetide is a tumor-penetrating enhancer and has the potential for the research of metastatic pancreatic ductal adenocarcinoma. -
ARV-471 is an oral estrogen receptor PROTAC degrader for breast cancer. ARV-471 robustly degrades ER in ER-positive breast cancer cell lines.
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AZD-9574 is a potent and brain penetrant PARP1 inhibitor and shows >8000-fold selectivity for PARP1 compared to PARP2/3/5a/6.
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BLU2864 is an orally active ATP-competitive PRKACA inhibitor. BLU2864 can be used in cancer and polycystic kidney disease research.
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SPH5030 is a potent, selective, irreversible and orally active HER2 Inhibitor and shows anti-cancer activity.
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LCS3 is a potent and reversible inhibitor of GSR and TXNRD1 with anti-tumour activity by non-competitive inhibition of the enzyme activity.
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EAI001 is a potent, selective mutant EGFR allosteric inhibitor. EAI001 has the potential for research on cancer.
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G12Si-5, a potent, selective and reversible covalent inhibitor of the K-Ras G12S, can be used for the research of cancer.
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Simmiparib is a highly potent and orally active PARP1 and PARP2 inhibitor with IC50s of 1.75 nM and 0.22 nM, respectively. Antitumor effect.
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TK4g is a potent JAK inhibitor and can be used for studies of lymphatic-related diseases and leukemic cancers.
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ARD-69 is a potent PROTAC androgen receptor degrader and induces degradation of AR protein in AR-positive prostate cancer cell lines.
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CP681301 is a Potent CDK5 Inhibitor
2022-09-26
CP681301 is a potent CDK5 inhibitor, inhibits glioma stem cells self-renewal and shows anti-tumor activity. -
SHR2415 is a highly potent, selective and orally active ERK1 and ERK2 inhibitor with IC50 values of 2.8 and 5.9 nM, respectively.
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EM127 is a SMYD3 Covalent Inhibitor
2022-10-01
EM127 is a potent and selectivity SMYD3 covalent inhibitor and impairs methyltransferase activity, can be used in SMYD3 positive tumours. -
BT5528 is a bicyclic peptide toxin conjugate, an EphA2 activator. BT5528 shows potent anti-tumor activity.
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BSP16 is a potent, orally active stimulator of interferon genes (STING) agonist. BSP16 has potent anti-cancer activity.
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PM-81I is a Potent STAT6 Inhibitor
2022-10-08
PM-81I is a potent STAT6 inhibitor that has potential for the research of allergic lung disease, allergic rhinitis and cancer. -
EPI-7170 is an AR N-terminal structural domain antagonist that blocks the transcriptional activity of full-length AR (FL-AR) and AR-Vs.
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GR-46611 is a 5-HT1D Receptor Agonist
2022-10-11
GR-46611 is a potent 5-HT1D receptor agonist and has the potential for the research of epilepsy and inhibits bladder activity. -
AZ31 is a potent, highly selective, and orally active ATM inhibitor, and is also a potent radiosensitizer in vitro.
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Ficlatuzumab is a monoclonal antibody (McAb) targeting human hepatocyte growth factor (HGF) with potent anti-cancer activity.
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Coleon-U-quinone is a potent P-gp inhibitor. It inhibits P-glycoprotein (P-gp) activity and reverts doxorubicin (DOX) resistance.
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Purinostat mesylate is a potent and selective inhibitor of HDAC. Purinostat mesylate can be used for the research of lymphoblastic leukemia.
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Parsatuzumab (RG 7414) is a humanized monoclonal antibody, that acts as an immunomodulator, and binds to EGFL7.
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Golcadomide is a potent and orally active CRBN E3 ligase modulator with immunomodulating and antineoplastic activities.
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GNE-9815 is a highly selective pan-RAF inhibitor, can be used to research KRAS mutant cancers
2022-10-24
GNE-9815 is a highly selective, pan-RAF inhibitor with good oral bioavailability and is used for cancer research. -
MPM-1, a marine Eusynstyelamides mimic, is a potent anticancer agent. MPM-1 causes perturbation of autophagy in cancer cells.
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RP-6685 is a potent, selective and orally active DNA Polθ inhibitor with an IC50 value of 5.8 nM. RP-6685 shows antitumor activity.
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Zilovertamab is a humanised monoclonal antibody against ROR1 that blocks Wnt5a-induced ROR1 signalling.
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CAM 833, a potent and selective inhibitor of the BRCA2-RAD51 interaction, and has the potential for the cancer research.
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SOR-C13 is a high-affinity TRPV6 antagonist with an IC50 value of 14 nM. SOR-C13 is used for Advanced Solid Tumors Research
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Etrolizumab is a Gut-selective, Anti-β7 Integrin McAb for Inflammatory Bowel Disease (IBD) Research
2022-11-05
Etrolizumab is a gut-selective, anti-β7 integrin monoclonal antibody and has the potential for the research of inflammatory bowel disease. -
JNJ-9350 is an inhibitor of spermine oxidase (SMOX). JNJ-9350 also inhibits polyamine oxidase (PAO). JNJ-9350 has anti-cancer activity.
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LY3177833 is an orally active CDC7 and pMCM2 inhibitor with IC50 values of 3.3 nM and 290 nM, respectively. LY3177833 is a senescence inducer
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Serplulimab is a humanized monoclonal anti-PD-1 antibody and has the potential for the research of small cell lung cancer.
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BI-0474 is a Potent KRAS G12C inhibitor
2022-11-14
BI-0474 is a potent KRAS G12C inhibitor and exhibits good anti-proliferative activity against NCI-H358 cells carrying the G12C mutation. -
ABT-510, a peptide analog of thrombospondin-1 (TSP-1), can block angiogenesis in vitro and in vivo, and slow tumor growth.
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GN25 is a specific inhibitor of p53-Snail binding and shows anti-tumor effect against K-Ras-mutated cancer.
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STX-0119 is a selective, orally active STAT3 dimerization inhibitor. STX-0119 shows potent antitumor activity.
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JBJ-09-063 is a mutant-selective allosteric EGFR inhibitor. JBJ-09-063 can be used for EGFR-mutant lung cancer research.
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Abexinostat, a potent and broad-spectrum inhibitor of histone deacetylases, can be used for the research of cancer.
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JS25 is a selective and covalent BTK inhibitor in hematological cancer. JS25 has blood brain barrier crossing property.
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STF-31 is a potent ans selective inhibitor of GLUT1 that inhibit glucose uptake in renal cell carcinoma (RCC) 4 cells.
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Reversin 121, a P-glycoprotein Inhibitor, Reverses P-glycoprotein-Mediated Multidrug Resistance
2022-12-01
Reversin 121 is a potent P-glycoprotein inhibitor that reverses P-glycoprotein-mediated multidrug resistance. -
Spiruchostatin A is a potent HDAC inhibitor that can induce apoptosis and has anticancer activity uesd for leukemia studies.
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CYD-2-11 is a selective Bax agonist with antitumor activities in vitro and vivo and the inducing of cell apoptosis.
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U7D-1 is a selective USP7 PROTAC degrader. U7D-1 induces apoptosis in Jeko-1 cells and shows anticancer activity.
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Targefrin is a potent EphA2-targeting agent, acts as an antagonist, and can be used to research pancreatic cancer.
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Mogamulizumab is an Anti-CCR4 monoclonal antibody. It enhances antibody-dependent cellular cytotoxicity and is effective against leukemia.
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Olutasidenib (FT-2102) is an orally active, brain penetrant inhibitor of mutant IDH1. Olutasidenib is used for AML or MDS Research.
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Mitonafide, a potent cytostatic agent, can inhibit DNA and RNA synthesis. Mitonafide is a potent antitumor agent.
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Polatuzumab vedotin is an antibody-drug conjugate targeting CD79b and has the potential for the research of Large B-cell lymphomas (LBCL).
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A947 is a selective SMARCA2 (PROTAC). A947 also is a moderately selective SMARCA2 degrader. A947 can be used for the research of cancer.
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Adagrasib (MRTX849) is an orally available, and mutation-selective covalent inhibitor of KRAS G12C. Can be used for NSCLC research.
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NecroIr2 is an iridium(III) complex, serves as necroptosis inducers in Cisplatin (HY-17394)-resistant lung cancer cells (A549R).
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CYD-4-61 is a novel Bax activator. It induces cytochrome c release, mitochondrial membrane penetration, consequently leads to cell apoptosis.
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Rohinitib is a potent and specific eIF4A inhibitor that induce apoptosis of AML cell lines and shows anti-AML effects in vivo.
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Ganitumab (AMG 479) is a recombinant human monoclonal antibody to the human IGF1R. Ganitumab can be used in research of cancer.
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AManzamine A is an orally active β-carboline alkaloid effective against HSV-1, Cancer, and Malaria.
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SJ988497 is a cell permeable PROTAC JAK2 degrader that degrades JAK2 in vitro and in vivo, and shows anticancer activity against leukemia.
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D6808 is a highly selective and potent c‑Met inhibitor. D6808 can be used for the research of NSCLC and gastric cancers
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MMRi62, a Ferroptosis inducer targeting MDM2-MDM4. MMRi62 shows a P53-independent pro-apoptotic activity against PDAC cells.
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TD1092 is a pan-IAP degrader, degrades cIAP1, cIAP2, and XIAP. TD1092 inhibits NF-κB pathway and epithelial-mesenchymal transition (EMT).
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Xentuzumab is an anti-IGF-1/2 mAb, also targets to INSR-A. Xentuzumab inhibits tumor proliferation and induces apoptosis.
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Tigatuzumab, a humanized IgG1 anti-DR5 monoclonal antibody, is aTRAIL-R2 agonist, with potent anticancer effects.
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OTS193320 is a potent SUV39H2 methyltransferase activity inhibitor. OTS193320 triggers apoptotic cell death.
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FA16 is a specific and metabolically stable ferroptosis inducer. It inhibits system Xc-, results in tumor progression suppression.
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SIAIS100 is a Potent BCR-ABL PROTAC Degrader
2023-01-10
SIAIS100 is a potent BCR-ABL PROTAC degrader with an DC50 value of 2.7 nM. SIAIS100 can be used to research chronic myeloid leukemia (CML). -
Benufutamab is a DR5-specific agonistic IgG1 antibody (Hx-DR5-01 and Hx-DR5-05), with potent antitumor effects.
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Salviolone is a natural diterpene identified from Salvia miltiorrhiza roots with an anti-melanoma activity.
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YX-2-107 is a PROTAC that selectively degrades CDK6.
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Bapotulimab (BAY-1905254) is an ILDR2 IgG antibody that blocks the immunosuppressive effects of ILDR2 on T-cell activation.
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YL-939 was a potent inhibitor of iron death and significantly improved liver injury in a model of iron death-related acute liver injury.
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Amivantamab is an EGFR-MET bispecific monoclonal antibody for the treatment of non-small cell lung cancer.
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Nanrilkefusp alfa is a selective and strong IL-15 agonist. It inhibits tumor metastasis and viability by activating natural killer (NK) cells.
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Enavatuzumab (PDL192; ABT-361) is a humanized IgG1 monoclonal antibody targeting the receptor of TWEAK with potent antitumor activity.
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Coibamide A is an N-methyl-stabilized cytotoxic depsipeptide with antiproliferative activity. Coibamide A induces autophagosome accumulation.
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Urabrelimab (SRF231) is an anti-CD47 monoclonal antibody, blocking the CD47-SIRPα interaction. It has the potential to research anticancer.
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SZUH280, a potent and selective PROTAC HDAC8 degrader, ,shows antitumor activity in an A549 nude mouse model.
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Talacotuzumab is an IgG1-type fully humanized, CD123-neutralizing monoclonal antibody containing a modified Fc structure.
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Lexatumumab is a TRAIL-R2 agonist antibody that can induce apoptosis. It shows stronger efficacy when combined with other anticancer agents.
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MS8815 is a selective EZH2 PROTAC degrader. MS8815 can be used for the research of triple-negative breast cancer (TNBC),
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Efineptakin alfa (NT-17) is a Long-Acting Recombinant Human IL-7 for Glioblastoma Research
2023-02-07
Efineptakin alfa (NT-17) is a long-acting recombinant human IL-7. Efineptakin alfa can be used for glioblastoma research. -
ML-SA5 is a potent TRPML1 cation channel agonist with some anticancer activity and can inhibit tumour growth.
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MC2590 is a potent pyridine-containing HDAC inhibitor and modulates pro- and anti-apoptotic microRNAs toward apoptosis induction.
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Pegdinetanib (BMS-844203) is a selective VEGFR-2 inhibitor with antitumor activity.
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Asunercept (APG101) is a soluble CD95-Fc fusion protein targeting CD95L.
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Ferristatin is a potent iron transport inhibitor and shows antiviral potency and anti-MTase (methyltransferase) activity.
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Elacestrant (RAD1901) is an orally available selective estrogen receptor degrader. Elacestrant used for Breast cancer research.
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Opnurasib (JDQ-443) is a structurally novel, potent, and selective covalent oral inhibitor of KRAS G12C that exhibits antitumor activity.
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BPDA2 is a competitive active site SHP2 inhibitor and suppresses SHP2-mediated signaling and breast cancer cell phenotypes.
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ARN24139 is a potential topoisomerase II (topoII) inhibitor that inhibits cancer cell proliferation and is useful in cancer research.
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Talotrexin (PT523), a classic antifolate, is an RFC (reduced folate carrier) specific inhibitor and selectively inhibits RFC transport.
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RLA-5331 is an iron activator containing anti-androgen. RLA-5331 is used for metastatic castrated tolerant prostate cancer (mCRPC) research.
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SH-BC-893 is an orally active sphingolipid analog. It can be used for the research of cancer and metabolism-related diseases.
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SG-094 is a potent TPC2 inhibitor with antiproliferative effects. SG-094 can be used for the research of cancer.
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Cetuximab is a potent human anti-EGFR monoclonal antibody. Besides, Cetuximab also shows anti-tumor activity.
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Navitoclax (ABT-263) is an Orally Active Bcl-2 Inhibitor for Chronic Lymphocytic Leukemia Research
2023-03-06
Navitoclax is an orally active Bcl-2 inhibitor targeting to Bcl-xL, Bcl-2, Bcl-w, with anti-tumor activity in vitro and in vivo. -
Tifcemalimab, a Humanized anti-BTLA monoclonal antibody, blocks the interaction of HVEM-BTLA by binding to BTLA and activates lymphocytes.
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SU056, a YB-1 Inhibitor, Induces Cell-cycle Arrest, Apoptosis and Inhibits Cell Migration in Cancer
2023-03-09
SU056 is a YB-1 inhibitor that induces cell cycle arrest, apoptosis and inhibits cell migration of cancer cells. -
Sotorasib is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor, which inhibits tumor growth in mice.
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Dazostinag is a STING Agonist and Can be used for Antibody-Drug Conjugates (ADCs) Synthesis
2023-03-13
Dazostinag is a STING agonist and a playload, to synthesis antibody-drug conjugates (ADCs). It has antitumor activity in vivo. -
Ruxolitinib is an orally-active JAK1/2 inhibitor. Ruxolitinib has the potential for the research of myeloproliferative neoplasm (MPN).
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Izalontamab is an EGFR/HER3 Bi-specific monoclonal antibody. Besides, Izalontamab has the potential for the research of cancer.
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Palbociclib is a potent, selective and orally active CDK4 and CDK6 inhibitor with strong anti-cancer activity.
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MC0704 is a STAT3 inhibitor (IC50=2.13 μM), which can be used for the research of metastatic triple-negative breast cancer (mTNBC).
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MPT0B014 is a potent tubulin polymerization inhibitor and induces cancer cell apoptosis in a dose-dependent manner.
Products
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All
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Inhibitors & Agonists
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Isotope-Labeled Compounds
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Inhibitory Antibodies
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Reference Standards
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Induced Disease Models Products
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GMP Small Molecules
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Biochemical Assay Reagents
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Natural Products
| Cat. No. | Product Name | Information | Application | Publication |
|---|---|---|---|---|
| HY-16658B | Z-VAD-FMK |
Z-VAD-FMK is a pan-caspase inhibitor and also an ICE-like protease inhibitor, which inhibits apoptosis by preventing the processing of CPP32 to its active form. Z-VAD-FMK sensitivity varies primarily due to differential expression of receptor-interacting protein 1 (RIP1). Z-VAD-FMK limits the cryopreservation-induced apoptosis by reducing caspase-3 activity of in vitro produced bovine embryos. Z-VAD-FMK is immunosuppressive in vitro and inhibits T cell proliferation without blocking the processing of caspase-8 and caspase-3. Z-VAD-FMK leads to a decrease in intracellular glutathione (GSH) with a concomitant increase in reactive oxygen species (ROS) levels in activated T cells. Z-VAD-FMK is due to oxidative stress via the depletion of GSH. Z-VAD-FMK can be used for the study of acute pancreatitis.
|
|
850
|
| HY-15760 | Necrostatin-1 |
Necrostatin-1 (Nec-1) is a potent and cross the blood-brain barrier necroptosis inhibitor with an EC50 of 490 nM in Jurkat cells. Necrostatin-1 inhibits RIP1 kinase (EC50=182 nM). Necrostatin-1 is also an IDO inhibitor.
|
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575
|
| HY-15886 | Mdivi-1 |
Mdivi-1 is a selective dynamin-related protein 1 (Drp1) inhibitor. Mdivi-1 is a mitochondrial division/mitophagy inhibitor.
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354
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| HY-16658 | Z-VAD(OMe)-FMK |
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211
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|
| HY-13205 | Belnacasan |
Belnacasan (VX-765) is an orally bioactive proagent of VRT-043198, which is a potent and selective inhibitor of IL-converting enzyme (ICE)/caspase-1 with Kis of 0.8 nM and less than 0.6 nM for caspase-1 and caspase-4, respectively. Belnacasan (VX-765) inhibits the release of LPS-induced IL-1β and IL-18 by human PBMCs with an IC50 of ~0.7 μM.
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180
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| HY-B0075 | Melatonin |
Melatonin is a hormone made by the pineal gland that can activate melatonin receptor and inhibit PANoptosis. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties. Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation. Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress.
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Melatonin Receptor
Autophagy
Mitophagy
Endogenous Metabolite
Apoptosis
PANoptosis
Ligands for Target Protein for PROTAC
Histone Acetyltransferase
Lung Cancer
Breast Cancer
Prostate Cancer
Liver Cancer
Viral Infection
Neurodegenerative Disease
Digestive System Inflammation
SARS-CoV-2 Infection
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149
|
| HY-100573 | Necrosulfonamide |
Necrosulfonamide is a MLKL and Gasdermin D (GSDMD) inhibitor, capable of separately inhibiting necroptosis and pyroptosis of cells. Necrosulfonamide does not affect the activation of upstream signals, but specifically inhibits the downstream executor oligomerization step. Necrosulfonamide reduces the expression of the key kinases NLRP3 and caspase-1 involved in necroptosis and pyroptosis, activate the Nrf2 pathway and the downstream antioxidant enzymes, and also downregulates a variety of inflammatory factors. Necrosulfonamide plays significant roles in various diseases such as neurodegenerative diseases (such as Parkinson’s disease), tissue damage and ischemia-reperfusion injury, inflammatory bowel disease, osteoarthritis and fracture repair, and hair loss by regulating two important programmed necrosis pathways.
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Mixed Lineage Kinase
Necroptosis
Pyroptosis
Caspase
NOD-like Receptor (NLR)
Keap1-Nrf2
TNF Receptor
Interleukin Related
NO Synthase
Heme Oxygenase (HO)
Digestive System Disease
Prostate Cancer
Leukemia/Lymphoma/Myeloma
Depression
Digestive System Inflammation
Cardiovascular Disease
Parkinson's Disease
Obesity
Lung Fibrosis
Rheumatoid Arthritis
|
147
|
| HY-12466 | Z-DEVD-FMK |
Z-DEVD-FMK is a specific and irreversible caspase-3 inhibitor with an IC50 of 18 μM.
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139
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| HY-P1410A | GsMTx4 TFA |
GsMTx4 TFA is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 TFA also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 TFA is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology.
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Neurological, Eye or Ear Disease
Inflammation or Immune System Disease
Blood or Cardio-cerebrovascular Disease
|
135
|
| HY-P1410 | GsMTx4 |
GsMTx4 is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology.
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Neurological, Eye or Ear Disease
Inflammation or Immune System Disease
Blood or Cardio-cerebrovascular Disease
|
135
|
| HY-18723 | Yoda 1 |
Yoda 1 is a potent and selective Piezo1 agonist. Yoda 1 activates purified Piezo1 channels. Yoda 1 potently inhibits macropinocytosis induced by epidermal growth factor (EGF). Yoda 1 enhances Ca2+ influx followed by activation of the calcium-activated potassium channel KCa3.1 and inhibition of Rac1 activation.
|
Pancreatic Cancer
Depression
Pain
Digestive System Inflammation
Cardiovascular Disease
Lung Fibrosis
|
120
|
| HY-12305 | Q-VD-OPh |
|
117
|
|
| HY-101872A | GSK-872 hydrochloride |
GSK-872 hydrochloride is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC50 of 1.8 nM, and inhibits kinase activity with an IC50 of 1.3 nM. GSK-872 hydrochloride decreases the RIPK3-mediated necroptosis and subsequent cytoplasmic translocation and expression of HMGB1, as well as ameliorates brain edema and neurological deficits in early brain injury.
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114
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| HY-101872 | GSK-872 |
GSK-872 is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC50 of 1.8 nM, and inhibits kinase activity with an IC50 of 1.3 nM. GSK-872 decreases the RIPK3-mediated necroptosis and subsequent cytoplasmic translocation and expression of HMGB1, as well as ameliorates brain edema and neurological deficits in early brain injury.
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|
114
|
| HY-19696 | Tauroursodeoxycholate |
Colorectal Cancer
Prostate Cancer
Liver Cancer
Viral Infection
Neurodegenerative Disease
Pain
Digestive System Inflammation
Glucose Metabolism
Obesity
|
111
|
|
| HY-15304 | Dynasore |
Dynasore is a cell-permeable dynamin inhibitor with an IC50 of 15 μM. Dynasore blocks cell migration.
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102
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| HY-L078 | Gut Microbial Metabolite Library |
Accumulating evidence has revealed that intestinal microbiota play an important role in human health and disease, including cardiovascular diseases, inflammatory bowel disease, diabetes, obesity, cancer, and depression, etc. Changes in the composition of gut microbiota associated with disease, referred to as dysbiosis, have been linked to pathologies. Indeed, the gut microbiome functions like an endocrine organ, generating bioactive metabolites which play important roles in human metabolism, health, and disease. Gut microbiome has become a novel therapeutic target for many diseases. Analysis and identification of gut microbial metabolite will contribute to the development of therapeutic methods.
In order to meet the need of gut microbiome research, MCE carefully selected a unique collection of 475 gut microbial metabolites. MCE gut microbial metabolite library is a powerful tool for gut microbiome research and gut microbiome -related drug discovery.
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85
|
| HY-L134 | Anti-Aging Natural Product Library |
Aging is an unavoidable process, leading to cell senescence due to physiochemical changes in an organism. Aging cells cease to divide and drive the progression of illness through various pathways, resulting in the death of an organism ultimately. Anti-aging activities are primarily involved in the therapies of age-related disorders such as Parkinson's Disease (PD), Alzheimer's Disease (AD), cardiovascular diseases, cancer, and chronic obstructive pulmonary diseases.
Natural products are known as effective molecules in anti-aging treatments, which delay the aging process through influencing several pathways and thus ensure an extended lifespan. MCE offers a unique collection of 193 natural products with validated anti-aging activity. MCE anti-aging natural product library is a useful tool for the study of aging-related diseases drugs and pharmacology.
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85
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| HY-L046 | Anti-Cardiovascular Disease Compound Library |
Cardiovascular diseases (CVDs) are a group of disorders of the heart and blood vessels which include coronary heart disease, cerebrovascular disease, peripheral arterial disease, rheumatic heart disease, etc. CVDs are the number 1 cause of death globally. Smoking, unhealthy nutrition, aging population, lack of physical activity, arterial hypertension, or diabetes can promote cardiovascular disease like myocardial infarction or stroke. It is multifactorial and encompasses a multitude of mechanisms, such as eNOS uncoupling, reactive oxygen species formation, chronic inflammatory disorders and abnormal calcium homeostasis. Antioxidant, anti-inflammatory and anti-diabetes agents may reduce the cardiovascular disease risk.
MCE supplies a unique collection of 2,468 compounds with confirmed anti-cardiovascular activity. These compounds mainly target metabolic enzyme, membrane transporter, ion channel, inflammation related signaling pathways. MCE Anti-Cardiovascular Disease Compound Library can be used for cardiovascular diseases related research and high throughput and high content screening for new drugs.
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84
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| HY-L059 | Pyroptosis Compound Library |
Programmed cell death pathways, including apoptosis, pyroptosis and necroptosis, are regulated by unique sets of host proteins that coordinate a variety of biological outcomes. Pyroptosis is a highly inflammatory form of programmed cell death that occurs most frequently upon infection with intracellular pathogens and is likely to form part of the antimicrobial response. This process promotes the rapid clearance of various bacterial, viral, fungal and protozoan infections by removing intracellular replication niches and enhancing the host's defensive responses. Pyroptosis has been widely studied in inflammatory and infection disease models. Recently, there are growing evidences that pyroptosis also plays an important role in the development of cancer, cardiovascular diseases and Metabolic disorder, etc.
MCE designs a unique collection of 2,034 pyroptosis-related compounds mainly focusing on the key targets in the pyroptosis signaling pathway and can be used in the research of pyroptosis signal pathway and related diseases.
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84
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| HY-L060 | Cytoskeleton Compound Library |
The cytoskeleton is responsible for contraction, cell motility, movement of organelles and vesicles through the cytoplasm, cytokinesis, intracellular signal transduction, and many other functions that are essential for cellular homeostasis and survival. It accomplishes these tasks through three basic structures: F-actin, microtubules, and intermediate filaments (IFs). The cytoskeleton is a dynamic structure where the three major filaments and tubules are under the influence of proteins that regulate their length, state of polymerization, and level of cross-linking. Since cytoskeleton is involved in virtually all cellular processes, cytoskeletal protein aberrations are the underlying reason for many pathological phenotypes, including several cardiovascular disease syndromes, neurodegeneration, cancer, liver cirrhosis, pulmonary fibrosis, and blistering skin diseases.
MCE designs a unique collection of 2,313 cytoskeleton-related compounds mainly focusing on the key targets in the cytoskeleton signal pathway and can be used in the research of cytoskeleton signal pathway and related diseases.
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84
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| HY-L180 | Mitophagy Compound Library |
Mitochondrial autophagy refers to the selective encapsulation and degradation of damaged mitochondria by cells through the autophagy mechanism, thereby maintaining mitochondrial and cellular homeostasis. The concept of mitochondrial autophagy has received extensive attention since it was proposed. Current studies have shown that the mechanisms of mitochondrial autophagy can generally be divided into two categories: Ubiquitin-dependent pathways and Ub-independent pathways. In addition, mitochondrial autophagy is a research hotspot related to the pathogenesis of neurodegenerative diseases, cardiovascular diseases, cancer, metabolic diseases and other clinical diseases. Therefore, high-throughput screening based on mitochondrial autophagy can effectively screen out compounds that are closely related to the occurrence of diseases and analyze their mechanisms.
MCE can provide a library of 655 mitophagy compounds, which can be used for drug development and mechanism research in cancer, immunity, infection and other hot research fields.
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84
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| HY-L088 | Angiogenesis-Related Compound Library |
Angiogenesis is the physiological process through which new blood vessels are formed from pre-existing vessels. It occurs in various physiological processes e.g. embryonic development, menstrual cycle, exercise and wound healing etc. Angiogenesis is regulated by both endogenous activators and inhibitors. Some key activators of angiogenesis include vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF), angiogenin, TGF-β, etc. whereas angiogenesis inhibitors are angiostatin, endostatin, interferon, platelet factor 4, etc. The loss of balance between these opposing signals leads to life threatening diseases like cancer, cardiovascular and ischemic diseases etc. which are thus controlled by exogenous angiogenesis activators (for cardiovascular/ischemic disorders) and inhibitors (for cancer).
MCE offers a unique collection of 3,660 compounds with validated angiogenesis targets modulating properties. MCE angiogenesis-related compound library is an effective tool for angiogenesis research and discovery of angiogenesis-related drugs.
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83
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| HY-L119 | Potassium Channel Compound Library |
Potassium channels are the most widely distributed type of ion channel and are found in virtually all living organisms. There are four major classes of K channels: voltage-gated potassium channel, calcium-activated potassium channel, inwardly rectifying potassium channel and tandem pore domain potassium channel. There is growing evidence that dysfunction in potassium channels correlates with several diseases, such as chronic hypertension, diabetes, hypercholesterolemia and atherosclerosis, etc.
MCE Potassium Channel Compound Library consists of 337 potassium channel inhibitor and activators, which is a useful tool to discover drugs for cardiovascular diseases and potassium channel research.
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83
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| HY-L155 | Mitochondrial Toxicity Compound Library |
Mitochondria, as the main place of energy supply in life, is essential to maintain normal life activities. Mitochondrial dysfunction is associated with common diseases, such as cardiovascular diseases, neurodegenerative diseases, diabetes and cancer. The heart, brain and liver rely heavily on mitochondrial function as the main organs for drug metabolism. In addition, mitochondria is also a target of many drugs, some of which induce organotoxicity by inducing mitochondrial toxicity.
MCE contains 545 mitochondrial toxic compounds, which can be used as tool compounds for drug development and disease mechanism research.
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83
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| HY-L174 | Macrophage Related Compound Library |
Macrophages are effector cells of the innate immune system, engulfing bacteria and secreting pro-inflammatory and antibacterial mediators. They are an important component of the first line defense against pathogens and tumor cells. In addition, macrophages play an important role in eliminating damaged cells through programmed cell death. Like all immune cells, macrophages originate from pluripotent hematopoietic stem cells in the bone marrow. Macrophages play key functions in many physiological processes beyond homeostasis and innate immunity, including metabolic function, cell debris clearance, tissue repair, and remodeling. In order to fulfill their different functional roles, macrophages can polarize into a series of phenotypes, including classic (pro inflammatory, M1) and alternative (anti-inflammatory, healing promoting, M2) activation states, as well as a wide range of regulatory phenotypes and subtypes. Macrophages exist in all vertebrate tissues and have a dual function in host protection and tissue damage, maintaining a good balance.
MCE designs a unique collection of 276 macrophage related compounds. It is a good tool to be used for research on Inflammation, cancer and other diseases.
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83
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| HY-L175 | Inflammasomes related Compound Library |
Inflammasomes are classic pattern recognition receptors for natural immune responses. Inflammasomes are polymeric protein complexes that regulate inflammatory responses and pyrolytic cell death, thereby exerting the host's defense against microorganisms. Inflammasomes sensors are associated with adapter proteins, activating inflammatory caspase-1, releasing inflammatory cytokines and inducing cell death, endowing the host with defense against pathogens. NLRP1, NLRP3, NLRC4, AIM2, and pyrin are considered typical inflammasomes because they convert cysteine asparaginase-1 into catalytically active capsaicin-1. In addition to infectious diseases, the importance of inflammasomes is also related to various clinical diseases, such as autoimmune diseases, neurodegeneration and metabolic disorders, and the development of cancer. Therefore, it is necessary to strictly regulate the activation and function of inflammasomes to avoid accidental host tissue damage while inducing pathogens to kill the inflammatory response.
MCE designs a unique collection of 178 inflammasomes related compounds. It is a good tool to be used for research on Inflammation, cancer and other diseases.
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83
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| HY-L261 | Classic FDA-Approved Drug Library |
MCE Classic FDA-Approved Drug Library features a curated selection of marketed drugs that have achieved the highest prescription volumes and greatest clinical impact in global practice since 2006. The collection covers eight major therapeutic areas, including cardiovascular diseases, oncology, metabolic disorders, infectious diseases, central nervous system disorders, respiratory diseases, digestive system diseases, and immunological conditions. All compounds have been validated through long‑term clinical use and possess well‑defined molecular targets, well‑established pharmacokinetic properties, quantifiable efficacy endpoints, and comprehensive toxicological safety profiles.
The library currently contains 167 representative drugs and is designed to serve as an efficient tool for drug repurposing, phenotypic screening, mechanism‑of‑action studies, and combination therapy strategy development.
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83
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| HY-L263 | Energy Metabolites Library |
Energy metabolism is the most fundamental biochemical process in living organisms, encompassing glycolysis, the TCA cycle, oxidative phosphorylation, the pentose phosphate pathway, and fatty acid oxidation. These core pathways directly regulate cell survival, proliferation, differentiation, and apoptosis. Dysregulation of energy metabolism is closely linked to major diseases including cancer, diabetes, obesity, cardiovascular diseases, neurodegenerative disorders, and ischemia‑reperfusion injury. Targeting these metabolic pathways has become a frontier in drug discovery and mechanistic research.
The MCE Energy Metabolite Compound Library features 89 structurally defined small‑molecule compounds. It covers energy substrates, pathway intermediates, coenzymes and redox carriers, nucleotide derivatives, and microenvironmental modulators. This library is applicable to research areas including tumor metabolism, insulin resistance, mitochondrial dysfunction, oxidative stress, neuroprotection, and cardiometabolic diseases, providing a high‑quality tool for mechanistic studies, biomarker discovery, and high‑throughput drug screening.
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83
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| HY-13755 | Sulforaphane |
Sulforaphane is an orally active inducer of the Keap1/Nrf2/ARE pathway. Sulforaphane promotes the transcription of tumor-suppressing proteins and effectively inhibits the activity of HDACs. Through the activation of the Keap1/Nrf2/ARE pathway and further induction of HO-1 expression, Sulforaphane protects the heart. Sulforaphane suppresses high glucose-induced pancreatic cancer through AMPK-dependent signal transmission. Sulforaphane exhibits both anticancer and anti-inflammatory properties.
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79
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| HY-B1081A | Oxidopamine hydrobromide |
Oxidopamine (6-OHDA) hydrobromide is an antagonist of the neurotransmitter dopamine. Oxidopamine hydrobromide is a widely used neurotoxin and selectively destroys dopaminergic neurons. Oxidopamine hydrobromide promotes COX-2 activation, leading to PGE2 synthesis and pro-inflammatory cytokine IL-1β secretion. Oxidopamine hydrobromide can be used for the research of Parkinson’s disease (PD), attention-deficit hyperactivity disorder (ADHD), and Lesch-Nyhan syndrome.
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Dopamine Receptor
Autophagy
Mitophagy
COX
PGE synthase
Interleukin Related
p38 MAPK
Apoptosis
Caspase
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50
|
| HY-14622A | Necrostatin 2 racemate |
Necrostatin 2 racemate (Nec-1S), the Necrostatin-1 (HY-15760) stable, is a potent and specific RIPK1 inhibitor lacking the IDO-targeting effect.
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39
|
| HY-14654 | Aspirin |
Aspirin (Acetylsalicylic acid) is an orally active, potent and irreversible inhibitor of cyclooxygenase COX-1 and COX-2, with IC50 values of 5 and 210 μg/mL, respectively. Aspirin induces apoptosis. Aspirin inhibits the activation of NF-κB. Aspirin also inhibits platelet prostaglandin synthetase, and can prevent coronary artery and cerebrovascular thrombosis.
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Breast Cancer
Colorectal Cancer
Prostate Cancer
Liver Cancer
Leukemia/Lymphoma/Myeloma
Pancreatic Cancer
Ovarian Cancer
Viral Infection
Neurodegenerative Disease
Depression
Pain
Digestive System Inflammation
Cardiovascular Disease
Non-Small Cell Lung Cancer
SARS-CoV-2 Infection
Obesity
Rheumatoid Arthritis
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38
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| HY-141511 | Coppersensor 1 |
Coppersensor-1 (CS1) is a membrane-permeable fluorescent dye. Coppersensor-1 has a picomolar affinity for Cu+ with high selectivity over competing cellular metalions. Coppersensor-1 as a probe, can selective and sensitive detection of copper(I) ions (Cu+) in biological samples, including live cells. Coppersensor-1 can be used for the research of imaging of severe diseases such as cancer, cardiovascular disorders and neurogenerative diseases.
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37
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| HY-W018746 | EDTA disodium |
EDTA disodium salt, also known as ethylenediaminetetraacetic acid disodium, belongs to the chelating agent category, which is formed by chelating a central metal ion with four carboxylate groups and two amine groups. This compound, with its ability to bind and chelate metal ions such as calcium, magnesium and iron, is commonly used in a variety of applications, including industrial, medical and research settings. It is used as a preservative in food and beverage, as a stabilizer in medicine, as a chelating agent in water treatment, and as a reagent in biochemical and biomedical research. In addition, EDTA disodium salt has been studied for potential research effects such as improving heavy metal poisoning and cardiovascular disease.
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31
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| HY-13863 | Hydroxy-Dynasore |
Hydroxy Dynasore (Dyngo-4a), a structural mimetic analog of Dynasore (HY-15304), is an improved, less cytotoxic and versatile dynamin inhibitor with IC50 values of 0.38 μM and 2.3 μM for brain recombinant dynamin I and recombinant mouse dynamin II, respectively. Hydroxy Dynasore inhibits dynamin-dependent transferrin endocytosis with an IC50 of 5.7 μM.
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18
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| HY-126010 | Dooku1 |
Dooku1 is a reversibly Yoda1 antagonist with IC50 value of 1.3 μM and 1.5 μM for 2 μM Yoda1-induced Ca2+ entry HEK 293 cells and HUVECs, respectively. Dooku1 can disrupt Yoda1-induced Piezo1 channel activity and inhibit Yoda1-induced relaxation of aorta. Dooku1 can be used for vascular physiology and disease research.
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17
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| HY-15594A | Phen-DC3 Trifluoromethanesulfonate |
Phen-DC3 Trifluoromethanesulfonate is a bisquinolinium G-quadruplex (G4) ligand. Phen-DC3 Trifluoromethanesulfonate selectively binds to and stabilizes the hybrid quadruplex-duplex hybrid (QDH) derived from the PIM1 promoter. Phen-DC3 Trifluoromethanesulfonate also binds to the c-myc promoter Pu24T G4 via extensive π-stacking, and induces polymerase stalling at α-synuclein DNA and RNA G4 sequences. Phen-DC3 Trifluoromethanesulfonate downregulates LPS (HY-D1056)-induced TNFRSF21, RIPK3 and p-MLKL in VECs, and ameliorates CLP-induced pulmonary vascular leakage in septic rats. Phen-DC3 Trifluoromethanesulfonate can be used in studies related to neurodegenerative diseases and sepsis-associated vascular injury.
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12
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| HY-113046 | 5-Methyltetrahydrofolic acid |
5-Methyltetrahydrofolic acid (5-Methyl THF) is the main circulating form of folic acid in the body and is involved in a variety of biochemical reactions. 5-Methyltetrahydrofolic acid regulates cardiovascular function by increasing the production of endothelin-1 (ET-1) in low-density lipoprotein-treated endothelial cells and can be used in the study of cardiovascular diseases.
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12
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| HY-N0935 | Ligustrazine hydrochloride |
Ligustrazine hydrochloride (Chuanxiongzine hydrochloride) is an orally active, blood-brain barrier-permeable alkaloid. It can be isolated from Ligusticum striatum DC. Ligustrazine hydrochloride reduces ROS, upregulates the levels of p-Akt/Akt and p-eNOS/eNOS, and decreases ALT and AST. It inhibits glutamate excitotoxicity, calcium overload, oxidative stress, ischemia-reperfusion injury and atherosclerotic plaque progression, enhances synaptic plasticity, and improves neurological function, cerebral infarct volume and brain water content. Ligustrazine hydrochloride possesses anti-inflammatory, antioxidant, lipid-lowering, endothelial protective and hepatoprotective activities. It can be used in studies related to ischemic stroke, cerebral ischemia-reperfusion injury and atherosclerosis.
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Cerebrovascular Disease
Lipid Metabolism
Ischemia-Reperfusion Injury
Atherosclerosis and Inflammation
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11
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| HY-N0264 | Ligustrazine |
Ligustrazine (Chuanxiongzine) is an orally active, blood-brain barrier-permeable alkaloid. It can be isolated from Ligusticum striatum DC. Ligustrazine reduces ROS, upregulates the levels of p-Akt/Akt and p-eNOS/eNOS, and decreases ALT and AST. It inhibits glutamate excitotoxicity, calcium overload, oxidative stress, ischemia-reperfusion injury and atherosclerotic plaque progression, enhances synaptic plasticity, and improves neurological function, cerebral infarct volume and brain water content. Ligustrazine possesses anti-inflammatory, antioxidant, lipid-lowering, endothelial protective and hepatoprotective activities. It can be used in studies related to ischemic stroke, cerebral ischemia-reperfusion injury and atherosclerosis.
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Cerebrovascular Disease
Lipid Metabolism
Ischemia-Reperfusion Injury
Atherosclerosis and Inflammation
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11
|
| HY-N0124 | Dioscin |
Dioscin (CCRIS 4123; Collettiside III) is a natural plant-derived steroidal saponin that has good anti-cancer activity against a variety of cancer cells. Dioscin causes DNA damage and induces apoptosis in HeLa and SiHa cells. Dioscin regulates ROS-mediated DNA damage and mitochondrial signaling pathways, exerting anticancer activity.
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11
|
| HY-100339 | GSK583 |
GSK583 is a highly potent, orally active and selective inhibitor of RIP2 Kinase, with IC50 of 5 nM. GSK583 inhibits both TNF-α and IL-6 production with an IC50 value of 200 nM.
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9
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| HY-N1441 | Afzelin |
Afzelin (Kaempferol-3-O-rhamnoside)It is a flavonol glycoside that has anti-inflammatory, anti-oxidative stress response, anti-apoptotic, and anti-cardiac cytotoxic effects. AfzelinIt can reduce mitochondrial damage, enhance mitochondrial biosynthesis, and reduce mitochondria-related proteins. Parkinand PTENinduced putative kinase 1 (putative kinase 1)s level. AfzelinCan be improved D-galactosamine(GalN)/LPSSurvival rate of mice treated with doxorubicin prophylaxis (HY-15142A)Induced cardiotoxicity and scopolamine (HY-N0296)-induced neurological injury. AfzelinAlso inhibits asthma and allergies caused by ovalbumin.
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Pancreatic Cancer
Bacterial Infection
Pain
Digestive System Inflammation
Cardiovascular Disease
Parkinson's Disease
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8
|
| HY-N0703 | Schaftoside |
Cancer
Digestive System Disease
Pain
Digestive System Inflammation
Parkinson's Disease
Obesity
Rheumatoid Arthritis
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8
|
|
| HY-144828 | RIP1/RIP3/MLKL activator 1 |
RIP1/RIP3/MLKL activator 1 (Compound 6i) is a potent anti-glioma agent. RIP1/RIP3/MLKL activator 1 induces necroptosis through RIP1/RIP3/MLKL pathway. RIP1/RIP3/MLKL activator 1 exerts acceptable BBB permeability.
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7
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| HY-108749 | Olive oil |
Olive oil (Cropure OL) is an oleaginous compound found in the fruit of the Olea europaea tree. Olive oil contains many phenolic components and exerts antioxidant activity. Olive oil exhibits hydroxyl radical scavenging, platelet aggregation inhibition and xanthine oxidase inhibitory activity. Olive oil can promote wound healing and relieve inflammation. Olive oil can be used for the research of inflammation, cancer, metabolic and cardiovascular disease, such as diabetic foot ulcers and inflammatory bowel disease.
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Cancer
Blood or Cardio-cerebrovascular Disease
Metabolic or Endocrine Disease
Inflammatory Bowel Disease
|
7
|
| HY-N0417 | Cucurbitacin E |
Cucurbitacin E is a CDK1 inhibitor that significantly inhibits the activity of the cyclin B1/CDC2 complex. Cucurbitacin E also induces PANoptosis in adrenocortical carcinoma cells in a ZBP1-dependent manner. Cucurbitacin E exhibits synergistic effects with Mitotane (HY-13690); when used in combination, they effectively eliminate tumors.
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Breast Cancer
Leukemia/Lymphoma/Myeloma
Ovarian Cancer
Glucose Metabolism
Experimental Autoimmune Encephalomyelitis
Experimental Autoimmune Encephalomyelitis
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6
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| HY-P1410C | D-GsMTx4 TFA |
D-GsMTx4 TFA is a spider peptide and the D enantiomer of GsMTx4 (HY-P1410). D-GsMTx4 TFA inhibits the mechanosensitive ion channel Piezo2. D-GsMTx4 TFA inhibits [Ca2+]i elevation. D-GsMTx4 TFA inhibits mTOR and PI3K-Akt signaling pathways. D-GsMTx4 TFA inhibits mechanical allodynia and thermal hyperalgesia. D-GsMTx4 TFA can be used in researches of mechanical stress, chronic pain and idiopathic pulmonary fibrosis.
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Neurological, Eye or Ear Disease
Inflammation or Immune System Disease
Blood or Cardio-cerebrovascular Disease
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6
|
| HY-P1410B | D-GsMTx4 |
D-GsMTx4 is a spider peptide and the D enantiomer of GsMTx4 (HY-P1410). D-GsMTx4 inhibits the mechanosensitive ion channel Piezo2. D-GsMTx4 inhibits [Ca2+]i elevation. D-GsMTx4 inhibits mTOR and PI3K-Akt signaling pathways. D-GsMTx4 inhibits mechanical allodynia and thermal hyperalgesia. D-GsMTx4 can be used in researches of mechanical stress, chronic pain and idiopathic pulmonary fibrosis.
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Neurological, Eye or Ear Disease
Inflammation or Immune System Disease
Blood or Cardio-cerebrovascular Disease
|
6
|
| HY-N6712 | Thiolutin |
Thiolutin (Acetopyrrothin) is a sulfur-containing antibiotic, which is a potent inhibitor of bacterial and yeast RNA polymerases. Thiolutin can be produced by Streptomyces. Thiolutin inhibits AMSH (IC50 = 4 μM) and Rpn11 (IC50 = 0.53 μM). Thiolutin is a dual inhibitor of BRCC36 and the NLRP3 inflammasome, exhibiting anti-inflammatory effects. Thiolutin effectively suppresses the interaction between BRCC36 and HMGCR, leading to the inhibition of HCC growth. Thiolutin attenuates pyroptosis and NLRP3 inflammasome activation. Thiolutin markedly alleviates renal injury and inflammatory process in IgAN. Thiolutin is an anti-angiogenic compound which can ease Doxorubicin-induced cardiotoxicity (DOXIC).
Source: Streptomyces |
Antibiotic
Bacterial
Deubiquitinase
NOD-like Receptor (NLR)
DNA/RNA Synthesis
Pyroptosis
HMG-CoA Reductase (HMGCR)
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4
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| HY-N6779 | Patulin |
Patulin (Terinin) is a mycotoxin produced by fungi including the Aspergillus, Penicillium, and Byssochlamys species, causes chromosome breakage, mutation, teratogenic and cytotoxic. Patulin induces autophagy-dependent apoptosis through lysosomal-mitochondrial axis, and causes DNA damage.
Source: Penicillium and Aspergillus |
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4
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| HY-139109 | IR-783 |
IR-783 (ADS 780WS) is a heptamethine cyanine dye. IR-783 induces Mitochondrial membrane potential loss, ATP depletion, mitochondrial permeability transition pore opening, Cytochrome c release and Apoptosis in breast cancer cells. IR-783 promotes the translocation of Drp1 from the cytosol to mitochondria. IR-783 increases the expression of mitochondrial fission proteins such as MFF and Fission-1. IR-783 possesses imaging, cancer-targeting and anticancer properties. IR-783 exerts anticancer effects against breast cancer. IR-783 can be used in breast cancer-related research.
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4
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| HY-N0385 | Gomisin J |
Gomisin J is a Schisandra chinensis-derived lignan that can inhibit multiple targets such as eNOS, AMPK (LKB1, CaMKIIβ), fetuin-A, NF-κB, Nrf2/HO-1, and can pass through the blood-brain barrier. Gomisin J increases NO bioavailability by activating eNOS, regulates lipid metabolism by activating the AMPK pathway, inhibits fetuin-A and NF-κB to exert anti-inflammatory effects, and activates Nrf2/HO-1 to enhance antioxidant capacity. Gomisin J has the activities of anti-hypertension, regulating liver lipid metabolism, and reducing cerebral ischemia-reperfusion injury, and can be used for research on hypertension, non-alcoholic fatty liver disease, cerebral ischemia-reperfusion injury, etc.
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Breast Cancer
Prostate Cancer
Liver Cancer
Leukemia/Lymphoma/Myeloma
Pancreatic Cancer
Ovarian Cancer
Depression
Pain
Ischemia-Reperfusion Injury
Nonalcoholic Steatohepatitis
Hypertension
Obesity
Lung Fibrosis
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3
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| HY-N1431 | Tabersonine |
Tabersonine is a selective, orally active NLRP3 inhibitor. Tabersonine directly binds to the NACHT domain of NLRP3, inhibiting its ATPase activity and oligomerization, thereby blocking ASC spot formation and caspase-1 activation, and reducing the release of pro-inflammatory cytokines such as IL-1β. Tabersonine also inhibits K63-linked ubiquitination of TRAF6, blocking NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. Tabersonine can inhibit inflammatory responses, induce apoptosis of liver cancer cells through mitochondrial pathways and death receptor pathways, reduce mitochondrial membrane potential, promote cytochrome c release, and activate caspase proteins. Tabersonine is mainly used in the study of NLRP3-driven inflammatory diseases (such as acute lung injury, sepsis, peritonitis) and tumors such as liver cancer.
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NOD-like Receptor (NLR)
NF-κB
CDK
p38 MAPK
Cytochrome P450
Akt
Interleukin Related
Apoptosis
PI3K
Caspase
Lung Cancer
Breast Cancer
Colorectal Cancer
Prostate Cancer
Gastric Cancer
Liver Cancer
Leukemia/Lymphoma/Myeloma
Pancreatic Cancer
Ovarian Cancer
Neurodegenerative Disease
Depression
Pain
Digestive System Inflammation
Obesity
Lung Fibrosis
Rheumatoid Arthritis
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3
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| HY-P1032 | Angiotensin I (human, mouse, rat) |
Angiotensin I is a decapeptide hormone. Angiotensin I is the precursor of Angiotensin II (HY-13948). Angiotensin I can be used in the study of cardiovascular diseases such as hypertension and vasospasm.
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3
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| HY-126741 | Azadirachtin |
Azadirachtin is an oral active triterpenoid compound with anticancer, antimalarial, anti-inflammatory, and insecticidal activities. Azadirachtin induces cell apoptosis through the mitochondrial pathway (by inhibiting Bcl-2/Bax ratio or activating Apaf-1 and caspase-3) or through death receptors (by inhibiting TNFR activation). Additionally, Azadirachtin exerts its anti-inflammatory effects by inhibiting NF-кB signaling pathway activation, and it exhibits insecticidal activity by inducing apoptosis in insect cells.
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Breast Cancer
Prostate Cancer
Liver Cancer
Leukemia/Lymphoma/Myeloma
Pancreatic Cancer
Ovarian Cancer
Parasitic Infection
Depression
Pain
Digestive System Inflammation
Obesity
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3
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| HY-P1723A | Spexin TFA |
Spexin (Neuropeptide Q) TFA is a selective agonist of galanin receptors GAL2 and GAL3, and is a conserved peptide that functions as a neurotransmitter/neuromodulator and endocrine factor. Spexin TFA can function through both central and peripheral actions. Spexin TFA upregulates Beclin 1 to inhibit ferroptosis induced by excessive autophagy, reduces the uptake of long-chain fatty acids by adipocytes, and regulates energy metabolism by increasing lipid oxidation (e.g., reducing the respiratory exchange ratio in rodents). Spexin TFA improves cardiac function in the Doxorubicin hydrochloride (HY-15142)-induced cardiotoxicity model, protects mitochondrial membrane potential, and reduces iron accumulation and lipid peroxidation. Spexin TFA can be used to study obesity and its related metabolic disorders, cardiovascular diseases (e.g., cardioprotection), and side effects of tumor chemotherapy.
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2
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| HY-P4911 | SDF-1α (human) |
SDF-1α (human) is a mononuclear cells chemoattractant that can bind to CXCR4. SDF-1α plays a central role in stem cell homing, retention, survival, proliferation, cardiomyocyte repair, angiogenesis and ventricular remodelling following myocardial infarction. SDF-1α (human) can be used in cardiovascular disease research.
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2
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| HY-W014841 | Sodium hippurate, 98% |
Sodium hippurate, 98% is an orally active metabolite. Sodium hippurate, 98% can be produced by intestinal microorganisms from the metabolism of polyphenols, benzoic acid. Sodium hippurate, 98% decreases NRF2, MMP9 and leads to ROS accumulation. Sodium hippurate, 98% activates TGFβ/SMAD signaling. Sodium hippurate, 98% improves hyperuricemia and colitis. Sodium hippurate, 98% can also be used in cardiovascular disease research.
.
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Metabolic or Endocrine Disease
Colorectal Cancer
Liver Cancer
Pancreatic Cancer
Ovarian Cancer
Pain
Cardiovascular Disease
Lung Fibrosis
Rheumatoid Arthritis
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2
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| HY-P1723 | Spexin |
Spexin (Neuropeptide Q) is a selective agonist of galanin receptors GAL2 and GAL3, and is a conserved peptide that functions as a neurotransmitter/neuromodulator and endocrine factor. Spexin can function through both central and peripheral actions. Spexin upregulates Beclin 1 to inhibit ferroptosis induced by excessive autophagy, reduces the uptake of long-chain fatty acids by adipocytes, and regulates energy metabolism by increasing lipid oxidation (e.g., reducing the respiratory exchange ratio in rodents). Spexin improves cardiac function in the Doxorubicin hydrochloride (HY-15142)-induced cardiotoxicity model, protects mitochondrial membrane potential, and reduces iron accumulation and lipid peroxidation. Spexin can be used to study obesity and its related metabolic disorders, cardiovascular diseases (e.g., cardioprotection), and side effects of tumor chemotherapy.
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2
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| HY-P4911A | SDF-1α (human) TFA |
SDF-1α (human) TFA is a mononuclear cells chemoattractant that can bind to CXCR4. SDF-1α plays a central role in stem cell homing, retention, survival, proliferation, cardiomyocyte repair, angiogenesis and ventricular remodelling following myocardial infarction. SDF-1α (human) TFA can be used in cardiovascular disease research.
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2
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| HY-N1990 | Gypenoside XLIX |
Gypenoside XLIX is a multifunctional bioactive compound that can be isolated from Gynostemma pentaphyllum, with a Ka value of 1.58 μM for its binding to SIRT1. Gypenoside XLIX acts as a PPAR-α agonist. It inhibits the activation of TLR4-mediated NF-κB signaling pathway by activating the Sirt1/Nrf2 signaling pathway, reduces ROS accumulation, and alleviates hepatic inflammatory injury in mice with sepsis-induced liver disease. Gypenoside XLIX targets SIRT1 to block YAP-NLRP3 activation and improve sepsis-induced cardiomyopathy. Gypenoside XLIX inhibits apoptosis (Apoptosis), pyroptosis (Pyroptosis), autophagy (Autophagy), lipid peroxidation, pro-inflammatory cytokines and anti-inflammatory cytokines. Gypenoside XLIX alleviates sepsis-induced splenic injury by inhibiting inflammation and oxidative stress, and mitigates sepsis-associated encephalopathy by targeting PPAR-α. Gypenoside XLIX prevents acute kidney injury by inhibiting IGFBP7/IGF1R-mediated programmed cell death and inflammation. Gypenoside XLIX inhibits the expression and activity of vascular cell adhesion molecule-1 in cytokine-induced human endothelial cells. Gypenoside XLIX is applicable to research related to acute liver injury, lung injury, cardiomyopathy, acute splenic injury, sepsis-associated encephalopathy, acute kidney injury, atherosclerosis and chronic inflammation.
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PPAR
Sirtuin
Keap1-Nrf2
Toll-like Receptor (TLR)
NF-κB
Reactive Oxygen Species (ROS)
NOD-like Receptor (NLR)
Apoptosis
Pyroptosis
Autophagy
Neurological, Eye or Ear Disease
Atherosclerosis and Inflammation
Acute Lung Injury
Cardiomyopathy
Liver Injury
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2
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| HY-N0745 | Senkyunolide I |
Senkyunolide I is an orally active, blood-brain barrier-permeable metabolite of Z-ligustilide (HY-N0401A). Senkyunolide I is isolated from Ligusticum chuanxiong. Senkyunolide I upregulates p-Erk1/2 and Nrf2/HO-1, and inhibits Caspase 3. Senkyunolide I alleviates Apoptosis. Senkyunolide I increases the pain threshold in mice and reduces acetic acid-induced writhing responses in mice. Senkyunolide I improves neurological deficits, reduces infarct volume and alleviates cerebral edema in rats with focal cerebral ischemia-reperfusion injury. Senkyunolide I protects renal function and structural integrity in a mouse model of renal ischemia-reperfusion injury. Senkyunolide I is applicable to research related to focal cerebral ischemia-reperfusion injury, migraine, and renal ischemia-reperfusion injury.
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2
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| HY-N0353 | Curdione |
Curdione ((+)-Curdione) is an orally active sesquiterpenoid. Curdione inhibits platelet aggregation. Curdione induces ferroptosis in colorectal cancer via m6A methylation mediated by METTL14 and YTHDF2. Curdione inhibits ferroptosis in Isoproterenol (HY-B0468)-induced myocardial infarction by regulating the Keap1/Trx1/GPX4 signaling pathway, suppressing oxidative stress (ROS) and apoptosis. Curdione ameliorates Doxorubicin (HY-15142)-induced cardiotoxicity by inhibiting oxidative stress (ROS) and activating the Nrf2/HO-1 pathway. Curdione ameliorates sepsis-induced lung injury by inhibiting platelet-mediated neutrophil extracellular trap formation. Curdione ameliorates Bleomycin (HY-17565A)-induced pulmonary fibrosis by inhibiting TGF-β-induced fibroblast-to-myofibroblast differentiation. Curdione exhibits neuroprotective effects against focal cerebral ischemia-reperfusion injury in rats. Curdione exerts antiproliferative effects against human uterine leiomyosarcoma by targeting IDO1. Curdione protects vascular endothelial cells and atherosclerosis by regulating DNMT1-mediated ERBB4 promoter methylation. Curdione inhibits inducible prostaglandin E2 production (IC50 = 1.1 μM) and cyclooxygenase 2 expression.
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Ferroptosis
Apoptosis
Reactive Oxygen Species (ROS)
Autophagy
Glutathione Peroxidase
Keap1-Nrf2
Heme Oxygenase (HO)
TGF-β Receptor
Indoleamine 2,3-Dioxygenase (IDO)
Colorectal Cancer
Pancreatic Cancer
Digestive System Inflammation
Cardiovascular Disease
Parkinson's Disease
Lung Fibrosis
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2
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| HY-131018 | Jedi2 |
Jedi2 is a Piezo1 activator, but not a specific Piezo2 activator. Jedi2 binds to the mouse Piezo1 proteins with a Kd of 2770??μM.
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2
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| HY-B0339 | Primidone |
Primidone is the orally active inhibitor for TRPM3 (IC50 = 0.6 μM), RIP kinase and voltage-gated sodium channel, and the antagonist for GABA receptor. Primidone can be used as the analgesic and anticonvulsant agent.
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Digestive System Disease
Pain
Digestive System Inflammation
SARS-CoV-2 Infection
Alzheimer's Disease
Parkinson's Disease
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2
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| HY-108801A | Aflibercept (VEGF Trap) |
Aflibercept (VEGF Trap) is a soluble decoy VEGFR constructed by fusing the Ig domains of VEGFR1 and VEGFR2 with the Fc region of human IgG1. Aflibercept inhibits VEGF signaling by reducing VEGF-regulated processes. Aflibercept can be used for thr research of age-related macular degeneration (AMD) and cardiovascular disease.
Species: Human |
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2
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| HY-108801 | Aflibercept |
Aflibercept is a soluble decoy VEGFR constructed by fusing the Ig domains of VEGFR1 and VEGFR2 with the Fc region of human IgG1. Aflibercept inhibits VEGF signaling by reducing VEGF-regulated processes. Aflibercept can be used for thr research of age-related macular degeneration (AMD) and cardiovascular disease.
Species: Human |
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2
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| HY-125918 | Bleomycin A5 hydrochloride |
Bleomycin A5 (Pingyangmycin) hydrochloride is a glycopeptide antibiotic with multiple biological activities, which can be isolated from Streptomyces. Bleomycin A5 hydrochloride exerts cytotoxic effects by binding to Fe2+ to form a complex, inducing single-strand and double-strand DNA breaks, and inhibiting DNA replication. Bleomycin A5 hydrochloride inhibits Drp1-mediated mitochondrial fission and suppresses PINK1/Parkin pathway-mediated mitophagy, ultimately triggering mitochondria-mediated cellular apoptosis. Bleomycin A5 hydrochloride can be used in cancer research.
Source: Streptomyces verticillus var |
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1
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| HY-13315S | Montelukast-d6 |
Montelukast-d6 is the deuterium labeled Montelukast (sodium). Montelukast sodium is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (Cysltr1). Montelukast sodium can be used for the reseach of asthma and liver injury. Montelukast sodium also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage.
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1
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| HY-13315S1 | Montelukast-d6 sodium |
Montelukast-d6 (sodium) is the deuterium labeled Montelukast (sodium). Montelukast sodium is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (Cysltr1). Montelukast sodium can be used for the reseach of asthma and liver injury. Montelukast sodium also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage.
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1
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| HY-P99121 | Anti-Mouse/Human CD11b Antibody (M1/70) |
Anti-Mouse/Human CD11b Antibody (M1/70) is an anti-mouse CD11b IgG2b monoclonal antibody. Anti-Mouse/Human CD11b Antibody (M1/70) can significantly inhibit the adhesion between dendritic cells (DCs) and platelets. Anti-Mouse/Human CD11b Antibody (M1/70) can kill ovarian cancer cells and inhibit their migration. Anti-Mouse/Human CD11b Antibody (M1/70) can alleviate renal fibrosis and inflammation. Anti-Mouse/Human CD11b Antibody (M1/70) can be used for researches on inflammation conditions and cancer such as ischemia-reperfusion injury (IRI), thrombotic inflammatory conditions and ovarian cancer.
Species: Mouse |
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1
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| HY-N8572 | 3',4'-Dimethoxyflavone |
3',4'-Dimethoxyflavone is a lipophilic flavone, can be isolated from the leaves of Primula veris. 3',4'-Dimethoxyflavone can reduce the synthesis and accumulation of PARP and protect cortical neurones against cell death induced by Parthanatos. 3',4'-Dimethoxyflavone is also an aryl hydrocarbon receptor antagonist in human breast cancer cells. 3',4'-Dimethoxyflavone can promote the proliferation of human hematopoietic stem cells. 3',4'-Dimethoxyflavone has various biological activities, including antioxidant, anti-cancer, anti-inflammatory, anti-atherogenic, hypolipidaemic, and neuroprotective or neurotrophic effects.
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Neurological, Eye or Ear Disease
Inflammation or Immune System Disease
Breast Cancer
Pancreatic Cancer
Ovarian Cancer
Cardiovascular Disease
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1
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| HY-W329357 | 15:0 Lyso PC |
15:0 Lyso PC is a lysophosphatidylcholine (Lyso PC), a product of phospholipase A2 (PLA2) hydrolysis of phosphatidylcholine (PC) and is involved in cell membrane remodeling and inflammatory signaling. 15:0 Lyso PC demonstrates significant lipid metabolism disturbances in the serum with ischemic heart disease (IHD) and ischemic cardiomyopathy (ICM). 15:0 Lyso PC can be used as a lipid biomarker for cardiovascular disease.
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1
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| HY-N10470 | Bleomycin A5 |
Bleomycin A5 (Pingyangmycin) is a glycopeptide antibiotic with multiple biological activities, which can be isolated from Streptomyces. Bleomycin A5 exerts cytotoxic effects by binding to Fe2+ to form a complex, inducing single-strand and double-strand DNA breaks, and inhibiting DNA replication. Bleomycin A5 inhibits Drp1-mediated mitochondrial fission and suppresses PINK1/Parkin pathway-mediated mitophagy, ultimately triggering mitochondria-mediated cellular apoptosis. Bleomycin A5 can be used in cancer research.
Source: Penicillium avellaneum |
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1
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| HY-162501 | Yaddle1 |
Yaddle1 is an agonist of the mechano-activated ion channel (Piezo1) with a half-maximal effective concentration (MEC50) of 0.40 μM. Yaddle1 can significantly trigger Ca2+ inflow in T cells and induce T cell activation response. Yaddle1 can be used in the study of vaccine adjuvants.
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1
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| HY-17609 | Difelikefalin |
Difelikefalin (CR-845; FE-202845) is an orally active peripherally acting kappa opioid receptor agonist. Difelikefalin reduces acute kidney injury, decreases oliguria, maintains urine flow, inhibits cytokine expression, and improves survival in endotoxemia after ischemia/reperfusion. Difelikefalin suppresses pruritus signals and exhibits neuromodulatory antipruritic activity. Difelikefalin can be used in research related to acute kidney injury, chronic kidney disease-associated pruritus, and atopic dermatitis.
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1
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| HY-W250116 | Co(III) protoporphyrin IX chloride |
Co(III) protoporphyrin IX chloride (Protoporphyrin IX cobaltic chloride) is an inducer of HO-1. Co(III) protoporphyrin IX chloride has activities such as anti-inflammation and antibacterial properties. Co(III) protoporphyrin IX chloride can also be used in the research of ischemia-reperfusion injury models.
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1
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| HY-107545 | Dynole 34-2 |
Dynole 34-2 is a potent dynamin GTPase inhibitor (IC50s=6.9 and 14.2 µM for dynamin1 and dynamin2 GTPase activity, respectively) with antimitotic effect. Dynole 34-2 induces apoptosis, as revealed by cell blebbing, DNA fragmentation, and PARP cleavage. Dynole 34-2 also potently inhibits receptor mediated endocytosis (RME).
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1
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| HY-P1137 | 10Panx |
10Panx is a competitive inhibitor of selective Pannexin 1 (PANX1) channels. 10Panx blocks the opening of PANX1 channels, inhibits ATP release and downstream P2X7 receptor-mediated signaling pathways, thereby reducing cell death and inflammatory responses. 10Panx can be used in the study of diseases such as neuropathic pain, inflammatory bowel disease, and Clostridioides difficile infection. 10Panx can effectively reduce mechanical hyperalgesia and enhanced C-reflexes, and inhibit the expression of pro-inflammatory factors such as IL-6[1][2][3].
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1
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| HY-P10368 | P110 heptapeptide |
P110 heptapeptide is a peptide inhibitor of the Drp1-Fis1 interaction. P110 heptapeptide has anti-inflammatory, immunomodulatory, mitochondrial protective, and neuroprotective activities. Without blocking the physiological functions of Drp1, P110 heptapeptide reduces pathological functions in many models of neurodegeneration, ischemia, and sepsis. P110 heptapeptide can be used for research on neurological and inflammatory diseases.
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Infection
Neurological, Eye or Ear Disease
Inflammation or Immune System Disease
Blood or Cardio-cerebrovascular Disease
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1
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| HY-W015061 | Phenylacetylglycine |
Phenylacetylglycine is a gut microbial metabolite that can activate β2AR. Phenylacetylglycine protects against cardiac injury caused by ischemia/reperfusion.
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1
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| HY-N2397 | 9''-Methyl salvianolate B |
9''-Methyl salvianolate B (MSB) is a blood-brain barrier-permeable inhibitor with high affinity for g5Rp, with a Kd value of 117 nM against African swine fever virus (ASFV) g5Rp. 9''-Methyl salvianolate B also acts as a ZBP1 inhibitor. It exhibits strong binding affinity to key proteins in the PPARγ/NF-κB pathway. 9''-Methyl salvianolate B blocks the interaction between ASFV g5Rp and host proteins eIF5A or RPS15. It restores hypusination modification of eIF5A, promotes autophagy (Autophagy), and inhibits ASFV replication. 9''-Methyl salvianolate B effectively disrupts ZBP1-mediated PANoptosome assembly. It effectively alleviates myocardial ischemia/reperfusion injury. 9''-Methyl salvianolate B can be used in studies related to African swine fever.
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1
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| HY-131683 | ES9-17 |
ES9-17 is an analog of ES9 (endosidin9), which is an inhibitor of clathrin heavy chain (CHC). ES9-17 is an inhibitor of clathrin-mediated endocytosis (CME), a major route for internalization of plasma membrane proteins and molecules from the extracellular environment in plants. ES9-17 inhibits the uptake of transferrin and FM4-64. ES9-17 also inhibits root growth of Arabidopsis seedings.
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1
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| HY-17503S2 | (S)-Metoprolol-d7 |
(S)-Metoprolol-d7 is the deuterium labeled Metoprolol. Metoprolol (Toprol) is a selective β1 receptor blocker used in treatment of several diseases of the cardiovascular system, especially hypertension[1][2].
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| HY-17503S1 | (R)-Metoprolol-d7 |
(R)-Metoprolol-d7 is the deuterium labeled Metoprolol. Metoprolol (Toprol) is a selective β1 receptor blocker used in treatment of several diseases of the cardiovascular system, especially hypertension[1][2].
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| HY-100489S | TBHQ-d12 |
TBHQ-d12 (tert-Butylhydroquinone-d12) is the deuterium labeled TBHQ (HY-100489). TBHQ (tert-Butylhydroquinone) is a widely used Nrf2 activator, protects against Doxorubicin (DOX)-induced cardiotoxicity through activation of Nrf2. TBHQ (tert-Butylhydroquinone) is also an ERK activator; rescues Dehydrocorydaline (DHC)-induced cell proliferation inhibitionin melanoma[2].
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| HY-N0566R | 23-Hydroxybetulinic acid (Standard) |
23-Hydroxybetulinic acid (Standard) is the analytical standard of 23-Hydroxybetulinic acid (HY-N0566). This product is intended for research and analytical applications. 23-Hydroxybetulinic acid (Anemosapogenin) is an orally active triterpenoid with broad-spectrum anticancer activity. 23-Hydroxybetulinic acid reduces the levels of Bcl-2 and survivin, elevates the level of Bax, promotes the cleavage/activation of caspase-3 and caspase-9, and induces apoptosis via the endogenous mitochondrial pathway involving cytochrome C release and mitochondrial membrane potential disruption. 23-Hydroxybetulinic acid arrests the cell cycle at S and G1 phases, inhibits cancer cell proliferation, blocks the MAPK signaling pathway, regulates MMP2, and induces autophagic apoptosis by upregulating beclin-1. 23-Hydroxybetulinic acid inhibits the activity and efflux function of P-gp, increases the intracellular accumulation of chemotherapeutic drugs, and synergistically enhances cytotoxicity with Doxorubicin (HY-15142). 23-Hydroxybetulinic acid inhibits the phosphorylation and nuclear translocation of STAT6, blocks M2 macrophage polarization, and reduces M2 macrophage-mediated apoptosis resistance of colon cancer cells. 23-Hydroxybetulinic acid can be used in related studies on chronic myeloid leukemia, hepatocellular carcinoma, sarcoma 180, multidrug-resistant breast cancer, leukemia, Doxorubicin-induced cardiotoxicity, and colorectal cancer.
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| HY-P2696 | EP 80317 |
EP 80317 is a selective CD36 ligand. EP 80317 protects the heart against damage and dysfunction elicited by myocardial ischaemia and reperfusion (MI/R), along with a transient reduction in peripheral lipolysis. EP 80317 can be used for the study of cardiovascular disease.
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| HY-N0353R | Curdione (Standard) |
Curdione (Standard) is the analytical standard of Curdione. This product is intended for research and analytical applications. Curdione ((+)-Curdione) is an orally active sesquiterpenoid. Curdione inhibits platelet aggregation. Curdione induces ferroptosis in colorectal cancer via m6A methylation mediated by METTL14 and YTHDF2. Curdione inhibits ferroptosis in Isoproterenol (HY-B0468)-induced myocardial infarction by regulating the Keap1/Trx1/GPX4 signaling pathway, suppressing oxidative stress (ROS) and apoptosis. Curdione ameliorates Doxorubicin (HY-15142)-induced cardiotoxicity by inhibiting oxidative stress (ROS) and activating the Nrf2/HO-1 pathway. Curdione ameliorates sepsis-induced lung injury by inhibiting platelet-mediated neutrophil extracellular trap formation. Curdione ameliorates Bleomycin (HY-17565A)-induced pulmonary fibrosis by inhibiting TGF-β-induced fibroblast-to-myofibroblast differentiation. Curdione exhibits neuroprotective effects against focal cerebral ischemia-reperfusion injury in rats. Curdione exerts antiproliferative effects against human uterine leiomyosarcoma by targeting IDO1. Curdione protects vascular endothelial cells and atherosclerosis by regulating DNMT1-mediated ERBB4 promoter methylation. Curdione inhibits inducible prostaglandin E2 production (IC50 = 1.1 μM) and cyclooxygenase 2 expression.
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Reference Standards
Ferroptosis
Apoptosis
Reactive Oxygen Species (ROS)
Autophagy
Glutathione Peroxidase
Keap1-Nrf2
Heme Oxygenase (HO)
TGF-β Receptor
Indoleamine 2,3-Dioxygenase (IDO)
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/
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| HY-P2619 | BPP 5a |
BPP 5a is a bradykinin-potentiating peptide with vasorelaxant activity, which is found in Bothrops jararaca venom. BPP 5a is an angiotensin-converting enzyme (ACE) inhibitor with a Ki value of 400 nM. BPP 5a is promising for research of hypertension and cardiovascular diseases.
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| HY-N16650 | Bisadinrone A |
Bisadinrone A is a sesquiterpene found in Curcuma longa. Bisadinrone A can inhibit LDH release and shows significant anti-myocardial ischemia-reperfusion injury activity. Bisadinrone A can be used for the research of cardiovascular disease, such as ischemic heart disease.
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| HY-P4201 | JKC 301 |
JKC 301 is a selective Endothelin A receptor antagonist. JKC 301 attenuates the pressor effects of nicotine in rats. JKC 301 can be used to study cardiovascular disease caused by smoking.
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| HY-P11607 | CyLip-10 |
CyLip-10 is a microbial-derived cyclic-lipid antimicrobial peptide. CyLip-10 has broad-spectrum antimicrobial efficacy, low hemolytic activity, and excellent stability. CyLip-10 can disrupt membrane integrity, inhibit biofilm formation and induce membrane permeabilization and bacterial cell death. CyLip-10 reduces bacterial load, promotes wound healing, and alleviates inflammatory responses in a mouse Methicillin (HY-121544)-resistant Staphylococcus aureus skin wound infection model. CyLip-10 can be used for the bacterial infection.
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| HY-N15524 | Thalictoside |
Thalictoside is found in A. squamosa L. Thalictoside is a sEH inhibitor (IC50: 20.2 µM). Thalictoside exerts anti-osteoporotic effects through an estrogen-like mechanism. Thalictoside can be used in the research of cardiovascular and urinary diseases.
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| HY-70037S | Cinacalcet-d3 |
Cinacalcet-d3 is the deuterium labeled Cinacalcet. Cinacalcet (AMG 073) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.
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| HY-P1556 | Vasonatrin Peptide (VNP) |
Vasonatrin Peptide (VNP) is a chimera of atrial natriuretic peptide (ANP) and C-type natriuretic peptide (CNP). Vasonatrin peptide possesses the venodilating actions of CNP, the natriuretic actions of ANP, and unique arterial vasodilating actions not associated with either ANP or CNP. Vasonatrin Peptide protects the diabetic heart against ischemia-reperfusion injury by inhibiting ER stress via the cGMP-PKG signaling pathway.
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| HY-B0932S1 | Levocarnitine propionate-d5 hydrochloride |
Levocarnitine propionate-d5 (hydrochloride) is the deuterium labeled Levocarnitine propionate hydrochloride. Levocarnitine propionate hydrochloride (L-Propionylcarnitine chloride; ST-261) is a ligand of carnitine acetyltransferase (CAT) with high enzyme affinity. Levocarnitine propionate hydrochloride possesses antioxidant activity. Levocarnitine propionate hydrochloride increases intracellular L-carnitine reserves. Levocarnitine propionate hydrochloride exerts a protective effect against myocardial ischemia-reperfusion injury. Levocarnitine propionate hydrochloride can be used in research related to myocardial ischemia-reperfusion injury and chronic ischemic heart disease.
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| HY-N13380 | 6′‐O‐Galloylsalidroside |
6’-O-Galloylsalidroside is an active component of Rhodiola. 6’-O-Galloylsalidroside is promising for research of Alzheimer’s disease, lung diseases, cerebrovascular disease, diabetes, cardiovascular disease and aging-related diseases.
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Neurological, Eye or Ear Disease
Blood or Cardio-cerebrovascular Disease
Metabolic or Endocrine Disease
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| HY-N21753 | Dehydrodicatechin A |
Dehydrodicatechin A is a biflavan catechin dimer and antioxidant. Dehydrodicatechin A is isolated from the roots of Hagenia abyssinica, the stem bark of Choerospondias axillaries, the stems of Entada phaseoloides, and Calligonum comosum. Dehydrodicatechin A exhibits ABTS+ radical cation, DPPH, ABTS, and superoxide anion radical scavenging activities, as well as ferric reducing/antioxidant power. Dehydrodicatechin A inhibits Lipase. Dehydrodicatechin A is used in studies on polycystic ovary syndrome, Ehrlich ascites, and Doxorubicin (HY-15142)-induced cardiotoxicity.
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| HY-P10821 | Myr-Tat-PKCβII |
Myr-Tat-PKCβII is a cell permeable protein kinase C β II peptide inhibitor. Myr-Tat-PKCβII mitigates the generation of reactive oxygen species in rat ex-vivo and porcine in-vivo ischemia-reperfusion injury.
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| HY-P11580 | Pap12-6-10 |
Pap12-6-10 is an MD-2 ligand that binds to the hydrophobic pocket of MD-2 to inhibit the dimerization of the TLR4/MD-2 complex and downstream inflammatory signal transduction. Pap12-6-10 also binds to LPS to permeabilize bacterial cell membranes and induce oxidative stress, leading to bacterial death. Pap12-6-10 regulates LPS-induced inflammatory responses through the TLR4 signaling pathway and exhibits antibacterial activity against multidrug-resistant Gram-negative bacteria. Pap12-6-10 shows low tendency to induce drug resistance and low preclinical cytotoxicity, and it prevents organ damage in a mouse model of sepsis. Pap12-6-10 can be used for research related to Gram-negative sepsis and carbapenem-resistant Acinetobacter baumannii infections.
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| HY-107337S | Delapril-d3 hydrochloride |
Delapril-d3 (hydrochloride) is the deuterium labeled Delapril hydrochloride. Delapril hydrochloride is an angiotensin-converting enzyme (ACE) inhibitor for the treatment of cardiovascular diseases.
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| HY-P10621 | SHLP-1 |
SHLP-1 is a mitochondrial-derived peptide, a biologically active microprotein encoded by the 16S ribosomal RNA (MT-RNR2) gene. SHLP-1 can be used in the research of diabetes, Alzheimer's disease, cardiovascular disease and prostate cancer.
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Cancer
Neurological, Eye or Ear Disease
Blood or Cardio-cerebrovascular Disease
Metabolic or Endocrine Disease
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| HY-W653969 | Arotinolol-d5 hydrochloride |
Arotinolol-d5 (hydrochloride) is deuterium labeled Arotinolol. Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol also shows potency for inhibiting the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites. Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases.
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| HY-B0356G | Ciprofloxacin (GMP) |
Ciprofloxacin GMP is Ciprofloxacin (HY-B0356) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Ciprofloxacin (Bay-09867) is an orally active, blood-brain barrier permeable fluoroquinolone antibacterial agent. Ciprofloxacin exerts bactericidal effects primarily by inhibiting topoisomerase II and IV. Ciprofloxacin inhibits the proliferation of human dental pulp stem cells and chondrocytes from young rats, and also activates the Akt signaling pathway and upregulates markers such as β-catenin and Nanog to maintain the morphological characteristics of stem cells. Ciprofloxacin induces significant neurotoxicity and tissue damage, including reducing serotonin and glutathione levels in the brain, inducing oxidative stress and depression-like behaviors, and causing articular cartilage damage. Ciprofloxacin can be applied to research related to infections of necrotic young permanent teeth and neurotoxicity.
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| HY-P5169 | LVGRQLEEFL (mouse) |
LVGRQLEEFL (mouse) can be named as G * peptide, corresponding to amino acids 113 to 122 in apolipoprotein J ([113,122] apoJ)}. LVGRQLEEFL (mouse) exhibits anti-inflammatory and anti-atherogenic properties. LVGRQLEEFL (mouse) can be added to an apoJ mimetic, to form HM-10/10 peptide, which is a mimetic peptide and a novel chimeric high density lipoprotein. HM-10/10 peptide protects retinal pigment epithelium (RPE) and photoreceptors from oxidant induced cell death.
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| HY-W104304 | 2-(3-Trifluoromethylphenyl)glycine hydrochloride |
2-(3-Trifluoromethylphenyl)glycine hydrochloride is a precursor of substituted 2-acetamido-5-aryl-l, 2,4-triazolones. Substituted 2-acetamido-5-aryl-l, 2,4-triazolones are dual V1a/V2 receptor antagonists and can be used in cardiovascular disease research.
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| HY-P99553 | Torapsel |
Torapsel (42-89-glycoprotein; WAY164339) is a fusion protein with immunoglobiln. Torapsel can be used to research the prevention of ischemia reperfusion injury.
Species: Human |
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| HY-P992212 | Anti-CD62L Antibody (DREG-200) |
Anti-CD62L Antibody (DREG-200) is a human monoclonal antibody targeting CD62L/L-selectin. Anti-CD62L Antibody (DREG-200) binds to residues 45, 46 and 47 of L-selectin, and blocks L-selectin-mediated interactions, neutrophil rolling, adhesion, aggregation, secondary anchoring, as well as leukocyte rolling on ligands. Anti-CD62L Antibody (DREG-200) reduces myocardial necrosis, coronary endothelial dysfunction, and neutrophil migration driven by neutrophil microparticles. Anti-CD62L Antibody (DREG-200) exerts cardioprotective effects in feline models. Anti-CD62L Antibody (DREG-200) can be used in studies related to myocardial ischemia-reperfusion injury. The recommended isotype control is Mouse IgG1 kappa (HY-P99977).
Species: Human |
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| HY-N11081 | Hexanorcucurbitacin D |
Hexanorcucurbitacin D, a cucurbitacin, is a weak ecdysteroid receptor agonist. Hexanorcucurbitacin D can be isolated from Trichosanthes cucumeroides roots. Hexanorcucurbitacin D can be used for the research of cardiovascular disease (CVD).
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| HY-P992470 | STT-5058 |
STT-5058 (ARGX-116; NN5058) is a human monoclonal antibody targeting ApoC3 and belongs to the class of ApoC3 inhibitors. STT-5058 exhibits pH-dependent circulation properties and binds to a unique epitope on ApoC3. STT-5058 reduces triglyceride levels and accelerates the clearance of atherogenic remnant lipoproteins containing ApoC3. STT-5058 can be used in research related to hypertriglyceridemia, dyslipidemia and cardiovascular diseases.
Species: Human |
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| HY-P11486 | NOTA-RHAU18 |
NOTA-RHAU18 is a conjugate of the chelator NOTA and the peptide RHAU18. NOTA-RHAU18 can be used to synthesize the radiolabeled peptide probe [18F]AlF-NOTA-RHAU18. [18F]AlF-NOTA-RHAU18 targets mitochondrial DNA G4. [18F]AlF-NOTA-RHAU18 can be used to visualize and detect solid tumors in homozygous mice. [18F]AlF-NOTA-RHAU18 can also be used in PET imaging studies.
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| HY-P99696 | Lerodalcibep |
Lerodalcibep (LIB003) is a recombinant fusion protein of a PCSK9-binding domain (adnectin) and human serum albumin. Lerodalcibep is a Lipid-lowering agent. Lerodalcibep can be used for the research of hypercholesterolemia and cardiovascular diseases.
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| HY-B0116S | Stavudine-d4 |
Stavudine-d4 is the deuterium labeled Stavudine. Stavudine (d4T) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Stavudine has activity against HIV-1 and HIV-2. Stavudine also inhibits the replication of mitochondrial DNA (mtDNA). Stavudine reduces NLRP3 inflammasome activation and modulates Amyloid-β autophagy. Stavudine induces apoptosis.
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Isotope-Labeled Compounds
Reverse Transcriptase
HIV
Nucleoside Antimetabolite/Analog
NOD-like Receptor (NLR)
Autophagy
Apoptosis
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| HY-16910G | WIKI4 (GMP) |
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| HY-W007328S | 5-Methoxyindole-d3 |
5-Methoxyindole-d3 is the deuterated-labeled 5-Methoxyindole (HY-W007328). 5-Methoxyindole is an L-tryptophan metabolite with antifungal activity, and also serves as a pharmaceutical intermediate. Metabolites of 5-Methoxyindole exhibit COX-2 inhibitory, anti-inflammatory and anti-tumor activities. 5-Methoxyindole induces morphological distortion of hyphae and conidia, ROS accumulation, apoptosis and cell death in Gaeumannomyces graminis. 5-Methoxyindole can be used in studies related to fungal infections and organic synthesis.
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Isotope-Labeled Compounds
Endogenous Metabolite
Drug Intermediate
Fungal
Reactive Oxygen Species (ROS)
Apoptosis
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| HY-15893G | DMOG (GMP) |
DMOG (GMP) is the GMP level of DMOG (HY-15893). GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. DMOG (GMP) is a HIF-1α stabilizer. DMOG (GMP) promotes the osteogenic, angiogenic, and chondrogenic differentiation of stem cells by stabilizing the expression of HIF-1α. DMOG (GMP) can enhance the osteogenic and angiogenic differentiation potential of stem cells, thereby improving bone regeneration in bone defects. DMOG (GMP) can be used in the research of bone defect repair, vascularized bone regeneration, and the treatment of bone-related diseases (such as osteoporosis and femoral head necrosis) .
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| HY-N6779S | Patulin-13C7 |
Patulin-13C7 (Terinin-13C7) is the 13C labeled Patulin (HY-N6779). Patulin (Terinin) is a mycotoxin produced by fungi including the Aspergillus, Penicillium, and Byssochlamys species, is suspected to be clastogenic, mutagenic, teratogenic and cytotoxic. Patulin induces autophagy-dependent apoptosis through lysosomal-mitochondrial axis, and causes DNA damage.
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| HY-P12125 | TAT-Epsilon-V1-2 TFA |
TAT-Epsilon-V1-2 TFA is a cell-permeable PKCε peptide inhibitor. TAT-Epsilon-V1-2 TFA reduces chronic immune responses after heart transplantation. TAT-Epsilon-V1-2 TFA is applicable to research related to delayed graft function and acute kidney injury caused by renal ischemia-reperfusion injury.
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| HY-N3486 | Isodunnianol |
Isodunnianol is a autophagy inducer. Isodunnianol induces autophagy and increases he expression of pAMPK172, pULK1555,decreases teh expression of pULK1757, SQSTM2. Isodunnianol decreases Doxorubicin (HY-15142A)-induced cardiotoxicity.
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| HY-172836S | GLP-1 receptor agonist 17-d3 |
GLP-1 receptor agonist 17-d3 (Compound 701) is the deuterium labeled GLP-1R agonist 17 (HY-148212). GLP-1R agonist 17 is a GLP-1 receptor agonist that can be used for the research of cardiovascular metabolic diseases.
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| HY-P991574 | MEDI-5884 |
MEDI-5884 (REG-101) is a humanized IgG4Pκ neutralizing monoclonal antibody targeting endothelial lipase (EL), with an IC50 of 1.3 nM and 1.7 nM against human and cynomolgus monkey EL, respectively; its Kd values for human and cynomolgus monkey EL are 4.1 nM and 1.6 nM, respectively. MEDI-5884 increases plasma levels of HDL-C, apolipoprotein A1 (ApoA1) and phospholipids, while causing a slight increase in LDL-C and apolipoprotein B (ApoB) levels. MEDI-5884 can be used in research related to cardiovascular diseases, coronary heart disease, coronary atherosclerosis and stable coronary artery disease.
Species: Human |
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| HY-P5640 | Tritrpticin |
Tritrpticin is a porcine-derived antimicrobial peptide with properties such as membrane disruption and hemolysis. Tritrpticin disrupts the cell membranes of bacteria, fungi and Jurkat T cell leukemia cells and induces their death. Tritrpticin also enhances the efficacy of Metronidazole (HY-B0318) against *Trichomonas vaginalis*, reduces plasma endotoxin and inflammatory cytokine levels, restricts bacterial growth in blood and visceral tissues, decreases the mortality rate of septic shock in rats and enhances the therapeutic effect of ertapenem. Tritrpticin exhibits selective cytotoxicity against Jurkat T cell leukemia cells, while showing low toxicity to normal peripheral blood mononuclear cells and red blood cells, and can serve as a template for antimicrobial peptide design. Tritrpticin can be applied to research related to bacterial infections, fungal infections, trichomoniasis, septic shock and leukemia.
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| HY-P991133 | Efranarelaxin alfa |
Efranarelaxin alfa is a relaxin receptor agonist. Efranarelaxin alfa is promising for research of cardiovascular diseases and tissue repair.
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| HY-W701252 | Methyl paraben-d3 |
Methyl paraben-d3 (Methyl 4-hydroxybenzoate-d3) is the deuterium labeled Methyl paraben (HY-N0349). Methyl Paraben is a standardized methyl paraben allergen isolated from Yunnan hemlock (Tsuga dumosa). Methyl Paraben is commonly used as a stable, non-volatile preservative. Methyl Paraben increases histamine release and cellular regulation of immunity, blocks sodium channels, and prevents ischemia-reperfusion injury.
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| HY-W724344 | Cetalkonium-d5 chloride |
Cetalkonium-d5 chloride (Benzyldimethylhexadecylammonium-d5 chloride) is the deuterium labeled Cetalkonium chloride (HY-B1597). Cetalkonium chloride is an ammonium antiseptic agent used in many topical agents for infections of mouth, throat and eye. Cetalkonium chloride acts as anti-inflammatory amphiphilic agent. Cetalkonium chloride is a cationic surfactant, that improves the precorneal residence time and bioavailability of drugs. Cetalkonium chloride interacts with the negative charges on the bacterial cell membrane, disrupts the integrity of the cell membrane, causes leakage of cell contents and ultimately leading to bacterial death.
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| HY-N15525 | Arabinothalictoside |
Arabinothalictoside is found in A. squamosa L. Arabinothalictoside is a sEH inhibitor (IC50: 47.1 µM). Arabinothalictoside can be used in the research of cardiovascular and urinary diseases.
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| HY-D3153 | PbQ |
PbQ is a tubulin inhibitor (with an IC50 of 5 μM against goat tubulin) and a fluorescent probe for cuprous ions Cu (I). PbQ can penetrate the membrane of peripheral blood mononuclear cells, form a stable 1:1 complex with Cu+ ions, and exhibits low toxicity and good biocompatibility toward macrophage cell lines. In addition, PbQ promotes tubulin degradation and disrupts the microtubule network in lung epithelial cells without affecting actin. PbQ also possesses genotoxicity by forming DNA base adducts, and it can activate caspase-3 and apoptosis-related genes, induce loss of mitochondrial membrane potential, and trigger cell apoptosis. PbQ can be used in studies related to chronic obstructive pulmonary disease.
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| HY-N0322GL | Cholesterol (GMP Like, synthetic) |
Cholesterol (GMP Like, synthetic) is Cholesterol (synthetic) (HY-N0322E) produced by using GMP like guidelines. GMP Like small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Cholesterol (synthetic) is a synthetic form of cholesterol. It is a lipid that sustains vital functions. Cholesterol (synthetic) can be used in research on cardiovascular diseases.
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| HY-187271S | [U-15N]-ApoA1 |
[U-15N]-ApoA1 is the 15N-labeled ApoA1. Reduced serum levels of apolipoprotein A1 (ApoA1) are closely associated with cardiovascular diseases, such as coronary heart disease. This isotope can be used in NMR studies to investigate disease mechanisms and in mass spectrometry analysis.
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| HY-D2004 | ATTO 488 streptavidin |
ATTO 488 streptavidin is a fluorescent reagent that specifically targets and binds to biotin (biotin), formed by the conjugation of ATTO 488 with streptavidin (HY-P3152). ATTO 488 streptavidin enables visualization of the activity of streptavidin immobilized on the surface of polymeric nanoparticles, or acts as a fluorescent probe to detect the selective binding and internalization process of anti-HB-EGF/NA with cells expressing HB-EGF (with no such effect on cells that do not express this receptor). ATTO 488 streptavidin effectively verifies the function of streptavidin conjugated to the surface of nanoparticles and is suitable for research related to atherosclerotic cardiovascular diseases.
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| HY-N2026S | Propylparaben-d7 |
Propylparaben-d7 (Propyl parahydroxybenzoate-d7) is the deuterium labeled Propylparaben (HY-N2026). Propylparaben (Propyl parahydroxybenzoate) is an antibacterial preservative that can be produced by plants and bacteria. Propylparaben is an orally active weak estrogen receptor agonist. Propylparaben regulates the PI3K-AKT and JNK signaling pathways, and induces oxidative stress. Propylparaben is commonly used in cosmetics, pharmaceuticals and foods, and can be used in studies related to ovarian aging and myocardial ischemia-reperfusion injury.
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| HY-13689G | Go 6983 (GMP) |
Go 6983 GMP is Go 6983 (HY-13689) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Go 6983 is a dual inhibitor targeting Suv39h1/2 (KMT1A/KMT1B) and PKC, as well as a transcriptional activator capable of inducing DNA hypomethylation. Go 6983 stimulates the transcription of Prdm14 by reducing Suv39h1/2 protein levels, decreasing histone modifications in the Prdm14 promoter region, and increasing the recruitment of RNA polymerase II. Go 6983 induces genome-wide DNA hypomethylation by inhibiting de novo methyltransferase expression and increasing Tet1/Tet2 levels, thereby promoting self-renewal and pluripotency maintenance of stem cells. Meanwhile, Go 6983 can block PKC-mediated signaling pathways to reduce the expression of EMT-related genes and eliminate the upregulation of antioxidant genes downstream of NRF2. Go 6983 is mainly used in mechanism studies related to myocardial ischemia/reperfusion injury.
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| HY-N2902 | Artocarpin |
Artocarpin is an orally active apoptosis inducer. Artocarpin targets NF-κB, Erk1/2, p38 MAPK, AktS473, p53, Akt 1 kinase and Akt 2 kinase. Artocarpin induces reactive oxygen species (ROS) production, mediates p53-dependent and p53-independent apoptotic signaling pathways, induces G1-phase cell cycle arrest, and triggers autophagic cell death. Artocarpin exerts cytotoxic and bactericidal effects on cancer cells, reduces bacterial load, and exhibits anti-inflammatory, analgesic and anti-angiogenic activities.
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| HY-N6712R | Thiolutin (Standard) |
Thromycin (Standard) is the analytical standard of thromycin (Acetopyrrothin) (HY-N6712). Thiolutin is a sulfur-containing antibiotic, which is a potent inhibitor of bacterial and yeast RNA polymerases. Thiolutin can be produced by Streptomyces. Thiolutin inhibits AMSH (IC50 = 4 μM) and Rpn11 (IC50 = 0.53 μM). Thiolutin is a dual inhibitor of BRCC36 and the NLRP3 inflammasome, exhibiting anti-inflammatory effects. Thiolutin effectively suppresses the interaction between BRCC36 and HMGCR, leading to the inhibition of HCC growth. Thiolutin attenuates pyroptosis and NLRP3 inflammasome activation. Thiolutin markedly alleviates renal injury and inflammatory process in IgAN. Thiolutin is an anti-angiogenic compound which can ease Doxorubicin (HY-15142A)-induced cardiotoxicity (DOXIC).
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Reference Standards
Antibiotic
Bacterial
Deubiquitinase
NOD-like Receptor (NLR)
DNA/RNA Synthesis
Pyroptosis
HMG-CoA Reductase (HMGCR)
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| HY-P991657 | MEDI7814 |
MEDI7814 is a humanized monoclonal antibody inhibitor targeting C5a and C5adesArg. MEDI7814 binds to recombinant human C5a and serum purified human C5a with affinities of 14 pM and 8 pM, respectively. MEDI7814 is acute inflammatory diseases such as sepsis and renal ischemia-reperfusion injury.
Species: Human |
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| HY-N12019 | Parishin K |
Parishin K is a cardioprotective agent obtained from the roots of Gastrodia elata Bl. Parishin K can be used in cardiovascular disease research.
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| HY-W327449R | Feruloylputrescine (Standard) |
Feruloylputrescine is an oral active phenolamide found in citrus plants and formed through the decarboxylation of L-Arginine. Feruloylputrescine inhibits monooxygenase (cntA) and reductase (cntB) and trimethylamine production. Feruloylputrescine can be used for cardiovascular diseases research.
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| HY-N0391G | L-Citrulline (GMP) |
L-Citrulline GMP is an orally active, blood-brain barrier permeable neutral α-amino acid. L-Citrulline GMP inhibits the mitochondrial translocation of Drp1 and maintains mitochondrial homeostasis via a NO-dependent pathway, thereby reducing excessive ROS production. Consequently, L-Citrulline GMP protects sperm DNA integrity, stabilizes the blood-testis barrier and improves semen quality. L-Citrulline GMP can be used in research related to male infertility, mycobacterial infection (tuberculosis) and radiation combined injury.
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| HY-14771S | Imeglimin-d3 |
Imeglimin-d3 (EMD 387008-d3) is deuterium labeled Imeglimin. Imeglimin (EMD 387008) is an oral glucose-lowering agent. Imeglimin improves insulin sensitivity. Imeglimin also reduces reactive oxygen species (ROS) production, increases mitochondrial DNA and improves mitochondrial function.
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| HY-W778391 | Bisphenol A-13C2 |
Bisphenol A-13C2 is 13C labeled Bisphenol A. Bisphenol A is a phenolic, organic synthetic compound widely used in the production of polycarbonate plastics and epoxy resins. Bisphenol A is a reproductive, developmental, and systemic toxicant, often classified as an endocrine-disrupting compound (EDC). Bisphenol A is associated with many diseases, including cardiovascular diseases, respiratory diseases, diabetes, kidney diseases, obesity, and reproductivedisorders.
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| HY-B0419S | Manidipine-d4 |
Manidipine-d4 is the deuterium labeled Manidipine (HY-B0419). Manidipine is an orally active calcium channel antagonist. Manidipine regulates the expression of cytokines (IL-1β, IL-6). Manidipine has a hypotensive effect. Manidipine can be used in the study of cardiovascular diseases (such as hypertension, myocardial ischemia-reperfusion injury, ventricular hypertrophy), kidney diseases (such as glomerular diseases), and epilepsy.
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| HY-P3199 | PKCβII Peptide Inhibitor I |
PKCβII Peptide Inhibitor I is a PKCβII inhibitor. PKCβII Peptide Inhibitor I shows cardioprotective effects in rat cardiac Ischemia/reperfusion injury model. PKCβII Peptide Inhibitor I also prevents vascular endothelial dysfunction.
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| HY-B0356S2 | Ciprofloxacin-d4 |
Ciprofloxacin-d4 (Bay-09867-d4) is deuterium labeled Ciprofloxacin. Ciprofloxacin (Bay-09867) is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin has anti-proliferative activity and induces apoptosis. Ciprofloxacin is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
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Isotope-Labeled Compounds
Apoptosis
Mitochondrial Metabolism
Bacterial
Reactive Oxygen Species (ROS)
Antibiotic
Topoisomerase
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| HY-P10342 | Soystatin |
Soystatin is a peptide extracted from soy protein, whose main activity is to inhibit the absorption of cholesterol. Soystatin, as a peptide with significant cholic acid binding ability, can be used in the study of cardiovascular diseases.
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| HY-B0932S2 | Levocarnitine propionate-d9 hydrochloride |
Levocarnitine propionate-d9 hydrochloride (L-Propionylcarnitine-d9 chloride) is deuterium labeled Levocarnitine propionate hydrochloride. Levocarnitine propionate hydrochloride (L-Propionylcarnitine chloride; ST-261) is a ligand of carnitine acetyltransferase (CAT) with high enzyme affinity. Levocarnitine propionate hydrochloride possesses antioxidant activity. Levocarnitine propionate hydrochloride increases intracellular L-carnitine reserves. Levocarnitine propionate hydrochloride exerts a protective effect against myocardial ischemia-reperfusion injury. Levocarnitine propionate hydrochloride can be used in research related to myocardial ischemia-reperfusion injury and chronic ischemic heart disease.
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| HY-P5169A | LVGRQLEEFL (mouse) TFA |
LVGRQLEEFL (mouse) TFA can be named as G * peptide, corresponding to amino acids 113 to 122 in apolipoprotein J ([113,122] apoJ)}. LVGRQLEEFL (mouse) TFA exhibits anti-inflammatory and anti-atherogenic properties. LVGRQLEEFL (mouse) TFA can be added to an apoJ mimetic, to form HM-10/10 peptide, which is a mimetic peptide and a novel chimeric high density lipoprotein. HM-10/10 peptide protects retinal pigment epithelium (RPE) and photoreceptors from oxidant induced cell death.
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| HY-P2275B | Peptide5 TFA |
Peptide5 TFA, a connexin 43 mimetic peptide, reduces animals swelling, astrogliosis, and neuronal cell death after spinal cord injury. Peptide5 TFA also inhibits NLRP3 inflammasome, and is an anti-inflammatory agent.
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| HY-P991721 | Ticalicibart |
Ticalicibart is a humanized IgG4κ monoclonal antibody inhibitor targeting PCSK9. Ticalicibart has anti-hyperlipidaemic activity. Ticalicibart can be used for cardiovascular disease like hypercholesterolaemia research.
Species: Human |
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| HY-W015061S | N-(Phenylacetyl-d5)glycine |
N-(Phenylacetyl-d5)glycine is the deuterium labeled Phenylacetylglycine. Phenylacetylglycine is a gut microbial metabolite that can activate β2AR. Phenylacetylglycine protects against cardiac injury caused by ischemia/reperfusion.
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| HY-N1441R | Afzelin (Standard) |
Afzelin (Standard) is the analytical standard of Afzelin. This product is intended for research and analytical applications. Afzelin (Kaempferol-3-O-rhamnoside)It is a flavonol glycoside that has anti-inflammatory, anti-oxidative stress response, anti-apoptotic, and anti-cardiac cytotoxic effects. AfzelinIt can reduce mitochondrial damage, enhance mitochondrial biosynthesis, and reduce mitochondria-related proteins. Parkinand PTENinduced putative kinase 1 (putative kinase 1)s level. AfzelinCan be improved D-galactosamine(GalN)/LPSSurvival rate of mice treated with doxorubicin prophylaxis (HY-15142A)Induced cardiotoxicity and scopolamine (HY-N0296)-induced neurological injury. AfzelinAlso inhibits asthma and allergies caused by ovalbumin.
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Infection
Neurological, Eye or Ear Disease
Inflammation or Immune System Disease
Blood or Cardio-cerebrovascular Disease
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| HY-N0264R | Ligustrazine (Standard) |
Ligustrazine (Standard) (Chuanxiongzine (Standard)) is the analytical standard of Ligustrazine (HY-N0264). This product is intended for research and analytical applications. Ligustrazine (Chuanxiongzine) is an orally active, blood-brain barrier-permeable alkaloid. It can be isolated from Ligusticum striatum DC. Ligustrazine reduces ROS, upregulates the levels of p-Akt/Akt and p-eNOS/eNOS, and decreases ALT and AST. It inhibits glutamate excitotoxicity, calcium overload, oxidative stress, ischemia-reperfusion injury and atherosclerotic plaque progression, enhances synaptic plasticity, and improves neurological function, cerebral infarct volume and brain water content. Ligustrazine possesses anti-inflammatory, antioxidant, lipid-lowering, endothelial protective and hepatoprotective activities. It can be used in studies related to ischemic stroke, cerebral ischemia-reperfusion injury and atherosclerosis.
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Cerebrovascular Disease
Lipid Metabolism
Ischemia-Reperfusion Injury
Atherosclerosis and Inflammation
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| HY-P1556A | Vasonatrin Peptide (VNP) TFA |
Vasonatrin Peptide (VNP) TFA is a chimera of atrial natriuretic peptide (ANP) and C-type natriuretic peptide (CNP). Vasonatrin peptide TFA possesses the venodilating actions of CNP, the natriuretic actions of ANP, and unique arterial vasodilating actions not associated with either ANP or CNP. Vasonatrin Peptide TFA protects the diabetic heart against ischemia-reperfusion injury by inhibiting ER stress via the cGMP-PKG signaling pathway.
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| HY-17503S | Metoprolol-d7 |
Metoprolol-d7 is the deuterium labeled Metoprolol. Metoprolol (Toprol) is a selective β1 receptor blocker used in treatment of several diseases of the cardiovascular system, especially hypertension[1][2].
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| HY-N1282 | Seneciphylline |
Seneciphylline is an orally effective hepatotoxic inducer. Seneciphylline is metabolized by CYP450 enzymes into active intermediates, which covalently bind to intracellular biomacromolecules such as proteins and DNA to form adducts, which in turn trigger a series of toxic reactions, such as inducing cell apoptosis and damaging mitochondrial function. Seneciphylline can be used in hepatotoxicity research
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| HY-70037AS | Cinacalcet-d3 hydrochloride |
Cinacalcet-d3 (hydrochloride) is the deuterium labeled Cinacalcet (hydrochloride). Cinacalcet hydrochloride (AMG-073 hydrochloride) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.
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| HY-N10151 | Notoginsenoside R3 |
Notoginsenoside R3 is an active principle components of P. notoginseng. Notoginsenoside R3 act as a signaling molecule that is associated with various physiological effects. P. notoginseng and its components are used as traditional Chinese medicine for cardiovascular disease.
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| HY-136648B | 2'-Deoxyadenosine-5'-triphosphate trisodium,100 mM Solution,PCR Grade |
2'-Deoxyadenosine-5'-triphosphate (dATP) trisodium, 100 mM Solution, PCR Gradeis one of the raw materials used by DNA polymerase to synthesize long DNA strands during DNA replication. 2'-Deoxyadenosine-5'-triphosphate trisodium,100 mM Solution,PCR Grade is used in reverse transcription polymerase chain reaction (RT-PCR) for DNA amplification. This product is supplied in the form of an aqueous solution.
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| HY-N10742 | Maritimetin |
Maritimein is an aurone that can be isolated from Coreopsis tinctoria. Maritimein shows strong diphenyl(2,4,6-trinitrophenyl)iminoazanium (DPPH) radical-scavenging activity with an IC50 value of 4.12 μM. Maritimein can be used for the research of cardiovascular disease.
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| HY-P99560 | Tadocizumab |
Tadocizumab (C4G1; YM-337) is a humanized monoclonal antibody tageting integrin αIIbβ3. Tadocizumab has antiplatelet and antithrombotic effects, and can be used for cardiovascular disease research.
Species: Human |
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| HY-117433S | 4-Hydroperoxy Cyclophosphamide-d4 |
4-Hydroperoxy Cyclophosphamide-d4 is the deuterium labeled 4-Hydroperoxy cyclophosphamide. 4-Hydroperoxy cyclophosphamide is the active metabolite form of the proagent Cyclophosphamide. 4-Hydroperoxy cyclophosphamide crosslinks DNA and induces T cell apoptosis independent of death receptor activation, but activates mitochondrial death pathways through production of reactive oxygen species (ROS). 4-Hydroperoxy cyclophosphamide has the potential for lymphomas and autoimmune disorders.
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| HY-N2439 | Methyl isoeugenol |
Methyl isoeugenol is an orally active, blood-brain barrier-permeable isoeugenol-type eugenol analog. Methyl isoeugenol promotes the nuclear translocation of Nrf2, upregulates the expressions of HO-1, NQO1 and SOD, and reduces the expression level of MDA. Methyl isoeugenol decreases the nuclear translocation of NF-κB. Methyl isoeugenol inhibits NLRP3 inflammasome-mediated pyroptosis. Methyl isoeugenol reduces cerebral infarction volume and regulates the M1/M2 phenotypic balance of microglia. Methyl isoeugenol can be used for the research of cerebral ischemia-reperfusion injury.
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| HY-121362 | Evernic Acid |
Evernic Acid is an orally active thioredoxin reductase 1 (TrxR1) inhibitor and antiproliferative agent. Evernic Acid inhibits the proliferation and migration of human breast cancer cells. Evernic Acid blocks the NF-κB pathway by inhibiting p65 nuclear translocation and IκBα phosphorylation, thereby suppressing downstream inflammatory mediators. Evernic Acid acts as an antioxidant, anti-inflammatory agent and neuroprotective agent, protects neurons from cell death, mitochondrial dysfunction and oxidative stress damage, reduces astrocyte activation, and ameliorates dopaminergic neuron loss and neuroinflammation. Evernic Acid inhibits enoyl reductases FabI and FabZ of Plasmodium falciparum. Evernic Acid downregulates the expression of lasB and rhlA genes in Pseudomonas aeruginosa, inhibits quorum sensing and biofilm formation, and exerts antibacterial activity against Gram-positive bacteria, Gram-negative bacteria and fungi. Evernic Acid is applicable to research related to breast cancer, Parkinson's disease, bacterial infections and fungal infections.
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| HY-N6642 | Ankaflavin |
Ankaflavin, isolated from Monascus-Fermented red rice, is an orally active PPARγ agonist. Ankaflavin exhibits selective cytotoxic effect and induces cell death through apoptosis on cancer cells. Ankaflavin has anti-inflammatory, anti-cancer, antiatherosclerotic, and hypolipidemic effects.
Source: Monascus |
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| HY-P11315 | MG1 peptide |
MG1 peptide is an M1 microglia-targeting peptide with blood-brain barrier permeability. MG1 peptide can be used in studies related to ischemic stroke and cerebral ischemia-reperfusion injury.
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| HY-165607S | MCB-22-174 |
MCB-22-174 is a deuterated Piezo1 agonist, with an EC50 value of 6.28 μM. MCB-22-174 remarkably activates the CaMKII/ERK signaling pathway and initiates Ca2+ influx in rMSCs. MCB-22-174 significantly decreases the expression of chondrogenesis markers (Comp, Acan) and adipogenesis markers (Lpl, Fabp4) in MSCs. MCB-22-174 can effectively improve bone quality in hind-limb unloading (HU) model rats. MCB-22-174 can be used for the study of disuse osteoporosis (OP).
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| HY-N3985 | Gyrophoric acid |
Gyrophoric acid is a good ultraviolet filter in lichen populations. Gyrophoric acid shows DPPH radical scavenging activity with an IC50 value of 105.75 μg/ml.
Source: lichen Umbilicaria hirsuta |
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| HY-W047191 | D-Glucono-1,4-lactone |
D-Glucono-1,4-lactone is a derivative of D-gluconic acid (HY-Y0569C). D-Glucono-1,4-lactone can be isolated from fruits, vegetables, honey, kombucha and wine. D-Glucono-1,4-lactone inhibits thrombin-induced arachidonic acid peroxidation and platelet activation. D-Glucono-1,4-lactone reduces superoxide anion production in thrombin-activated platelets. D-Glucono-1,4-lactone exerts antioxidant activity on platelets under oxidative stress conditions and prevents excessive platelet activation through antioxidant mechanisms. D-Glucono-1,4-lactone can be used in research related to cardiovascular diseases.
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| HY-W357818 | Glycinexylidide |
Glycinexylidide (GX) is the active metabolite of Lidocaine. Lidocaine is a local agent that can suppress or relieve pain, that inhibits sodium channels involving complex voltage and dependence. Lidocaine also reduces the growth, migration and invasion of gastric cancer cells. Glycinexylidide has research potential for use in anesthesia, cancer, and cardiovascular disease.
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Breast Cancer
Colorectal Cancer
Prostate Cancer
Gastric Cancer
Liver Cancer
Leukemia/Lymphoma/Myeloma
Pancreatic Cancer
Ovarian Cancer
Depression
Pain
Digestive System Inflammation
Obesity
Rheumatoid Arthritis
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| HY-106275 | FX-06 |
FX-06 (Fibrin-derived peptide Bβ15-42) is a fibrin Bbeta chain-derived peptide. FX-06 binds to VE-cadherin and inhibits leukocyte transmigration and initiates VE-cadherin-mediated signaling. FX-06 can be used in the research of ischemia/reperfusion injury, Dengue shock syndrome (DSS).
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| HY-111954 | (+)-Erinacin A |
(+)-Erinacin A (Erinacine A) is a cyanoditerpenoid isolated from Hericium erinaceus with anticancer, anti-inflammatory and neuroprotective activities. (+)-Erinacin A can induce cancer cell death by activating extrinsic and intrinsic apoptosis pathways. (+)-Erinacin A can also inhibit the expression of NO synthase (iNOS) and the production of nitrotyrosine to exert inflammatory and neuroprotective effects, thereby reducing ischemic brain damage.
Source: Hericium erinaceus |
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| HY-W661499 | Orellanine |
Orellanine, a nephrotoxic alkaloid found in Cortinarius orellanus, is an orally active and selective non-competitive inhibitor of alkaline phosphatase. Orellanine chelates iron, generates reactive oxygen species (ROS), induces DNA scission, forms ortho-semiquinone radicals, downregulates antioxidant defenses, and inhibits mitochondrial function. Orellanine induces caspase 8/9-mediated apoptosis. Orellanine inhibits synthesis of proteins, RNA, DNA, and mitochondrial protein synthesis, with metabolic activation required for cell-free protein synthesis inhibition. Orellanine can be used for the research of metastatic clear cell renal cell carcinoma, acute renal failure, chronic renal insufficiency, and kidney damage.
Source: Cortinarius orellanus |
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| HY-148748G | Butyzamide (GMP) |
Butyzamide (GMP) is Butyzamide (HY-148748) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Butyzamide is an orally active activator of Mpl, a thrombopoietin (TPO) receptor. Butyzamide increases the phosphorylation level of JAK2, STAT3, STAT5 and MAPK. Butyzamide increases the level of platelets in mouse xenotransplantation assay.
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| HY-110397G | KP-457 (GMP) |
KP-457 (GMP) is KP-457 (HY-110397) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture.KP-457 is a selective a disintegrin and metalloproteinase 17 (ADAM17) inhibitor, with higher selectivity for ADAM17 than for other MMPs and ADAM10, and IC50s are 11.1 nM (ADAM17), 748 nM (ADAM10), 717 nM (MMP2), 9760 nM (MMP3), 2200 nM (MMP8), 5410 nM (MMP9), 930 nM (MMP13), 2140 nM (MMP14), and 7100 nM (MMP17), respectively.
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| HY-P991222 | AMG-529 |
AMG-529 is a humanized monoclonal antibody against ASGR1 that binds to ASGR1, blocks ligand binding, and causes a dose-dependent increase in ALP (a biomarker of ASGR1 inhibition). AMG-529 can be used for the research of cardiovascular diseases.
Species: Human |
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| HY-P6442 | Chemerin15 |
Chemerin15 is an anti-inflammatory peptide derived from Chemerin. Chemerin15 binds to ChemR23. Chemerin15 inhibits TNFα-induced activation of Syk, ERK and Src kinases. Chemerin15 increases the expression of p-p38 mRNA and protein. Chemerin15 mediates phagocytosis, resolution of inflammation, CD62L shedding and downregulation of PSGL-1 expression in macrophages and microglia. Chemerin15 inhibits neutrophil-mediated vascular inflammation and myocardial ischemia-reperfusion injury via ChemR23. Chemerin15 enhances microglial phagocytosis, thereby alleviating cerebral ischemia-reperfusion injury.
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| HY-DY1087 | Coppersensor 1 (solution) |
Coppersensor 1 (solution) is a membrane-permeable fluorescent dye. Coppersensor-1 has a picomolar affinity for Cu+ with high selectivity over competing cellular metalions. Coppersensor-1 as a probe, can selective and sensitive detection of copper(I) ions (Cu+) in biological samples, including live cells. Coppersensor-1 can be used for the research of imaging of severe diseases such as cancer, cardiovascular disorders and neurogenerative diseases.
Solvent and concentration: DMSO: 2 mM |
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| HY-112486G | TA-316 (GMP) |
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| HY-119152 | CMX-2043 |
CMX-2043 is a novel analogue of α-Lipoic Acid (HY-N0492). CMX-2043 is effective in antioxidant effect, activation of insulin receptor kinase, soluble tyrosine kinase, and Akt phosphorylation. CMX-2043 shows protection against ischemia-reperfusion injury (IRI) in rat model.
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| HY-W015061R | Phenylacetylglycine (Standard) |
Phenylacetylglycine (Standard) is the analytical standard of Phenylacetylglycine. This product is intended for research and analytical applications. Phenylacetylglycine is a gut microbial metabolite that can activate β2AR. Phenylacetylglycine protects against cardiac injury caused by ischemia/reperfusion.
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| HY-N5025 | Bullatine A |
Bullatine A, a diterpenoid alkaloid, is a potent P2X7 antagonist. Bullatine A possesses anti-rheumatic, anti-inflammatory and anti-nociceptive effects. Bullatine A inhibits ATP-induced BV-2 cell death/apoptosis and P2X receptor-mediated inflammatory responses. Bullatine A suppresses glioma cell growth by targeting SIRT6. Bullatine A specifically attenuates pain hypersensitivity in rats. Bullatine A attenuates LPS (HY-D1056)-induced systemic inflammatory response by inhibiting the ROS/JNK/NF-κB pathway in mice. Bullatine A improves despair behavior in Chronic chronic social defeat stress (CSDS) mice. Bullatine A can be used for the study of inflammation, glioblastoma (GBM) and depression.
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Lung Cancer
Breast Cancer
Colorectal Cancer
Prostate Cancer
Gastric Cancer
Liver Cancer
Leukemia/Lymphoma/Myeloma
Pancreatic Cancer
Ovarian Cancer
Neurodegenerative Disease
Depression
Pain
Digestive System Inflammation
Obesity
Lung Fibrosis
Rheumatoid Arthritis
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| HY-B0932S | Levocarnitine propionate-d3 hydrochloride |
Levocarnitine propionate-d3 (hydrochloride) is the deuterium labeled Levocarnitine propionate hydrochloride. Levocarnitine propionate hydrochloride (L-Propionylcarnitine chloride; ST-261) is a ligand of carnitine acetyltransferase (CAT) with high enzyme affinity. Levocarnitine propionate hydrochloride possesses antioxidant activity. Levocarnitine propionate hydrochloride increases intracellular L-carnitine reserves. Levocarnitine propionate hydrochloride exerts a protective effect against myocardial ischemia-reperfusion injury. Levocarnitine propionate hydrochloride can be used in research related to myocardial ischemia-reperfusion injury and chronic ischemic heart disease.
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| HY-175416 | Yoda2 |
Yoda2 (KC289), the potassium salt of Yoda1 (HY-18723), is a PIEZO1 agonist with an EC50 of 150 nM. Yoda2 evokes Ca2+ elevation and NO-dependent relaxation. Yoda2 induces relaxation in mouse arterial and cavernous tissues. Yoda2 inhibits glucocorticoid-induced osteoclast formation and bone resorptive activity, reverses glucocorticoid-induced bone density loss and architectural deterioration, and does not induce medication-related osteonecrosis of the jaw in mice. Yoda2 can be used for the researches of hypertension and osteoporosis.
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| HY-N0124R | Dioscin (Standard) |
Dioscin (Standard) is the analytical standard of Dioscin. This product is intended for research and analytical applications. Dioscin (CCRIS 4123; Collettiside III) is a natural plant-derived steroidal saponin that has good anti-cancer activity against a variety of cancer cells. Dioscin causes DNA damage and induces apoptosis in HeLa and SiHa cells. Dioscin regulates ROS-mediated DNA damage and mitochondrial signaling pathways, exerting anticancer activity.
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| HY-N0566 | 23-Hydroxybetulinic acid |
23-Hydroxybetulinic acid (Anemosapogenin) is an orally active triterpenoid with broad-spectrum anticancer activity. 23-Hydroxybetulinic acid reduces the levels of Bcl-2 and survivin, elevates the level of Bax, promotes the cleavage/activation of caspase-3 and caspase-9, and induces apoptosis via the endogenous mitochondrial pathway involving cytochrome C release and mitochondrial membrane potential disruption. 23-Hydroxybetulinic acid arrests the cell cycle at S and G1 phases, inhibits cancer cell proliferation, blocks the MAPK signaling pathway, regulates MMP2, and induces autophagic apoptosis by upregulating beclin-1. 23-Hydroxybetulinic acid inhibits the activity and efflux function of P-gp, increases the intracellular accumulation of chemotherapeutic drugs, and synergistically enhances cytotoxicity with Doxorubicin (HY-15142). 23-Hydroxybetulinic acid inhibits the phosphorylation and nuclear translocation of STAT6, blocks M2 macrophage polarization, and reduces M2 macrophage-mediated apoptosis resistance of colon cancer cells. 23-Hydroxybetulinic acid can be used in related studies on chronic myeloid leukemia, hepatocellular carcinoma, sarcoma 180, multidrug-resistant breast cancer, leukemia, Doxorubicin-induced cardiotoxicity, and colorectal cancer.
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| HY-P4987 | TRAP-7 |
TRAP-7 is a thrombin receptor (PAR) activating peptide. TRAP-7 stimulates total inositol phosphate (IP) accumulation and phosphorylation of a specific endogenous substrate for activated PKC. TRAP-7 can be used in cardiovascular disease research.
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| HY-112624K | Dextran T5 (MW 5,000) |
Dextran T5 (MW 5,000) is a sulfated polysaccharide anti-apoptotic and autophagic agent. Dextran T5 (MW 5,000) has sulfated groups and interacts with cell membranes by mimicking endogenous glycosaminoglycans, inhibiting the mitochondrial apoptotic pathway and delaying DNA fragmentation to exert anti-apoptotic activity. Dextran T5 (MW 5,000) also promotes the conversion of LC3-I to LC3-II and the formation of autophagosomes to activate the autophagic pathway. Dextran T5 (MW 5,000) can prolong the survival cycle of CHO cells and increase the production of recombinant erythropoietin (EPO). The Dextran series of compounds are also natural polysaccharide drug carriers that can be connected to drugs through covalent bonding methods such as ester bonds, amide bonds or click chemistry, or self-assembled to form carriers such as nanoparticles and hydrogels. Dextran is biodegradable and biocompatible, and can achieve targeted delivery and controlled release of drugs. Dextran derivatives can prolong drug half-life, increase local concentration and reduce immune clearance activity. The Dextran series of compounds are also natural polysaccharide drug carriers that can be connected to drugs through covalent bonding methods such as ester bonds, amide bonds or click chemistry, or self-assembled to form carriers such as nanoparticles and hydrogels. Dextran is biodegradable and biocompatible, and can achieve targeted delivery and controlled release of drugs. Dextran derivatives can prolong the half-life of drugs, increase local concentrations, and reduce the activity of immune clearance.
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| HY-135009 | 2-Di-1-ASP |
2-Di-1-ASP (DASPI; Compound 18a) is a mono-stryryl dye, and widely used as mitochondrial stain and groove-binding fluorescent probes for double-stranded DNA. 2-Di-1-ASP is selective for G-quadruplex (G4) and double-stranded DNA.
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| HY-P990785 | Etentamig |
Etentamig is a BCMA × CD3 bispecific T-cell engager (BiTE) that can inhibit the activity of B-cell maturation antigen (BCMA) and activate the T-cell surface glycoprotein CD3 complex. Etentamig can be used for research in multiple myeloma, immunoglobulin light chain amyloidosis, and cardiovascular diseases.
Species: Human |
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| HY-W046353 | 2-Methoxycinnamaldehyde |
2-Methoxycinnamaldehyde (o-Methoxycinnamaldehyde) is a natural compound that can be isolated from Cinnamomum cassia. 2-Methoxycinnamaldehyde inhibits topoisomerase-I/II and NF-κB signaling pathway, causes mitochondrial dysfunction, induces lysosomal vesiculation, thereby leading to DNA damage and cell apoptosis. 2-Methoxycinnamaldehyde exhibits antitumor effects.
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| HY-W007328 | 5-Methoxyindole |
5-Methoxyindole is an L-tryptophan metabolite with antifungal activity, and also serves as a pharmaceutical intermediate. Metabolites of 5-Methoxyindole exhibit COX-2 inhibitory, anti-inflammatory and anti-tumor activities. 5-Methoxyindole induces morphological distortion of hyphae and conidia, ROS accumulation, apoptosis and cell death in Gaeumannomyces graminis. 5-Methoxyindole can be used in studies related to fungal infections and organic synthesis.
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| HY-125773 | β-cyano-L-Alanine |
β-cyano-L-Alanine (Beta-cyano-l-alanine), a nitrile of widespread occurrence in higher plants, is enzymatically produced by cyanoalanine synthase from cyanide and cysteine as substrates. β-cyano-L-Alanine abolishes the protective effect of ethanol on cerebral ischemia/reperfusion (I/R) injury.
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| HY-P10409 | SHLP2 |
SHLP2 (Small humanin-like peptide 2) is a small molecule peptide encoded by mitochondrial DNA, belonging to mitochondria derived peptide. SHLP2 has the activity of regulating apoptosis and inhibits cell death. SHLP2 binds to mitochondrial complex 1. SHLP2 improves mitochondrial metabolism by increasing respiration and biogenesis, reducing ROS, and decreasing mtDNA oxidation. SHLP2 also regulated energy homeostasis through the activation of hypothalamic neurons. SHLP2 can be used in the study of diseases related to mitochondrial dysfunction and anti-aging diseases, such as age-related macular degeneration and Parkinson’s disease.
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| HY-121360 | Cylindrospermopsin |
Cylindrospermopsin, a cyanotoxin, is a polycyclic uracil derivative containing guanidine and sulfate groups, which can inhibit protein synthesis and covalently modify DNA or RNA. Cylindrospermopsin induces hepatocellular hypertrophy, renal cellular hypertrophy, intracellular reactive oxygen species (ROS), DNA strand breaks, mitochondrial hyperpolarisation, ultrastructural damage, and altered gene expression in liver, kidney, and intestinal cells. Cylindrospermopsin can be used in research including hepatocellular carcinoma and water quality testing.
Source: Cylindrospermopsis raciborskii |
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| HY-W327449 | Feruloylputrescine |
Feruloylputrescine is an oral active phenolamide found in citrus plants and formed through the decarboxylation of L-Arginine. Feruloylputrescine inhibits monooxygenase (cntA) and reductase (cntB) and trimethylamine production. Feruloylputrescine can be used for cardiovascular diseases research.
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| HY-N0660 | Jujuboside B |
Jujuboside B is a bioactive saponin component isolated from Ziziphi Spinosae Semen (sour jujube seed), with oral efficacy and blood-brain barrier permeability. Jujuboside B induces acute leukemia cell death and drives necroptosis apoptosis by activating the RIPK1/RIPK3/MLKL pathway. Jujuboside B upregulates the expression of NOXA, PARP and caspase-3, activates AMPK, inhibits the proliferation of breast cancer cells, and induces cell apoptosis and autophagy. Jujuboside B inhibits angiogenesis and tumor growth by blocking the VEGFR-2 signaling pathway. Jujuboside B alleviates liver injury in mice by regulating the Nrf2-STING signaling pathway. Jujuboside B alleviates liver injury by regulating anti-inflammatory responses and downregulating the expression of 11β-HSD2. Jujuboside B induces ferroptosis and overcomes radioresistance in non-small cell lung cancer via the PPARγ-ATF3-Gpx4 signaling pathway. Jujuboside B exerts inhibitory effects on platelet aggregation. Jujuboside B inhibits febrile seizures by suppressing the activity of AMPA receptors. Jujuboside B reverses chronic unpredictable mild stress-promoted tumor progression by blocking the PI3K/Akt and MAPK/ERK pathways and dephosphorylating CREB signaling. Jujuboside B is applicable to related studies on acute leukemia, breast cancer, PM2.5-induced lung injury, hepatotoxicity, liver injury, colorectal cancer, non-small cell lung cancer, thromboembolic diseases, cardiovascular diseases associated with high platelet aggregation, febrile seizures, and depressive-like phenotypes.
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Apoptosis
PARP
Caspase
AMPK
Autophagy
VEGFR
Keap1-Nrf2
STING
11β-HSD
Ferroptosis
PI3K
Akt
p38 MAPK
ERK
Inflammation or Immune System Disease
Metabolic or Endocrine Disease
Breast Cancer
Colorectal Cancer
Leukemia/Lymphoma/Myeloma
Depression
Non-Small Cell Lung Cancer
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| HY-129763 | Di-4-ANEPPS |
Di-4-ANEPPS is a voltage-sensitive dye that acts on voltage-gated ion channels (such as sodium channels) and inhibits sodium current, significantly reducing sodium current density, although specific values like IC50 remain unclear. It mainly binds to the voltage-sensitive regions on the cell membrane, changing its fluorescence properties to reflect membrane potential changes and thus affecting the function of ion channels to exert its activity. This substance can be used in cardiovascular research, such as the electrophysiology of cardiomyocytes, myocardial ischemia, and the effects of drugs on cardiomyocytes. It is of great value in evaluating drug cardiotoxicity and exploring the mechanisms of arrhythmias.
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| HY-Y1887 | Cottonseed oil |
Cottonseed oil is an edible oil extracted from the seeds of cotton (Gossypium hirsutum). Its fatty acid composition includes 26-35% saturated fatty acids, 42-52% polyunsaturated fatty acids, and 18-24% monounsaturated fatty acids. Cottonseed oil is regarded as an Insecticide, as it is used to protect the trunks of apple trees from damage by the apple clearwing moth. Cottonseed oil possesses anti-inflammatory and cardioprotective properties. It also has extensive applications in many fields such as biofuels, animal husbandry, cosmetics, agriculture, and chemical industry.
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| HY-110228 | Metformin-d6 hydrochloride |
Metformin-d6 hydrochloride is a deuterium labeled Metformin hydrochloride. Metformin hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin hydrochloride also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, metformin hydrochloride regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo.
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| HY-P99555 | Tomaralimab |
Tomaralimab (OPN-305) is a humanized anti-TLR2 IgG4 monoclonal antibody. Tomaralimab inhibits TLR2, MyD88, NLRP3, and reduces pro-inflammatory cytokine (IL-1β, IL-6, IL-8) production. Tomaralimab reduces tau pathology. Tomaralimab improves cognition, atopic dermatitis. Tomaralimab has anticancer effects on pancreatic ductal adenocarcinoma. Tomaralimab is being studied in myelodysplastic syndrome (MDS), atopic dermatitis, pancreatic ductal adenocarcinoma, Alzheimer's disease, and myocardial ischemia/reperfusion injury.
Species: Human |
Cancer
Neurological, Eye or Ear Disease
Inflammation or Immune System Disease
Blood or Cardio-cerebrovascular Disease
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| HY-NP007 | Myoglobin |
Myoglobin is an oxygen-binding heme protein. Myoglobin scavenges ROS via its peroxidase activity, and binds to and inactivates NO in the heart and oxidative skeletal muscle. Myoglobin stores, buffers and facilitates intracellular oxygen diffusion, maintains aerobic metabolism under hypoxic/anoxic conditions, and provides oxygen supply support for mitochondria. Myoglobin alleviates oxidative stress, protects cardiac function and affects cardiac redox pathways. Myoglobin can be used in studies related to ischemia-reperfusion injury, oxidative stress-induced cardiac dysfunction and acute myocardial infarction.
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| HY-152086A | DRP1i27 dihydrochloride |
DRP1i27 dihydrochloride is a potent inhibitor of human Drp1 (dynamin-related protein 1). DRP1i27 dihydrochloride binds to the GTPase site of Drp1, with hydrogen bonds to Gln34 and Asp218. DRP1i27 dihydrochloride targets Drp1-mediated mitochondrial fission in cell line models and protects against simulated ischemia-reperfusion injury.
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| HY-P2280 | TAT-P110 |
TAT-P110, a peptide inhibitor of Drp1-Fis1 interaction, reduces pathology in numerous models of neurodegeneration, ischemia, and sepsis without blocking the physiological functions of Drp1.
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| HY-P991049 | Atrosimab |
Atrosimab is an Fv-Fc1K fusion protein with an EC50 value of 0.37 nM against humans. Atrosimab inhibits TNF-induced TNFR1 activation, release of IL-6 and IL-8, and cell death, and alleviates neuroinflammation. Atrosimab is applicable to research related to inflammatory diseases, neurodegenerative diseases, acute and chronic inflammation, experimental arthritis, non-alcoholic steatohepatitis, and experimental autoimmune encephalomyelitis.
Species: Human |
Experimental Autoimmune Encephalomyelitis
Experimental Autoimmune Encephalomyelitis
Fatty Liver Disease
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| HY-157442 | GLPG3312 |
GLPG3312 (Compound 28) is an orally active SIK inhibitor with IC50 values of 2.0 nM, 0.7 nM and 0.6 nM for SIK1, SIK2 and SIK3, respectively. GLPG3312 exhibits anti-inflammatory and immunomodulatory activity in vitro on human primary myeloid cells and in vivo in mouse models. GLPG3312 has good oral bioavailability and can be used for research on inflammatory and immune diseases.
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Salt-inducible Kinase (SIK)
Discoidin Domain Receptor
RIP kinase
LIM Kinase (LIMK)
MAP3K
Bcr-Abl
Src
TGF-β Receptor
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| HY-P99116 | Faricimab |
Faricimab, an overall good safety and tolerability profile, is a bispecific antibody targeting Angiopoietin-2 (Ang-2) and vascular endothelial growth factor-A (VEGF-A). Faricimab prevents retinal vascular leakage, cell death and inflammation in retinal ischemia/reperfusion (I/R) injury and sCNV mouse models. Faricimab demonstrates statistically superior visual acuity gains versus Ranibizumab (HY-P9951). Faricimab can be used for retinal diseases, such as age-related macular degeneration (w-AMD), diabetic macular edema (DME) and macular edema following retinal vein occlusion (RVO).
Species: Human |
Blood or Cardio-cerebrovascular Disease
Metabolic or Endocrine Disease
Visual System Disease
Ischemia-Reperfusion Injury
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| HY-NP165 | Advanced glycation end products |
Advanced glycation end products (AGEs) are a series of stable compounds generated through non-enzymatic reactions between reducing sugars and proteins, lipids, or nucleic acids. Advanced glycation end products are often used as targets to evaluate the inhibitory effects of anti-glycation compounds. Advanced glycation end products can be applied to research on diabetes, cardiovascular and cerebrovascular diseases, inflammation, aging, and other conditions.
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Inflammation or Immune System Disease
Blood or Cardio-cerebrovascular Disease
Metabolic or Endocrine Disease
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| HY-P811587 | GOLPH3 Antibody |
GOLPH3 Antibody is a Rabbit-derived and non-conjugated IgG polyclonal antibody, targeting to GOLPH3.
Host: Rabbit; Reactivity: Human, Mouse, Rat |
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| HY-P812038 | GOLPH3 Antibody(YA10509) |
GOLPH3 Antibody(YA10509) is a Mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to GOLPH3.
Host: Mouse; Reactivity: Human, Mouse, Rat |
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| HY-P812038A | GOLPH3 Antibody(YA10509) (PBS only) |
GOLPH3 Antibody(YA10509) is a Mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to GOLPH3.
Host: Mouse; Reactivity: Human, Mouse, Rat |
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