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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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PROTAC, which exploit the ubiquitin-proteasome pathway to specifically degrade target proteins. PROTACs not only solve the problem of undruggability but they also have other advantages compared to traditional drug targeting strategies.
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PROTAC — Target Selection and Design
2022-07-08
A PROTAC molecule consists of three components: a target protein binding ligand, an E3 ligase ligand, and a linker connecting these two moieties. Here, we will discuss the conventional approaches for the rational design of PROTAC molecules. -
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. -
BacPROTACs is composed of a POI ligand, a chemical linker and a ClpCNTD anchor. BacPROTACs can induce in vitro and in vivo degradation of non-eukaryotic proteins in bacteria without the ubiquitin proteasome system.
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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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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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PROTAC - Design Strategy for Targeting
2023-04-23
Protein degradation targeting chimera (PROTAC) is a technology that uses the ubiquitin proteasome pathway to silent target protein. However, PROTAC still has problems such as solubility, membrane permeability, and selectivity. In this article, we have summarized three strategies for optimization: light-controlled linker, PAC molecule, and specific E3 ligase. -
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! -
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! -
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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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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Science | A "new" mechanism for non-ubiquitinated Midnolin-proteasomal degradation pathway
2024-04-26
“ubiquitin-mediated protein degradation” won the Nobel Prize in Chemistry in 2004! In fact, proteasomes degrade not only ubiquitinated proteins but also non-ubiquitinated ones. The mechanism remains shrouded in mystery. After reading this piece today, you might have a lightbulb moment! -
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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Degrade target proteins through the autophagy-lysosome pathway including LYTAC, AUTAC, and ATTEC have gained increasing attention in recent years due to their significant research potential!
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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. -
Science’s 2023 Breakthrough: GLP-1R Agonists
2024-08-13
GLP-1RAs, which achieved great success in 2023 and draws people’s attention back to obesity treatments and GLP-1 therapies worldwide, was chosen as the breakthrough of year 2023 by Science [2]. -
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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Unlocking the Power of Intermittent Fasting: The 16+8 Method
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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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nside cells, the homeostasis and degradation of proteins is a precisely regulated process. If proteins cannot be degraded in time, it may lead to the occurrence of various diseases such as neurodegenerative diseases and cancer. This article will tell you the process of how proteins are recognized, labeled and then degraded!
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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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Have you ever noticed that after staying up late, your appetite—especially for high-calorie foods—gets out of control? If this sounds familiar, today’s article might offer some good news.
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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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Finding adipogenic induction media too expensive and tricky to prepare? This comprehensive guide to 3T3-L1 adipogenic differentiation simplifies the process, helping you achieve great results!
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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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Cracking the PROTAC Permeability Barrier: CD36-Mediated Endocytosis as a Potential Breakthrough
2025-12-03
This article provides an in-depth analysis of cutting-edge literature revealing CD36 as a key mediator of cellular uptake for PROTACs and bRO5 compounds. By structurally optimizing PROTAC molecules to enhance their affinity for CD36, membrane permeability can be markedly improved, leading to significantly enhanced antitumor efficacy. -
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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In the hunt for the next ‘GLP-1,’ amylin therapeutics, which have shown strong weight-loss results in clinical trials, have become a major focus for both multinational pharma and the scientific community.
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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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Molecular glue degraders have evolved from a serendipitous observation to one of the most dynamic and transformative fields in biomedical research.
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GLP-1 and Obesity Research
2026-08-14
Obesity substantially increases the risk of chronic diseases such as T2D and cardiovascular disease. The breakout success of GLP-1 therapies has spotlighted GLP-1R and a wave of emerging obesity targets. -
Targeting the ‘Undruggable’ with PROTACs
2025-06-18
This review introduces the fundamental principles and mechanisms of PROTACs, highlights recent advances in molecular design and clinical development, and discusses emerging opportunities and remaining challenges in targeted protein degradation. -
This review explores the molecular mechanisms of the DNA damage response, reviews therapeutic strategies targeting DDR pathways in cancer, and examines their roles in cancer drug resistance.
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Summarize LLPS principles, regulatory mechanisms, experimental strategies, and pathological roles to inspire mechanism-driven research and translational applications.
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Explore lysosomal nutrient sensing, quality control, cellular adaptation, disease mechanisms, and emerging therapeutic approaches.
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Review the evolution of molecular glues from serendipitous discovery to rational design, highlighting how emerging targets and advances in screening, proteomics, structural biology, and AI are expanding the druggable proteome.
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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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MK-0429 is An Oral Integrin (αvβ3) Inhibitor
2019-04-11
MK-0429, an orally active αvβ3 inhibitor, is a potential therapeutic agent for the prevention of kidney fibrosis, melanoma and osteoporosis. -
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. -
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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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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NRX-252262 is a β-catenin:β-TrCP interaction enhancer, and its cognate E3 ligase, SCFβ-TrCP, induces mutant β-catenin degradation, with an EC50 of 3.8 nM
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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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IWP-O1, a Highly Potent Porcupine Inhibitor, Functions by Preventing the Secretion of Wnt Proteins
2019-06-03
IWP-O1 is a Porcupine (Porcn) inhibitor, with an EC50 of 80 pM in L-Wnt-STF cells. IWP-O1 functions by preventing the secretion of Wnt proteins[ -
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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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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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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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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Butaprost is a selective prostaglandin E receptor (EP2) agonist. Butaprost can effectively mitigate kidney fibrogenesis in various fibrosis models.
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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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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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EMD527040 is a highly selective αvβ6 antagonist with antifibrotic activities.
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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.
-
MRTX1133, a selective, first-in-class inhibitor of KRAS G12D, selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells.
-
Zebularine is a potent DNA methyltransferase inhibitor with anti-tumor activity. Zebularine also inhibits cytidine deaminase.
-
MS4322 is a first-in-class PRMT5 degrader and a valuable chemical tool for exploring the PRMT5 functions in vitro and in vivo.
-
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.
-
Almonertinib is an orally available, third-generation EGFR TKI with selectivity for EGFR-sensitizing and T790M resistance mutations.
-
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.
-
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.
-
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.
-
Deguelin acts as a chemopreventive agent by blocking multiple pathways like PI3K-Akt, IKK-NF-κB, and MAPK-mTOR-survivin-mediated apoptosis.
-
XL092 is a potent inhibitor of the activity of Axl, Mer and C-Met kinase with IC50s of <10 nM, respectively. Anti-tumor Activity.
-
Dovitinib is a multi-targeted tyrosine kinase inhibitor. Dovitinib inhibits cell proliferation and has potent antitumor activity.
-
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.
-
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. -
Zingerone is a natural orally active nontoxic methoxyphenol potent anti-inflammatory, antidiabetic, antioxidize, and anti-tumor properties.
-
ML-099 is a pan Ras-related GTPases activator. ML-099 can activate Rac1, cell division cycle 42, Ras, Rab7, and Rab-2A.
-
IACS-15414, a potent and orally active SHP2 inhibitor, exhibits significant anti-tumor efficacy in mouse xenograft model.
-
GS-493 is a selective SHP2 inhibitor and blocks cellular motility and growth of cancer cells in vitro and in vivo.
-
HM43239 is a potent, selective, and orally active FLT3 inhibitor and shows effectiveness in AML with FLT3 mutations.
-
PFM39 is a potent and selective MRE11 exonuclease inhibitor, and does not inhibit endonuclease, nuclease activity.
-
Hesperadin, an ATP competitive inhibitor of Aurora A/B, inhibits Aurora B with an IC50 of 250 nM. A broad-spectrum influenza antiviral.
-
VAL-083 is an alkylating agent that creates N7 methylation on DNA, VAL-083 exhibits antitumor activity in vitro and in vivo.
-
Lomeguatrib is a highly potent MGMT inactivator, improves the therapeutic effect of alkylating agents in a number of tumour models.
-
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.
-
Rigosertib (ON-01910), a multi-kinase inhibitor, inhibits PLK1 (IC50=9 nM), and induces G2/M arrest in cell cycle and apoptosis.
-
PX-12 is an irreversible inhibitor of Trx-1 and inhibits the growth, migration, and invasion of colorectal cancer cell lines.
-
Chelerythrine is a potent inhibitor pf protein kinase C with anti-cancer activity.
-
Tanomastat is an orally active, non-peptidic biphenyl MMPs inhibitor, with antiangiogenic, anti-invasive and antimetastatic activities.
-
Linzagolix is a potent, non-peptide, and orally active GnRH antagonist used for the research of endometriosis and uterine myomas.
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AUTAC2 is a FKBP12-targeting autophagy-mediated degrader (AUTAC). AUTAC2 contains an FBnG and an SLF moiety.
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Mirin is a potent MRN complex inhibitor. Mirin prevents MRN-dependent activation of ATM without affecting ATM protein kinase activity.
-
Monastrol, a potent and cell-permeable inhibitor of the mitotic kinesin Eg5, has potential for cancer research.
-
FH535 is a potent inhibitor of Wnt/β-catenin and PPAR.
-
GNE-149 is an orally bioavailable full antagonist of estrogen receptor α. GNE-149 has potent antitumor activity.
-
Bafetinib is an orally active dual Abl/Lyn tyrosine kinase inhibitor. Bafetinib suppresses the growth of Ph+ leukemia cells.
-
Pirarubicin, an anthracycline antibiotics, is a topoisomerase II Inhibitor.
-
WAY 316606 is an inhibitor of the secreted protein sFRP-1.
-
Ulixertinib is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases.
-
Nimbolide, a triterpene derived from the leaves and flowers of neem, induces apoptosis through inactivation of NF-κB.
-
Telatinib is an orally active inhibitor of VEGFR2, VEGFR3, PDGFα, and c-Kit.
-
Reversine is a potent, ATP-competitive Aurora kinases inhibitor. Reversine is a potential anticancer agent for ALL.
-
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.
-
Bisantrene is topoisomerase II poisons and DNA intercalators. Bisantrene intercalates with and disrupts the configuration of DNA.
-
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.
-
5-Azacytidine is a DNMT inhibitor. 5-Azacytidine can be used for the research of myelodysplastic syndrome.
-
Epoxomicin is an epoxyketone-containing natural product and a selective and irreversible proteasome inhibitor. Cross the blood-brain barrier.
-
Vistusertib is an ATP competitive mTOR inhibitor with an IC50 of 2.81 nM. AZD2014 inhibits both mTORC1 and mTORC2 complexes.
-
Seliciclib, a potent, selective and orally active CDKs inhibitor, preferentially inhibits CDK2, CDK7 and CDK9.
-
Temoporfin, a photosensitizer agent, can be used for the research of squamous cell carcinoma of the head and neck.
-
Namodenoson (CF-102) is a selective A3 adenosine receptor (A3AR) agonist.
-
Marimastat (BB2516) is a broad spectrum and orally bioavailable inhibitor of MMPs (Matrix metalloproteinases).
-
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.
-
Vatalanib is an inhibitor of VEGFR2/KDR. Vatalanib induces inhibition of the angiogenic response to VEGF and PDGF.
-
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.
-
Actinomycin D (Dactinomycin) is an autophagy activator inhibiting DNA repair with an IC50 of 0.42 μM.
-
Pitstop 2 is a clathrin inhibitor which inhibits clathrin-mediated endocytosis (CME) by associating with the terminal domain of clathrin.
-
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.
-
CQ211 is a selective RIOK2 inhibitor (Kd=6.1 nM). CQ211 exhibits anti-proliferation inhibition activity against multiple cancer cell lines.
-
FPDT is an anti-glioblastoma agent. Besides, FPDT shows anti-proliferative activity for GBM cells and astrocytes.
-
SBI-581 is an orally active and selective serine-threonine kinase TAO3 inhibitor with potent antitumor activity.
-
AZD7254 is a potent and orally active Smoothened (SMO) inhibitor, against sonic Hh protein (shh), with strong anti-cancer effects.
-
Toceranib is a selective and orally active inhibitor of RTK and has the potential for the research of canine mast cell tumors.
-
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.
-
Pulrodemstat is a potent, selective, reversible and orally active LSD1 inhibitor, with anticancer effects.
-
Tiragolumab is an immune checkpoint inhibitor binding to TIGIT. Tiragolumab is effective against multiple solid malignancies.
-
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.
-
Panobinostat, a potent and orally active non-selective HDAC inhibitor, exhibits antineoplastic activities.
-
DD1, a proteasome inhibitor, targets Bax activation and P70S6K degradation during acute myeloid leukemia (AML) apoptosis.
-
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.
-
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.
-
PU-H54 is a potent purine-based (PU) Grp94-selective inhibitor. PU-H54 has the potential for the research of breast cancer.
-
Vamotinib is a novel, potent and selective BCR-ABL tyrosine kinase inhibitor that can induce apoptosis in chronic myelogenous leukemia cells.
-
BI-1622 is an orally active, potent and highly selective HER2 inhibitor, and shows antiproliferative and anti-tumor activity.
-
BNS-22 is a potent and selective inhibitor of TOP2α and TOP2β that exhibits anti-proliferative activities.
-
FL118 is a survivin inhibitor and a camptothecin analogue. FL118 has the potential for the research of cancer.
-
BM-1074 is a potent and specific Bcl-2 and Bcl-xL inhibitor and shows antiproliferative and anti-tumor activity.
-
MS159 is a frist-In-class nuclear receptor binding SET NSD2 PROTAC degrader for multiple myeloma research.
-
DC-S239 is a potent and selective SET7 Inhibitor, and DC-S239 shows antiproliferative activity for some cancer cells.
-
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.
-
AZD-9574 is a potent and brain penetrant PARP1 inhibitor and shows >8000-fold selectivity for PARP1 compared to PARP2/3/5a/6.
-
BLU2864 is an orally active ATP-competitive PRKACA inhibitor. BLU2864 can be used in cancer and polycystic kidney disease research.
-
SPH5030 is a potent, selective, irreversible and orally active HER2 Inhibitor and shows anti-cancer activity.
-
LCS3 is a potent and reversible inhibitor of GSR and TXNRD1 with anti-tumour activity by non-competitive inhibition of the enzyme activity.
-
EAI001 is a potent, selective mutant EGFR allosteric inhibitor. EAI001 has the potential for research on cancer.
-
G12Si-5, a potent, selective and reversible covalent inhibitor of the K-Ras G12S, can be used for the research of cancer.
-
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.
-
TK4g is a potent JAK inhibitor and can be used for studies of lymphatic-related diseases and leukemic cancers.
-
ARD-69 is a potent PROTAC androgen receptor degrader and induces degradation of AR protein in AR-positive prostate cancer cell lines.
-
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.
-
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.
-
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.
-
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.
-
Ficlatuzumab is a monoclonal antibody (McAb) targeting human hepatocyte growth factor (HGF) with potent anti-cancer activity.
-
Coleon-U-quinone is a potent P-gp inhibitor. It inhibits P-glycoprotein (P-gp) activity and reverts doxorubicin (DOX) resistance.
-
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.
-
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.
-
Zilovertamab is a humanised monoclonal antibody against ROR1 that blocks Wnt5a-induced ROR1 signalling.
-
CAM 833, a potent and selective inhibitor of the BRCA2-RAD51 interaction, and has the potential for the cancer research.
-
SOR-C13 is a high-affinity TRPV6 antagonist with an IC50 value of 14 nM. SOR-C13 is used for Advanced Solid Tumors Research
-
JNJ-9350 is an inhibitor of spermine oxidase (SMOX). JNJ-9350 also inhibits polyamine oxidase (PAO). JNJ-9350 has anti-cancer activity.
-
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
-
Serplulimab is a humanized monoclonal anti-PD-1 antibody and has the potential for the research of small cell lung cancer.
-
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.
-
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.
-
JBJ-09-063 is a mutant-selective allosteric EGFR inhibitor. JBJ-09-063 can be used for EGFR-mutant lung cancer research.
-
Abexinostat, a potent and broad-spectrum inhibitor of histone deacetylases, can be used for the research of cancer.
-
JS25 is a selective and covalent BTK inhibitor in hematological cancer. JS25 has blood brain barrier crossing property.
-
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.
-
Targefrin is a potent EphA2-targeting agent, acts as an antagonist, and can be used to research pancreatic cancer.
-
Mogamulizumab is an Anti-CCR4 monoclonal antibody. It enhances antibody-dependent cellular cytotoxicity and is effective against leukemia.
-
Olutasidenib (FT-2102) is an orally active, brain penetrant inhibitor of mutant IDH1. Olutasidenib is used for AML or MDS Research.
-
Mitonafide, a potent cytostatic agent, can inhibit DNA and RNA synthesis. Mitonafide is a potent antitumor agent.
-
Polatuzumab vedotin is an antibody-drug conjugate targeting CD79b and has the potential for the research of Large B-cell lymphomas (LBCL).
-
A947 is a selective SMARCA2 (PROTAC). A947 also is a moderately selective SMARCA2 degrader. A947 can be used for the research of cancer.
-
Adagrasib (MRTX849) is an orally available, and mutation-selective covalent inhibitor of KRAS G12C. Can be used for NSCLC research.
-
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.
-
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.
-
SJ988497 is a cell permeable PROTAC JAK2 degrader that degrades JAK2 in vitro and in vivo, and shows anticancer activity against leukemia.
-
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.
-
TD1092 is a pan-IAP degrader, degrades cIAP1, cIAP2, and XIAP. TD1092 inhibits NF-κB pathway and epithelial-mesenchymal transition (EMT).
-
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.
-
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.
-
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.
-
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.
-
Pegdinetanib (BMS-844203) is a selective VEGFR-2 inhibitor with antitumor activity.
-
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.
-
Opnurasib (JDQ-443) is a structurally novel, potent, and selective covalent oral inhibitor of KRAS G12C that exhibits antitumor activity.
-
BPDA2 is a competitive active site SHP2 inhibitor and suppresses SHP2-mediated signaling and breast cancer cell phenotypes.
-
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.
-
RLA-5331 is an iron activator containing anti-androgen. RLA-5331 is used for metastatic castrated tolerant prostate cancer (mCRPC) research.
-
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.
-
Cetuximab is a potent human anti-EGFR monoclonal antibody. Besides, Cetuximab also shows anti-tumor activity.
-
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.
-
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).
-
Izalontamab is an EGFR/HER3 Bi-specific monoclonal antibody. Besides, Izalontamab has the potential for the research of cancer.
-
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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Fluorescent Dye
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Antibodies
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Screening Libraries
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Reference Standards
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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-13030 | (+)-JQ-1 |
|
309
|
|
| HY-A0281 | 4-Phenylbutyric acid |
Lung Cancer
Breast Cancer
Liver Cancer
Leukemia/Lymphoma/Myeloma
Pancreatic Cancer
Viral Infection
SARS-CoV-2 Infection
|
262
|
|
| HY-15144 | Trichostatin A |
|
201
|
|
| HY-A0004 | Decitabine |
Decitabine (NSC 127716) is an orally active deoxycytidine analogue antimetabolite and DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell Apoptosis. Decitabine has potent anticancer activity.
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Pancreatic Cancer
Viral Infection
Digestive System Inflammation
Urogenital Cancer
Non-Small Cell Lung Cancer
Acute Myeloid Leukemia
SARS-CoV-2 Infection
Rheumatoid Arthritis
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183
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| HY-10221 | Vorinostat |
Vorinostat (SAHA) is a potent and orally active pan-inhibitor of HDAC1, HDAC2 and HDAC3 (Class I), HDAC6 and HDAC7 (Class II) and HDAC11 (Class IV), with ID50 values of 10 nM and 20 nM for HDAC1 and HDAC3, respectively. Vorinostat induces cell apoptosis. Vorinostat is also an effective inhibitor of human papillomaviruse (HPV)-18 DNA amplification.
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Neurological, Eye or Ear Disease
Breast Cancer
Prostate Cancer
Liver Cancer
Leukemia/Lymphoma/Myeloma
Pancreatic Cancer
Viral Infection
Digestive System Inflammation
Lung Fibrosis
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175
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| HY-10586 | 5-Azacytidine |
Lung Cancer
Prostate Cancer
Leukemia/Lymphoma/Myeloma
Pancreatic Cancer
Bacterial Infection
SARS-CoV-2 Infection
Rheumatoid Arthritis
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142
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| HY-N0005 | Curcumin |
Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin is a photosensitizer against microorganisms. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
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Histone Acetyltransferase
Epigenetic Reader Domain
Keap1-Nrf2
Autophagy
Mitophagy
Influenza Virus
Ferroptosis
Apoptosis
Prostate Cancer
Leukemia/Lymphoma/Myeloma
Pancreatic Cancer
Viral Infection
Pain
Digestive System Inflammation
Glucose Metabolism
Metastatic Breast Cancer
SARS-CoV-2 Infection
Obesity
Lung Fibrosis
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138
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| HY-13470 | GSK126 |
GSK126 (GSK2816126A) is a potent, highly selective inhibitor of EZH2 methyltransferase with an IC50 of 9.9 nM.
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105
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| HY-L005 | Epigenetics Compound Library |
Epigenetics refers to changes in phenotype that are not rooted in DNA sequence. Many types of epigenetic processes have been identified, including DNA methylation, alteration in the structure of histone proteins and gene regulation by small noncoding microRNAs. Modification of DNA, protein, or RNA, resulting in changes to the function and/or regulation of these molecules, without altering their primary sequences, reveals the complexities of cellular differentiation, embryology, the regulation of gene expression, aging, cancer, and other diseases.
MCE provide a unique collection of 2,031 epigenetics-related compounds that can be used in the research of the related diseases.
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102
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| HY-13803 | Tazemetostat |
Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat also inhibits EZH1 with an IC50 of 392 nM. Tazemetostat induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells.
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98
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| HY-12163 | Entinostat |
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95
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| HY-10224 | Panobinostat |
Panobinostat (LBH589; NVP-LBH589) is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities. Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells. Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma.
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Prostate Cancer
Liver Cancer
Leukemia/Lymphoma/Myeloma
Pancreatic Cancer
Viral Infection
Digestive System Inflammation
Small Cell Lung Cancer
Non-Small Cell Lung Cancer
HER-2 Positive Breast Cancer
Metastatic Breast Cancer
SARS-CoV-2 Infection
Lung Fibrosis
|
90
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| HY-L024 | Histone Modification Research Compound Library |
A histone modification, a covalent post-translational modification (PTM) to histone proteins, includes methylation, phosphorylation, acetylation, ubiquitylation, and sumoylation, etc. In general, histone modifications are catalyzed by specific enzymes that act predominantly at the histone N-terminal tails involving amino acids such as lysine or arginine, as well as serine, threonine, tyrosine, etc. The PTMs made to histones can impact gene expression by altering chromatin structure or recruiting histone modifiers. Histone modifications act in diverse biological processes such as transcriptional activation/inactivation, chromosome packaging, and DNA damage/repair. Deregulation of histone modification contributes to many diseases, including cancer and autoimmune diseases.
MCE owns a unique collection of 931 bioactive compounds targeting Epigenetic Reader Domain, HDAC, Histone Acetyltransferase, Histone Demethylase, Histone Methyltransferase, Sirtuin, etc. Histone Modification Research Compound Library is a useful tool for histone modification research and drug screening.
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85
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| HY-L034 | Anti-Aging Compound Library |
Aging is a complex biological process characterized by functional decline of tissues and organs, structural degeneration, and reduced adaptability and resistance, all of which contribute to an increase in morbidity and mortality caused by multiple chronic diseases, such as Alzheimer's disease, cancer, and diabetes. Many theories, which fall into two main categories: programmed and error theories, have been proposed to explain the process of aging, but neither of them appears to be fully satisfactory. The programmed theories imply that aging relies on specific gene regulation, and the error theories emphasize the internal and environmental damages accumulated to living organisms. The damage theories proposed the nine hallmarks that were generally considered to contribute to the aging process: genomic instability, telomere attrition, epigenetic alterations, loss of proteostasis, deregulated nutrient-sensing, mitochondrial dysfunction, cellular senescence, stem cell exhaustion, and altered intercellular communication.
MCE Anti-Aging Compound Library contains 7,771 compounds, mainly targeting Sirtuin, mTOR, IGF-1R, AMPK, p53, Telomerase, Mitophagy, Mitochondrial Metabolism, COX, Cytochrome P450, Oxidase, etc. This library is a useful tool for anti-aging research.
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84
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| HY-L080 | Targeted Therapy Drug Library |
Targeted cancer therapies are drugs or other substances that block the growth and spread of cancer by interfering with specific molecular targets that are involved in the growth, progression, and spread of cancer.
There are several different types of targeted therapy. The most common types are small-molecule drugs and monoclonal antibodies. Small-molecule drugs are small enough to enter cells easily, so they are used for targets that are inside cells, while monoclonal antibodies are usually used for targets that are located outside the cells. Because of high specificity, low side effect and potent anticancer activity, targeted therapy has become the mainstream of new anti-tumor drugs. Various targeted therapies have been approved by FDA and used in the treatment of diseases.
MCE carefully collects a unique of 106 targeted therapy drugs used in cancer treatment. MCE Targeted therapy drug library is a useful tool for the research of targeted therapy.
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84
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| HY-L005M | Epigenetics Compound Library Mini |
Epigenetics involves heritable phenotypic changes that occur without alterations to the underlying DNA sequence. Key mechanisms include DNA methylation, histone modifications, and regulation by small non-coding RNAs such as microRNAs. By modifying DNA, histones, or RNA—while leaving their primary sequences intact—these processes influence molecular function and regulation, thereby playing critical roles in cellular differentiation, embryonic development, gene expression control, aging, and diseases such as cancer.
MCE provide a unique collection of 295 epigenetics-related compounds. For each regulatory target and its subtype, 3 to 5 highly specific representative compounds have been retained, which can be used in epigenetic and related disease research.
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83
|
| HY-L039 | Reprogramming Compound Library |
Techniques for reprogramming somatic cells create new opportunities for drug screening, disease modeling, artificial organ development, and cell therapy. The development of reprogramming techniques has grown exponentially since Yamanaka reprogrammed somatic cells to become induced pluripotent stem cells (iPSCs) using four transcription factors, OCT4, SOX2, KLF4, and c-MYC in 2006. Despite the development of efficient reprogramming methods, most methods are inappropriate for clinical applications because they carry the risk of integrating exogenous genetic factors or use oncogenes. Alternative approaches, such as those based on miRNA, non-viral genes, non-integrative vectors, and small molecules, have been studied as possible solutions to the problems. Among these alternatives, small molecules are attractive options for clinical applications. Reprogramming using small molecules is inexpensive and easy to control in a concentration- and time-dependent manner. It offers a high level of cell permeability, ease of synthesis and standardization, and it is appropriate for mass-producing cells.
MCE Reprogramming Compound Library contains a unique collection of 3,231 compounds that act on reprogramming signaling pathways. These compounds are potential stimulators for reprogramming. This library is a useful tool for researching reprogramming and regenerative medicine.
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83
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| HY-L169 | Anti-Drug-Resistant Compound Library |
Resistance refers to the decrease in the effectiveness of drugs in treating diseases or symptoms. Due to the increasing global antibiotic resistance, it may threaten our ability to treat common infectious diseases. Drug resistance is also the main cause of chemotherapy failure in malignant tumors. In approximately 50% of cases, drug resistance exists even before chemotherapy begins. There are many mechanisms of anticancer drug resistance, including increased protein expression that leads to drug removal, mutations in drug binding sites, recovery of tumor protein production, and pre-existing genetic heterogeneity in tumor cell populations. In addition, the issue of drug resistance seems to have affected the development of new anticancer drugs. Drug resistance may be caused by various conditions, such as mutations, epigenetic modifications, and upregulation of drug efflux protein expression. Overcoming multidrug resistance in cancer treatment is becoming increasingly important.
MCE designs a unique collection of 706 anti-drug-resistant compounds. It is a good tool to be used for research on cancer and other diseases.
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83
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| HY-L203 | Methylation Compound Library |
Methylation is an epigenetic modification mechanism that involves adding methyl groups to molecules such as DNA and histones, which can alter gene expression without changing the DNA sequence. This process is catalyzed by enzymes such as DNA methyltransferases (DNMTs) and histone methyltransferases (HMTs), and can be reversed by demethylases.
The balance of methylation and demethylation is crucial for maintaining cellular function and genomic stability. Abnormal regulation of methylation may lead to a variety of diseases, including cancer, neurological disorders, and developmental abnormalities. A deep understanding of the molecular mechanisms of methylation metabolism is essential for developing therapeutic strategies for diseases associated with methylation dysregulation.
MCE contains 351 compounds targeting methylation/demethylation enzymes, which is of significant value for studying the pathways of methylation metabolism and exploring their mechanisms of action in diseases.
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83
|
| HY-L248 | RNA Binding Bioactive Compound Library |
The RNA-targeted bioactive compound library is a high-quality collection of small molecules specifically designed and curated to target RNA structures and functions. It is widely applied in cutting-edge drug discovery and life science research. Unlike traditional strategies that focus on protein targets, RNA-targeted compounds can directly modulate various functional RNA molecules by influencing their splicing, translation, stability, or structural conformation, thereby enabling precise intervention in key biological processes. In the field of drug development, these compounds provide a novel approach to addressing previously “undruggable” targets and have demonstrated significant potential in areas such as oncology, antiviral therapies, and neurodegenerative diseases. For example, by targeting disease-associated RNA structural domains or regulating the aberrant expression of non-coding RNAs, these compounds can effectively inhibit disease progression or restore normal cellular function. In mechanistic studies, RNA-targeted compounds serve as valuable chemical biology tools to elucidate the roles of RNA in gene expression regulation, cellular signaling pathways, and disease development.
The MCE RNA-targeted bioactive compound library contains 858 compounds, sourced from databases such as TargetRX Atlas and R-BIND. The library features excellent structural diversity and biological activity, making it suitable for high-throughput screening (HTS), target validation, phenotypic screening, and lead compound discovery. It represents a valuable resource for RNA-related research and innovative drug development.
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83
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| HY-L249 | Lactylation Compound Library |
Protein lactylation, an emerging post-translational modification identified in recent years, plays a critical role in linking cellular metabolic reprogramming, epigenetic regulation, and signaling networks. Based on a systematic framework encompassing lactate metabolism, lactylation, and downstream signaling pathways, this compound library comprehensively targets multiple regulatory layers, including histone modification enzymes (such as p300 and HDACs), key glycolytic enzymes (such as PKM2, LDHA, and GAPDH), transcriptional regulators (such as STAT3, HMGB1, and p53), as well as central signaling pathway nodes including HIF-1α, NF-κB, and PI3K-AKT-mTOR. This integrated design enables a comprehensive representation of the regulatory roles of lactylation across the “metabolism–epigenetics–signaling” axis.
MCE has assembled a collection of 6,182 known bioactive compounds and potential functional molecules, making this library suitable for a wide range of applications, including high-throughput drug screening, inhibitor identification, and mechanistic studies. It can be used to systematically evaluate the functional roles of lactylation in biological processes such as tumor metabolism, immune regulation, and inflammatory responses, and to efficiently identify small-molecule candidates with regulatory potential, thereby facilitating the development of innovative therapeutics targeting the interplay between metabolism and epigenetic regulation.
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83
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| HY-L250 | Lactic Acid Metabolite Compound Library |
In the progression of various diseases, metabolic reprogramming has emerged as a key hallmark. Lactate, as an important metabolic signaling molecule, is widely involved in tumorigenesis, immune regulation, and inflammatory responses. Particularly within the tumor microenvironment, the abnormal accumulation of lactate not only affects cellular energy metabolism but also promotes disease progression by modulating immune cell functions and mediating protein lactylation, thereby participating in epigenetic regulation and signaling networks. Therefore, systematic investigation of lactate metabolic pathways and their associated metabolites is of great significance for understanding disease mechanisms and developing novel therapeutic strategies.
The MCE lactic acid metabolite compound library contains 61 compounds and is constructed around key metabolic pathways involving lactate production, transport, and utilization. This library systematically includes core intermediates from glycolysis, the tricarboxylic acid (TCA) cycle, and the lactate cycle. Focusing on disease-associated metabolic reprogramming, it is suitable for research in oncology, inflammation, and metabolic disorders. The library can be used to elucidate the roles of lactate in tumor microenvironment regulation, immune evasion, and epigenetic modifications (such as protein lactylation). In addition, it provides high-quality small-molecule resources for drug screening, facilitating the discovery of potential modulators targeting key enzymes (such as LDH) or transporters (such as MCTs) involved in lactate metabolism.
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83
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| HY-L253 | Fungal-Sourced Compound Library |
For thousands of years, natural products have always been an important source for drug discovery. Fungi, due to their unique and diverse secondary metabolic capabilities, have become a valuable resource for natural active molecules. Since the discovery of penicillin, natural products derived from fungi have demonstrated significant application value in areas such as anti-infection, anti-tumor, immune regulation, and metabolic disease research. A large number of clinical drugs, such as antibiotics, immunosuppressants, and lipid-lowering drugs, are derived from fungal metabolites or their structurally optimized derivatives.
MCE fungal-derived compound library contains 91 structurally diverse and bioactive fungal natural products and their derivatives. It can be widely applied in various research fields such as antibacterial, anti-tumor, anti-inflammatory, immune regulation, epigenetics, and cell signaling pathways, providing high-quality tools for natural product drug development and high-throughput 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-15149 | Romidepsin |
Romidepsin (FK 228) is a Histone deacetylase (HDAC) inhibitor with anti-tumor activities. Romidepsin (FK 228) inhibits HDAC1, HDAC2, HDAC4, and HDAC6 with IC50s of 36 nM, 47 nM, 510 nM and 1.4 μM, respectively. Romidepsin (FK 228) is produced by Chromobacterium violaceum, induces cell G2/M phase arrest and apoptosis.
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75
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| HY-10585A | Valproic acid sodium |
Valproic acid (Sodium Valproate) sodium is an orally active HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium is used in the treatment of epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches.
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70
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| HY-10585 | Valproic acid |
Valproic acid (VPA) is an orally active HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM. Valproic acid inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid is used in the epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches.
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Infection
Neurological, Eye or Ear Disease
Metabolic or Endocrine Disease
Respiratory Disease
Small Cell Lung Cancer
|
70
|
| HY-B2227 | Lactic acid |
Lactic acid (DL-Lactic acid) is a hydroxycarboxylic acid receptor 1 (HCAR1) activator and an epigenetic modulator inducing lysine residues lactylation. Lactic acid is a glycolysis end-product, bridging the gap between glycolysis and oxidative phosphorylation. Lactic acid is an oncometabolite and has immune protective role of lactate in anti-tumor immunity. Lactic acid also has antimicrobial activity, which can be used as a food preservative.
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67
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| HY-W250163 | NAD+ lithium |
NAD+ lithium (β-DPN lithium) is a lithium salt of nicotinamide adenine dinucleotide. NAD+ is a coenzyme in the REDOX reaction. NAD+ can directly or indirectly affect several key cellular functions, including metabolic pathways, DNA repair, chromatin remodeling, cell aging, and immune cell function.
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52
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| HY-119374 | BRM/BRG1 ATP Inhibitor-1 |
BRM/BRG1 ATP Inhibitor-1 (compound 14) is an orally active allosteric dual brahma homolog (BRM)/SWI/SNF related matrix associated actin dependent regulator of chromatin subfamily A member 2 (SMARCA2) and brahma related gene 1 (BRG1)/SMARCA4 ATPase activity inhibitor, both IC50s are below 0.005 µM. BRM/BRG1 ATP Inhibitor-1 has anticancer activity.
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42
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| HY-10442 | 3-Deazaneplanocin A |
3-Deazaneplanocin A (DZNep) is a potent histone methyltransferase EZH2 inhibitor. 3-Deazaneplanocin A is a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor. 3-Deazaneplanocin A shows anti-orthopoxvirus activity.
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Respiratory Disease
Leukemia/Lymphoma/Myeloma
Glucose Metabolism
Non-Small Cell Lung Cancer
Orthopoxvirus Infection
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37
|
| HY-112288 | C188-9 |
C188-9 (TTI-101) is a STAT3 inhibitor with a Kd value of 4.7 nM. C188-9 targets the SH2 domain of STAT3, blocks the processes of STAT3 ligand binding, receptor recruitment, homodimerization and phosphorylation, and regulates STAT3-mediated genes associated with tumorigenesis and radioresistance. C188-9 regulates STAT1-mediated genes related to radioresistance and reduces the activation level of STAT1. C188-9 downregulates the expression of DNMT1, enhances DAC-induced demethylation and re-expression of RASSF1A, and simultaneously potentiates the anti-tumor effect of DAC on pancreatic cancer cells. C188-9 inhibits both anchorage-dependent and anchorage-independent growth of cancer cells, induces Apoptosis, blocks the growth of tumor xenografts, and suppresses muscle atrophy. C188-9 maintains muscle mass, increases body weight and improves grip strength in tumor-bearing mice. C188-9 can be used in research related to head and neck squamous cell carcinoma, pancreatic cancer, sepsis-related skeletal muscle wasting, non-small cell lung cancer, acute myeloid leukemia and cancer cachexia.
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Lung Cancer
Breast Cancer
Prostate Cancer
Liver Cancer
Leukemia/Lymphoma/Myeloma
Pancreatic Cancer
Digestive System Inflammation
Obesity
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37
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| HY-13500 | GSK343 |
GSK343, a chemical probe, is a highly potent and selective EZH2 inhibitor with an IC50 of 4 nM.
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33
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| HY-101563 | Pemrametostat |
GSK3326595 is a protein arginine methyltransferase 5 (PRMT5) inhibitor. GSK3326595 decreases SARS-CoV-2 infection, inhibits cancer cell proliferation and induces pro-inflammatory macrophage polarization and increases hepatic triglyceride levels without affecting atherosclerosis. GSK3326595 can be used for research of relapsed/refractory mantle cell lymphoma.
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Leukemia/Lymphoma/Myeloma
Pancreatic Cancer
Viral Infection
HER-2 Positive Breast Cancer
SARS-CoV-2 Infection
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33
|
| HY-15593 | Pinometostat |
Pinometostat (EPZ-5676) is a potent DOT1L histone methyltransferase inhibitor with a Ki of 80 pM.
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33
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| HY-111558A | Bobcat339 hydrochloride |
Bobcat339 hydrochloride is a potent and selective cytosine-based inhibitor of TET enzyme, with the IC50s of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 hydrochloride is useful to the field of epigenetics and serves as a starting point for new therapeutics that target DNA methylation and gene transcription.
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29
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| HY-111558 | Bobcat339 |
Bobcat339 is a potent and selective cytosine-based inhibitor of TET enzyme, with IC50s of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 is useful to the field of epigenetics and serves as a starting point for new therapeutics that target DNA methylation and gene transcription.
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29
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| HY-B0350A | Sodium butyrate |
Sodium butyrate ((Butanoic acid; Butyric acid) sodium) is an orally active HDAC inhibitor. Sodium butyrate induces hyperacetylation of core histones and affects phosphorylation of H1/H2A, thereby altering chromatin structure and regulating gene expression. Sodium butyrate can be used in research related to various cancers, inflammatory bowel disease, and sickle cell anemia.
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28
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| HY-10587 | BIX-01294 |
BIX-01294 is a reversible and highly selective G9a and GLP Histone Methyltransferase inhibitor, with IC50s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 has antitumor activity in recurrent tumor cells.
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27
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| HY-135146 | GSK-3484862 |
GSK-3484862 is a highly potent non-covalent inhibitor and demethylating agent of DNMT1. GSK-3484862 induces genome-wide DNA demethylation, including the regulatory elements of DNMT3B and the promoter region of TERT, and significantly inhibits cell viability, growth, proliferation and self-renewal. GSK-3484862 blocks the transformation of young AT2 cells, induces apoptosis, and generates transcriptomic features similar to those of senescent cells. GSK-3484862 is widely used in studies related to lung cancer, oral squamous cell carcinoma and lung adenocarcinoma.
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26
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| HY-B2227D | Calcium 2-hydroxypropanoate pentahydrate |
Calcium 2-hydroxypropanoate (pentahydrate) is a hydroxycarboxylic acid receptor 1 (HCAR1) activator and an epigenetic modulator inducing lysine residues lactylation. Calcium 2-hydroxypropanoate (pentahydrate) is a glycolysis end-product, bridging the gap between glycolysis and oxidative phosphorylation. Calcium 2-hydroxypropanoate (pentahydrate) is an oncometabolite and has immune protective role of lactate in anti-tumor immunity.
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20
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| HY-13962 | SGI-1027 |
SGI-1027 is a DNA methyltransferase (DNMT) inhibitor, with IC50s of 7.5 μM, 8 μM, and 12.5 μM for DNMT3B, DNMT3A, and DNMT1 with poly(dI-dC) as substrate.
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Digestive System Disease
Leukemia/Lymphoma/Myeloma
Digestive System Inflammation
Rheumatoid Arthritis
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20
|
| HY-13642 | RG108 |
RG108 (N-Phthalyl-L-tryptophan) is a non-nucleoside DNA methyltransferases (DNMTs) inhibitor (IC50=115 nM) that blocks the DNMTs active site. RG108 (N-Phthalyl-L-tryptophan) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences.
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15
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| HY-145388 | AU-15330 |
AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4. AU-15330 induces potent inhibition of tumour growth in xenograft models of prostate cancer and synergizes with the AR antagonist enzalutamide. AU-15330 induces disease remission in castration-resistant prostate cancer (CRPC) models without toxicity.
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15
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| HY-139664 | GSK-3685032 |
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15
|
|
| HY-13765 | 6-Thioguanine |
6-Thioguanine (Thioguanine; 2-Amino-6-purinethiol) is an anti-leukemia and immunosuppressant agent, acts as an inhibitor of SARS and MERS coronavirus papain-like proteases (PLpros) and also potently inhibits USP2 activity, with IC50s of 25 μM and 40 μM for Plpros and recombinant human USP2, respectively.
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Digestive System Disease
Leukemia/Lymphoma/Myeloma
Viral Infection
Digestive System Inflammation
SARS-CoV-2 Infection
Rheumatoid Arthritis
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14
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| HY-128359 | ACBI1 |
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11
|
|
| HY-136328 | EZM0414 TFA |
EZM0414 (SETD2-IN-1) TFA is the TFA salt form of EZM0414 (HY-144858). EZM0414 TFA is a potent, selective, orally active inhibitor of SETD2 (IC50=18 nM in SETD2 biochemical assay; IC50=34 nM in cellular assay). EZM0414 TFA can be used for the research of relapsed or refractory multiple myeloma and diffuse large B-cell lymphoma.
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10
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| HY-W396714 | Succinic acid sodium |
Succinic acid sodium is a potent and orally active anxiolytic agent. Succinic acid sodium shows inhibitory effects on colonic epithelial cell proliferation in vivo. Succinic acid sodium can down-regulate the expression of KCNMB1 (potassium channel subunit β1) and TET1 (ten?eleven translocation 1). Succinic acid sodium can be used for gestational hypertension research.
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7
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| HY-N0739 | Betaine chloride |
Betaine chloride is a natural compound found in many foods and also an active methyl-donor which can maintain normal DNA methylation patterns.
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7
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| HY-B0710 | Betaine |
Betaine (Trimethylglycine) is a natural compound found in many foods and also an active methyl-donor which can maintain normal DNA methylation patterns. Betaine is found ubiquitously in plants, animals, microorganisms, and rich dietary sources including seafood, spinach, and wheat bran. Betaine also acts as an osmolyte, to maintain the avian’s cellular water and ion balance to improve the avian’s capacity against heat stress via preventing dehydration and osmotic inactivation. It helps in maintaining the protective osmolytic activity, especially in heat-stressed birds. Betaine may promote various intestinal microbes against osmotic variations and thus improve microbial fermentation activity.
Source: Widespread |
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7
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| HY-12409 | PFI-3 |
PFI-3, a chemical probe, is a selective, potent and cell-permeable SMARCA2/4 bromodomain inhibitor with a Kd of 89 nM.
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5
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| HY-109108 | Valemetostat |
Valemetostat (DS-3201), a first-in-class EZH1/2 dual inhibitor with IC50 values <10 nM. Valemetostat can be used for the research of relapsed/refractory peripheral T-cell lymphoma.
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5
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| HY-139611 | Navlimetostat |
Navlimetostat is a potent, orally active, selective PRMT5-MTA complex inhibitor, with IC50 of 3.6 and 20.5 nM for PRMT5-MTA and PRMT5. Navlimetostat binds to the PRMT5-MTA complex, with KD value of 0.14 pM. Navlimetostat shows antineoplastic activity in vitro and in vivo, and can be used for cancer study.
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4
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| HY-W012078 | 5-Methyl-2'-deoxycytidine |
5-Methyl-2'-deoxycytidine (5mdC) is an endogenous substrate of DNA methyltransferases (such as mammalian 5-C-MTase) and binds to DNA dependent on the formation of DNA stem-loop structures. 5-Methyl-2'-deoxycytidine guides de novo DNA methylation by acting as a methylation mark and activates the methylation of adjacent CpG sites in single-stranded DNA through cis action. 5-Methyl-2'-deoxycytidine regulates DNA methylation patterns by recruiting methyltransferases to specific chromatin regions, affecting chromatin condensation and gene expression. Its distribution in plant cells is related to cell proliferation and differentiation stages. The methylation level of 5-Methyl-2'-deoxycytidine is low in proliferating cells and high in differentiated cells.
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3
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| HY-N0005R | Curcumin (Standard) |
Curcumin (Standard) is the analytical standard of Curcumin (HY-N0005). This product is intended for research and analytical applications. Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin is a photosensitizer against microorganisms. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
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Reference Standards
Histone Acetyltransferase
Epigenetic Reader Domain
Keap1-Nrf2
Autophagy
Mitophagy
Influenza Virus
Ferroptosis
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3
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| HY-I0626 | Cytosine |
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3
|
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| HY-144835 | Camibirstat |
FHD-286 is a selective, oral inhibitor of SMARCA4/SMARCA2 ATPase (BRG1 and BRM) inhibitor. FHD-286 has the potential for the research of BAF (BRG1/BRM-associated factor)-related disorders such as acute myeloid leukemia.
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3
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| HY-W008091R | 5-Methylcytosine (Standard) |
5-Methylcytosine (Standard) is the analytical standard of 5-Methylcytosine (HY-W008091). This product is intended for research and analytical applications. 5-Methylcytosine is a well-characterized DNA modification in prokaryotes and eukaryotes. 5-Methylcytosine forms symmetrical methylation on CpG dinucleotides in DNA, stabilizes tRNA/rRNA structure in RNA, and affects mRNA translation. 5-Methylcytosine can be oxidized to generate 5hmC, 5fC, and 5caC. 5-Methylcytosine can be used in epigenetics, developmental biology, and the study of diseases such as colorectal cancer and hepatocellular carcinoma.
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2
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| HY-W008091 | 5-Methylcytosine |
5-Methylcytosine is a well-characterized DNA modification in prokaryotes and eukaryotes. 5-Methylcytosine forms symmetrical methylation on CpG dinucleotides in DNA, stabilizes tRNA/rRNA structure in RNA, and affects mRNA translation. 5-Methylcytosine can be oxidized to generate 5hmC, 5fC, and 5caC. 5-Methylcytosine can be used in epigenetics, developmental biology, and the study of diseases such as colorectal cancer and hepatocellular carcinoma.
Source: prokaryotes and eukaryotes |
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2
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| HY-144896 | FHT-1015 |
FHT-1015 is a selective SMARCA4 (IC50 = 4 nM) and SMARCA2 (IC50 = 5 nM) (also known as BRG1 and BRM) inhibitor. FH-1015 is an allosteric inhibitor that causes conformation change in the BRG1/BRM protein upon interaction with an allosteric site, inhibiting ATPase activity. FH-1015 interferes with tumor cell growth and migration. FH-1015 can be studied in research for uveal melanoma and hematologic cancer.
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2
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| HY-163410 | AU-24118 |
AU-24118 is an orally active PROTAC degrader that recruits cereblon to target the degradation of SMARCA2, SMARCA4 and PBRM1. AU-24118 impairs the chromatin accessibility of oncogenic transcription factors, inhibits colony formation, dislodges chromatin-bound transcription factors, attenuates downstream signal transduction, induces apoptosis, and exerts antiproliferative and cytotoxic effects. AU-24118 can be used in research related to castration-resistant prostate cancer, colorectal cancer, small cell lung cancer and multiple myeloma (including the t (4;14) subtype).
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2
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| HY-158301 | MY-1B |
MY-1B is a covalent inhibitor of the RNA Methyltransferase NSUN2 (IC50: 1.3 μM). MY-1B stereoselectively ligands active-site cysteine residues (C271) of NSUN2. MY-1B can stereoselectively and covalently bind to PSME1, disrupting the proteasome regulatory complex and downregulating the presentation of specific MHC-I subtypes.
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2
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| HY-120395 | UC-514321 |
UC-514321, a structural analog of NSC370284 with higher activity, directly targets STAT3/5 and represses TET1 expression, but not TET2 or TET3. UC-514321 has the potential to treat acute myeloid leukemia (AML) both in vitro and in vivo, with low toxicity.
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Lung Cancer
Breast Cancer
Prostate Cancer
Liver Cancer
Leukemia/Lymphoma/Myeloma
Pancreatic Cancer
Digestive System Inflammation
Obesity
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1
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| HY-160638 | NSC-311068 |
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1
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| HY-143711S | Trimethyllysine-d9 |
Trimethyllysine-d9 is the deuterium labeled Trimethyllysine (HY-143711). Trimethyllysine is an important post-translationally modified amino acid, involving in carnitine biosynthesis and epigenetic processes.
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1
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| HY-P1108 | Astressin 2B |
Astressin 2B is a blood-brain barrier-impermeable, highly selective CRFR2 antagonist (rCRFR2, IC50=0.57 nM). Astressin 2B blocks the protective effects mediated by CRFR2, thereby exacerbating indomethacin (HY-14397)-induced hemorrhagic intestinal injury in rats. Astressin 2B reverses the protective effects of Urocortin 1 against intestinal hypermotility, bacterial invasion and upregulation of inflammatory mediators. Astressin 2B also blocks the anxiogenic effect of Urocortin 2 and attenuates stress-induced anxiety-related behaviors. In the Clostridioides difficile toxin A (C. difficile toxin A)-mediated enteritis model, Astressin 2B mimics the phenotype of CRFR2-deficient mice, significantly exacerbating intestinal epithelial damage, edema, neutrophil migration and the expression of multiple proinflammatory cytokines. Astressin 2B is an important tool molecule for investigating the intestinal protective mechanisms of CRFR2.
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1
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| HY-A0248A | Polymyxin B1 |
Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment.
Source: Bacilus polymyxa |
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1
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| HY-122258 | NSC-370284 |
Lung Cancer
Breast Cancer
Prostate Cancer
Liver Cancer
Leukemia/Lymphoma/Myeloma
Pancreatic Cancer
Obesity
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1
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| HY-P1108A | Astressin 2B TFA |
Astressin 2B TFA is a blood-brain barrier-impermeable, highly selective CRFR2 antagonist (rCRFR2, IC50=0.57 nM). Astressin 2B TFA blocks the protective effects mediated by CRFR2, thereby exacerbating indomethacin (HY-14397)-induced hemorrhagic intestinal injury in rats. Astressin 2B TFA reverses the protective effects of Urocortin 1 against intestinal hypermotility, bacterial invasion and upregulation of inflammatory mediators. Astressin 2B TFA also blocks the anxiogenic effect of Urocortin 2 and attenuates stress-induced anxiety-related behaviors. In the Clostridioides difficile toxin A (C. difficile toxin A)-mediated enteritis model, Astressin 2B TFA mimics the phenotype of CRFR2-deficient mice, significantly exacerbating intestinal epithelial damage, edema, neutrophil migration and the expression of multiple proinflammatory cytokines. Astressin 2B TFA is an important tool molecule for investigating the intestinal protective mechanisms of CRFR2.
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1
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| HY-12303 | OAC1 |
OAC1 is a potent Oct4 activator. OAC1 activates Oct4 and Nanog promoters and enhances induced pluripotent stem cells (iPSC) formation. OAC1 activates OCT4 through upregulation of HOXB4 expression. OAC1 increases transcription of the Oct4-Nanog-Sox2 triad and TET1. OAC1 facilitates the reprogramming of cells by enhancing efficiency and shortening the reprogramming time.
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1
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| HY-145446 | SGC-SMARCA-BRDVIII |
SGC-SMARCA-BRDVIII, a chemical probe, is a potent and selective inhibitor of SMARCA2/4 and PB1(5), with Kds of 35 nM, 36 nM, and 13 nM, respectively. SGC-SMARCA-BRDVIII also inhibits PB1(2) and PB1(3), with Kds of 3.7 and 2.0 μM, respectively. SGC-SMARCA-BRDVIII can block adipogenesis of 3T3-L1 murine fibroblasts.
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1
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| HY-151623 | ACBI2 |
ACBI2 is a highly potent and orally active VHL PROTAC SMARCA2 degrader (EC50: 7 nM), which selectively degrades SMARCA2 with a DC50 value of 1 nM in RKO cells. ACBI2 can be used in the research of lung cancer.
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1
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| HY-113061 | Pseudouridine |
Pseudouridine is an isomer of uridine and the most abundant modified nucleoside in non-coding RNA. It fine-tunes and stabilizes regional structures in rRNA and tRNA, maintaining their functions in mRNA decoding, ribosome assembly, processing, and translation.
Pseudouridine-modified tRNA fragments can inhibit aberrant protein synthesis and hold promise for research on myelodysplastic syndrome (MDS)-related leukemia..
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1
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| HY-402410 | TETi76 |
TETi76 is an orally active TET family inhibitor with IC50 values ??of 1.5, 9.4 and 8.8 μM for TET1, TET2 and TET3, respectively. TETi76 competitively binds to the active site of TET enzymes, reduces cytosine hydroxymethylation and restricts clonal growth of TET2 mutants in vitro and in vivo, but does not affect the growth of normal hematopoietic precursor cells. TETi76 can be used for leukemia research.
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1
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| HY-134124 | Glutathione ethyl ester |
Glutathione ethyl ester is a cell-permeable GSH donor and provides an efficient supply of GSH to the oocyte. Glutathione ethyl ester shows positive effect on the in vitro production of embryos by enhancement of the antioxidative defense.
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1
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| HY-W768571 | Pseudouridine-13C,15N2 |
Pseudouridine-13C,15N2 is the 13C- and 15N-labeled Pseudouridine (HY-113061). Pseudouridine is an isomer of uridine and the most abundant modified nucleoside in non-coding RNA. It fine-tunes and stabilizes regional structures in rRNA and tRNA, maintaining their functions in mRNA decoding, ribosome assembly, processing, and translation. Pseudouridine-modified tRNA fragments can inhibit aberrant protein synthesis and hold promise for research on myelodysplastic syndrome (MDS)-related leukemia..
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| HY-114346A | BODIPY FL EDA free base |
ODIPY FL EDA free base is an amine-based, green fluorescent probe. The R-NH2 of ODIPY FL EDA free base can be coupled with aldehydes or ketones to form reversible Schiff base products. Convert to stable amine derivatives using reducing agents such as sodium borohydride or sodium cyanoborohydride. ODIPY FL EDA free base can be used to detect modified or normal deoxynucleotides and demonstrate DNA damage and genomic DNA methylation.
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| HY-P3035 | Corazonin |
Corazonin is a highly conserved neuropeptide hormone of wide-spread occurrence in insects, serves a central regulator of caste identity and behavior in social insects. Corazonin is also preferentially expressed in workers and/or foragers from other social insect species.
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| HY-A0067S1 | Oxybenzone-13C6 |
Oxybenzone-13C6 (Benzophenone 3-13C6) is the 13C-labeled Oxybenzone (HY-A0067). Oxybenzone (Benzophenone 3) is a commonly used UV filter in sun tans and skin protectants. Oxybenzone act as endocrine disrupting chemicals (EDCs) and can pass through the placental and blood-brain barriers. Benzophenone-3 impairs autophagy, alters epigenetic status, and disrupts retinoid X receptor signaling in apoptotic neuronal cells.
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| HY-P10111A | Histone H3K9me3 (1-15) TFA |
Histone H3K9me3 (1-15) (H3(1-15)K9me3) TFA is used as substrate. Histone H3K9me3 is a histone posttranslational modification (PTM) that has emerged as hallmark of pericentromeric heterochromatin.
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| HY-113061S | Pseudouridine-O18 |
Pseudouridine-18O is the 18O labeled Pseudouridine (HY-113061). Pseudouridine is an isomer of the nucleoside uridine, and the most abundant modified nucleoside in non-coding RNAs. Pseudouridine in rRNA and tRNA can fine-tune and stabilize the regional structure and help maintain their functions in mRNA decoding, ribosome assembly, processing and translation.
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| HY-135146G | GSK-3484862 (GMP) |
GSK-3484862 GMP is GSK-3484862 (HY-135146) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. GSK-3484862 is a highly potent non-covalent inhibitor and demethylating agent of DNMT1. GSK-3484862 induces genome-wide DNA demethylation, including the regulatory elements of DNMT3B and the promoter region of TERT, and significantly inhibits cell viability, growth, proliferation and self-renewal. GSK-3484862 blocks the transformation of young AT2 cells, induces apoptosis, and generates transcriptomic features similar to those of senescent cells. GSK-3484862 is widely used in studies related to lung cancer, oral squamous cell carcinoma and lung adenocarcinoma.
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| HY-W653958 | Oxybenzone-d3 |
Oxybenzone-d3 (Benzophenone 3-d3) is a deuterium labeled Oxybenzone (HY-A0067). Oxybenzone (Benzophenone 3) is a commonly used UV filter in sun tans and skin protectants. Oxybenzone act as endocrine disrupting chemicals (EDCs) and can pass through the placental and blood-brain barriers. Benzophenone-3 impairs autophagy, alters epigenetic status, and disrupts retinoid X receptor signaling in apoptotic neuronal cells.
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| HY-P10563 | Noraramtide |
Noraramtide (BHV-1100) is an antibody-recruiting molecule. Noraramtide binds to CD38 and recruits natural killer (NK) cells to mediate antibody-dependent cellular cytotoxicity. Noraramtide enhances the capacity of autologous cytokine-induced memory-like (CIML) NK cells to produce IFNγ and CD107a, thereby improving their cytotoxicity against multiple myeloma cells. Noraramtide can be used in the research of multiple myeloma.
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| HY-P10828 | MAPI |
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| HY-13642G | RG108 (GMP) |
RG108 (GMP) is RG108 (HY-13642) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. RG108 (N-Phthalyl-L-tryptophan) is a non-nucleoside DNA methyltransferases (DNMTs) inhibitor (IC50=115 nM) that blocks the DNMTs active site. RG108 (N-Phthalyl-L-tryptophan) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences.
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| HY-I0626S | Cytosine-13C2,15N3 |
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| HY-W769991 | Lactate sodium-13C2 |
Lactic acid-13C2 (DL-Lactic acid-13C2) sodium is the 13C-labeled Lactic acid sodium . Lactic acid (DL-Lactic acid) sodium is a hydroxycarboxylic acid receptor 1 (HCAR1) activator and an epigenetic modulator inducing lysine residues lactylation. Lactic acid sodium is a glycolysis end-product, bridging the gap between glycolysis and oxidative phosphorylation. Lactic acid sodium is an oncometabolite and has immune protective role of lactate in anti-tumor immunity. Lactic acid sodium also has antimicrobial activity, which can be used as a food preservative.
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| HY-W004924S | 5-Hydroxymethyluracil-d3 |
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| HY-P3822 | PRMT5-IN-23 |
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| HY-113352S | 7-Methylguanine-d3 |
7-Methylguanine-d3 is the deuterium labeled 7-Methylguanine. 7-Methylguanine is a metabolite of DNA methylation. It can be generated by methylating agents, and used as a probe of protein–DNA interactions and a key component of DNA sequencing method.
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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-P10111 | Histone H3K9me3 (1-15) |
Histone H3K9me3 (1-15) (H3(1-15)K9me3) is a histone posttranslational modification (PTM) that has emerged as hallmark of pericentromeric heterochromatin. Trimethylation of histone H3 at lysine 9 is associated with gene repression, prevents transcription factor binding.
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| HY-W653970 | 5-Azacytidine-15N4 |
5-Azacytidine-15N4 is 13C and 15N labeled 5-Azacytidine. 5-Azacytidine (Azacitidine; 5-AzaC; Ladakamycin) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation. 5-Azacytidine is incorporated into DNA to covalently trap DNA methyltransferases and contributes to reverse epigenetic changes. 5-Azacytidine induces cell autophagy.
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Isotope-Labeled Compounds
Organoid
Bacterial
DNA Methyltransferase
Nucleoside Antimetabolite/Analog
Antibiotic
Autophagy
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| HY-13599S2 | Cladribine-15N |
Cladribine-15N (2-Chloro-2′-deoxyadenosine-15N) is 15N labeled Cladribine. Cladribine (2-Chloro-2′-deoxyadenosine), a purine nucleoside analog, is an orally active adenosine deaminase inhibitor. Cladribine functions as an inhibitor of DNA synthesis to block the repair of the damaged DNA. Cladribine can inhibit DNA methylation. Cladribine has anti-lymphoma activity. Cladribine can be used for the research of several hematologic malignancies and multiple sclerosis.
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| HY-N0005S1 | Curcumin-d3 |
Curcumin-d3 (Diferuloylmethane-d3 ) is deuterium labeled Curcumin (HY-N0005). Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin is a photosensitizer against microorganisms. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
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Isotope-Labeled Compounds
Keap1-Nrf2
Epigenetic Reader Domain
Histone Acetyltransferase
Mitophagy
Autophagy
Influenza Virus
Ferroptosis
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| HY-13599S | Cladribine-d4 |
Cladribine-d4 (2-Chloro-2′-deoxyadenosine-d4) is deuterium labeled Cladribine. Cladribine (2-Chloro-2′-deoxyadenosine), a purine nucleoside analog, is an orally active adenosine deaminase inhibitor. Cladribine functions as an inhibitor of DNA synthesis to block the repair of the damaged DNA. Cladribine can inhibit DNA methylation. Cladribine has anti-lymphoma activity. Cladribine can be used for the research of several hematologic malignancies and multiple sclerosis.
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| HY-W018324S | 5-Hydroxymethylcytosine-13C,d2 |
5-Hydroxymethylcytosine-13C,d2 is the 13C and deuterium labeled 5-Hydroxymethylcytosine (HY-W018324). 5-Hydroxymethylcytosine (5hmC) is an oxidized forms of 5-methylcytosine (5mC) in mammalian DNA. 5-Hydroxymethylcytosine is produced from 5mC in an enzymatic pathway involving three 5mC oxidases, Ten-eleven translocation (TET)1, TET2, and TET3. The conversion of 5mC into 5hmC can be the first step in a pathway leading towards DNA demethylation. 5-Hydroxymethylcytosine is associated with gene transcription and frequently used as a mark to investigate dynamic DNA methylation conversion during mammalian development. 5-Hydroxymethylcytosine can be used for the study of non-small cell lung cancer (NSCLC), neurodegenerative diseases (Alzheimer’s, Parkinson’s) and hematological malignancies (acute myeloid leukemia, myelodysplastic syndromes).
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| HY-13599S1 | Cladribine-13C5,15N2 |
Cladribine-13C5,15N2 (2-Chloro-2′-deoxyadenosine-13C5,15N2) is 13C and 15N labeled Cladribine. Cladribine (2-Chloro-2′-deoxyadenosine), a purine nucleoside analog, is an orally active adenosine deaminase inhibitor. Cladribine functions as an inhibitor of DNA synthesis to block the repair of the damaged DNA. Cladribine can inhibit DNA methylation. Cladribine has anti-lymphoma activity. Cladribine can be used for the research of several hematologic malignancies and multiple sclerosis.
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| HY-W004924R | 5-Hydroxymethyluracil (Standard) |
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| HY-P11094 | Tet1-Cys peptide |
Tet1-Cys peptide is a peptide with the sequence HLNILSTLWKYRC. Tet1 (HLNILSTLWKYR) (HY-P10998) can specifically bind to the neuronal ganglioside receptor GT1b, possessing neuronal targeting capabilities. The Tet1-Cys peptide sequence has an added Cys, which can be used for drug conjugation for research on drug delivery.
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| HY-N0739R | Betaine chloride (Standard) |
Betaine (chloride) (Standard) is the analytical standard of Betaine (chloride). This product is intended for research and analytical applications. Betaine hydrochloride is a natural compound found in many foods and also an active methyl-donor which can maintain normal DNA methylation patterns.
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| HY-P10998 | Tet1 peptide |
Tet1 peptide is a peptide that specifically binds to neurons. Tet1 peptide binds to GT1B ganglioside and trisialoganglioside clostridial toxin receptor on the surface of neuronal cells, and can be used in peptide conjugation and drug delivery research.
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| HY-P3066 | SKF 100398 |
SKF 100398 (d(CH2)5Tyr(Et)VAVP), an arginine vasopressin (AVP) analogue, is a specific antagonist of the antidiuretic effect of exogenous and endogenous AVP.
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| HY-I0626S1 | Cytosine-13C,15N2 |
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| HY-A0248AS | Polymyxin B1-d7 TFA |
Polymyxin B1-d7 TFA is the deuterium labeled Polymyxin B1 TFA (HY-A0248A). Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment.
Source: Bacilus polymyxa |
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| HY-W740027 | 5-Methyl-2'-deoxycytidine-d3 |
5-Methyl-2'-deoxycytidine-d3 (5-Methyldeoxycytidine-d3) is the deuterium labeled Methyl-2'-deoxycytidine (HY-W012078). 5-Methyl-2'-deoxycytidine (5mdC) is an endogenous substrate of DNA methyltransferases (such as mammalian 5-C-MTase) and binds to DNA dependent on the formation of DNA stem-loop structures. 5-Methyl-2'-deoxycytidine guides de novo DNA methylation by acting as a methylation mark and activates the methylation of adjacent CpG sites in single-stranded DNA through cis action. 5-Methyl-2'-deoxycytidine regulates DNA methylation patterns by recruiting methyltransferases to specific chromatin regions, affecting chromatin condensation and gene expression. Its distribution in plant cells is related to cell proliferation and differentiation stages. The methylation level of 5-Methyl-2'-deoxycytidine is low in proliferating cells and high in differentiated cells.
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| HY-P2255 | H3K4(Me) (1-20) |
H3K4(Me) (1-20), a histone peptide. H3K4me is an intricately regulated posttranslational modification, which is broadly associated with enhancers and promoters of actively transcribed genomic loci.
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| HY-P10143 | MMP-2/MMP-9 Substrate |
MMP-2/MMP-9 Substrate (Ac-Pro-Leu-Gly-[(S)-2-mercapto-4-methyl-pentanoyl]-Leu-Gly-OEt) is a synthetic chromogenic polypeptide substrate whose core structure mimics the cleavage sites of MMP-2 and MMP-9 (gelatinase A and B) in collagen. After being hydrolyzed by collagenase, MMP-2/MMP-9 Substrate reacts with 4,4'-dithiodipyridine or Ellman's Reagent via its thiol fragment to produce a product with ultraviolet absorption properties.
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| HY-113061R | Pseudouridine (Standard) |
Pseudouridine (Standard) is the analytical standard of Pseudouridine. This product is intended for research and analytical applications. Pseudouridine is an isomer of the nucleoside uridine, and the most abundant modified nucleoside in non-coding RNAs. Pseudouridine in rRNA and tRNA can fine-tune and stabilize the regional structure and help maintain their functions in mRNA decoding, ribosome assembly, processing and translation[4].
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| HY-A0067S | Oxybenzone-d5 |
Oxybenzone-d5 is the deuterium labeled Oxybenzone. Oxybenzone (Benzophenone 3) is a commonly used UV filter in sun tans and skin protectants. Oxybenzone act as endocrine disrupting chemicals (EDCs) and can pass through the placental and blood-brain barriers. Benzophenone-3 impairs autophagy, alters epigenetic status, and disrupts retinoid X receptor signaling in apoptotic neuronal cells.
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| HY-P2258 | Histone H3 (1-34) |
Histone H3 (1-34) is a peptide derived from human histone isotype 3.1. Histones are the main protein components of eukaryotic chromatin. Histone variants and histone modifications modulate chromatin structure, ensuring the precise operation of cellular processes associated with genomic DNA.
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| HY-W008091S | 5-Methylcytosine-d4 |
5-Methylcytosine-d4 is the deuterium labeled 5-Methylcytosine (HY-W008091). 5-Methylcytosine is a well-characterized DNA modification in prokaryotes and eukaryotes. 5-Methylcytosine forms symmetrical methylation on CpG dinucleotides in DNA, stabilizes tRNA/rRNA structure in RNA, and affects mRNA translation. 5-Methylcytosine can be oxidized to generate 5hmC, 5fC, and 5caC. 5-Methylcytosine can be used in epigenetics, developmental biology, and the study of diseases such as colorectal cancer and hepatocellular carcinoma.
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| HY-B0710S | Betaine-13C3 |
Betaine-13C3 (Trimethylglycine-13C3) is the 13C labeled isotope of Betaine (HY-B0710). Betaine (Trimethylglycine) is a natural compound found in many foods and also an active methyl-donor which can maintain normal DNA methylation patterns. Betaine is found ubiquitously in plants, animals, microorganisms, and rich dietary sources including seafood, spinach, and wheat bran. Betaine also acts as an osmolyte, to maintain the avian’s cellular water and ion balance to improve the avian’s capacity against heat stress via preventing dehydration and osmotic inactivation. It helps in maintaining the protective osmolytic activity, especially in heat-stressed birds. Betaine may promote various intestinal microbes against osmotic variations and thus improve microbial fermentation activity.
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| HY-78197 | 3,5-Dimethylisoxazole-4-boronic acid pinacol ester |
3,5-Dimethylisoxazole-4-boronic acid pinacol ester is a drug intermediate that can be used for the synthesis of bromodomain inhibitors.
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| HY-D1603 | BODIPY FL-EDA |
BODIPY FL-EDA is a widely used fluorescent dye for quantitative analysis of nucleotides. BODIPY FL-EDA is an aliphatic amine analog that can react with aldehydes and ketones. BODIPY FL-EDA can be used to detect both modified and unmodified deoxynucleotides and to determine DNA damage and genomic DNA methylation through capillary electrophoresis with laser-induced fluorescence (CE-LIF). Additionally, it can be used for quantifying intracellular ATP levels. The excitation wavelength is 500 nm, and the emission wavelength is 510 nm.
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| HY-113039 | L-2-Hydroxyglutaric acid |
L-2-Hydroxyglutaric acid is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid can inhibit histone demethylases and hence promote histone methylation. L-2-Hydroxyglutaric acid inhibits mitochondrial creatine kinase (Mi-CK) activity with Km and Ki of 2.52 mM and 11.13 mM, respectively.
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| HY-W004924 | 5-Hydroxymethyluracil |
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| HY-I0626R | Cytosine (Standard) |
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| HY-W018324 | 5-Hydroxymethylcytosine |
5-Hydroxymethylcytosine (5hmC) is an oxidized forms of 5-methylcytosine (5mC) in mammalian DNA. 5-Hydroxymethylcytosine is produced from 5mC in an enzymatic pathway involving three 5mC oxidases, Ten-eleven translocation (TET)1, TET2, and TET3. The conversion of 5mC into 5hmC can be the first step in a pathway leading towards DNA demethylation. 5-Hydroxymethylcytosine is associated with gene transcription and frequently used as a mark to investigate dynamic DNA methylation conversion during mammalian development. 5-Hydroxymethylcytosine can be used for the study of non-small cell lung cancer (NSCLC), neurodegenerative diseases (Alzheimer’s, Parkinson’s) and hematological malignancies (acute myeloid leukemia, myelodysplastic syndromes).
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Metabolic or Endocrine Disease
Lung Cancer
Leukemia/Lymphoma/Myeloma
Alzheimer's Disease
Parkinson's Disease
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| HY-P5285 | Lunasin |
Lunasin is a bioactive peptide with antioxidant, anti-inflammatory, anticancer and anti-aging properties. Lunasin can be isolated from soybean. Lunasin also has an epigenetic mechanism of action associated with histone acetylation. Lunasin can be internalized into cells and inhibit Oncosphere formation in cancer cells.
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| HY-I0626S2 | Cytosine-d2 |
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| HY-N0005S | Curcumin-d6 |
Curcumin-d6 (Diferuloylmethane-d6 ) is deuterium labeled Curcumin (HY-N0005). Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin is a photosensitizer against microorganisms. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
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Isotope-Labeled Compounds
Keap1-Nrf2
Ferroptosis
Autophagy
Histone Acetyltransferase
Epigenetic Reader Domain
Mitophagy
Influenza Virus
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| HY-116887 | N6-Methyladenine |
N6-Methyladenine is a DNA epigenetic modification that involves the addition of a methyl group to the sixth position of adenine. N6-Methyladenine plays an important role in distinguishing host DNA from exogenous DNA and controls many biological functions, such as DNA replication, transcription, mismatch repair, and chromosome replication. N6-Methyladenine can be used for the kidney diseases.
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| HY-B0710R | Betaine (Standard) |
Betaine (Standard) is the analytical standard of Betaine. This product is intended for research and analytical applications. Betaine (Trimethylglycine) is a natural compound found in many foods and also an active methyl-donor which can maintain normal DNA methylation patterns. Betaine is found ubiquitously in plants, animals, microorganisms, and rich dietary sources including seafood, spinach, and wheat bran. Betaine also acts as an osmolyte, to maintain the avian’s cellular water and ion balance to improve the avian’s capacity against heat stress via preventing dehydration and osmotic inactivation. It helps in maintaining the protective osmolytic activity, especially in heat-stressed birds. Betaine may promote various intestinal microbes against osmotic variations and thus improve microbial fermentation activity.
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| HY-N6588 | 3,4,5-Tricaffeoylquinic acid |
3,4,5-Tricaffeoylquinic acid (3,4,5-triCQA) inhibits tumor necrosis factor-α-stimulated production of inflammatory mediators in keratinocytes via suppression of Akt- and NF-κB-pathways. 3,4,5-Tricaffeoylquinic acid induces cell cycle arrest at G0/G1, actin cytoskeleton organization, chromatin remodeling, neuronal differentiation, and bone morphogenetic protein signaling in human neural stem cells. 3,4,5-Tricaffeoylquinic acid has the potential for the research of aging-associated diseases.
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| HY-N2126 | Parishin E |
Parishin E is a modulator of hexokinase 2, lactate dehydrogenase A, and silent information regulator 6 (sirtuin 6), and is also a component present in Gastrodia elata Blume. Parishin E reduces the expression of hexokinase 2 and lactate dehydrogenase A, thereby regulating the process of cellular glycolysis. Parishin E regulates the deacetylation mediated by silent information regulator 6 (Sirtuin 6), and inhibits histone 3 lactylation modifications at the H3K18la and H3K27la sites. Parishin E inhibits macrophage polarization. Parishin E alleviates LPS-induced inflammatory responses and suppresses the expression of pro-inflammatory cytokines. Parishin E exerts ameliorating effects on rheumatoid arthritis. Parishin E can be used in studies related to rheumatoid arthritis.
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| HY-P1958 | Histone H4 (2-21) |
Histone H4 (2-21) is a substrate peptide derived from the N-terminal region of histone H4, which serves as an acyl acceptor for lysine acetyltransferases of the MYST family (KAT). Histone H4 (2-21) participates in enzymatic reactions together with acyl-coenzyme A (acyl-CoA, and undergoes lysine acetylation and propionylation modifications catalyzed by KATs such as MOF. The apparent Km of Histone H4 (2-21) for MOF is 788.8 μM, while in the picNuA4 catalytic system, the Km and Kd values of the H4 peptide are 192 μM and 251 μM, respectively. Histone H4 (2-21) can be used in studies related to histone post-translational modifications, epigenetic regulation, and lysine acylation.
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| HY-B2227R | Lactic acid (Standard) |
Lactic acid (Standard) (DL-Lactic acid (Standard)) is the analytical standard of Lactic acid (HY-B2227). This product is intended for research and analytical applications. Lactic acid (DL-Lactic acid) is a hydroxycarboxylic acid receptor 1 (HCAR1) activator and an epigenetic modulator inducing lysine residues lactylation. Lactic acid is a glycolysis end-product, bridging the gap between glycolysis and oxidative phosphorylation. Lactic acid is an oncometabolite and has immune protective role of lactate in anti-tumor immunity. Lactic acid also has antimicrobial activity, which can be used as a food preservative.
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| HY-P10272 | Rusfertide |
Rusfertide is a peptide mimetic of natural hepcidin, which targets and degrades ferroportin, reduces serum iron and transferrin-saturation, and thus regulates the production of red blood cells. Rusfertide ameliorates the polycythemia vera, β-thalassemia and hereditary hemochromatosis.
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| HY-W015114 | L-2-Hydroxyglutaric acid disodium |
L-2-Hydroxyglutaric acid disodium is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid disodium can inhibit histone demethylases and hence promote histone methylation. L-2-Hydroxyglutaric acid inhibits mitochondrial creatine kinase (Mi-CK) activity with Km and Ki of 2.52 mM and 11.13 mM, respectively.
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| HY-113491 | 3-Phosphoglyceric acid |
3-Phosphoglyceric acid is a metabolic intermediate in both glycolysis and the Calvin cycle. 3-Phosphoglyceric acid is involved in alveolar macrophage epigenetic regulation.
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| HY-P74601 | RBBP4 Protein, Human (sf9, His) |
The RBBP4 protein regulates chromatin assembly by binding to core histones and interacting with chromatin assembly factors, remodelers, and histone deacetylases. Its activity is determined by its interaction with nucleosomal DNA. RBBP4 Protein, Human (sf9, His) is the recombinant human-derived RBBP4 protein, expressed by Sf9 insect cells , with N-His labeled tag.
Species: Human; Source: Sf9 insect cells |
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| HY-P73024 | Ephrin-A1/EFNA1 Protein, Mouse (HEK293, His) |
The Ephrin-A1/EFNA1 protein is a GPI-binding ligand critical for migration, repulsion, and adhesion in developing neurons, blood vessels, and epithelia. It binds to nearby Eph receptors, initiating bidirectional signaling. Ephrin-A1/EFNA1 Protein, Mouse (HEK293, His) is the recombinant mouse-derived Ephrin-A1/EFNA1 protein, expressed by HEK293 , with C-His labeled tag.
Species: Mouse; Source: HEK293 |
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| HY-P74600 | RBBP4 Protein, Mouse (sf9, His) |
The RBBP4 protein is a core histone-binding subunit that directs chromatin regulators and histone deacetylases to their substrates and participates in chromatin metabolism.RBBP4 Protein, Mouse (sf9, His) is the recombinant mouse-derived RBBP4 protein, expressed by Sf9 insect cells , with N-His labeled tag.
Species: Mouse; Source: Sf9 insect cells |
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| HY-P703421 | SPT16 Protein, Arabidopsis thaliana |
SPT16 Protein, Arabidopsis thaliana is the recombinant SPT16, expressed by E. coli , with tag Free labeled tag. ,
Species: Others; Source: E. coli |
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| HY-P701613 | CECR2 Protein, Human (His) |
The CECR2 protein is a regulatory subunit in the CERF-1 and CERF-5 ISWI chromatin remodeling complexes that assembles ordered nucleosome arrays to help DNA enter replication, transcription, and repair. Despite lacking mononucleosome sliding ability, these complexes make crucial contributions to various developmental processes. CECR2 Protein, Human (His) is the recombinant human-derived CECR2 protein, expressed by E. coli , with N-6*His labeled tag.
Species: Human; Source: E. coli |
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| HY-P85564 | SMARCC1 Antibody (YA5256) |
SMARCC1 Antibody (YA5256) is a Mouse-derived and non-conjugated monoclonal antibody, targeting to SMARCC1.
Host: Mouse; Reactivity: Human |
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| HY-P86786 | BAF170 Antibody (YA6479) |
BAF170 Antibody (YA6479) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to BAF170.
Host: Rabbit; Reactivity: Human, Mouse, Rat |
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