Articles
-
All
-
Scientific Reviews
-
EDM
-
Blog
-
Most Recent
-
Oldest
-
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.
-
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.
-
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.
-
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.
-
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.
-
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.
-
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.
-
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.
-
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.
-
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.
-
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.
-
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.
-
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.
-
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.
-
Mammalian cells can also photosynthesize like plants! Photosynthesis can improve cell anabolism and exhibit good clinical effect in degenerative diseases (osteoarthritis).
-
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.
-
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.
-
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.
-
FDA Annual Review | Record-breaking number of new drug approvals in 2023!
-
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!
-
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?
-
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?
-
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.
-
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!
-
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.
-
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!
-
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~
-
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!
-
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.
-
A New Form of Cell Death: PANoptosis!
-
Unlocking the Power of Intermittent Fasting: The 16+8 Method
-
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!
-
Advancing Chronic Kidney Disease Research with GJ103 and Lamin B1 Antibody!
-
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.
-
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.
-
Autophagy is a fundamental process that degrades various components within the cell.
-
This article will tell you about the common methods of modeling liver disease in animal models.
-
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!
-
This article introduces some common cardiovascular disease models, inducers, modeling protocols and successful modeling cases in the research.
-
Do you feel confused when you start culturing cells? This article will show you the basic methods and steps of cell culture!
-
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.
-
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.
-
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.
-
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!
-
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.
-
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.
-
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.
-
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.
-
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.
-
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!
-
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.
-
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.
-
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.
-
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.
-
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.
-
This article walks you through the experimental design and workflow of flow cytometry, delivering a clear, dynamic, and professional overview to elevate your research.
-
Molecular glue degraders have evolved from a serendipitous observation to one of the most dynamic and transformative fields in biomedical research.
-
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. -
This review introduces the major forms of programmed cell death, with a focus on the molecular mechanisms of ferroptosis and the methods used for its detection.
-
This review provides a practical guide to the fundamental mechanisms, regulatory pathways, and detection methods of pyroptosis.
-
Explore lysosomal nutrient sensing, quality control, cellular adaptation, disease mechanisms, and emerging therapeutic approaches.
-
Explore how mitochondrial quality control, inflammatory signaling, and metabolic–epigenetic reprogramming regulate cellular senescence and the SASP, along with strategies to restore mitochondrial homeostasis.
-
Review the metabolic regulation of ferroptosis through iron homeostasis, lipid peroxidation and antioxidant defence, and the emerging polyamine–iron buffering axis.
-
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.
-
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.
-
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.
-
CCB02 is an tubulin binder and has potential in the therapy of cancer cells with extra centrosomes. CCB02 also activates spindle assembly checkpoint.
-
H3B-5942 is a selective and irreversible estrogen receptor covalent antagonist, inactivates both ERαWT and ERα mutation.
-
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.
-
COH000 is an allosteric, covalent and irreversible inhibitor of SUMO-activating enzyme, with an IC50 of 0.2 μM for SUMOylation in vitro.
-
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.
-
PhiKan 083 is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a Kd of 167 μM.
-
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.
-
SSE15206 is a microtubule polymerization inhibitor, with a GI50 of 197 nM in HCT116 cells. Causes aberrant mitosis resulting in G2/M arrest.
-
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.
-
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.
-
JNJ-64619178 is a selective and pseudo-irreversible PRMT5 inhibitor with an IC50 of 0.14 nM. Has potent Activity In Lung Cancer.
-
(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.
-
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.
-
BTR-1 potently inhibits cell growth. It induces S phase arrest, affects DNA replication. Dose-dependently induces cytotoxicity in leukemic cell lines.
-
Y06137 is a potent and selective BET inhibitor, which binds to the BRD4(1) bromodomain with a Kd of 81 nM. Antitumor activity.
-
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.
-
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).
-
CB-6644 is a selective non-ATP-competitive inhibitor of the RUVBL1/2 complex. CB-6644 significantly reduces tumor growth without obvious toxicity.
-
A1874 is a nutlin-based and BRD4-degrading PROTAC with a DC50 of 32 nM. Effective in inhibiting many cancer cell lines proliferation
-
NSC 228155 is a activator of EGFR and a potent inhibitor of KIX-KID interaction. NSC 228155 shows excellent anti-tumor activity.
-
BSJ-03-123, a Degrader with Proteome-wide Selectivity for CDK6 (PROTAC). Induces a G1 cell-cycle arrest without a measurable increase in apoptosis.
-
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.
-
BSc5371 is a potent and irreversible FLT3 inhibitor. BSc5371 is cytotoxic to FLT3-dependent cell line. BSc5371 has potential to treat Acute Leukemia.
-
-
MRTX-1257 is a selective, irreversible, covalent and oral active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation.
-
SJ572403 (SJ403) is an inhibitor of disordered protein p27 (Kip1). p27 (Kip1) is a regulator of the CDKs that control eukaryotic cell division.
-
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.
-
JR-AB2-011 inhibits mTORC2 activity by blocking Rictor-mTOR association. JR-AB2-011 has anti-glioblastoma multiforme (GBM) properties.
-
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.
-
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.
-
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.
-
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.
-
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.
-
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.
-
ORIC-101 is a highly potent and selective glucocorticoid receptor antagonist, with an EC50 of 5.6 nM. ORIC-101 has anti-cancer activity.
-
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.
-
MDL-800 is an allosteric and selective SIRT6 activator. MDL-800 increases SIRT6 deacetylation activity with an EC50 of 10.3 µM
-
TAS-114 is a dual dUTPase/dihydropyrimidine dehydrogenase (DPD) inhibitor, can improving the therapeutic efficacy of fluoropyrimidine.
-
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.
-
RIPGBM is a selective inducer of apoptosis in glioblastoma multiforme (GBM) cancer stem cells (CSCs) with an EC50 less than 500 nM.
-
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.
-
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. -
-
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.
-
OTS186935 is a methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 reveales significant inhibition of tumor growth in animal models.
-
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.
-
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.
-
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).
-
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.
-
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.
-
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.
-
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
-
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.
-
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.
-
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.
-
RO-5963 is a dual p53-MDM2 and p53-MDMX inhibitor with IC50s of ~17 nM and ~24 nM, respectively. Potently shows apoptotic activity.
-
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.
-
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.
-
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.
-
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
-
TAS4464 is a highly potent and selective inhibitor of NEDD8 activating enzyme (NAE), with an IC50 of 0.955 nM. TAS4464 shows antitumor activity.
-
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.
-
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.
-
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.
-
NSC 95397 inhibits MKP-1 and suppresses proliferation and induces apoptosis in colon cancer cells through MKP-1 and ERK1/2 pathway.
-
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
-
DS21360717 is a potent and orally active FER tyrosine kinase inhibitor, with an IC50 of 0.49 nM. DS21360717 has anti-cancer activity.
-
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.
-
BAY1238097 is a selective inhibitor of BET binding to histones and has strong anti-proliferative activity through down-regulation of c-Myc levels.
-
CCT020312, the G1/S checkpoint activator, is a selective EIF2AK3/PERK activator. CCT020312 elicits EIF2A phosphorylation in cells.
-
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.
-
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.
-
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).
-
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 .
-
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.
-
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.
-
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.
-
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.
-
MZP-55 is a selective PROTAC degrader of BRD3/4, shows no obvious effect on BRD2. MZP-55 exhibits excellent activity in cancer research.
-
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.
-
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.
-
FGTI-2734 is a dual farnesyl and geranylgeranyl transferase-1 inhibitor. FGTI-2734 prevents membrane localization of KRAS and mutant KRAS pancreatic tumors.
-
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.
-
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.
-
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.
-
GSK3368715 is an orally active and SAM uncompetitive type I PRMT inhibitor that produces a shift in arginine methylation states.
-
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.
-
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).
-
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.
-
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.
-
LSN 3213128 is a selective, nonclassical, orally bioavailable antifolate with anti-cancer activity. LSN 3213128 potently and specifically inhibits AICARFT.
-
CA-5f is a potent late-stage macroautophagy (autophagy) inhibitor via inhibiting autophagosome-lysosome fusion. CA-5f increases LC3B-II and SQSTM1 protein.
-
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).
-
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.
-
VERU-111 (ABI-231) is a potent and orally bioavailable α and β tubulin inhibitor, which displays strong antiproliferative activity.
-
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.
-
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.
-
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.
-
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.
-
NXT629 is a potent, selective, and competitive PPAR-α antagonist and shows high selectivity over other nuclear hormone receptor.
-
GNA002 is a highly potent, specific and covalent EZH2 inhibitor, which efficiently reduces EZH2-mediated H3K27 trimethylation.
-
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.
-
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.
-
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.
-
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.
-
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.
-
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.
-
RG7112 is a potent, selective, first clinical and orally active MDM2-p53 inhibitor, with a KD of 11 nM for binding to MDM2.
-
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.
-
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.
-
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.
-
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.
-
CITCO is a selective agonist of constitutive androstane receptor, with an EC50 of 49 nM, with potent activity against brain tumor stem cells.
-
RRx-001 is a hypoxia-selective epigenetic agent, triggers apoptosis and overcomes drug resistance in multi myeloma cells.
-
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.
-
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.
-
SGC-iMLLT is a potent, selective MLLT1/3-histone interactions inhibitor and shows high binding activity towards MLLT1 YEATS domain and MLLT3 YD.
-
YUKA1 is a potent, selective and cell permeable KDM5A inhibitor, with an IC50 of 2.66 μM. YUKA1 exhibits anti-cancer activity.
-
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.
-
BAY 61-3606 is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor and sensitizes apoptosis by in breast cancer.
-
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.
-
UPGL00004 is a allosteric glutaminase C inhibitor which strongly inhibits the proliferation of highly aggressive triple-negative breast cancer cell lines.
-
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.
-
IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1) R132 mutations.
-
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.
-
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.
-
VU0155069 is a selective phospholipase D1 inhibitor with an IC50 of 46 nM, which strongly inhibits the invasive migration of several cancer cell lines.
-
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.
-
AZD0424 is a selective Src/Abl kinase inhibitor with potential antineoplastic activity. AZD0424 induces apoptosis and cell cycle arrest in lymphoma cells
-
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.
-
PTC596, an orally active and selective BMI-1 inhibitor, induces p53-independent mitochondrial apoptosis in acute myeloid leukemia progenitor cells.
-
CSRM617 is a selective inhibitor of ONECUT2 (OC2). CSRM617 induces apoptosis. Well tolerated in the prostate cancer mouse model.
-
BPK-29 disrupts the NR0B1 protein-protein interactions and impairs the anchorage-independent growth of KEAP1-mutant cancer cells.
-
LDN-192960 is a potent Haspin and DYRK2 dual inhibitor. LDN-192960 may have potential therapeutic utility in treating cancer.
-
-
SCH772984 is a highly selective and ATP-competitive ERK inhibitor. SCH772984 shows robust efficacy in RAS- or BRAF-mutant cancer cells.
-
LY3214996 is a highly potent and selective ERK1 and ERK2 inhibitor and shows potent antitumor activities in cancer models with MAPK pathway alterations.
-
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.
-
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.
-
CGS 15943 is an orally bioavailable adenosine receptor antagonist with low nanomolar range Ki values for human A1, A2A, A2B, and A3 adenosine receptors.
-
CG-200745 is a potent and pan HDAC inhibitor. CG200745 inhibits the deacetylation of histone H3 and tubulin, inducing p53 accumulation.
-
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.
-
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.
-
sAJM589 is a Myc inhibitor which potently disrupts the Myc-Max heterodimer in a dose dependent manner with an IC50 of 1.8 μM.
-
Tasisulam is an anticancer agent and induces apoptosis, which also inhibits mitotic progression and induces vascular normalization.
-
JTE-013 is a potent and specific S1P2 antagonist and increases the excitability of sensory neurons independently of the receptor.
-
OTS964 is an orally active, high affinity and selective TOPK inhibitor and is also a potent inhibitor of the cyclin-dependent kinase CDK11.
-
IPR-803 is a potent inhibitor of the uPAR•uPA protein-protein interaction, and binds directly to uPAR with sub-micromolar affinity.
-
FTI-2153 is a potent and highly selectiveof farnesyltransferase (FTase) inhibitor and a highly potent antagonist of oncogenic H-Ras signaling.
-
TVB-3166 is an orally-available, reversible, and selective FASN inhibitor and it induces apoptosis, and inhibits in-vivo xenograft tumor growth.
-
Vorolanib is an orally active, multikinase VEGF/PDGF receptor inhibitor with antitumor activity and is expected to disrupt tumor angiogenesis.
-
CCG-222740 is a potent and selective MRTF pathway inhibitor. It effectively reduces fibrosis in the skin and blocks melanoma metastasis.
-
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.
-
MN58b, a selective choline kinase α (CHKα) inhibitor, results in inhibition of phosphocholine synthesis, induces of apoptosis, and has antitumoral activity.
-
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).
-
SU16f is a selective PDGFRβ inhibitor and significantly decreases the enhanced migratory ability of SGC-7901 cells by GC-MSC.
-
IACS-8803 is a highly potent cyclic dinucleotide stimulator of interferon genes (STING) agonist with robust systemic antitumor efficacy.
-
MRTX849 is a potent, orally-available, and mutation-selective covalent inhibitor of KRASG12C with potential antineoplastic activity.
-
AG-825 is a selective and ATP-competitive ErbB2 inhibitor and leads to a decrease in ErbB2–nucleolin interaction, which suppresses tyrosine phosphorylation.
-
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.
-
AC-73 is a first specific, orally active the cluster of differentiation 147 (CD147) inhibitor and specifically disrupts CD147 dimerization.
-
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.
-
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.
-
PK11007 is a Mild Alkylating Agent with Anticancer Activity and induces mutant p53 cancer cell death by increasing reactive oxygen species (ROS) levels.
-
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.
-
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.
-
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.
-
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.
-
Sotorasib, a first-in-class, selective KRAS G12C covalent inhibitor, irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state.
-
Telaglenastat is a first-in-class, reversible, orally bioavailable glutaminase 1 splice variants (KGA and GAC) inhibitor. It shows antitumor activity.
-
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).
-
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.
-
TK216 is a potent ETS inhibitor. TK216 blocks the binding between EWS-FLI1 and RNA helicase A. TK216 has anticancer activity.
-
DRF-1042 is an orally active derivative of Camptothecin and acts to inhibit DNA topoisomerase I with good anticancer activity.
-
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.
-
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.
-
FPA-124 is a cell-permeable copper complex and a selective Akt inhibitor. FPA-124 induces apoptosis in multiple human cancer cells.
-
KB02-JQ1 is a highly potent and selective PROTAC BRD4 degrader that degrades nuclear proteins by engaging CUL4-DDB1 E3 ubiquitin ligases DCAF16.
-
CH6953755 is a potent, orally active and selective YES1 kinase inhibitor leading to antitumor activity against YES1 Gene -amplified cancers.
-
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.
-
CKI-7 is a potent CK1 and Cdc7 kinase inhibitor, which induces cytotoxicity of established leukemia and lymphoma cell lines.
-
GPP78 is a potent Nampt inhibitor. GPP78 is cytotoxic to neuroblastoma cell line SH-SY5Y cells. GPP78 has anti-cancer and anti-tumor activity.
-
CC-223 is an orally bioavailable mTOR kinase inhibitor and demonstrates mTORC1/2 and growth inhibitory activity across a variety of tumor cell types.
-
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.
-
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.
-
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.
-
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.
-
BCI-215 is a potent and tumor cell-selective DUSP-MKP inhibitor without affecting normal cells. Anti-migratory and proapoptotic activities in cancer cells.
-
PKI-166 is an orally active EGFR tyrosine kinase inhibitor and inhibits pancreatic cancers. Combined with Gemcitabine produces a decrease in tumor growth.
-
BAY-474 is a tyrosine-protein kinase c-Met inhibitor. BAY-474 is a structural genomics consortium (SGC) epigenetics probe.
-
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.
-
M8891 is an orally active, reversible and brain penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor with antiangiogenic and antitumoral activity.
-
BRD7389 is a specific RSK family kinase inhibitor and is a small-molecule inducer of insulin expression in pancreatic α-cells.
-
MRT199665 is a potent, ATP-competitive, and selective MARK/SIK/AMPK inhibitor, and causes apoptosis in MEF2C-activated human AML cells.
-
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.
-
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.
-
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.
-
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.
-
6RK73 is a covalent irreversible and specific UCHL1 inhibitor,which specifically inhibits UCHL1 activity in breast cancer.
-
AGN194204 is an orally active and selective RXR agonist. AGN194204 is inactive against RAR and has anti-inflammatory and anticarcinogenic actions.
-
BI-9321 is a potent, selective and cellular active NSD3-PWWP1 domain antagonist, and specifically disrupts histone interactions of the NSD3-PWWP1 domain.
-
BPI-9016M is a dual c-Met and AXL tyrosine kinases inhibitor. BPI-9016M suppresses lung cancer cell lines growth, migration, and invasion.
-
MSN-125, a potent Bax and Bak oligomerization inhibitor, efficiently prevents mitochondrial outer membrane permeabilization.
-
F1324 is a potent and high-affinity peptidic inhibitor of BCL6 with anti-cancer activity. F1324 has strong inhibition activity against BCL6 PPI.
-
BTSA1 is a high affinity and orally active BAX activator and induces conformational changes to BAX leading to BAX-mediated apoptosis.
-
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.
-
ZCL278 is a potent and selective Cdc42 inhibitor with anticancer and antiviral activity. ZCL278 targets Cdc42-ITSN interaction.
-
CID2950007 is an allosteric inhibitor that binds the guanine nucleotide-associated Cdc42 and induces ligand dissociation.
-
CID-1067700 is a pan GTPase inhibitor, and competitively inhibits Rab7. CID-1067700 is a competitive guanine nucleotide binding inhibitor.
-
Ro 90-7501, an Aβ42 fibril assembly inhibitor, inhibits PP5 in a TPR-dependent manner and has radiosensitizing effects on cervical cancer cells.
-
CM-272, a first-in-class, selective, substrate-competitive and reversible dual G9a/DNMTs inhibitor, inhibits cell proliferation and promotes apoptosis.
-
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.
-
PS315 is an allosteric PKC inhibitor by binding to the PIF-pocket of aPKC and inducing a displacement of the active site residue Lys111.
-
JBJ-04-125-02 is a mutant-selective, allosteric and orally active EGFR inhibitor. JBJ-04-125-02 inhibits cancer cell proliferation.
-
DB1976 is a selenophene analog of DB270 and a potent and fully efficacious transcription factor PU.1 inhibitor with apoptosis-inducing effect.
-
CM10 is a potent and selective aldehyde dehydrogenase 1A family inhibitor and regulates metabolism and has anti-cancer activity.
-
E64FC26 is a highly potent pan-style inhibitor of the protein disulfide isomerase (PDI) family with anti-myeloma activities.
-
EB-3D, a selective ChoKα1 inhibitor, induces deregulation of the AMPK-mTOR pathway and apoptosis in leukemia T-cells, and shows antiproliferative activity.
-
NU1025 is a potent PARP inhibitor and potentiates the cytotoxicity of ionizing radiation drug. NU1025 has anti-cancer and neuroprotective activity.
-
Mobocertinib is a potent epidermal growth factor receptor (EGFR, ErbB1) inhibitor, which displays antineoplastic activity.
-
Mepazine is an effective MALT1 inhibitor. Antipsychotic and tranquilizing agent. Mepazine affects viability of ABC-DLBCL cells by enhancing apoptosis.
-
LBW242, a Smac mimetic, is a potent and orally active proapoptotic IAP inhibitor. LBW242 shows effects on mutant FLT3-expressing cells.
-
LCH-7749944 is a potent PAK4 inhibitor and effectively suppresses the proliferation of human gastric cancer cells and induces apoptosis.
-
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.
-
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.
-
BAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor, which is highly effective in inhibiting Pten-null prostate cancer growth.
-
M2698 is an orally active, ATP competitive, selective p70S6K and Akt dual-inhibitor with anti-cancer activity. M2698 can cross the blood-brain barrier.
-
ARCC-4 is a low-nanomolar AR degrader, and effectively degrades clinically relevant AR mutants associated with antiandrogen therapy.
-
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.
-
PIK-75 is a reversible DNA-PK and p110α selective inhibitor. Impairs cell proliferation, survival, and tumor growth. Induce apoptosis.
-
BO-264, an orally active TACC3 inhibitor, specifically blocks the function of FGFR3-TACC3 fusion protein and has broad-spectrum antitumor activity.
-
MK-2206 is an orally active, highly potent and selective allosteric AKT inhibitor, with IC50s in the nanomolar range and antitumor activity.
-
CPTH2 is a potent histone acetyltransferase (HAT) inhibitor and selectively inhibits the acetylation of histone H3 by recombinant human Gcn5.
-
ONO-7475 is a selective and orally active novel Anexelekto (AXL) inhibitor. It sensitizes AXL-overexpressing EGFR-mutant NSCLC cells to the EGFR-TKIs.
-
iFSP1 is a potent, selective FSP1inhibitor that induces ferroptosis in GPX4-knockout cells which overexpressed FSP1.
-
SB-633825 is a potent and ATP-competitive inhibitor of TIE2, LOK (STK10) and BRK. SB-633825 can inhibit cancer cell growth and angiogenesis.
-
Zotatifin is a potent and selective eIF4A inhibitor. Zotatifin effectively reduces viral infectivity by inhibiting SARS-CoV-2 NP protein biogenesis.
-
SNDX-5613 is a potent, selective, small molecule inhibitor of the Menin-MLL binding interaction for targeted therapy in MLL-rearranged leukemias.
-
OTS514 is a TOPK inhibitor induces complete tumor regression in xenograft models of human cancer through inhibition of cytokinesis.
-
BAY1082439, an orally bioavailable, selective PI3K inhibitor, inhibits mutated forms of PIK3CA and is effective in treating prostate cancer with PTEN-loss.
-
RBN-2397 is an orally active accross species NAD+ competitive inhibitor of PARP7. RBN-2397 binds to PARP7 and restores interferon (Type I) signaling.
-
TNO155 is an allosteric inhibitor of wild-type SHP2. TNO155 has the potential for the study of RTK-dependent malignancies, especially advanced solid tumors.
-
UT-34 is a potent, selective and orally active second-generation pan-androgen receptor (AR) antagonist and degrader with anti-prostate cancer efficacy.
-
MYCMI-6 is a selective MYC:MAX protein interactions inhibitor, which blocks MYC-driven transcription and binds selectively to the MYC bHLHZip domain.
-
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.
-
HSD1590 is potent ROCK inhibitor, with IC50s of 1.22 and 0.51 nM for ROCK1 and ROCK2, respectively. HSD1590 displays low cytotoxicity.
-
PD-161570 is a potent inhibitor of FGF-1R, PDGFR, EGFR, c-Src tyrosine kinases and inhibits PDGF-stimulated autophosphorylation and FGF-1R phosphorylation.
-
OT-82 is a selective inhibitor of NAMPT. Selectively toxic to cells of hematopoietic origin. OT-82 is a promising antineoplastic agent.
-
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.
-
TED-347 is a potent, irreversible, covalent and allosteric inhibitor at YAP-TEAD protein-protein interaction with antitumor activity.
-
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.
-
CID44216842 is a potent Cdc42 selective guanine nucleotide binding lead inhibitor. Cdc42 plays important roles in cell cycle progression.
-
AZA1, a potent dual inhibitor of Rac1 and Cdc42, induces apoptosis and inhibits prostate cancer cells proliferation, migration and invasion.
-
HM03 is a potent and selective HSPA5 inhibitor with anticancer activity. HSPA5 plays a key role in monitoring protein transport through the cell.
-
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.
-
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.
-
DI-82 is a potent deoxycytidine kinase (dCK) inhibitor. DI-82 is potent against hematological malignancies and other cancers.
-
MYLS22 is a first-in-class and selective optic atrophy 1 (OPA1) inhibitor with anti-angiogenesis and anti-cancer activity.
-
RA-9 is a potent and selective proteasome-associated DUBs inhibitor with favorable toxicity profile and anticancer activity.
-
DI-87, an orally active and selective dCK inhibitor, has antitumor activity and is used in combination therapy against tumors expressing dCK.
-
XMU-MP-3, a noncovalent inhibitor that suppresses BTK kinase activity both in vitro and in vivo.
-
HLI373 represents a potential drug-able lead for the development of therapeutically efficacious inhibitors of Hdm2. Hdm2 is an ubiquitin protein ligase.
-
GSK143 is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor. GSK143 reduces inflammation in the intestinal muscularis in mice.
-
GSK621 is a potent and specific AMPK activator and induces autophagy and apoptosis in acute myeloid leukemia (AML) cells.
-
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.
-
LQZ-7I orally and effectively inhibits xenograft tumor growth and induces survivin loss in tumors.
-
M-808 is a highly potent and efficacious covalent Menin-MLL interaction inhibitor. M-808 has a binding IC50 value of 2.6 nM.
-
S2116 is a potent lysine-specific demethylase 1 (LSD1) inhibitor and increases H3K9 methylation, reciprocal H3K27 deacetylation at super-enhancer regions.
-
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.
-
TH1834 is a specific Tip60 (KAT5) histone acetyltransferase (HAT) inhibitor. TH1834 induces apoptosis and increases DNA damage in breast cancer.
-
RA375, a RPN13 inhibitor, inhibits proteasome function in muscle. RA375 is highly active against cell lines of multiple myeloma and diverse solid cancers.
-
MRK-740 is a selective PRDM9 inhibitor. MRK-740 is more selective for PRDM9 than other histone methyltransferases and other non-epigenetic targets.
-
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.
-
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.
-
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.
-
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.
-
GSK778 is a potent and selective inhibitor of bromodomain (BRD) BD1 and offers a super survival advantage in the aggressive MLL-AF9 AML model.
-
JX06 is a potent, selective and covalent inhibitor of PDK via covalently binding to a cysteine residue in an irreversible manner.
-
DM-01 is a EZH2 inhibitor with anticancer activity. DM-01 has significant ability to reduce the cellular H3K27me3 level in K562 cells.
-
MS117 is a potent, selective, and cell-active PRMT6 inhibitor. MS117 is an invaluable tool for testing biological and therapeutic hypotheses.
-
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.
-
KCC-07 prevents binding of MBD2 to methylated DNA and activates BAI1 inducing anti-proliferative BAI1/p53/p21 signaling. Anticancer activity.
-
CYH33 is an orally active, highly selective PI3Kα inhibitor and inhibits phosphorylation of Akt, ERK with potent activity against solid tumors.
-
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.
-
SC-43 is a potent and orally active SHP-1 (PTPN6) agonist. SC-43 inhibits the phosphorylation of STAT3 and induces cell apoptosis.
-
ATH686 is a potent, selective, and ATP-competitive FLT3 inhibitor with an antileukemic effect. ATH686 induces apoptosis and inhibits cell cycle.
-
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.
-
SBP-0636457 is a smac mimetic and small-molecule IAP antagonist. Act as potent TRAIL-sensitizing agents in a variety of cancer cell lines.
-
BM-1197 is a potent and specific Bcl-2/Bcl-xL inhibitor inducing complete and long-lasting tumor regression in vivo. Antitumor activity.
-
JH295 is a potent, irreversible and selective Nek2 inhibitor. JH295 is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1.
-
YKL-5-124 is a potent, selective, irreversible and covalent CDK7 inhibitor and induces a strong cell-cycle arrest, inhibits E2F-driven gene expression.
-
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.
-
IPI-9119 is an orally active, selective and irreversible FASN inhibitor with potent anti-cancer activity. IPI-9119 induces cell cycle arrest, apoptosis.
-
CAY10404 is a potent and highly selective COX-2 inhibitor. CAY10404 is a potent inhibitor of PKB/Akt and MAPK signalling pathways.
-
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
-
CRT0044876 is a potent and selective APE1 inhibitor. CRT0044876 inhibits the AP endonuclease, 3′-phosphodiesterase and 3′-phosphatase activities of APE1.
-
EPI-001 is a selective inhibitor of Androgen Receptor (AR) and can inhibit transactivation of the AR amino-terminal domain (NTD).
-
MSA-2 is an orally available non-nucleotide STING agonist. MSA-2 shows antitumor activity and stimulates interferon-β secretion in tumors.
-
MPT0G211, an orally active and selective HDAC6 inhibitor, ameliorates tau phosphorylation, and cognitive deficits in an Alzheimer’s disease model.
-
SC99 is an orally active, selective STAT3 inhibitor targeting JAK2-STAT3 pathway. SC99 displays potent anti-myeloma, anti-thrombotic activity.
-
PU02, a derivative of 6-MP, is an allosteric antagonist of 5-HT3 receptor. PU02 possesses anti-cancer cativity by inducing aopotosis.
-
SP-8356, an orally active CD147inhibitor, exerts anti-breast cancer effects by inhibiting NF-κB signaling. Anti-atherosclerotic effects.
-
AZD-9833 is a potent and orally active ER antagonist. AZD-9833 has the potential for the study of ER+ HER2-advanced breast cancer.
-
RapaLink-1, a third-generation bivalent mTOR inhibitor, potently blocking cancer-derived, activating mutants of mTOR. It can cross the blood-brain barrier.
-
CMLD012073, an Amidino-Rocaglates, is a Potent eIF4A Inhibitor. Amidino- and amino-rocaglates act as potent translation inhibitors and anti-cancer agents.
-
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.
-
EEDi-5285 is an exceptionally potent and orally active embryonic ectoderm development (EED) inhibitor with potent anti-cancer activity.
-
CB-1158, a potent and orally bioavailable inhibitor of arginase, blocks myeloid cell-mediated immune suppression in the tumor microenvironment.
-
AG-494 is a potent and selective EGFR tyrosine kinase inhibitor. AG-494 inhibits the autophosphorylation of EGFR, ErbB2, HER1-2 and PDGFR.
-
SRX3207 is an orally active and first-in-class dual Syk/PI3K inhibitor. SRX3207 possesses effective anti-tumor activity in vitro and in vivo.
-
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.
-
D-3263 is an enteric-coated, orally bioavailable (transient receptor potential melastatin member 8) TRPM8 agonist with antineoplastic activity.
-
Giredestrant is an orally active and selective estrogen receptor (ER) antagonist with anti-tumor activity. Giredestrant is a non-steroidal ER ligand.
-
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.
-
Mavelertinib is a high-affinity irreversible inhibitor targeting oncogenic EGFR mutants with selectivity over wild-type EGFR.
-
Verucopeptin inhibits v-ATPase activity by directly targeting the v-ATPase ATP6V1G subunit but not ATP1V1B2 or ATP6V1D. Also a potent HIF-1 inhibitor.
-
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.
-
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.
-
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.
-
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.
-
MSAB, a strongest and selective inhibitor of Wnt/β-catenin signaling activity, represents an effective strategy for cancers.
-
APS6-45 is an orally active tumor-calibrated inhibitor. A highly efficacious lead. Inhibits RAS/MAPK signaling and exhibits antitumor activity.
-
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).
-
E7820, sulfonamide derivative, is a unique angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium.
-
Cyclo(-RGDfK) is a selective inhibitor of the αvβ3 integrin. Cyclo(-RGDfK) potently targets cancer cells through binding to the cell surface αvβ3 integrin.
-
Cilengitide is a compound targeting angiogenesis, the cornerstone of tumor growth and metastasis. ανβ3 and ανβ5 are the target of Cilengitide.
-
Tetrac inhibits the cellular actions of thyroid hormone initiated at the hormone receptor on plasma membrane integrin alphavbeta3.
-
DT2216 is a potent and selective BCL-XL degrader based on PROTAC technology. DT2216 inhibits leukemia and has potent anti-cancer activity.
-
dTRIM24 will be a useful tool to further probe the function of TRIM24 by rapid chemical depletion in hematopoietic cancers and other biological contexts.
-
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.
-
GNE-987, a potent chimeric BET degrader, exhibits picomolar cell BRD4 degradation activity. GNE-987 can be used in PROTAC-Antibody Conjugate (PAC).
-
BI-3663 is a highly selective PTK2/FAK PROTAC (DC50=30 nM), with cereblon ligands to hijack E3 ligases for PTK2 degradation.
-
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.
-
UNC6852 is a chemical degrader that targets polycomb repressive complex 2 (PRC2). Anti-proliferative in diffuse large B cell lymphoma cell lines.
-
VZ185 is a highly selective, potent, and rapid dual degrader with a slight preference for BRD9 over BRD7.
-
PQR530 is a potent, ATP-competitive, orally bioavailable and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor. Antitumor activity.
-
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.
-
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.
-
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.
-
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.
-
CHDI-390576, a potent and CNS penetrant class IIa HDAC inhibitor, show selectivity over class I HDACs, HDAC8 and the class IIb HDAC6 isoform.
-
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.
-
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.
-
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.
-
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.
-
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.
-
APG-1387 is a bivalent SMAC mimetic and an IAP antagonist. APG-1387 induces apoptosis with anti-cancer activity.
-
WL47, a high-affinity cavolin-1 (CAV1) ligand (Kd=23 nM), act as a potent and selective disrupter of CAV1 oligomers.
-
NHWD-870 is a potent, orally active and selective BET family bromodomain inhibitor with potent tumor suppressive efficacies.
-
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.
-
NSC 80467, a potent DNA damaging agent, selectively inhibits survivin, and preferentially inhibits DNA synthesis.
-
G5-7, an orally active and allosteric JAK2 inhibitor. G5-7 induces cell cycle arrest, apoptosis and possesses antiangiogenic effect.
-
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.
-
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.
-
NSC-105808, a potent, specific DNA2 nuclease inhibitor, inhibits HR repair, DSB end resection and suppresses proliferation of cancer cells.
-
Afatinib is an irreversible EGFR family inhibitor and shows potent activity against wild-type and mutant forms of EGFR and HER2.
-
Senaparib, a selective and orally active PARP1/2 inhibitor, has great potential as a monotherapy as well as in combination with other agents.
-
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.
-
ICCB280, a inducer of C/EBPα, exhibits anti-leukemic properties including terminal differentiation, proliferation arrest, and apoptosis.
-
NVS-CECR2-1, a non-BET family Bromodomain (BRD) inhibitor, is a potent and selective CECR2 inhibitor with potent anti-cancer activity.
-
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
-
Triciferol combines VDR agonism and HDAC inhibition to enhance the cytostatic and cytotoxic activities of 1,25D.
-
Fasentin inhibits GLUT-1 and GLUT-4 transporters. Fasentin blocks glucose uptake in cancer cell lines and has anti-angiogenic activity.
-
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.
-
dCBP-1 is a potent and selective degrader of p300/CBP based on PROTAC. dCBP-1 is exceptionally potent at killing multiple myeloma cells.
-
Tuxobertinib (BDTX-189) is a small molecule ATP-competitive inhibitor against a family of allosteric EGFR and HER2 mutations.
-
Piclidenoson (IB-MECA) is an A3 adenosine receptor (A3AR) agonist. Piclidenoson is used for the research of cancer, inflammatory diseases and COVID-19.
-
PF 477736 (PF 00477736) is a Chk1 inhibitor. Breaching the DNA damage checkpoint. PF-00477736 combines with Gemcitabine to abrogates cell cycle arrest.
-
CXD101 is a selective and orally active class I HDAC inhibitor for advanced cancer.
-
AKI603 is a potent Aurora kinase inhibitor. AKI603 attenuates breast tumor-initiating cells and overcomes drug resistance.
-
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.
-
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.
-
GW806742X, an ATP mimetic and a potent MLKL inhibitor, retards MLKL membrane translocation and inhibits necroptosis.
-
ENMD-1198 is an orally active microtubule-targeting agent with antiproliferative and antiangiogenic activity.
-
DTHIB is a Direct and Selective Heat Shock Factor 1 (HSF1) Inhibitor. Selectively accelerates the degradation of nuclear HSF1.
-
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).
-
BrBzGCp2 is a Glyoxalase 1 (GLO1) inhibitor for a variety of disorders. Possesses antitumor and neuroprotective activity.
-
IACS-13909 is a Selective and Orally Active SHP2 Inhibitor. Overcomes tumor resistance to Osimertinib. Targeting SHP2. Therapeutic strategy.
-
IMT1 is a first-in-class specific and noncompetitive human POLRMT inhibitor for mitochondrial transcription disorders related diseases.
-
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.
-
BIM-23190, a somatostatin analog, is a selective SSTR2 and SSTR5 agonist. BIM-23190 can be used in the study for cancer and acromegaly.
-
Conglobatin inhibits proliferation and induces apoptosis by binding to N-terminus of Hsp90 and disrupting Hsp90-Cdc37 complex formation.
-
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).
-
YUM70 inhibits GRP78. Induces endoplasmic reticulum stress-mediated apoptosis. Pancreatic cancer. Acts as a novel anticancer agent.
-
DBPR112 is an orally active furanopyrimidine-based EGFR (WT and L858R/T790M) inhibitor with significant antitumor efficacy.
-
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.
-
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.
-
DC_AC50 is a dual inhibitor of Atox1 and CCS (copper chaperones). DC_AC50 can be used for cancer research.
-
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.
-
PF-06260414 is an orally active and nonsteroidal selective androgen receptor modulator (SARM) and has the potential for muscle weakening.
-
Stafib-1 is the First Selective Inhibitor of STAT5b SH2 Domain. Anticancer agent. STAT5b acts as a target for tumor therapy.
-
LDN193189 is a selective BMP type I receptor inhibitor, which efficiently inhibits ALK2 and ALK3, with weaker effects on ALK4, ALK5 and ALK7.
-
Retro-2 is an inhibitor of retrograde protein trafficking at the endosome-trans-Golgi network interface. Retro-2 induces cell autophagy
-
APS-2-79 is a MEK inhibitor. Stabilization of the KSR inactive state. An effective strategy to target other pseudokinases.
-
BMS-354825 is a dual Src and Abl kinase inhibitor. Antitumor activity. Orally active in the chronic myelogenous leukemia.
-
Miransertib is an orally active, selective and allosteric Akt inhibitor. Miransertib is also a potent the AKT1-E17K mutant protein inhibitor.
-
L-Moses is the first potent, selective, and cell-active PCAF Brd inhibitor. L-Moses disrupts PCAF-Brd histone H3.3 interaction.
-
MS049 is a potent, selective dual inhibitor of PRMT4 and PRMT6. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells.
-
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.
-
AZD1208 is a potent, selective, ATP-competitive, and orally active pan-Pim kinase inhibitor. AZD1208 inhibits acute myeloid leukaemia.
-
ML-00253764 is a brain penetrant nonpeptidic melanocortin receptor 4 (MC4R) antagonist with a Ki/IC50 of 0.16 µM/0.103 µM, respectively.
-
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.
-
A-674563 is an orally active and selective Akt1 inhibitor. A-674563 induces G2 cell cycle arrest and apoptosis in STS cells.
-
Pirtobrutinib, a highly selective and non-covalent next generation BTK inhibitor, inhibits diverse BTK C481 substitution mutations.
-
SHP394 acts as a Potent, Selective, and Orally Efficacious SHP2 Inhibitor. SHP2 is a multifunctional therapeutic target.
-
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.
-
PROTAC MDM2 degrader MD-222 is highly potent and effective in inducing degradation of MDM2 and in activating wild-type p53 in cells.
-
BI-3406 is a selective, orally bioavailable SOS1 inhibitor that binds to the catalytic domain of SOS1, preventing the interaction with KRAS.
-
GSK973, a selective, orally bioavailable inhibitor of the BD2s of the BET family, shows good potency against BRD2 BD2, BRD3 BD2 and BRDT BD2.
-
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.
-
FTI-277 is a farnesyl transferase inhibitor, selectively blocks oncogenic Ras signaling. It inhibits hepatitis delta virus infection.
-
Butaprost is a selective prostaglandin E receptor (EP2) agonist. Butaprost can effectively mitigate kidney fibrogenesis in various fibrosis models.
-
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.
-
Trilaciclib is a CDK4/6 inhibitor with IC50s of 1 nM/4 nM for CDK4/6, respectively. Use for chemotherapy-induced myelosuppression in vivo.
-
SMAP-2 is an orally active PP2A activator. SMAP-2 reduces cell viability of pancreatic ductal adenocarcinoma (PDA) cell lines.
-
LJI308 inhibits the phosphorylation of RSK and YB-1 after irradiation, treatment with EGF, and in cells expressing a KRAS mutation.
-
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.
-
Elacestrant is an orally available selective estrogen receptor degrader (SERD). Elacestrant is an effective breast cancer cell antagonist.
-
PTC-209, a specific BMI-1 inhibitor, irreversibly impairs colorectal cancer-initiating cells (CICs) and impairs the tumor microenvironment.
-
NU9056 is a selective Tip60 (KAT5) histone acetyltransferase inhibitor. NU9056 shows >16-fold selectivity for Tip60 over PCAF, p300 and GCN5.
-
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.
-
Acolbifene is a 4th generation SERM with potent and pure anticarcinogenic properties in the mammary gland and uterus.
-
ARV-110 is an orally active, specific androgen receptor (AR) PROTAC degrader. ARV-110 can be used for the research of prostate cancer.
-
CCI-007, a selective MLL-r leukemia cell lines inhibitor, and inhibits the viability of CALM-AF10 and SET-NUP214 leukemia.
-
NCGC00378430 is a potent SIX1/EYA2 interaction inhibitor and inhibits SIX1-mediated breast cancer metastasis.
-
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.
-
Vorasidenib is an orally available, brain penetrant second-generation dual mutant isocitrate dehydrogenases 1 and 2 (mIDH1/2) inhibitor.
-
Motesanib (AMG 706) is an orally active VEGFR inhibitor. Potently inhibits angiogenesis and induces regression in tumor xenografts.
-
Rociletinib is a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC.
-
Venadaparib is a selective and orally active PARP1/2 inhibitor with significant in vitro and in vivo activities in multiple cancer models.
-
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.
-
Capivasertib is an orally active AKT inhibitor with pharmacodynamic activity in multiple solid and hematologic tumors.
-
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.
-
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.
-
GL0388 activates Bax and induces Bax-mediated apoptosis. GL0388 suppresses breast cancer xenograft tumor growth in vivo.
-
Lumiracoxib is a COX-2 inhibitor. Lumiracoxib acts as nonselective NSAID with anti-inflammatory, analgesic and antipyretic activities.
-
SJ6986 is a selective and orally active GSPT1/GSPT2 degrader, displaying selectivity over classical IMiD neosubstrates, such as IKZF1/3
-
DP-C-4 is a CRBN-Based dual PROTAC for EGFR and PARP could provide an effective study for cancer diseases.
-
ABBV-744 is a first-in-class, orally active and selective BET BDII inhibitor could provide an effective study for prostate cancer.
-
Inupadenant is an orally active, highly selective A2A receptor antagonist with potent anti-tumor activity.
-
GGTI-2154 is a potent and selective inhibitor of GGTase I and has the potential for the research of cancer.
-
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.
-
Nimotuzumab is a humanized IgG1 monoclonal antibody targeting EGFR. Nimotuzumab is a strong antitumor drug.
-
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.
-
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.
-
NRX-2663 is a potent enhancer of the interaction between β-catenin SCFβ-TrCP, potentiates the ubiquitylation of mutant β-Catenin by β-TrCP.
-
M3258 is an orally bioavailable, potent, reversible, and highly selective immunoproteasome subunit LMP7 (β5i) inhibitor.
-
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.
-
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.
-
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.
-
VT-107 is a potent and pan-TEAD auto-palmitoylation inhibitor. VT-107 can inhibit the proliferation of NF2-deficient mesothelioma cells.
-
IV-361 is an orally active, potent, and selective CDK7 inhibitor. IV-361 exhibits excellent anti-tumor activity.
-
HS-131, a near infrared dye tethered Hsp90 inhibitor, is able to detect oncogene-driven many breast cancers.
-
Z-VAD-FMK is a cell-permeant, irreversible pan-caspase inhibitor, which prevents apoptosis in many different cell types.
-
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.
-
LY294002, a broad-spectrum inhibitor of PI3K (IC50s ranging 0.5-0.97 μM for PI3Kα, PI3Kδ, and PI3Kβ), is an apoptosis inducer.
-
Trichostatin A (TSA) is a potent and specific inhibitor of HDAC class I/II. Trichostatin A exhibits anti-tumor activity.
-
Fulvestrant is a pure antiestrogen and a potent estrogen receptor (ER) antagonist. Fulvestrant induces autophagy and has antitumor efficacy.
-
Iberdomide (CC-220) is an orally active cereblon (CRBN) E3 ligase modulator (CELMoD) with antitumor and immunostimulatory activities。
-
Ruxolitinib is a potent and selective JAK1/2 inhibitor and has 130-fold selectivity for JAK1/2 over JAK3. Ruxolitinib induces autophagy.
-
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.
-
Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor with good anticancer activity.
-
Sorafenib (Bay 43-9006) is an orally active Raf inhibitor and induces autophagy and apoptosis with anti-tumor activity.
-
ARQ 531 is a potent, ATP-competitive, reversible non-covalent and orally active BTK inhibitor, with anti-tumor activities.
-
Wortmannin is a potent, selective, irreversible and orally active PI3K inhibitor, with anticancer effects.
-
Birinapant (TL32711), a bivalent Smac mimetic, is a potent antagonist for XIAP and cIAP1 and induces apoptosis.
-
GSK2606414 is an orally available PERK inhibitor and is a potent compound of cancer and neurological diseases.
-
AZD4635 is a potent, selective and orally active antagonist of A2AR that reverses adenosine-mediated immune suppression.
-
IACS-010759 is an orally active, potent mitochondrial complex I of oxidative phosphorylation (OXPHOS) inhibitor with antitumor activity.
-
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.
-
Sapanisertib is an orally available, potent, and highly selective mTORC1/2 inhibitor demonstrating promise in numerous malignancies.
-
Elesclomol is an oxidative stress inducer that induces cancer cell apoptosis. Elesclomol is a reactive oxygen species (ROS) inducer.
-
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.
-
Cytochalasin B is a cell-permeable mycotoxin binding to the barbed end of actin filaments, disrupting the formation of actin polymers.
-
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.
-
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.
-
CX-5461 is a potent and orally bioavailable inhibitor of Pol I-mediated rRNA synthesis with potent antitumor activity.
-
Daunorubicin is a topoisomerase II inhibitor with a wide spectrum of anticancer activity and anti-HBV effect.
-
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.
-
Nintedanib a potent and orally active triple vascular kinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β.
-
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.
-
Crizotinib is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Anti-tumor activity.
-
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.
-
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.
-
PR-104A is a hypoxia-selective DNA cross-linking agent/DNA-damaging agent and cytotoxin. Antitumor Activity. Leukemia (T-ALL).
-
Axitinib is a multi-targeted tyrosine kinase inhibitor and potently inhibitor VEGFR1, VEGFR2, VEGFR3 and PDGFRβ.
-
Fadrozole is a potent, selective, and nonsteroidal inhibitor of aromatase with an IC50 of 6.4 nM. Can be used for cancer research.
-
Troglitazone is a potent PPARγ agonist with antitumor activies. Troglitazone has the potential for the research of the pancreatic cancer.
-
Spautin-1 is a specific and potent autophagy inhibitor which inhibits ubiquitin-specific peptidases, USP10 and USP13.
-
Flavopiridol is a broad spectrum and competitive inhibitor of CDKs, inhibiting CDK1, CDK2, CDK4 with IC50s of 30, 170, 100 nM, respectively.
-
Lonidamine, an antitumor agent and an indazole derivative, interferes with energy-yielding processes in cancer cells.
-
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.
-
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.
-
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.
-
AUTAC2 is a FKBP12-targeting autophagy-mediated degrader (AUTAC). AUTAC2 contains an FBnG and an SLF moiety.
-
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.
-
Oprozomib (PR-047) is an orally active peptide epoxyketone proteasome inhibitor.
-
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.
-
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.
-
Rebeccamycin, an antitumor antibiotic, inhibits DNA topoisomerase I. Rebeccamycin can be used for leukemia research.
-
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.
-
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.
-
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.
-
Parsatuzumab (RG 7414) is a humanized monoclonal antibody, that acts as an immunomodulator, and binds to EGFL7.
-
Golcadomide is a potent and orally active CRBN E3 ligase modulator with immunomodulating and antineoplastic activities.
-
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.
-
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.
-
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.
-
CYD-2-11 is a selective Bax agonist with antitumor activities in vitro and vivo and the inducing of cell apoptosis.
-
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).
-
CYD-4-61 is a novel Bax activator. It induces cytochrome c release, mitochondrial membrane penetration, consequently leads to cell apoptosis.
-
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.
-
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
-
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.
-
Tigatuzumab, a humanized IgG1 anti-DR5 monoclonal antibody, is aTRAIL-R2 agonist, with potent anticancer effects.
-
OTS193320 is a potent SUV39H2 methyltransferase activity inhibitor. OTS193320 triggers apoptotic cell death.
-
FA16 is a specific and metabolically stable ferroptosis inducer. It inhibits system Xc-, results in tumor progression suppression.
-
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.
-
YX-2-107 is a PROTAC that selectively degrades CDK6.
-
Bapotulimab (BAY-1905254) is an ILDR2 IgG antibody that blocks the immunosuppressive effects of ILDR2 on T-cell activation.
-
YL-939 was a potent inhibitor of iron death and significantly improved liver injury in a model of iron death-related acute liver injury.
-
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.
-
Enavatuzumab (PDL192; ABT-361) is a humanized IgG1 monoclonal antibody targeting the receptor of TWEAK with potent antitumor activity.
-
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.
-
SZUH280, a potent and selective PROTAC HDAC8 degrader, ,shows antitumor activity in an A549 nude mouse model.
-
Talacotuzumab is an IgG1-type fully humanized, CD123-neutralizing monoclonal antibody containing a modified Fc structure.
-
Lexatumumab is a TRAIL-R2 agonist antibody that can induce apoptosis. It shows stronger efficacy when combined with other anticancer agents.
-
MS8815 is a selective EZH2 PROTAC degrader. MS8815 can be used for the research of triple-negative breast cancer (TNBC),
-
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.
-
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.
-
Ferristatin is a potent iron transport inhibitor and shows antiviral potency and anti-MTase (methyltransferase) activity.
-
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.
-
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.
-
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.
-
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.
-
MC0704 is a STAT3 inhibitor (IC50=2.13 μM), which can be used for the research of metastatic triple-negative breast cancer (mTNBC).
-
MPT0B014 is a potent tubulin polymerization inhibitor and induces cancer cell apoptosis in a dose-dependent manner.
Products
-
All
-
Inhibitors & Agonists
-
Isotope-Labeled Compounds
-
Fluorescent Dye
-
Peptides
-
Recombinant Proteins
-
Antibodies
-
Screening Libraries
-
Inhibitory Antibodies
-
Reference Standards
-
GMP Small Molecules
-
Enzyme
-
Biochemical Assay Reagents
-
Natural Products
| Cat. No. | Product Name | Information | Application | Publication |
|---|---|---|---|---|
| HY-B0240 | Disulfiram |
Disulfiram (Tetraethylthiuram disulfide) is a specific inhibitor of aldehyde-dehydrogenase (ALDH1), used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells. Disulfiram, a copper ion carrier, with Cu2+ increases intracellular ROS levels and induces cuproptosis.
|
Metabolic or Endocrine Disease
Breast Cancer
Prostate Cancer
Pancreatic Cancer
Ovarian Cancer
Viral Infection
Depression
Pain
Autoimmune Disease
Digestive System Inflammation
SARS-CoV-2 Infection
|
162
|
| HY-12040 | Elesclomol |
Elesclomol (STA-4783) is a potent copper ionophore and promotes copper-dependent cell death (cuproptosis). Elesclomol specifically binds ferredoxin 1 (FDX1) α2/α3 helices and β5 strand. Elesclomol inhibits FDX1-mediated Fe-S cluster biosynthesis. Elesclomol is an oxidative stress inducer that induces cancer cell apoptosis. Elesclomol is a reactive oxygen species (ROS) inducer. Elesclomol can be used for Menkes and associated disorders of hereditary copper deficiency research.
|
Digestive System Disease
Prostate Cancer
Digestive System Inflammation
SARS-CoV-2 Infection
Parkinson's Disease
|
131
|
| HY-N6782 | Oligomycin |
Oligomycin, an antifungal antibiotic, is an inhibitor of H+-ATP-synthase. Oligomycin blocks oxidative phosphorylation and the electron transport chain. Oligomycin inhibits HIF-1alpha expression in hypoxic tumor cells.
Source: Streptomyces |
|
122
|
| HY-L012 | Metabolism/Protease Compound Library |
Metabolism is the set of life-sustaining chemical reactions in organisms. Metabolic pathways are enzyme-mediated biochemical reactions that lead to biosynthesis (anabolism) or breakdown (catabolism) of natural product small molecules within a cell or tissue. Acting as catalysts, enzymes are crucial to metabolism - they allow a reaction to proceed more rapidly - and they also allow the regulation of the rate of a metabolic reaction. Proteases are used throughout an organism for various metabolic processes. Proteases control a great variety of physiological processes that are critical for life, including the immune response, cell cycle, cell death, wound healing, food digestion, and protein and organelle recycling. Imbalances in metabolic activities have been found to be critical in a number of pathologies, such as cardiovascular diseases, inflammation, cancer, and neurodegenerative diseases.
MCE designs a unique collection of 7,360 Metabolism/Protease-related small molecules that act as a useful tool for drug discovery of metabolism-related diseases.
|
|
89
|
| HY-L089 | Mitochondria-Targeted Compound Library |
Mitochondria plays an important role in many vital processes in cells, including energy production, fatty-acid oxidation and the Tricarboxylic Acid (TCA) cycle, calcium signaling, permeability transition, apoptosis and heat production. At present, it is recognized that many diseases are associated with impaired mitochondrial function, such as increased accumulation of ROS and decreased OXPHOS and ATP production. Mitochondria are recognized as one of the most important targets for new drug design in cancer, cardiovascular, and neurological diseases, etc. Some small molecule drugs or biologics can act on mitochondria through various pathways, including ETC inhibition, OXPHOS uncoupling, mitochondrial Ca2+ modulation, and control of oxidative stress via decrease or increase of mitochondrial ROS accumulation.
MCE supplies a unique collection of 1,182 mitochondria-targeted compound that mainly targeting Mitochondrial Metabolism, ATP Synthase, Mitophagy, Reactive Oxygen Species, etc. MCE Mitochondria-Targeted Compound Library is a useful tool for mitochondria-targeted drug discovery and related research.
|
|
89
|
| HY-L058 | Glycolysis Compound Library |
Glycolysis is a series of metabolic processes by which one molecule of glucose is catabolized to two molecules of pyruvate with a net gain of two ATP. Glycolysis takes place in 10 steps and catalyzed by a series of enzyme, such as hexokinase, Glucose-6-phosphate isomerase, Phosphofructokinase, etc. Glycolysis is used by all cells in the body for energy generation.
Most cancer cells exhibit increased glycolysis and use this metabolic pathway for generation of ATP as a main source of their energy supply. This phenomenon is known as the Warburg effect and is considered as one of the most fundamental metabolic alterations during malignant transformation. Because increased aerobic glycolysis is commonly seen in a wide spectrum of human cancers, development of novel glycolytic inhibitors as a new class of anticancer agents is likely to have broad therapeutic applications.
MCE provides a unique collection of 1,379 glycolysis compounds that mainly target hexokinase, glucokinase, enolase, pyruvate kinase, PDHK, etc. MCE Glycolysis Compound Library is a useful tool for glucose metabolism research and anti-cancer drug discovery.
|
|
86
|
| HY-L092 | Glucose Metabolism Compound Library |
Glucose homeostasis is tightly regulated to meet the energy requirements of the vital organs and maintain an individual’s health. Glucose metabolism includes glycolysis, tricarboxylic acid cycle, pentose phosphate pathway, oxidative phosphorylation and other metabolic pathways. Glucose is the major carbon source that provides the main energy for life. Glucose metabolism dysregulation is also implicated in many diseases such as diabetes, heart disease, neurodegenerative diseases and even cancer.
MCE offers a unique collection of 1,777 compounds related to glucose metabolism, which target glucose metabolism related targets, such as GLUT, Hexokinase, Pyruvate Kinase, IDH, etc. MCE glucose metabolism library is a powerful tool for studying glucose metabolism and drug discovery of diseases related to glucose metabolism.
|
|
85
|
| 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.
|
|
84
|
| HY-L059 | Pyroptosis Compound Library |
Programmed cell death pathways, including apoptosis, pyroptosis and necroptosis, are regulated by unique sets of host proteins that coordinate a variety of biological outcomes. Pyroptosis is a highly inflammatory form of programmed cell death that occurs most frequently upon infection with intracellular pathogens and is likely to form part of the antimicrobial response. This process promotes the rapid clearance of various bacterial, viral, fungal and protozoan infections by removing intracellular replication niches and enhancing the host's defensive responses. Pyroptosis has been widely studied in inflammatory and infection disease models. Recently, there are growing evidences that pyroptosis also plays an important role in the development of cancer, cardiovascular diseases and Metabolic disorder, etc.
MCE designs a unique collection of 2,034 pyroptosis-related compounds mainly focusing on the key targets in the pyroptosis signaling pathway and can be used in the research of pyroptosis signal pathway and related diseases.
|
|
84
|
| HY-L076 | Drug-Induced Liver Injury (DILI) Compound Library |
Drug-induced liver injury (DILI; also known as drug-induced hepatotoxicity) is caused by medications (prescription or OTC), herbal and dietary supplements (HDS), or other xenobiotics that result in abnormalities in liver tests or in hepatic dysfunction that cannot be explained by other causes. Drugs are an important cause of liver injury. Drug-induced hepatic injury is the most common reason cited for withdrawal of an approved drug.
DILI is thought to occur via several different mechanisms. Among these are direct impairment of the structural (e.g., mitochondrial dysfunction) and functional integrity of the liver; production of a metabolite that alters hepatocellular structure and function; production of a reactive drug metabolite that binds to hepatic proteins to produce new antigenic drug-protein adducts, which are targeted by hosts’ defenses (the hapten hypothesis); and initiation of a systemic hypersensitivity response (i.e., drug allergy) that damages the liver.
MCE Drug-induced Liver Injury (DILI) Compound Library contains a unique collection of 641 hepatotoxicity causing compounds and is a powerful tool to research DILI and other drug toxicities. This library can be used to understand the mechanisms of DILI, identify biomarkers for early DILI prediction, and allow timely recognition during drug development, thus finally achieving successful DILI prevention and assessment in the pre-marketing phase.
|
|
84
|
| HY-L083 | Anti-Cancer Metabolism Compound Library |
Mutations in oncogenes and tumor suppressor genes can modify multiple signaling pathways and in turn cell metabolism, which facilitates tumorigenesis. The paramount hallmark of tumor metabolism is “aerobic glycolysis” or the Warburg effect, coined by Otto Warburg in 1926, in which cancer cells produce most of energy from glycolysis pathway regardless of whether in aerobic or anaerobic condition. Usually, cancer cells are highly glycolytic (glucose addiction) and take up more glucose than do normal cells from outside. The increased uptake of glucose is facilitated by the overexpression of several isoforms of membrane glucose transporters (GLUTs). Likewise, the metabolic pathways of glutamine, amino acid and fat metabolism are also altered. Recent trends in anti-cancer drug discovery suggests that targeting the altered metabolic pathways of cancer cells result in energy crisis inside the cancer cells and can selectively inhibit cancer cell proliferation by delaying or suppressing tumor growth.
MCE provides a unique collection of 3,806 compounds which cover various tumor metabolism-related signaling pathways. These compounds can be used for anti-cancer metabolism targets identification, validation as well anti-cancer drug discovery.
|
|
84
|
| HY-L034M | Anti-Aging Compound Library Mini |
Research has shown that drugs targeting aging pathways demonstrate promising potential in models of age-related diseases such as Alzheimer's disease, cardiovascular diseases, metabolic syndrome, osteoarthritis, and various malignancies. This suggests that intervening in the biological processes of aging may enable synergistic prevention and treatment of multiple chronic diseases. Against the backdrop of the gradual elucidation of core aging mechanisms-including cellular senescence, telomere attrition, epigenetic dysregulation, and chronic inflammation anti-aging research has shifted from traditional phenotypic interventions toward targeting key pathways that regulate biological age.
The MCE Anti-Aging Compound Library Mini is precisely built upon this cutting-edge concept. It focuses on aging-related targets validated through genetic or functional studies, comprising 381 compounds designed to provide systematic research tools for aging biology and intervention strategy development. The library covers core mechanisms such as mTOR, SIRT, energy metabolism, clearance of senescent cells, optimization of mitochondrial function, and telomere maintenance. For each target, 1-5 compounds with clear activity and strong representativeness have been carefully selected, spanning the entire translational spectrum from preclinical tool molecules to clinically investigational drugs.
|
|
83
|
| HY-L064 | Glutamine Metabolism Compound Library |
Glutamine is an important metabolic fuel that helps rapidly proliferating cells meet the increased demand for ATP, biosynthetic precursors, and reducing agents. Glutamine Metabolism pathway involves the initial deamination of glutamine by glutaminase(GLS), yielding glutamate and ammonia. Glutamate is converted to the TCA cycle intermediate α-ketoglutarate (α-KG) by either glutamate dehydrogenase (GDH) or by the alanine or aspartate transaminases (TAs), to produce both ATP and anabolic carbons for the synthesis of amino acids, nucleotides and lipids. During periods of hypoxia or mitochondrial dysfunction, α-KG can be converted to citrate in a reductive carboxylation reaction catalyzed by IDH2. The newly formed citrate exits the mitochondria where it is used to synthesize fatty acids and amino acids and produce the reducing agent, NADPH.
Cancer cells display an altered metabolic circuitry that is directly regulated by oncogenic mutations and loss of tumor suppressors. Mounting evidence indicates that altered glutamine metabolism in cancer cells has critical roles in supporting macromolecule biosynthesis, regulating signaling pathways, and maintaining redox homeostasis, all of which contribute to cancer cell proliferation and survival. Thus, intervention in glutamine metabolic processes could provide novel approaches to improve cancer treatment.
MCE owns a unique collection of 1,827 compounds targeting the mainly proteins and enzymes involved in glutamine metabolism pathway. Glutamine Metabolism compound library is a useful tool for intervention in glutamine metabolic processes.
|
|
83
|
| HY-L085 | Anti-Parkinson's Disease Compound Library |
Parkinson’s disease (PD), the second most common age-associated neurodegenerative disorder, is characterized by the loss of dopaminergic (DA) neurons and the presence of α-synuclein-containing aggregates in the substantia nigra pars compacta (SNpc). Motor features such as tremor, rigidity, bradykinesia and postural instability are common traits of PD. To date, there is no treatment to stop or at least slow down the progression of the disease. The etiology and pathogenesis of PD is still elusive, however, a large body of evidence suggests a prominent role of oxidative stress, inflammation, apoptosis, mitochondrial dysfunction and proteasome dysfunction in the pathogenesis of PD.
MCE offers a unique collection of 2,199 compounds with anti- Parkinson’s Disease activities or targeting the unique targets of PD. MCE Anti- Parkinson's Disease Compound Library is a useful tool for exploring the mechanism of PD and discovering new drugs for PD.
|
|
83
|
| HY-L133 | Cuproptosis Compound Library |
Copper is an important co-factor of all biological enzymes, but if the concentration exceeds the threshold of maintaining the homeostasis mechanism, copper will lead to cytotoxicity. This death mechanism has been named "Cuproptosis".
The mechanism of cuproptosis distinct from all other known mechanisms of regulated cell death, including apoptosis, pyroptosis, necroptosis, and ferroptosis.
Copper combine with the lipoylated components of the tricarboxylic acid cycle (TCA), leading to lipoylated protein aggregation and subsequent loss of iron-sulfur cluster proteins, ultimately resulting in protein toxicity stress and cell death. Studies have shown that the necessary factors for cuproptosis include the presence of glutathione, mitochondrial metabolism of galactose and pyruvate, and glutamine metabolism.
Targeted regulation of cuproptosis is a potential choice to treat cancer, rheumatoid arthritis, and other diseases. For example, up-regulation of LIPT1 may inhibit the occurrence and development of tumors by destroying TCA in mitochondria and then inducing cuproptosis.
MCE supplies a unique collection of 446 cuproptosis-related compounds, all of which act on the targets or signaling pathways related to cuproptosis and may have in inhibitory or activated effect on cuproptosis. MCE Cuproptosis Library is a useful tool for drug research related to cancer, rheumatoid arthritis, and other diseases.
|
|
83
|
| HY-L144 | Mitochondrial Protection Compound Library |
Normal mitochondrial function is critical for maintaining cellular homeostasis because mitochondria produce ATP and are the major intracellular source of free radicals. Cellular dysfunctions induced by intracellular or extracellular insults converge on mitochondria and induce a sudden increase in permeability on the inner mitochondrial membrane, the so-called mitochondrial membrane permeability transition (MMPT). MMPT is caused by the opening of pores in the inner mitochondrial membrane, matrix swelling, and outer membrane rupture. The MMPT is an endpoint to initiate cell death because the pore opening together with the release of mitochondrial cytochrome c activates the apoptotic pathway of caspases.
The normal operation of mitochondrial function is important for maintaining normal cell death and treatment of mitochondrial diseases. MCE offers a unique collection of 1,112 compounds with identified and potential mitochondrial protective activity. MCE Mitochondrial Protection Compound Library is critical for drug discovery and development.
|
|
83
|
| HY-L148 | TCA Cycle Compound Library |
The TCA cycle (tricarboxylic acid cycle)—is also known as the Krebs cycle or the citric acid cycle (CAC). The TCA cycle is a series of chemical reactions that release stored energy through the oxidation of acetyl-CoA in carbohydrates, fats, and proteins.
For decades, the TCA cycle has been considered as the central pathway for cell oxidative phosphorylation to produce energy and biosynthesis. Research shows that TCA cycle is associated with many diseases, especially cancer. In colon carcinoma, liver cancer and other cancers, there are mutations that lead to the imbalance of TCA cycle metabolites, indicating that TCA cycle may be related to the occurrence of cancer. Understanding the role and molecular mechanism of TCA cycle in inhibiting or promoting cancer progression will promote the development of new metabolite-based cancer treatment methods in the future.
MCE supplies a unique collection of 72 compounds related to the TCA cycle. MCE TCA Cycle Compound Library is a useful tool for the TCA cycle related research and anti-cancer drug development. p>
|
|
83
|
| HY-L155 | Mitochondrial Toxicity Compound Library |
Mitochondria, as the main place of energy supply in life, is essential to maintain normal life activities. Mitochondrial dysfunction is associated with common diseases, such as cardiovascular diseases, neurodegenerative diseases, diabetes and cancer. The heart, brain and liver rely heavily on mitochondrial function as the main organs for drug metabolism. In addition, mitochondria is also a target of many drugs, some of which induce organotoxicity by inducing mitochondrial toxicity.
MCE contains 545 mitochondrial toxic compounds, which can be used as tool compounds for drug development and disease mechanism research.
|
|
83
|
| HY-L162M | Cell Death Inhibitor Library Mini |
Cell death is a core biological process that maintains homeostasis in multicellular organisms, playing a dual role in life activities. On one hand, cell death participates in physiological processes such as cell renewal and damage repair through precise regulation; on the other hand, it actively eliminates damaged, infected, or cancerous cells, thereby blocking pathological progression and preserving organism health. Cell death not only ensures the normal development and growth regulation of organisms but is also closely associated with the occurrence and development of various diseases. Numerous studies have shown that specific types of programmed cell death play critical roles in disease progression, providing an important theoretical basis for developing novel therapeutic strategies by regulating cell death pathways.
MCE offers 23 types of commonly used cell death inhibitors, such as apoptosis, ferroptosis, pyroptosis, and cuproptosis, suitable for use as positive controls in the study of novel cell death mechanisms.
|
|
83
|
| HY-L168 | Extracellular Vesicles (EVs) Compound Library |
Extracellular vesicles (EVs) are small membrane binding structures that are released from cells into the surrounding environment and play a crucial role in mediating and regulating intercellular communication related to physiological and pathological processes. EVs are lipid membrane vesicles composed of proteins, lipids, and nucleic acids. EVs can be divided into several types based on their source, such as extracellular vesicles, microcapsules, and apoptotic vesicles. The size range of exosomes is 30-150nm, which are endocrine in multi vesicular endosomes (MVEs); microvesicles (50-1000nm) are secreted directly through extracellular interactions, thereby releasing plasma membrane vesicles. In contrast, apoptotic bodies are usually larger, ranging in size from 1 to 5 μ m. This is generated during programmed cell death. EV plays a crucial role in transmitting information between cells and influencing the behavior and function of receptor cells.
MCE designs a unique collection of 707 small molecules related to extracellular vesicles (EVs). It is a good tool to be used for research on metabolize, cancer and other diseases.
|
|
83
|
| HY-L175 | Inflammasomes related Compound Library |
Inflammasomes are classic pattern recognition receptors for natural immune responses. Inflammasomes are polymeric protein complexes that regulate inflammatory responses and pyrolytic cell death, thereby exerting the host's defense against microorganisms. Inflammasomes sensors are associated with adapter proteins, activating inflammatory caspase-1, releasing inflammatory cytokines and inducing cell death, endowing the host with defense against pathogens. NLRP1, NLRP3, NLRC4, AIM2, and pyrin are considered typical inflammasomes because they convert cysteine asparaginase-1 into catalytically active capsaicin-1. In addition to infectious diseases, the importance of inflammasomes is also related to various clinical diseases, such as autoimmune diseases, neurodegeneration and metabolic disorders, and the development of cancer. Therefore, it is necessary to strictly regulate the activation and function of inflammasomes to avoid accidental host tissue damage while inducing pathogens to kill the inflammatory response.
MCE designs a unique collection of 178 inflammasomes related compounds. It is a good tool to be used for research on Inflammation, cancer and other diseases.
|
|
83
|
| HY-L201 | Cell Proliferation Compound Library |
Cell proliferation, the increase in cell numbers resulting from cell division, is a complex and tightly regulated process. Cell proliferation is regulated by coordinated entry into the cell cycle, and changes in proliferation are closely linked to disease development. Evolutionary dynamics links tumor growth and progression with cell proliferation, cell death, and mutation rates. In addition, cell proliferation is central to degenerative diseases, the development of which is often accompanied by accelerated multiplication of cancer cells. Therefore, assays of cell proliferation levels are frequently used for laboratory research purposes and increasingly for clinical assessment of tumor aggressiveness and potentially to guide care. It has been shown that multiple key targets are collectively involved in regulating the process of cell proliferation, such as CDK, E2F, pRB, β-Catenin, and others.
MCE collects 3,628 compounds that target and regulate key targets of cell proliferation, which can be used in studies of cell proliferation mechanisms and drug discovery.
|
|
83
|
| HY-L204 | Lactic Acid Metabolic Compound Library |
Lactic acid metabolism is one of the key metabolic pathways within living organisms. It plays a crucial role not only in cellular energy conversion but is also closely related to a variety of physiological and pathological processes. The production and clearance of lactic acid are important indicators of cellular metabolic balance, and its abnormal regulation may lead to conditions such as lactic acidosis, muscle fatigue, and hereditary metabolic diseases. Moreover, lactic acid is closely related to the malignancy of tumors and is considered a biomarker for malignant tumors and poor prognosis. Lactic acid can serve as a metabolic substrate to support the metabolic needs of tumor cells under hypoxic conditions, and it can also cause acidification of the tumor microenvironment, suppress immune cell function to promote immune evasion, and induce drug resistance in tumor cells. Currently, targeting lactic acid-lactylation and its related metabolic pathways has become a new research avenue for cancer treatment. In-depth exploration of the molecular mechanisms of lactic acid metabolism can help in screening lead compounds that regulate the lactic acid metabolism.
MCE contains 582 small molecule compounds targeting enzymes involved in lactic acid metabolism. This library is of significant value for researching the role of lactate metabolism in the mechanisms of diseases.
|
|
83
|
| HY-L227 | Amino Acid Metabolite Compound Library |
Amino acids are the fundamental components that sustain life activities, playing roles in ATP generation, promoting nucleotide synthesis, and maintaining cellular redox balance. Moreover, dysregulation of amino acid consumption is a significant potential regulatory mechanism leading to impaired anti-tumor immunity in immune cells. The normal functioning of immune cells relies on amino acid metabolic pathways to obtain energy and materials, and upon activation, they reprogram their metabolism to support growth, proliferation, and effector functions. Additionally, metabolic disorders of specific amino acids (such as branched-chain amino acids, glutamine, and arginine) can exacerbate mitochondrial dysfunction and oxidative stress, thereby promoting myocardial fibrosis and cardiac cell damage. Therefore, conducting research related to amino acid metabolism holds promise for discovering potential drugs for diseases related to cancer, immunity, and metabolism.
MCE can provide 195 kinds of metabolites of amino acid metabolic pathways, which can be used for drug screening in various diseases such as cancer, immune disorders, metabolic diseases, mitochondrial-targeted diseases
|
|
83
|
| HY-L228 | Lipid Metabolite Compound Library |
Lipids are important energy storage substances in the human body. They are involved in the regulation of cell structure and function, as well as signaling pathways and gene expression. Abnormal lipid levels in tissues or their dysregulation can lead to various diseases. These include obesity, type 2 diabetes, non-alcoholic fatty liver disease, neurodegenerative diseases, infections, and cancer. Therefore, maintaining normal levels of lipid metabolism is critical to overall health.
One of the key features of cancer is aberrant lipid metabolism. This includes alterations in lipid uptake, lipid desaturation, neolipogenesis, lipid droplets, and fatty acid oxidation in cancer cells. These changes all contribute to cellular survival in an ever-changing microenvironment. They do this by modulating feed-forward oncogenic signals and key oncogenic functions. Additionally, they affect oxidative stress, other types of stress, immune responses, and intercellular communication. Alterations in lipid metabolism have a strong impact on the properties of cancer stem cells. This includes aspects such as self-renewal, differentiation, invasion, metastasis, drug sensitivity, and resistance. Furthermore, these alterations also modulate T cell responses.
MCE can offer 146 metabolites of lipid metabolism pathways, which can be used for drug screening in cancer, immune-based diseases, metabolic diseases, and other diseases.
|
|
83
|
| HY-L231 | TCA Cycle Metabolite Compound Library |
The TCA cycle (tricarboxylic acid cycle)—is also known as the Krebs cycle or the citric acid cycle (CAC). The TCA cycle is a series of chemical reactions that release stored energy through the oxidation of acetyl-CoA in carbohydrates, fats, and proteins.
For decades, the TCA cycle has been considered as the central pathway for cell oxidative phosphorylation to produce energy and biosynthesis. Research shows that TCA cycle is associated with many diseases, especially cancer. In colon carcinoma, liver cancer and other cancers, there are mutations that lead to the imbalance of TCA cycle metabolites, indicating that TCA cycle may be related to the occurrence of cancer. Understanding the role and molecular mechanism of TCA cycle in inhibiting or promoting cancer progression will promote the development of new metabolite-based cancer treatment methods in the future.
MCE supplies a unique collection of 25 key intermediates of the TCA cycle, which can be utilized for TCA-related research and metabolomics identification studies.
|
|
83
|
| 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.
|
|
83
|
| HY-L252 | Carbohydrate Metabolite Compound Library |
Carbohydrate metabolism serves as a central hub for energy supply and biosynthesis in living organisms and plays a critical role in the onset and progression of various diseases. In recent years, studies have shown that tumor cells reprogram their energy metabolism through aerobic glycolysis (the Warburg effect) to support rapid proliferation. Immune cells also rely on specific carbohydrate metabolic pathways to regulate their activation and differentiation states, while disorders such as diabetes and metabolic syndrome arise directly from dysregulation of carbohydrate metabolism. In addition, enzymes and key metabolic nodes involved in carbohydrate metabolism have become important targets for drug discovery, and therapeutic strategies targeting glycolysis, the pentose phosphate pathway, and energy metabolism are continuously advancing the treatment of cancer and metabolic diseases. Therefore, systematic analysis of carbohydrate metabolic networks and their associated metabolites is of great significance for elucidating disease mechanisms and developing novel therapeutic approaches.
The MCE Carbohydrate Metabolism Metabolite Library is constructed based on classical carbohydrate metabolic pathways and contains 76 metabolites. It systematically integrates key metabolic networks, including glycolysis, the pentose phosphate pathway, the tricarboxylic acid (TCA) cycle, monosaccharide metabolism, and sugar acid interconversions. The library comprehensively covers core metabolic nodes from glucose uptake and utilization to energy production and biosynthesis, while also incorporating important upstream and downstream intermediates. It enables accurate representation of intracellular metabolic flux dynamics and is well suited for applications such as metabolic flux analysis, target validation, and mechanistic studies. Furthermore, it provides robust support for multi-omics integration and the development of precision intervention strategies.
|
|
83
|
| HY-L263 | Energy Metabolites Library |
Energy metabolism is the most fundamental biochemical process in living organisms, encompassing glycolysis, the TCA cycle, oxidative phosphorylation, the pentose phosphate pathway, and fatty acid oxidation. These core pathways directly regulate cell survival, proliferation, differentiation, and apoptosis. Dysregulation of energy metabolism is closely linked to major diseases including cancer, diabetes, obesity, cardiovascular diseases, neurodegenerative disorders, and ischemia‑reperfusion injury. Targeting these metabolic pathways has become a frontier in drug discovery and mechanistic research.
The MCE Energy Metabolite Compound Library features 89 structurally defined small‑molecule compounds. It covers energy substrates, pathway intermediates, coenzymes and redox carriers, nucleotide derivatives, and microenvironmental modulators. This library is applicable to research areas including tumor metabolism, insulin resistance, mitochondrial dysfunction, oxidative stress, neuroprotection, and cardiometabolic diseases, providing a high‑quality tool for mechanistic studies, biomarker discovery, and high‑throughput drug screening.
|
|
83
|
| HY-L264 | DNA Damage Repair Inhibitor Library |
DNA damage response (DDR) is a fundamental mechanism for maintaining genomic stability. When DNA damage occurs, such as single- or double-strand breaks or replication fork stalling, cells rely on key proteins including ATM, ATR, PARP, and DNA-PK to sense the damage and transmit signals, thereby regulating DNA repair, cell-cycle arrest, and cell death. Inhibition of specific DNA repair or checkpoint pathways can prevent tumor cells from effectively repairing accumulated DNA damage, ultimately leading to tumor cell death.
MCE DNA Damage Repair Inhibitor Library contains 1,544 compounds, focusing on key nodes involved in DNA damage response and DNA repair. The library covers multiple DNA repair and cell-cycle checkpoint pathways, providing a systematic compound screening tool for research on precision oncology, synthetic lethality, drug resistance mechanisms, and chemo- or radiosensitization.
|
|
83
|
| HY-L265 | Cholesterol Metabolism Compound Library |
Cholesterol is a crucial lipid that maintains cell membrane structure, serves as a precursor for the synthesis of steroid hormones and bile acids, and plays an important role in cell signal transduction and membrane function regulation. Intracellular cholesterol levels are precisely controlled by multiple processes, including synthesis, uptake, transport, esterification, storage, and efflux. Dysregulation of cholesterol metabolism is closely associated with diseases such as atherosclerosis, fatty liver disease, metabolic syndrome, and various cancers.
The Cholesterol Metabolism Compound Library contains 558 compounds and focuses on cholesterol metabolism and homeostatic regulation. It provides an efficient tool for mechanistic studies of cholesterol metabolism and for drug discovery in metabolism‑related diseases.
|
|
83
|
| 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.
|
|
67
|
| HY-Y1269D | Ammonium chloride, for molecular biology |
Ammonium chloride (Salmiac), for molecular biology is an inhibitor of Slc26a4 and SMAD2. Ammonium chloride, for molecular biology reduces the protein expression level of Slc26a4 in lung tissue, and attenuates ozone-induced increases in proinflammatory cytokines, inflammatory cells, pulmonary resistance, goblet cell hyperplasia, peribronchial inflammation and thiocyanate levels in mouse tissues and bronchoalveolar lavage fluid. Ammonium chloride, for molecular biology decreases the level of phosphorylated SMAD2, inhibits autophagy by reducing autophagy-related proteins, and enhances Cisplatin (HY-17394)-induced cancer cell apoptosis and DNA double-strand breaks. Ammonium chloride, for molecular biology also inhibits the TCA cycle, reduces ATP production, increases glucose utilization, regulates the levels of lactic acid, glutamic acid and ATP, and induces morphological degeneration of neuroblastoma cells. Ammonium chloride, for molecular biology can be used in studies related to ozone-induced airway injury, hepatocellular carcinoma, human cervical cancer, hepatic encephalopathy, Reye syndrome, epilepsy and neurodegenerative diseases.
|
|
62
|
| HY-114118C | Semaglutide sodium |
Semaglutide sodium is a long-acting, selective, competitive GLP-1R agonist that can penetrate the blood-brain barrier. After activating GLP-1R, Semaglutide sodium promotes insulin secretion, inhibits gastric emptying and appetite, and at the same time enhances autophagy, inhibits oxidative stress and apoptosis. Semaglutide sodium also regulates mitochondrial function and lipid metabolism (such as reducing de novo lipogenesis in the liver). Semaglutide sodium has activities such as lowering blood sugar, reducing weight, neuroprotection (such as improving motor function in Parkinson's disease models, reducing α-synuclein aggregation) and improving hepatic steatosis. Semaglutide sodium can be used for the study of neurodegenerative diseases and liver diseases such as type 2 diabetes, obesity, Parkinson's disease, metabolic associated fatty liver disease (MASLD), and cancer.
|
|
50
|
| HY-114118B | Semaglutide acetate |
Semaglutide acetate is a long-acting, selective, competitive GLP-1R agonist that can penetrate the blood-brain barrier. After activating GLP-1R, Semaglutide acetate promotes insulin secretion, inhibits gastric emptying and appetite, and at the same time enhances autophagy, inhibits oxidative stress and apoptosis. Semaglutide acetate also regulates mitochondrial function and lipid metabolism (such as reducing de novo lipogenesis in the liver). Semaglutide acetate has activities such as lowering blood sugar, reducing weight, neuroprotection (such as improving motor function in Parkinson's disease models, reducing α-synuclein aggregation) and improving hepatic steatosis. Semaglutide acetate can be used for the study of neurodegenerative diseases and liver diseases such as type 2 diabetes, obesity, Parkinson's disease, metabolic associated fatty liver disease (MASLD), and cancer.
|
|
50
|
| HY-114118A | Semaglutide TFA |
Semaglutide TFA is a long-acting, selective, competitive GLP-1R agonist that can penetrate the blood-brain barrier. After activating GLP-1R, Semaglutide TFA promotes insulin secretion, inhibits gastric emptying and appetite, and at the same time enhances autophagy, inhibits oxidative stress and apoptosis. Semaglutide TFA also regulates mitochondrial function and lipid metabolism (such as reducing de novo lipogenesis in the liver). Semaglutide TFA has activities such as lowering blood sugar, reducing weight, neuroprotection (such as improving motor function in Parkinson's disease models, reducing α-synuclein aggregation) and improving hepatic steatosis. Semaglutide TFA can be used for the study of neurodegenerative diseases and liver diseases such as type 2 diabetes, obesity, Parkinson's disease, metabolic associated fatty liver disease (MASLD), and cancer.
|
|
50
|
| HY-114118 | Semaglutide |
Semaglutide is a long-acting, selective, competitive GLP-1R agonist that can penetrate the blood-brain barrier. After activating GLP-1R, Semaglutide promotes insulin secretion, inhibits gastric emptying and appetite, and at the same time enhances autophagy, inhibits oxidative stress and apoptosis. Semaglutide also regulates mitochondrial function and lipid metabolism (such as reducing de novo lipogenesis in the liver). Semaglutide has activities such as lowering blood sugar, reducing weight, neuroprotection (such as improving motor function in Parkinson's disease models, reducing α-synuclein aggregation) and improving hepatic steatosis. Semaglutide can be used for the study of neurodegenerative diseases and liver diseases such as type 2 diabetes, obesity, Parkinson's disease, metabolic associated fatty liver disease (MASLD), and cancer.
|
|
50
|
| HY-N0148A | Rutin hydrate |
Rutin (Rutoside) hydrate is a flavonoid found in many plants and shows a wide range of biological activities including anti-inflammatory, antidiabetic, antioxidant, neuroprotective, nephroprotective, hepatoprotective and reducing Aβ oligomer activities. Rutin hydrate can cross the blood brain barrier. Rutin hydrate attenuates vancomycin-induced renal tubular cell apoptosis via suppression of apoptosis, mitochondrial dysfunction, and oxidative stress.
|
Cancer
Digestive System Disease
Digestive System Inflammation
Glucose Metabolism
Alzheimer's Disease
Parkinson's Disease
|
35
|
| HY-N6687 | Calcimycin |
Calcimycin (A-23187) is an antibiotic and a unique divalent cation ionophore (like calcium and magnesium). Calcimycin induces Ca2+-dependent cell death by increasing intracellular calcium concentration. Calcimycin inhibits the growth of Gram-positive bacteria and some fungi. Calcimycin also inhibits the activity of ATPase and uncouples oxidative phosphorylation (OXPHOS) of mammalian cells. Calcimycin induces apoptosis and autophagy.
Source: Streptomyces chartreusensis |
|
26
|
| HY-W105518 | L-Carnitine tartrate |
L-Carnitine tartrate is a highly polar, small zwitterion. L-Carnitine tartrate is an essential co-factor for the mitochondrial β-oxidation pathway. L-Carnitine tartrate functions to transport long chain fatty acyl-CoAs into the mitochondria for degradation by β-oxidation. L-Carnitine tartrate is an antioxidant. L-Carnitine tartrate can ameliorate metabolic imbalances in many inborn errors of metabolism[3].
|
|
22
|
| HY-B2246 | L-Carnitine hydrochloride |
L-Carnitine hydrochloride ((R)-Carnitine hydrochloride), a highly polar, small zwitterion, is an essential co-factor for the mitochondrial β-oxidation pathway. L-Carnitine hydrochloride functions to transport long chain fatty acyl-CoAs into the mitochondria for degradation by β-oxidation. L-Carnitine hydrochloride is an antioxidant. L-Carnitine hydrochloride can ameliorate metabolic imbalances in many inborn errors of metabolism.
|
|
22
|
| HY-B0399 | L-Carnitine |
L-Carnitine ((R)-Carnitine), a highly polar, small zwitterion, is an essential co-factor for the mitochondrial β-oxidation pathway. L-Carnitine functions to transport long chain fatty acyl-CoAs into the mitochondria for degradation by β-oxidation. L-Carnitine is an antioxidant. L-Carnitine can ameliorate metabolic imbalances in many inborn errors of metabolism.
|
|
22
|
| 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.
|
|
20
|
| HY-B0572 | Zinc Pyrithione |
Zinc Pyrithione is an antifungal and antibacterial agent disrupting membrane transport by blocking the proton pump. Zinc Pyrithione is also a copper ionophore that delivers copper into cells and is a useful tool for studying cuproptosis.
|
|
12
|
| HY-W250154 | β-Nicotinamide adenine dinucleotide reduced dipotassium |
β-Nicotinamide adenine dinucleotide reduced dipotassium is an orally effective reduced coenzyme. β-Nicotinamide adenine dinucleotide reduced dipotassium plays a role in regenerating electron donors during cellular energy metabolism, including glycolysis, β-oxidation, and the tricarboxylic acid (TCA) cycle. β-Nicotinamide adenine dinucleotide reduced dipotassium regulates calcium homeostasis by promoting the opening of IP3-gated Ca2+ channels and inhibiting Ryanodine receptor, and affects mitochondrial function through direct interaction with VDAC. β-Nicotinamide adenine dinucleotide reduced dipotassium is used in cytoprotective studies related to cerebral ischemic injury, neurodegenerative diseases, aging, and signal transduction.
|
|
11
|
| HY-W015410 | Disodium succinate |
Disodium succinate is an anti-anxiety agent with oral activity. Disodium succinate is the salt form of Succinic acid. Disodium succinate is an intermediate product of the tricarboxylic acid cycle. Disodium succinate is an important platform chemical. Disodium succinate can be used as surfactant, additive, ion chelating agent, flavoring agent and other applications in chemical, pharmaceutical and food fields.
|
|
11
|
| HY-153169 | 6PPD-Q |
6PPD-Q (6PPD-Quinone) is an environmental pollutant that can be detected in human urine and is widely present in the environment. 6PPD-Q targets and binds to CNR2, CNR1, AA2AR, LCAT, and TRPA1, with CNR2 exhibiting the highest binding affinity, potentially acting as a CNR2 receptor agonist to activate cannabinoid receptors. 6PPD-Q induces intestinal inflammation and barrier damage by disrupting mitochondrial function, reducing neuronal glycolysis metabolites and TCA cycle intermediates, and exacerbating α-synuclein (α-syn) aggregation.
6PPD-Q is applicable in research on environmental toxicology, neurodegenerative diseases, and inflammation-related disorders.
|
|
11
|
| HY-N0420 | Succinic acid |
Succinic acid is an anti-anxiety agent with oral activity. Disodium succinate is the salt form of Succinic acid. Succinic acid is an intermediate product of the tricarboxylic acid cycle. Succinic acid is an important platform chemical. Succinic acid can be used as surfactant, additive, ion chelating agent, flavoring agent and other applications in chemical, pharmaceutical and food fields.
|
|
11
|
| HY-F0001 | NADH disodium salt |
NADH disodium salt (Disodium NADH) is an orally effective reduced coenzyme. NADH disodium salt plays a role in regenerating electron donors during cellular energy metabolism, including glycolysis, β-oxidation, and the tricarboxylic acid (TCA) cycle. NADH disodium salt regulates calcium homeostasis by promoting the opening of IP3-gated Ca2+ channels and inhibiting Ryanodine receptor, and affects mitochondrial function through direct interaction with VDAC. NADH disodium salt is used in cytoprotective studies related to cerebral ischemic injury, neurodegenerative diseases, aging, and signal transduction.
|
|
11
|
| HY-12695B | Guanosine triphosphate trisodium salt hydrate |
Guanosine triphosphate (GTP) trisodium salt hydrate is a critical nucleotide and regulator of cellular metabolism. Guanosine triphosphate trisodium salt hydrate promotes ribosomal DNA localization, pre-rRNA transcription and ribosome biogenesis by binding to RNA polymerase I and GPN proteins (GPN1/3). Guanosine triphosphate trisodium salt hydrate links MYC-dependent ribosome biogenesis to nucleotide sufficiency, acts as a metabolic gatekeeper supporting protein synthesis, DNA/RNA synthesis and cellular signal transduction, while also participating in the physiological activities of pancreatic β-cells and serving as an oxidative substrate for reactive oxygen species. In small cell lung cancer with high MYC expression, Guanosine triphosphate trisodium salt hydrate accumulates through the IMPDH-driven synthetic pathway, thereby affecting apoptosis and mitotic processes. Guanosine triphosphate trisodium salt hydrate is used in the research of small cell lung cancer, hepatoblastoma and cellular metabolism.
|
|
9
|
| HY-W010737 | Guanosine triphosphate disodium |
Guanosine triphosphate (GTP) disodium is a critical nucleotide and regulator of cellular metabolism. Guanosine triphosphate disodium promotes ribosomal DNA localization, pre-rRNA transcription and ribosome biogenesis by binding to RNA polymerase I and GPN proteins (GPN1/3). Guanosine triphosphate disodium links MYC-dependent ribosome biogenesis to nucleotide sufficiency, acts as a metabolic gatekeeper supporting protein synthesis, DNA/RNA synthesis and cellular signal transduction, while also participating in the physiological activities of pancreatic β-cells and serving as an oxidative substrate for reactive oxygen species. In small cell lung cancer with high MYC expression, Guanosine triphosphate disodium accumulates through the IMPDH-driven synthetic pathway, thereby affecting apoptosis and mitotic processes. Guanosine triphosphate disodium is used in the research of small cell lung cancer, hepatoblastoma and cellular metabolism.
|
|
9
|
| HY-B0158 | Cytidine |
Cytidine is a pyrimidine nucleoside and acts as a component of RNA. Cytidine is a precursor of uridine. Cytidine controls neuronal-glial glutamate cycling, affecting cerebral phospholipid metabolism, catecholamine synthesis, and mitochondrial function.
Source: Widespread |
|
8
|
| HY-114293 | Acetyl coenzyme A |
Acetyl-coenzyme A (Acetyl-CoA) is a membrane-impermeant central metabolic intermediate, participates in the TCA cycle and oxidative phosphorylation metabolism. Acetyl-coenzyme A, regulates various cellular mechanisms by providing (sole donor) acetyl groups to target amino acid residues for post-translational acetylation reactions of proteins. Acetyl Coenzyme A is also a key precursor of lipid synthesis.
|
|
7
|
| HY-113596A | Acetyl coenzyme A lithium |
Acetyl-coenzyme A (Acetyl-CoA) lithium is a membrane-impermeant central metabolic intermediate, participates in the TCA cycle and oxidative phosphorylation metabolism. Acetyl-coenzyme A lithium, regulates various cellular mechanisms by providing (sole donor) acetyl groups to target amino acid residues for post-translational acetylation reactions of proteins. Acetyl Coenzyme A lithium is also a key precursor of lipid synthesis.
|
|
7
|
| HY-17473 | Embelin |
Embelin (Embelic acid), a potent, nonpeptidic XIAP inhibitor (IC50=4.1 μM), inhibits cell growth, induces apoptosis, and activates caspase-9 in prostate cancer cells with high levels of XIAP. Embelin blocks NF-kappaB signaling pathway leading to suppression of NF-kappaB-regulated antiapoptotic and metastatic gene products. Embelin also induces autophagic and apoptotic cell death in human oral squamous cell carcinoma cells.
|
Breast Cancer
Prostate Cancer
Liver Cancer
Leukemia/Lymphoma/Myeloma
Pancreatic Cancer
Ovarian Cancer
Depression
Pain
Digestive System Inflammation
Obesity
|
7
|
| HY-156376 | Cu(II)-Elesclomol |
Cu(II)-Elesclomol is a complex formed by Elesclomol (HY-12040) and Cu2+ (copper ions). Cu(II)-Elesclomol is also a weak inhibitor of DNA topoisomerase I. Cu(II)-Elesclomol exerts anticancer effects by inducing oxidative stress and DNA damage through copper chelation. Cu(II)-Elesclomol can inhibit tumor cell proliferation and induce cell cycle arrest and apoptosis. Cu(II)-Elesclomol can be used in the study of cancer.
|
|
7
|
| HY-113596 | Acetyl Coenzyme A trisodium |
Acetyl-coenzyme A (Acetyl-CoA) trisodium is a membrane-impermeant central metabolic intermediate, participates in the TCA cycle and oxidative phosphorylation metabolism. Acetyl-coenzyme A trisodium, regulates various cellular mechanisms by providing (sole donor) acetyl groups to target amino acid residues for post-translational acetylation reactions of proteins. Acetyl Coenzyme A trisodium is also a key precursor of lipid synthesis.
|
|
7
|
| HY-113225 | Guanosine triphosphate |
Guanosine triphosphate (GTP) is a critical nucleotide and regulator of cellular metabolism. Guanosine triphosphate promotes ribosomal DNA localization, pre-rRNA transcription and ribosome biogenesis by binding to RNA polymerase I and GPN proteins (GPN1/3). Guanosine triphosphate links MYC-dependent ribosome biogenesis to nucleotide sufficiency, acts as a metabolic gatekeeper supporting protein synthesis, DNA/RNA synthesis and cellular signal transduction, while also participating in the physiological activities of pancreatic β-cells and serving as an oxidative substrate for reactive oxygen species. In small cell lung cancer with high MYC expression, Guanosine triphosphate accumulates through the IMPDH-driven synthetic pathway, thereby affecting apoptosis and mitotic processes. Guanosine triphosphate is used in the research of small cell lung cancer, hepatoblastoma and cellular metabolism.
|
|
6
|
| HY-N9933 | Tauro-β-muricholic acid |
Tauro-β-muricholic acid (TβMCA) is an orally active trihydroxylated bile acid and a competitive, reversible FXR antagonist (IC50=40 μM). Tauro-β-muricholic acid inhibits bile acid-induced hepatocyte apoptosis by maintaining mitochondrial membrane potential, while simultaneously inhibiting intestinal FXR signaling, affecting bile acid synthesis, hepatic lipid metabolism, and insulin sensitivity. Accumulation of tauro-β-muricholic acid disrupts metabolic homeostasis, promoting cancer stem cell proliferation and tumor progression. The mechanisms of tauro-β-muricholic acid involve two aspects: first, inhibiting the translocation of the pro-apoptotic protein Bax to mitochondria and maintaining mitochondrial membrane potential (MMP); and second, blocking the FXR signaling pathway to regulate bile acid metabolism, reduce serum ceramide production, and downregulate the hepatic SREBP1C/CIDEA pathway. Tauro-β-muricholic acid possesses anti-hepatocyte apoptosis, bile acid homeostasis regulation, and liver fat accumulation reduction properties, and also functions as a biomarker, making it useful in the study of diseases such as bile acid metabolism disorders, non-alcoholic fatty liver disease, colorectal cancer, and liver fibrosis.
Source: rat |
|
6
|
| HY-113224 | Desmosterol |
Desmosterol is a cholesterol-like molecule. In the Bloch pathway of cholesterol biosynthesis, Desmosterol is a direct precursor of cholesterol. As an endogenous metabolite, Desmosterol is used to study cholesterol metabolism . Desmosterol is an LXR activator and SREBP inhibitor, which can suppress macrophage inflammasome activation and prevent vascular inflammation and atherosclerosis. A reduction in Desmosterol promotes the production of mitochondrial reactive oxygen species (ROS) in macrophages and pyrin domain-dependent inflammasome activation of NLRP3. Desmosterol holds potential for research in inflammation, metabolism, and cardiovascular diseases .
|
Endogenous Metabolite
LXR
Fatty Acid Synthase (FASN)
Interleukin Related
Reactive Oxygen Species (ROS)
NOD-like Receptor (NLR)
Inflammation or Immune System Disease
Blood or Cardio-cerebrovascular Disease
Metabolic or Endocrine Disease
Hepatitis C Virus Infection
|
6
|
| HY-125623 | MitoPerOx |
MitoPerOx is a mitochondrial-targeted, lipid peroxidation-indicating fluorescent probe with BODIPY581/591 fluorophores. The triphenylphosphine cation (TPP+) of MitoPerOx can be selectively enriched in mitochondria (depending on membrane potential) and can be used to detect lipid peroxidation in the inner mitochondrial membrane. Under the action of lipid peroxides, the BODIPY581/591 fluorophores of MitoPerOx shift their emission wavelength from 590 nm (reduced state) to 520 nm (oxidized state), and ratiometric detection can be performed at an excitation wavelength of 488 nm. MitoPerOx can specifically monitor the peroxidation of mitochondrial phospholipids (especially cardiolipin) and is used in the study of oxidative stress-related diseases (such as aging, neurodegenerative diseases, and mitochondrial dysfunction)[1][2].
|
|
6
|
| HY-12695 | Guanosine triphosphate trisodium |
Guanosine triphosphate (GTP) trisodium is a critical nucleotide and regulator of cellular metabolism. Guanosine triphosphate trisodium promotes ribosomal DNA localization, pre-rRNA transcription and ribosome biogenesis by binding to RNA polymerase I and GPN proteins (GPN1/3). Guanosine triphosphate trisodium links MYC-dependent ribosome biogenesis to nucleotide sufficiency, acts as a metabolic gatekeeper supporting protein synthesis, DNA/RNA synthesis and cellular signal transduction, while also participating in the physiological activities of pancreatic β-cells and serving as an oxidative substrate for reactive oxygen species. In small cell lung cancer with high MYC expression, Guanosine triphosphate trisodium accumulates through the IMPDH-driven synthetic pathway, thereby affecting apoptosis and mitotic processes. Guanosine triphosphate trisodium is used in the research of small cell lung cancer, hepatoblastoma and cellular metabolism.
|
|
6
|
| HY-137808 | Succinyl-Coenzyme A sodium |
Succinyl CoA (Succinyl-coenzyme A) sodium is a pivotal intermediate metabolite in the tricarboxylic acid cycle and a key coenzyme A metabolite. Succinyl CoA sodium is biosynthesized from α-ketoglutarate or propionyl-CoA. Succinyl CoA sodium acts as a critical precursor and substrate for heme biosynthesis and gluconeogenesis. Succinyl CoA sodium insufficiency caused by cobalamin deficiency is directly linked to growth retardation, impaired heme synthesis, tissue glycine accumulation and neurological abnormalities. Succinyl CoA sodium can be used in research on metabolic, neurological, and hematological abnormalities (such as porphyria) caused by nutritional vitamin B12 deficiency (leading to a lack of Succinyl-Coenzyme A synthesis).
|
|
5
|
| HY-Y0836 | Diethyl succinate |
Diethyl succinate (Diethyl Butanedioate) can be utilized at physiological pH, allowing it to penetrate biological membranes and integrate into the cells of tissue cultures, where it is metabolized via the tricarboxylic acid cycle. Diethyl succinate modulates the polarization and activation of microglial cells by reducing mitochondrial fission and the levels of reactive oxygen species (ROS), thereby exerting an inflammatory protective effect in primary microglial cells. Furthermore, Diethyl succinate is non-toxic and can be used in flavorings and seasonings.
|
|
5
|
| HY-P0119A | Lixisenatide acetate |
Lixisenatide acetate is a glucagon-like peptide-1 (GLP-1) receptor agonist. Lixisenatide acetate inhibits the inflammatory response through down regulation of pro-inflammatory cytokines, and suppresses of the Akt-MEK1/2 signaling pathway. Lixisenatide acetate can inhibit oxidative stress, mitochondrial dysfunction and apoptosis. Lixisenatide acetate can be used for the researches of inflammation, metabolic disease, neurological disease and cardiovascular disease, such as rheumatoid arthritis, diabetes, Alzheimer's disease and atherosclerosis.
|
Neurological, Eye or Ear Disease
Inflammation or Immune System Disease
Blood or Cardio-cerebrovascular Disease
Metabolic or Endocrine Disease
|
4
|
| HY-W094516 | Disodium succinate hexahydrate |
Disodium succinate hexahydrate (Wormwood acid disodium hexahydrate) is an anti-anxiety agent with oral activity. Disodium succinate hexahydrate is an intermediate product of the tricarboxylic acid cycle. Disodium succinate hexahydrate is an important platform chemical. Disodium succinate hexahydrate can be used as surfactant, additive, ion chelating agent, flavoring agent and other applications in chemical, pharmaceutical and food fields.
|
|
4
|
| HY-113081 | 1-Methyladenosine |
1-Methyladenosine is an RNA modification that can serve as a tumor marker, with elevated levels in the body associated with cancer development. Following 1-methyladenosine methylation, upregulation of PPARδ expression regulates cholesterol metabolism and activates Hedgehog signaling pathway, driving liver tumorigenesis.
|
|
4
|
| HY-B0300 | Penicillamine |
Penicillamine (D-(-)-Penicillamine) is a penicillin metabolic degradation product, can be used as a heavy metal chelator. Penicillamine increases free copper and increases oxidative stress. Penicillamine has effect of seizures through nitric oxide/NMDA pathways. Penicillamine is a potential immune modulator. Penicillamine can be used for the research of Wilson disease, rheumatoid arthritis, and cystinuria.
Source: Penicillium |
|
4
|
| HY-44134 | Dimethyl 2-oxoglutarate |
Dimethyl 2-oxoglutarate (Dimethyl α-ketoglutarate) is a cell-permeable derivative of 2-oxoglutarate and tricarboxylic acid cycle metabolite with antioxidant properties. Dimethyl 2-oxoglutarate inhibits Autophagy. Dimethyl 2-oxoglutarate prevents mitochondrial damage and reduces ROS production. Dimethyl 2-oxoglutarate alleviates Carbon tetrachloride (HY-Y0298)-induced liver fibrosis. Dimethyl-2-oxoglutaric acid can be used in the research of diseases such as Alzheimer's disease, diabetes, and cardiomyopathy.
|
Endogenous Metabolite
Drug Derivative
Autophagy
Mitochondrial Metabolism
Reactive Oxygen Species (ROS)
|
4
|
| HY-116330 | Hyperforin |
Hyperforin is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin modulates Ca2+ levels by activating Ca2+-conducting non-selective canonical TRPC6 channels and triggers adipose tissue thermogenesis via the Dlat-AMPK signaling axis to suppress obesity. Hyperforin also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model.
|
|
3
|
| HY-N7056 | 4'-Hydroxychalcone |
4'-Hydroxychalcone is a chalcone isolated from licorice root, with hepatoprotective activity. 4'-Hydroxychalcone inhibits TNFα-induced NF-κB activation via proteasome inhibition. 4'-Hydroxychalcone induces a rapid potassium release from mitochondrial vesicles and causes deterioration of respiratory control and oxidative phosphorylation of isolated rat liver mitochondria.
|
|
3
|
| HY-N2181 | Acetylshikonin |
Acetylshikonin is an oral active anti-cancer, anti-inflammatory, antioxidant, anti-fertility, antibacterial, and neuroprotective agent. Acetylshikonin is a inhibitor of acetylcholinase (AChE) (IC50=34.6 μM) and nonselective cytochrome P450. Acetylshikonin can induce Apoptosis and Autophagy in cancer cells. Acetylshikonin regulates blood glucose, liver fat metabolism, and renal fibrosis, and is used in the study of diabetes, diabetic nephropathy (DN), obesity, and nonalcoholic fatty liver disease (NAFLD).
|
Cancer
Neurological, Eye or Ear Disease
Digestive System Disease
Bacterial Infection
Digestive System Inflammation
Glucose Metabolism
|
3
|
| HY-P1723A | Spexin TFA |
Spexin (Neuropeptide Q) TFA is a selective agonist of galanin receptors GAL2 and GAL3, and is a conserved peptide that functions as a neurotransmitter/neuromodulator and endocrine factor. Spexin TFA can function through both central and peripheral actions. Spexin TFA upregulates Beclin 1 to inhibit ferroptosis induced by excessive autophagy, reduces the uptake of long-chain fatty acids by adipocytes, and regulates energy metabolism by increasing lipid oxidation (e.g., reducing the respiratory exchange ratio in rodents). Spexin TFA improves cardiac function in the Doxorubicin hydrochloride (HY-15142)-induced cardiotoxicity model, protects mitochondrial membrane potential, and reduces iron accumulation and lipid peroxidation. Spexin TFA can be used to study obesity and its related metabolic disorders, cardiovascular diseases (e.g., cardioprotection), and side effects of tumor chemotherapy.
|
|
2
|
| HY-N1970 | 5,7-Dihydroxychromone |
5,7-Dihydroxychromone is a flavonoid compound with antioxidant properties. 5,7-Dihydroxychromone induces Nrf2 nuclear translocation, increases Nrf2/ARE binding activity, and up-regulates Nrf2-dependent antioxidant genes HO-1, NQO1, GCLc. 5,7-Dihydroxychromone attenuates excessive ROS generation, inhibits activated caspase-3, caspase-9, cleaved PARP expression, and prevents neuronal apoptosis and cell death. 5,7-Dihydroxychromone increases LXRα and PPARγ mRNA expression, induces preadipocyte differentiation, and regulates blood glucose levels. 5,7-Dihydroxychromone inhibits radial growth of soil pathogenic fungi, radicle elongation of select seedlings, and transiently inhibits Bradyrhizobium sp. growth in high mannitol medium. 5,7-Dihydroxychromone can be used for the research of Parkinson’s disease, type 2 diabetes mellitus and pathogenic fungal infection.
|
Inflammation or Immune System Disease
Pancreatic Cancer
Viral Infection
Parkinson's Disease
Obesity
Lung Fibrosis
|
2
|
| HY-N0840 | Bruceantin |
|
2
|
|
| HY-P1723 | Spexin |
Spexin (Neuropeptide Q) is a selective agonist of galanin receptors GAL2 and GAL3, and is a conserved peptide that functions as a neurotransmitter/neuromodulator and endocrine factor. Spexin can function through both central and peripheral actions. Spexin upregulates Beclin 1 to inhibit ferroptosis induced by excessive autophagy, reduces the uptake of long-chain fatty acids by adipocytes, and regulates energy metabolism by increasing lipid oxidation (e.g., reducing the respiratory exchange ratio in rodents). Spexin improves cardiac function in the Doxorubicin hydrochloride (HY-15142)-induced cardiotoxicity model, protects mitochondrial membrane potential, and reduces iron accumulation and lipid peroxidation. Spexin can be used to study obesity and its related metabolic disorders, cardiovascular diseases (e.g., cardioprotection), and side effects of tumor chemotherapy.
|
|
2
|
| HY-W010970 | 5'-Guanylic acid disodium salt |
5'-Guanylic acid disodium salt is the disodium salt form of 5'-Guanylic acid (HY-N5134). 5'-Guanylic acid disodium salt is a purine nucleotide that participates in physiological processes such as energy metabolism, signal transduction, and gene expression regulation. 5'-Guanylic acid disodium salt regulates the expression of genes related to fatty acid metabolism. 5'-Guanylic acid disodium salt is the weak agonist for ionotropic glutamate receptors (iGluR), reduces the activity of the glutamatergic system and exhibits neuroprotective effect. 5'-Guanylic acid disodium salt also causes neuronal cell death at high concentrations.
|
|
2
|
| HY-N1925 | Tea polyphenol |
Tea polyphenol is the floorboard of phenolic compounds in tea. Tea polyphenol exhibits biological activity including antioxidant and anti-cancer activities, inhibition of cell proliferation, induction of apoptosis, cell cycle arrest and modulation of carcinogen metabolism.
|
Cancer
Neurological, Eye or Ear Disease
Digestive System Disease
Digestive System Inflammation
Glucose Metabolism
|
2
|
| HY-N2522 | Carboxyatractyloside dipotassium |
Carboxyatractyloside dipotassium is a diterpenoid. Carboxyatractyloside dipotassium can be isolated from plants of the genus Xanthium. Carboxyatractyloside dipotassium is an ADP/ATP carrier inhibitor, inhibiting mitochondrial ADP/ATP transport. Carboxyatractyloside dipotassium promotes ROS production, induces Ca2+ release, and leads to mitochondrial dysfunction. Carboxyatractyloside dipotassium induces lethargy, weakness, and epileptic seizures in rats.
|
|
2
|
| HY-101017 | Palmitoylcarnitine chloride |
Palmitoylcarnitine chloride is a C16:0 long-chain acylcarnitine and an intermediate product of fatty acid oxidation. The level of Palmitoylcarnitine chloride in human prostate cancer tissues is higher than that in non-cancerous tissues. Palmitoylcarnitine chloride can be used in studies related to lipid metabolism associated with prostate cancer.
|
|
2
|
| HY-N2118 | Bilobetin |
Bilobetin, an active component of Ginkgo biloba, can reduce blood lipids and improve the effects of insulin. Bilobetin ameliorated insulin resistance, increased the hepatic uptake and oxidation of lipids, reduced very-low-density lipoprotein triglyceride secretion and blood triglyceride levels, enhanced the expression and activity of enzymes involved in β-oxidation and attenuated the accumulation of triglycerides and their metabolites in tissues. Bilobetin also increased the phosphorylation, nuclear translocation and activity of PPARα accompanied by elevated cAMP level and PKA activity.
|
Metabolic or Endocrine Disease
Lung Cancer
Pancreatic Cancer
Neurodegenerative Disease
Depression
Pain
Digestive System Inflammation
|
2
|
| HY-N2406 | Dihydrocaffeic acid |
Dihydrocaffeic acid is a microbial metabolite of flavonoids. Dihydrocaffeic acid scavenges intracellular ROS and increases nitric oxide synthase activity. Dihydrocaffeic acid reduces phosphorylation of MAPK p38 and prevent UVB-induced skin damage. Dihydrocaffeic acid has antioxidant, anti-inflammatory and anti-cartilage degradation activities.
|
Lung Cancer
Prostate Cancer
Gastric Cancer
Ovarian Cancer
Neurodegenerative Disease
Depression
Pain
Obesity
Lung Fibrosis
Rheumatoid Arthritis
|
2
|
| HY-N1502 | Carboxyatractyloside tripotassium |
Carboxyatractyloside tripotassium is a diterpenoid. Carboxyatractyloside tripotassium can be isolated from plants of the genus Xanthium. Carboxyatractyloside tripotassium is an ADP/ATP carrier inhibitor, inhibiting mitochondrial ADP/ATP transport. Carboxyatractyloside tripotassium promotes ROS production, induces Ca2+ release, and leads to mitochondrial dysfunction. Carboxyatractyloside tripotassium induces lethargy, weakness, and epileptic seizures in rats.
|
|
2
|
| HY-B0762 | Acetyl-L-carnitine hydrochloride |
Acetyl-L-carnitine (O-Acetyl-L-carnitine; ALCAR) hydrochloride is an orally active mitochondrial energy metabolism regulator and neuroprotectant that can penetrate the blood-brain barrier. Acetyl-L-carnitine hydrochloride selectively enters cells and the brain through the organic cation transporter OCTN2. Acetyl-L-carnitine hydrochloride can participate in fatty acid β-oxidation, promote acetylcholine synthesis, regulate mitochondrial function and inhibit oxidative stress as an acetyl donor. Acetyl-L-carnitine hydrochloride exerts its activity by enhancing energy metabolism, protecting neurons and improving synaptic plasticity. Acetyl-L-carnitine hydrochloride is mainly used in the study of neurodegenerative diseases and metabolic disorder-related diseases such as neonatal hypoxic-ischemic brain damage, Alzheimer's disease, and depression.
|
Digestive System Disease
Prostate Cancer
Viral Infection
Depression
Digestive System Inflammation
Alzheimer's Disease
Parkinson's Disease
|
2
|
| HY-113218 | Acetyl-L-carnitine |
Acetyl-L-carnitine (O-Acetyl-L-carnitine; ALCAR) is an orally active mitochondrial energy metabolism regulator and neuroprotectant that can penetrate the blood-brain barrier. Acetyl-L-carnitine selectively enters cells and the brain through the organic cation transporter OCTN2. Acetyl-L-carnitine can participate in fatty acid β-oxidation, promote acetylcholine synthesis, regulate mitochondrial function and inhibit oxidative stress as an acetyl donor. Acetyl-L-carnitine exerts its activity by enhancing energy metabolism, protecting neurons and improving synaptic plasticity. Acetyl-L-carnitine is mainly used in the study of neurodegenerative diseases and metabolic disorder-related diseases such as neonatal hypoxic-ischemic brain damage, Alzheimer's disease, and depression.
Source: Homo sapiens |
Digestive System Disease
Viral Infection
Digestive System Inflammation
Alzheimer's Disease
Parkinson's Disease
|
2
|
| HY-N5134 | 5'-Guanylic acid |
5'-Guanylic acid is a purine nucleotide that participates in physiological processes such as energy metabolism, signal transduction, and gene expression regulation. 5'-Guanylic acid regulates the expression of genes related to fatty acid metabolism. 5'-Guanylic acid is the weak agonist for ionotropic glutamate receptors (iGluR), reduces the activity of the glutamatergic system and exhibits neuroprotective effect. 5'-Guanylic acid also causes neuronal cell death at high concentrations.
|
|
2
|
| HY-Y0808 | Dimethyl succinate |
Dimethyl succinate is an orally active cell permeable succinate analogue. Dimethyl succinate can disrupt the TCA cycle by elevating intracellular succinate levels, leading to reduced protein synthesis and impairs myogenic differentiation. Dimethyl succinate can induce apoptosis. Dimethyl succinate can decrease maximal cellular respiration and reserve capacity. Dimethyl succinate can rescue synapse loss in AD. Dimethyl succinate can be used for the researches of metabolic and neurological disease.
|
|
2
|
| HY-P71676 | PDCE2 Protein, Mouse (HEK293, His) |
PDCE2 Protein, a vital element in the pyruvate dehydrogenase complex, is integral to cellular metabolism. It catalyzes the conversion of pyruvate to acetyl-CoA and CO2, connecting glycolysis to the tricarboxylic acid (TCA) cycle. PDCE2's catalytic function is essential for efficient pyruvate utilization, ensuring the flow of carbon compounds through key metabolic pathways crucial for energy production and cellular homeostasis. PDCE2 Protein, Mouse (HEK293, His) is the recombinant mouse-derived PDCE2 protein, expressed by HEK293 , with N-10*His labeled tag.
Species: Mouse; Source: HEK293 |
|
2
|
| HY-Y1325E | Sodium acetate trihydrate, United States Pharmacopeia (USP) Reference Standard |
Sodium acetate trihydrate, United States Pharmacopeia (USP) Reference Standard (Sodium acetate trihydrate (Pharmaceutical primary standard, USP)) is a carboxylic acid and short-chain fatty acid (SCFAs). Sodium acetate trihydrate activates AMPK, increases ROS, cleaved caspase 9, PPARα, downregulates SREBP-1c, ChREBP expression. Sodium acetate trihydrate exhibits antifungal activity against Saccharomyces cerevisiae W303-1A. Sodium acetate trihydrate regulates energy metabolism. Sodium acetate trihydrate has anticancer activity against gastric cancer. Sodium acetate trihydrate induces writhing reaction and ulcerative colitis. Sodium acetate trihydrate can be used in the researches for gastric cancer, ulcerative colitis, hepatic steatosis, and pain.
|
Environmental Pollutants
Caspase
Reactive Oxygen Species (ROS)
Endogenous Metabolite
AMPK
Fungal
PPAR
|
1
|
| HY-N6906 | Oleuroside |
Oleuroside is a phenolic secoiridoid in olive. Oleuroside can protect against mitochondrial dysfunction in models of early Alzheimer's disease and brain ageing.
|
|
1
|
| HY-N3316 | Martynoside |
Martynoside protects ex vivo bone marrow cells from 5-fluorouracil (5-FU)-induced cell death and inflammation response by down-regulating the TNF signaling pathway.Martynoside is a potent antiestrogen in MCF-7 cells, increasing IGFBP3 levels
|
|
1
|
| HY-N7063 | Nerol |
Nerol is a constituent of neroli oil. Nerol Nerol triggers mitochondrial dysfunction and induces apoptosis via elevation of Ca2+ and ROS. Antifungal activity.
|
|
1
|
| HY-119976 | Boscalid |
Boscalid is a succinate dehydrogenase (SDHI) inhibitor with antifungal activity. Boscalid binds to the ubiquinone-binding site of fungal mitochondrial complex II, blocks ATP production and aerobic respiration, exhibits good control efficacy against a variety of plant fungal diseases including gray mold, sclerotinia rot and powdery mildew, and is widely used for disease control in agriculture. Boscalid induces apoptosis, altered lipid metabolism, mitochondrial dysfunction, respiratory impairment, oxidative stress, ROS accumulation and neurodevelopmental disorders in zebrafish. Boscalid reduces foraging ability, shortens median death time and causes chronic toxicity in exposed honeybees. Boscalid also possesses genotoxicity, cytotoxicity, elevated mitochondrial superoxide levels and early-stage apoptosis.
|
|
1
|
| HY-N0819 | Raddeanin A |
Raddeanin A is an oleanane-type triterpenoid saponin with oral activity. Raddeanin A inhibits SRC, mTOR, JNK, VEGFR2, NLRP3 inflammasome, Wnt/β-catenin, Wee1, PI3K/AKT signaling pathway, MAPK/ERK signaling pathway, AR-FL, AR-Vs, and downregulates the expression of p-PI3K and p-AKT. Raddeanin A inhibits osteoclast formation, bone resorption, osteolysis, cancer cell invasion, migration, proliferation, angiogenesis and epithelial-mesenchymal transition, while induces apoptosis, cell cycle arrest, ROS production, immunogenic cell death and dendritic cell maturation. Raddeanin A improves blood-retinal barrier function, alleviates inflammation, regulates the tumor microenvironment, and enhances the activity of anti-PD-1 antibody. Raddeanin A is applicable to the research of breast cancer-associated osteolysis, human osteosarcoma, colorectal cancer, glioblastoma, Alzheimer's disease, cholangiocarcinoma, melanoma, non-small cell lung cancer, castration-resistant prostate cancer and multiple myeloma.
|
Colorectal Cancer
Leukemia/Lymphoma/Myeloma
Cancer Immunology
Digestive System Inflammation
Non-Small Cell Lung Cancer
Immunotherapy for Melanoma
Alzheimer's Disease
|
1
|
| HY-F0001R | NADH disodium salt (Standard) |
NADH disodium salt (Disodium NADH) Standard is the analytical standard of NADH disodium salt (HY-F0001). This product is intended for research and analytical applications. NADH disodium salt (Disodium NADH) is an orally effective reduced coenzyme. NADH disodium salt plays a role in regenerating electron donors during cellular energy metabolism, including glycolysis, β-oxidation, and the tricarboxylic acid (TCA) cycle. NADH disodium salt regulates calcium homeostasis by promoting the opening of IP3-gated Ca2+ channels and inhibiting Ryanodine receptor, and affects mitochondrial function through direct interaction with VDAC. NADH disodium salt is used in cytoprotective studies related to cerebral ischemic injury, neurodegenerative diseases, aging, and signal transduction.
|
|
1
|
| HY-113004 | 3-Hydroxyvaleric acid |
3-Hydroxyvaleric acid is a five-carbon ketone body byproduct that can undergo an anaplerotic reaction to replenish the intermediates of the tricarboxylic acid cycle. 3-Hydroxyvaleric acid is one of the important monomers for the synthesis of polyhydroxyalkanoates (PHA). PHA is a type of biodegradable plastic that is widely used in environmentally friendly packaging, disposable products, and medical materials.
|
|
1
|
| HY-N0420S1 | Succinic acid-d4 |
Succinic-2,2,3,3-d4 acid is the deuterium labeled Succinic acid. Succinic acid is an intermediate product of the tricarboxylic acid cycle, as well as one of fermentation products of anaerobic metabolism.
|
|
1
|
| HY-W250122 | Glutamic acid sodium salt |
Glutamic acid sodium salt (Monosodium glutamate) is an orally active food flavor enhancer. Glutamic acid sodium salt causes ROS generation, mitochondrial dysfunction, and Apoptosis. Glutamic acid sodium salt upregulates CHOP, Grp78, and Bcl-2. Glutamic acid sodium salt impairs cognition, induces depressive-like behavior, induces hyperalgesia, and induces obesity and insulin resistance. Glutamic acid sodium salt can be used to study neurotoxicity (e.g., brain damage, cognitive impairment), metabolic disorders (e.g., obesity, insulin resistance), hepatotoxicity, and renal toxicity, as well as pain-related disorders.
|
Biochemical Assay Reagents
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
Apoptosis
HSP
Bcl-2 Family
Neurological, Eye or Ear Disease
Inflammation or Immune System Disease
Metabolic or Endocrine Disease
|
1
|
| HY-113168 | Butyrylcarnitine |
Butyrylcarnitine is an endogenous metabolite found in plasma. Elevated levels of Butyrylcarnitine are closely associated with abnormalities in lipid and energy metabolism. Butyrylcarnitine can serve as a diagnostic and prognostic indicator for certain diseases, such as heart failure and head and neck cancer.
|
|
1
|
| HY-Y1325H | Sodium acetate trihydrate, meets analytical specification of Ph. Eur. BP USP FCC E262, ≤0.00002% Al |
Sodium acetate trihydrate, meets analytical specification of Ph. Eur. BP USP FCC E262, ≤0.00002% Al is a carboxylic acid and short-chain fatty acid (SCFAs). Sodium acetate trihydrate activates AMPK, increases ROS, cleaved caspase 9, PPARα, downregulates SREBP-1c, ChREBP expression. Sodium acetate trihydrate exhibits antifungal activity against Saccharomyces cerevisiae W303-1A. Sodium acetate trihydrate regulates energy metabolism. Sodium acetate trihydrate has anticancer activity against gastric cancer. Sodium acetate trihydrate induces writhing reaction and ulcerative colitis. Sodium acetate trihydrate can be used in the researches for gastric cancer, ulcerative colitis, hepatic steatosis, and pain.
|
Environmental Pollutants
Caspase
Reactive Oxygen Species (ROS)
Endogenous Metabolite
AMPK
Fungal
PPAR
|
1
|
| HY-W615108B | β-Nicotinamide mononucleotide, reduced form disodium |
β-Nicotinamide mononucleotide, reduced form (NMNH) disodium is an orally active reduced version of β-Nicotinamide mononucleotide (HY-F0004). β-Nicotinamide mononucleotide, reduced form disodium can significantly increase the levels of NAD+ and NADH, inhibit glycolysis, the tricarboxylic acid cycle, and cell growth, with its effects being dependent on nicotinamide mononucleotide adenylyltransferase (NMNAT).
|
|
1
|
| HY-134238 | Cardiolipin (Heart, Bovine) sodium |
Cardiolipin (Heart, Bovine) sodium is a mitochondria-exclusive phospholipid that can be extracted from Bovine hear. Cardiolipin (Heart, Bovine) sodium can maintain mitochondrial function, regulate cellular metabolism and signaling and induce apoptosis and autophagy. Cardiolipin (Heart, Bovine) sodium can be coated on microtitre plates for ELISA assay. Cardiolipin (Heart, Bovine) sodium can be used for the researches of inflammation, immunology, cardiovascular and neurological disease.
|
Inflammation or Immune System Disease
Blood or Cardio-cerebrovascular Disease
Alzheimer's Disease
Parkinson's Disease
|
1
|
| HY-113076 | Thiamine pyrophosphate |
Thiamine pyrophosphate is the coenzyme form of Vitamin B1, and is a required intermediate in the pyruvate dehydrogenase complex and the ketoglutarate dehydrogenase complex. Thiamine pyrophosphate is necessary for oxidative phosphorylation and the pentose phosphate pathway by acting as a cofactor for α-ketoacid dehydrogenases.
|
|
1
|
| HY-P81070 | Pyruvate Dehydrogenase E2 Antibody (YA912) |
Pyruvate Dehydrogenase E2 Antibody (YA912) is a Mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to Pyruvate Dehydrogenase E2.
Host: Mouse; Reactivity: Human, Mouse |
|
1
|
| HY-P82260 | ADX/FDX1 Antibody (YA2005) |
ADX/FDX1 Antibody (YA2005) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to ADX.
Host: Rabbit; Reactivity: Human, Mouse, Rat |
|
1
|
| HY-B0831S | Buprofezin-d6 |
Buprofezin-d6 is the deuterium labeled Buprofezin. Buprofezin is a broad-spectrum insecticide and chitin synthesis inhibitor that targets developmental stage coleopteran pests.Buprofezin promotes the conversion of energy metabolism from the aerobic tricarboxylic acid (TCA) cycle and oxidative phosphorylation to anaerobic glycolysis. Buprofezin also promotes the production of reactive oxygen species (ROS) by inhibiting cytochrome c oxidase.
|
|
/
|
| HY-Y0836S1 | Diethyl succinate-d4 |
Diethyl succinate-d4 is the deuterium labeled Diethyl succinate. Diethyl succinate (Diethyl Butanedioate) is used at physiological pH and crosses biological membranes, incorporates into cells in tissue culture and is metabolized by the TCA cycle. Diethyl succinate is known to be non-toxic and used in fragrances and flavoring.
|
|
/
|
| HY-P10416 | Q14 |
Q14 is a polypeptide derived from the USP30 (ubiquitin specific peptidase 30) transmembrane (TM) domain with the ability to inhibit the deubiquitination activity of USP30 (IC50=57.2 nM). Q14 reduces USP30 activity by inhibiting the interaction between the USP30 transmembrane domain and its catalytic domain. Q14 peptide contains the LC3 interaction region (LIR) motif, which enables it to bind to the LC3 and accelerate the formation of autophagosomes, thereby promoting mitophagy. Q14 can be used in the study of neurodegenerative diseases as well as mitochondrial quality control and cell metabolism.
|
|
/
|
| HY-B0399G | L-Carnitine (GMP) |
L-Carnitine (GMP) is L-Carnitine (HY-B0399) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. L-Carnitine, a highly polar, small zwitterion, is an essential co-factor for the mitochondrial β-oxidation pathway. L-Carnitine functions to transport long chain fatty acyl-CoAs into the mitochondria for degradation by β-oxidation. L-Carnitine is an antioxidant. L-Carnitine can ameliorate metabolic imbalances in many inborn errors of metabolism.
|
|
/
|
| HY-182917 | MMB-DTCs-1,3-diaminopropane-DTCs-MMB |
MMB-DTCs-1,3-diaminopropane-DTCs-MMB is a Cuproptosis/Ferroptosis/Apoptosis inducer, and serves as the active metabolite of DMAPT-DTCs-1,3-diaminopropane-DTCs-DMAPT dimethanesulfonate (HY-182918). MMB-DTCs-1,3-diaminopropane-DTCs-MMB induces mitochondrial dysfunction, promotes reactive oxygen species (ROS) production, disrupts redox homeostasis, and triggers apoptosis, ferroptosis and cuproptosis in lung cancer cells. MMB-DTCs-1,3-diaminopropane-DTCs-MMB can be used in the research of lung cancer.
|
|
/
|
| HY-W768207 | Cytidine-1',2',3',4',5'-13C5 |
Cytidine-1',2',3',4',5'-13C5 is the 13C-labeled Cytidine (HY-B0158). Cytidine is a pyrimidine nucleoside and acts as a component of RNA. Cytidine is a precursor of uridine. Cytidine controls neuronal-glial glutamate cycling, affecting cerebral phospholipid metabolism, catecholamine synthesis, and mitochondrial function.
|
|
/
|
| HY-B0863S5 | Glyphosate-13C,15N-1 |
Glyphosate-13C,15N-1 is the 13C- and 15N-labeled Glyphosate (HY-B0863). Glyphosate, a non-selective systemic biocide with broad-spectrum activity, is an herbicidal derivative of the amino acid glycine. Glyphosate inhibits the enzymatic activity of the 5-endopyruvylshikimate 3-phosphate synthase (EPSPS) in the shikimic acid pathway, preventing the synthesis of the aromatic amino acids tyrosine, phenylalanine, and tryptophan. Glyphosate induces oxidative stress, neuroinflammation, and mitochondrial dysfunction, processes that lead to neuronal death by autophagia, necrosis, or apoptosis, as well as the appearance of behavioral and motor disorders.
|
|
/
|
| HY-P11114 | Periplanetasin-4 |
Periplanetasin-4 is an antimicrobial peptide that can be derived from the American cockroach (Periplaneta americana). Periplanetasin-4 reduces cell rounding and apoptosis. Periplanetasin-4 blocks Clostridium difficile toxin A-induced ROS production and the activation of downstream p38 MAPK and p21. Periplanetasin-4 significantly increases mitochondrial calcium level, reduces DPH fluorescence intensity and vacuolar dysfunction in Candida albicans ATCC 90028 cells. Periplanetasin-4 significantly ameliorates toxin A-induced mucosal damage in the mouse gut. Periplanetasin-4 can be used for the study of colitis.
|
|
/
|
| HY-W017540S | Cyclocreatine-13C3 |
Cyclocreatine-13C3 is the 13C-labeled Cyclocreatine (HY-W017540). Cyclocreatine, a creatine analogue, acts as a brain-penetrant and potent bioenergetic protective agent by providing high levels of ATP. Cyclocreatine can be phosphorylated and dephosphorylated by creatine kinases. Cyclocreatine suppresses creatine metabolism ameliorating the cognitive, autistic and epileptic phenotype in a mouse model of creatine transporter defciency. Cyclocreatine protects against ischemic injury and enhances cardiac recovery during early reperfusion in dogs and rats. Cyclocreatine decreases plaque-adjacent neuronal dystrophy in TREM2-deficient mice with amyloid-β pathology. Cyclocreatine is proming for research of ischemic heart disease, cardiovascular diseases, Alzheimer’s disease and other neurodegenerative diseases associated with microglial dysfunction, prostate cancer.
|
Cancer
Neurological, Eye or Ear Disease
Blood or Cardio-cerebrovascular Disease
Metabolic or Endocrine Disease
|
/
|
| HY-P11580 | Pap12-6-10 |
Pap12-6-10 is an MD-2 ligand that binds to the hydrophobic pocket of MD-2 to inhibit the dimerization of the TLR4/MD-2 complex and downstream inflammatory signal transduction. Pap12-6-10 also binds to LPS to permeabilize bacterial cell membranes and induce oxidative stress, leading to bacterial death. Pap12-6-10 regulates LPS-induced inflammatory responses through the TLR4 signaling pathway and exhibits antibacterial activity against multidrug-resistant Gram-negative bacteria. Pap12-6-10 shows low tendency to induce drug resistance and low preclinical cytotoxicity, and it prevents organ damage in a mouse model of sepsis. Pap12-6-10 can be used for research related to Gram-negative sepsis and carbapenem-resistant Acinetobacter baumannii infections.
|
|
/
|
| HY-P992356 | GENA-104A16 |
GENA-104A16 is a humanized monoclonal antibody targeting CNTN4, with multiple functions including immunostimulation, cytotoxicity and immunoregulation. By binding to CNTN4, GENA-104A16 blocks its interaction with APP, thereby restoring T cell function, inducing tumor cell death and regulating tumor-infiltrating immune cell populations. GENA-104A16 also exerts topoisomerase I inhibitory activity via the payload Exatecan (HY-13631). GENA-104A16 can be used in research related to colon cancer liver metastasis and other CNTN4-expressing solid tumors.
Species: Human |
|
/
|
| HY-178989 | PGK1-IN-2 |
PGK1-IN-2 (Compound 60) is a PGK1 inhibitor with an IC50 of 8.24 μM. PGK1-IN-2 demonstrates a significant ability to inhibit the proliferation of osteosarcoma cells. PGK1-IN-2 interferes with the glycolytic pathway of tumor cells by inhibiting PGK1. PGK1-IN-2 inhibits cell migration and invasion, and induces cell S phase and G2-M phase cycle arrest. PGK1-IN-2 may kill cells by inducing cuproptosis. PGK1-IN-2 shows a significant anti-tumor effect in the MNNG-HOS osteosarcoma xenograft mouse model. PGK1-IN-2 can be used for the study of osteosarcoma.
|
|
/
|
| HY-Y0319G1 | Magnesium acetate tetrahydrate, for molecular biology |
Magnesium acetate tetrahydrate, for molecular biology is a carboxylic acid and short-chain fatty acid (SCFAs). Magnesium acetate tetrahydrate, for molecular biology activates AMPK, increases ROS, cleaved caspase 9, PPARα, downregulates SREBP-1c, ChREBP expression. Magnesium acetate tetrahydrate, for molecular biology exhibits antifungal activity against Saccharomyces cerevisiae W303-1A. Magnesium acetate tetrahydrate, for molecular biology regulates energy metabolism. Magnesium acetate tetrahydrate, for molecular biology has anticancer activity against gastric cancer. Magnesium acetate tetrahydrate, for molecular biology induces writhing reaction and ulcerative colitis. Magnesium acetate tetrahydrate, for molecular biology can be used in the researches for gastric cancer, ulcerative colitis, hepatic steatosis, and pain.
|
|
/
|
| HY-P10586 | Macrophage-activating lipopeptide 2 |
Macrophage-activating lipopeptide 2 (MALP-2) is an agonist of Toll like receptors TLR-2/TLR-6. Macrophage-activating lipopeptide-2 can enhance endothelial nitric oxide synthase (eNOS) phosphorylation and endothelial cell release of NO, thereby improving vasodilation. Macrophage-activating lipopeptide-2 can enhance endothelial adhesion of white blood cells and improve perfusion recovery and collateral growth in the hind limbs of hypercholesterolemic Apoe deficient mice undergoing experimental femoral artery ligation (FAL).
|
|
/
|
| HY-W795740 | (R)-Mono-ethyl 3-acetoxyglutarate |
(R)-Mono-ethyl 3-acetoxyglutarate is an important metabolic intermediate that promotes the activity of tricarboxylic acid (TCA) cycle enzymes. (R)-Mono-ethyl 3-acetoxyglutarate can help study key processes in metabolic pathways. (R)-Mono-ethyl 3-acetoxyglutarate has important application value in cell metabolism research.
|
|
/
|
| HY-17473R | Embelin (Standard) |
Embelin (Standard) is the analytical standard of Embelin. This product is intended for research and analytical applications. Embelin (Embelic acid), a potent, nonpeptidic XIAP inhibitor (IC50=4.1 μM), inhibits cell growth, induces apoptosis, and activates caspase-9 in prostate cancer cells with high levels of XIAP. Embelin blocks NF-kappaB signaling pathway leading to suppression of NF-kappaB-regulated antiapoptotic and metastatic gene products. Embelin also induces autophagic and apoptotic cell death in human oral squamous cell carcinoma cells.
|
|
/
|
| HY-182919 | Antitumor photosensitizer-10 |
Antitumor photosensitizer-10 is an antitumor photosensitizer. Upon near-infrared irradiation, Antitumor photosensitizer-10 generates superoxide anions, reduces the copper-binding capacity of glutathione, releases copper ions, and thereby induces cuproptosis in tumor cells (cuproptosis). Antitumor photosensitizer-10 can be used in breast cancer-related research.
|
|
/
|
| HY-B1729S1 | Phenoxyethanol-d4 |
Phenoxyethanol-d4 is the deuterium labeled Phenoxyethanol. Phenoxyethanol has a broad spectrum of antimicrobial agent. Phenoxyethanol is an uncouple agent in oxidative phosphorylation from respiration and competitively inhibits malate dehydrogenase. Phenoxyethanol is used as a preservative in cosmetic, vaccine, and textile, et al.
|
|
/
|
| HY-N21828 | Annonin VI |
Annonin VI is an inhibitor of NADH:ubiquinone oxidoreductase (complex I; complex I) and glucose:ubiquinone oxidoreductase discovered in the seeds of Annona squamosa. Annonin VI exhibits an IC50 of 0.02 nmol/mg protein against bovine heart complex I, and an IC50 of 12.4 nmol/mg protein against glucose dehydrogenase (GDH) derived from Gluconobacter oxydans. Annonin VI acts in a partially competitive manner on the region associated with the ubiquinone catalytic site of complex I, blocking electron transfer from high-potential iron-sulfur clusters to ubiquinone. Annonin VI binds competitively with ubiquinone at the homologous ubiquinone site on GDH. Annonin VI can be used in the research of bacterial infections, insecticides, and cancer.
|
|
/
|
| HY-B1092AS2 | Gluconate-d6 sodium |
Gluconate-d6 sodium (D-Gluconic acid sodium salt-d6) is the deuterium labeled Gluconate sodium (HY-B1092A). Gluconate sodium (D-Gluconic acid sodium salt) is an orally active glucose derivative. Gluconate sodium reduces nitric oxide and inflammatory cytokines (IL-1β and IL-6). Gluconate sodium inhibits ERK phosphorylation. Gluconate sodium has antioxidant and antiplatelet activation activities. Gluconate sodium has antitumor activity against colorectal cancer. Gluconate sodium improves osteoarthritis, intestinal damage and acute lung injury.
|
|
/
|
| HY-16900G | Rolipram (GMP) |
Rolipram GMP is Rolipram (HY-16900) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Rolipram is a PDE4 inhibitor, with blood-brain barrier permeability, that reverses β-amyloid-induced learning and memory impairment in rats. Rolipram elevates intracellular cAMP and clevels and regulates the cAMP/CREB signaling pathway, thereby alleviating neuroinflammation and apoptotic responses. Rolipram promotes neuronal differentiation of human bone marrow mesenchymal stem cells and inhibits Methamphetamine- and morphine-induced hyperlocomotion in mice. Rolipram also reduces the viability of glioblastoma stem-like cells and enhances Bevacizumab (HY-P9906)-induced cell death. Rolipram inhibits the expression of proinflammatory cytokines and enhances central noradrenergic transmission. Rolipram is mainly used in studies related to various central nervous system diseases including Alzheimer's disease, major depressive disorder, glioblastoma multiforme, and multiple sclerosis.
|
|
/
|
| HY-143951S | Disulfiram impurity 1-d10 |
Disulfiram impurity 1-d10 is the deuterium labeled Disulfiram impurity 1.
|
|
/
|
| HY-W010201S1 | Citronellol-d3 |
Citronellol-d3 ( (±)-Citronelloll-d3) is the deuterium labeled Citronellol (HY-W010201). Citronellol ((±)-Citronellol) is an orally active inducer of apoptosis. Citronellol can prevent oxidative stress, mitochondrial dysfunction, and apoptosis in the SH-SY5Y cell Parkinson's disease model induced by 6-OHDA by regulating the ROS-NO, MAPK/ERK, and PI3K/Akt signaling pathways. Citronellol can induce necroptosis in human lung cancer cells through the TNF-α pathway and accumulation of ROS. Citronellol can reduce the levels of LC-3 and p62 to regulate the autophagy pathway, inhibit oxidative stress and neuroinflammation, and thus have neuroprotective effects on Parkinson's rats. Citronellol exhibits anti-fungal activity against Trichophyton rubrum by inhibiting ergosterol synthesis.
|
p62
Isotope-Labeled Compounds
Apoptosis
TNF Receptor
Necroptosis
PI3K
Autophagy
Atg8/LC3
Fungal
ERK
Reactive Oxygen Species (ROS)
|
/
|
| 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.
|
|
/
|
| HY-P10707A | Tpp-CAQK TFA |
Tpp-CAQK TAF can bind to mitochondria, enabling the construction of an engineered mitochondrial compound, Mito-Tpp-CAQK TFA, with excellent bioactivity. Mito-Tpp-CAQK TFA can be internalized by macrophages, thereby enhancing the phagocytosis of myelin debris, alleviating mitochondrial dysfunction, and reducing proinflammatory profiles, ultimately facilitating tissue repair and functional recovery in mice after spinal cord injury.
|
|
/
|
| HY-B1729S | Phenoxyethanol-d2 |
Phenoxyethanol-d2 is the deuterium labeled Phenoxyethanol. Phenoxyethanol has a broad spectrum of antimicrobial agent. Phenoxyethanol is an uncouple agent in oxidative phosphorylation from respiration and competitively inhibits malate dehydrogenase. Phenoxyethanol is used as a preservative in cosmetic, vaccine, and textile, et al.
|
|
/
|
| HY-P11358 | IRW |
IRW is an orally active tripeptide produced from egg white with angiotensin converting enzyme (ACE) inhibitory properties. IRW can prevent high-fat diet (HFD)-induced Non-alcoholic fatty liver disease (NAFLD) by modulating hepatic lipid metabolism and increasing mitochondrial content. IRW decreases hepatic triglyceride content and lipid droplet size. IRW increases the hepatic mitochondrial complexes and citrate synthase activity, phosphorylation of 5’-AMP-activated protein kinase and microsomal triglyceride transfer protein abundance. IRW increases phosphorylated acetyl CoA carboxylase and mitochondrial complexes, IRW can be used for the research of inflammation.
|
|
/
|
| HY-P991432 | VTX-0811 |
VTX-0811 is a human IgG4 monoclonal antibody (mAb) targeting PSGL1/CD162. VTX-0811 up-regulates TNF-α/NF-κB and chemokine-mediated signaling and down-regulates oxidative phosphorylation, fatty acid metabolism, and Myc signaling pathways. VTX-0811 increases the proportion of CD8+ T cells among infiltrating T cells. VTX-0811 has antitumor activity in a humanized mouse PDX model of melanoma.
Species: Human |
|
/
|
| HY-34740S1 | Ethylmalonic acid-d5 |
Ethylmalonic acid-d5 is the deuterium labeled Ethylmalonic acid (HY-34740). Ethylmalonic acid is a short-chain organic dicarboxylic acid. Ethylmalonic acid synergistically induces mitochondrial permeability transition (MP) with Ca2+, inhibits Mi-CK, and disrupts mitochondrial energy metabolism. Ethylmalonic acid can be used in the research of SCADD, EE and other genetic metabolic diseases characterized by EMA accumulation.
|
|
/
|
| HY-182918 | DMAPT-DTCs-1,3-diaminopropane-DTCs-DMAPT dimethanesulfonate |
DMAPT-DTCs-1,3-diaminopropane-DTCs-DMAPT dimethanesulfonate is an orally active prodrug of MMB-DTCs-1,3-diaminopropane-DTCs-MMB (HY-182917). DMAPT-DTCs-1,3-diaminopropane-DTCs-DMAPT dimethanesulfonate induces apoptosis, ferroptosis, and cuproptosis in lung cancer cells. DMAPT-DTCs-1,3-diaminopropane-DTCs-DMAPT dimethanesulfonate can be used in the research of lung cancer.
|
|
/
|
| HY-12040S | Elesclomol-d2 |
Elesclomol-d2 (STA-4783-d2) is a deuterium labeled Elesclomol (HY-12040). Elesclomol (STA-4783) is a potent copper ionophore and promotes copper-dependent cell death (cuproptosis). Elesclomol specifically binds ferredoxin 1 (FDX1) α2/α3 helices and β5 strand. Elesclomol inhibits FDX1-mediated Fe-S cluster biosynthesis. Elesclomol is an oxidative stress inducer that induces cancer cell apoptosis. Elesclomol is a reactive oxygen species (ROS) inducer. Elesclomol can be used for Menkes and associated disorders of hereditary copper deficiency research.
|
|
/
|
| HY-P10707 | Tpp-CAQK |
Tpp-CAQK can bind to mitochondria, enabling the construction of an engineered mitochondrial compound, Mito-Tpp-CAQK, with excellent bioactivity. Mito-Tpp-CAQK can be internalized by macrophages, thereby enhancing the phagocytosis of myelin debris, alleviating mitochondrial dysfunction, and reducing proinflammatory profiles, ultimately facilitating tissue repair and functional recovery in mice after spinal cord injury.
|
|
/
|
| HY-P12010 | Ac-ETDK(myr)-AMC |
Ac-ETDK(myr)-AMC is a DLAT-derived ε-N-myristoyllysine peptide substrate for fatty-acid deacylase HDAC11, used in fluorescence-based HDAC11 activity assays. Ac-ETDK(myr)-AMC undergoes cleavage of ε-N-myristoyllysine by HDAC11, followed by trypsin-mediated cleavage of C-terminal lysine to release measurable fluorophore AMC.
|
|
/
|
| HY-B1914S | Tebufenpyrad-d3 |
Tebufenpyrad-d3 is the deuterium labeled Tebufenpyrad (HY-B1914). Tebufenpyrad can induce mitochondrial dysfunction and oxidative damage. Tebufenpyrad induces dose-dependent cell death on N27 cells, with an EC50 value of 3.98 μM.
|
|
/
|
| HY-P0245 | Speract |
Speract, a sea urchin egg peptide that regulates sperm motility, also stimulates sperm mitochondrial metabolism.
|
|
/
|
| HY-N1970R | 5,7-Dihydroxychromone (Standard) |
5,7-Dihydroxychromone (Standard) is the analytical standard of 5,7-Dihydroxychromone (HY-N1970). This product is intended for research and analytical applications. 5,7-Dihydroxychromone is a flavonoid compound with antioxidant properties. 5,7-Dihydroxychromone induces Nrf2 nuclear translocation, increases Nrf2/ARE binding activity, and up-regulates Nrf2-dependent antioxidant genes HO-1, NQO1, GCLc. 5,7-Dihydroxychromone attenuates excessive ROS generation, inhibits activated caspase-3, caspase-9, cleaved PARP expression, and prevents neuronal apoptosis and cell death. 5,7-Dihydroxychromone increases LXRα and PPARγ mRNA expression, induces preadipocyte differentiation, and regulates blood glucose levels. 5,7-Dihydroxychromone inhibits radial growth of soil pathogenic fungi, radicle elongation of select seedlings, and transiently inhibits Bradyrhizobium sp. growth in high mannitol medium. 5,7-Dihydroxychromone can be used for the research of Parkinson’s disease, type 2 diabetes mellitus and pathogenic fungal infection.
|
Cancer
Infection
Neurological, Eye or Ear Disease
Inflammation or Immune System Disease
Metabolic or Endocrine Disease
|
/
|
| HY-152007S | Butyrylcarnitine-d3 hydrochloride |
Butyrylcarnitine-d3 hydrochloride is deuterium labeled Butyrylcarnitine (HY-113168). Butyrylcarnitine is an endogenous metabolite found in plasma. Elevated levels of Butyrylcarnitine are closely associated with abnormalities in lipid and energy metabolism. Butyrylcarnitine can serve as a diagnostic and prognostic indicator for certain diseases, such as heart failure and head and neck cancer.
|
|
/
|
| HY-P2620 | Ac-LETD-AFC |
|
/
|
|
| HY-P0119S | Lixisenatide (Leu-13C6,15N) TFA |
Lixisenatide (Leu-13C6,15N) TFA is the 13C- and 15N-labeled Lixisenatide (HY-P0119). Lixisenatide is a glucagon-like peptide-1 (GLP-1) receptor agonist. Lixisenatide inhibits the inflammatory response through down regulation of pro-inflammatory cytokines, and suppresses of the Akt-MEK1/2 signaling pathway. Lixisenatide can inhibit oxidative stress, mitochondrial dysfunction and apoptosis. Lixisenatide can be used for the researches of inflammation, metabolic disease, neurological disease and cardiovascular disease, such as rheumatoid arthritis, diabetes, Alzheimer's disease and atherosclerosis.
|
Neurological, Eye or Ear Disease
Inflammation or Immune System Disease
Blood or Cardio-cerebrovascular Disease
Metabolic or Endocrine Disease
|
/
|
| HY-N0420S4 | Succinic acid-13C2-2 |
Succinic acid-13C2 is the 13C labeled Succinic acid[1]. Succinic acid is a potent and orally active anxiolytic agent. Succinic acid is an intermediate product of the tricarboxylic acid cycle. Succinic acid can be used as a precursor of many industrially important chemicals in food, chemical and pharmaceutical industries[2][3].
|
|
/
|
| HY-D2315 | Probe-Cys |
Probe-Cys is a water-soluble and selective near-infrared fluorescent probe for Cysteine (Cys) (λex= 680 nm, λem=710 nm) that is not interfered by Hcy, GSH, and HS-. Probe-Cys can react with the stimulant DTT (HY-15917) and the NEM (HY-D0843) in HepG2 cells and zebrafish for the detection of endogenous Cys. Probe-Cys can also be used for imaging Cys in Arabidopsis thaliana. Probe-Cys provides a method for cancer diagnosis and exploration of plant sulfur metabolism.
|
|
/
|
| HY-B0139AS1 | Flucytosine-15N2 hydrochloride |
Flucytosine-15N2 (5-Fluorocytosine-15N2) hydrochloride is the 15N-labeled Flucytosine hydrochloride (HY-B0139). Flucytosine (5-Fluorocytosine) is an antifungal compound with oral activity. Flucytosine is a widely used cytotoxic drug that, after further metabolism, produces fluorinated ribonucleotides and deoxyribonucleotides, inhibits DNA and protein synthesis, and has multiple effects such as inhibiting candida and candida neoplasm infection and producies cytotoxicity to cancer cells.
|
|
/
|
| HY-W015777R | 4-Methoxybenzyl alcohol (Standard) |
4-Methoxybenzyl alcohol (Standard) (P-Methoxy-benzyl alcoho (Standard); (4-Methoxyphenyl)methanol (Standard)) is the analytical standard of 4-Methoxybenzyl alcohol (HY-W015777). This product is intended for research and analytical applications. 4-Methoxybenzyl alcohol (P-Methoxy-benzyl alcoho; (4-Methoxyphenyl) methanol) is a naturally derived volatile aromatic compound. 4-Methoxybenzyl alcohol upregulates the phosphorylation level of PI3K/Akt pathway proteins, downregulates the expression of pro-inflammatory factors, increases the content of tight junction proteins occludin and claudin-5, and alleviates structural damage to the blood-brain barrier. 4-Methoxybenzyl alcohol improves the decrease in viability and NO level of cerebral microvascular endothelial cells induced by oxygen-glucose deprivation/reperfusion, and reduces the release of lactate dehydrogenase. 4-Methoxybenzyl alcohol serves as a substrate in the two-phase persulfate-mediated electro-oxidation system, where it is directionally oxidized to p-anisaldehyde. 4-Methoxybenzyl alcohol acts as a substrate for wild-type fungal aryl alcohol oxidase. 4-Methoxybenzyl alcohol can be used in studies related to ischemic stroke, as well as in research across various fields such as chemical synthesis, including the synthesis of fragrances and flavorings.
|
|
/
|
| HY-Y0396R | N-Hydroxyphthalimide (Standard) |
N-Hydroxyphthalimide (Standard) is the analytical standard of N-Hydroxyphthalimide (HY-Y0396). This product is intended for research and analytical applications. N-Hydroxyphthalimide is a blocking agent and catalyst. N-Hydroxyphthalimide promotes oxidation reactions by generating PINO free radicals and activating hydrogen atom transfer processes. N-Hydroxyphthalimide reduces the expression of anti-apoptotic proteins Survivin and Bcl-xL and activates caspase 9 and caspase 3. N-Hydroxyphthalimide induces Apoptosis. N-Hydroxyphthalimide inhibits the phosphorylation of mTOR (Ser2448, Ser2481) and Akt (Ser473). N-Hydroxyphthalimide has anticancer effects against breast and colon cancer.
|
|
/
|
| HY-N14780 | Pochonin D |
Pochonin D ((+)-Pochonin D) is an inhibitor of heat shock protein 90 (Hsp90) with antiviral and anti-inflammatory activities. Pochonin D inhibits Hsp90, affects the homeostasis, folding and assembly processes of viral proteins, and reduces the replication capacity of viruses. Pochonin D is a copper ion carrier that can induce cuproptosis in triple-negative breast cancer cells by targeting PRDX1. Pochonin D reduces the infiltration of inflammatory cells, decreases the secretion of inflammatory cytokines such as TNF-α and IL-1β, and alleviates inflammatory responses. Pochonin D is a promising candidate for research on human rhinovirus (HRV) infection and cancer.
Source: Humicola sp. FO-2942 |
|
/
|
| HY-W010201S | Citronellol-d6 |
Citronellol-d6 is deuterated labeled Citronellol (HY-W010201). Citronellol ((±)-Citronellol) is an orally active inducer of apoptosis. Citronellol can prevent oxidative stress, mitochondrial dysfunction, and apoptosis in the SH-SY5Y cell Parkinson's disease model induced by 6-OHDA by regulating the ROS-NO, MAPK/ERK, and PI3K/Akt signaling pathways. Citronellol can induce necroptosis in human lung cancer cells through the TNF-α pathway and accumulation of ROS. Citronellol can reduce the levels of LC-3 and p62 to regulate the autophagy pathway, inhibit oxidative stress and neuroinflammation, and thus have neuroprotective effects on Parkinson's rats. Citronellol exhibits anti-fungal activity against Trichophyton rubrum by inhibiting ergosterol synthesis.
|
|
/
|
| HY-158726 | Complex 3 |
Complex 3 is a fluorescent dithiocarbazate-copper complex with anticancer activity, which localizes to mitochondria. Complex 3 displays excitation/emission maxima of 455-495/535 nm, respectively. Complex 3 inhibits the growth of BxPC-3, AsPC-1, PANC-1, and WI38 pancreatic cancer cells with IC50 values of 0.74, 0.41, 0.62, and 2.06 µM, respectively. Complex 3 induces lipid peroxidation and mitochondrial rupture and shrinkage in AsPC-1 cells. Complex 3 also induces mitochondrial apoptosis and cytokine-cytokine receptor interaction dysfunction in AsPC-1 cells. Complex 3 reduces tumor volume in an AsPC-1 mouse xenograft model.
|
|
/
|
| HY-W011086R | Tri-O-tolyl phosphate (Standard) |
Tri-O-tolyl phosphate (Tri-O-cresyl phosphate; TOTP) (Standard) is an analytical standard of Tri-O-tolyl phosphate (HY-W011086). This product is intended for research and analytical applications. Tri-O-tolyl phosphate is an aryl phosphate compounds commonly utilized as flame retardants and lubricant additives across various industrie. Tri-O-tolyl phosphate has neurotoxicity and reproductive toxicity, decreasing cell viability, inhibiting cell proliferation, triggering cell cycle arrest, induceing apoptosis, causing mitochondrial dysfunction, disrupts calcium homeostasis.
|
|
/
|
| HY-B0356S2 | Ciprofloxacin-d4 |
Ciprofloxacin-d4 (Bay-09867-d4) is deuterium labeled Ciprofloxacin. Ciprofloxacin (Bay-09867) is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin has anti-proliferative activity and induces apoptosis. Ciprofloxacin is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
|
Isotope-Labeled Compounds
Apoptosis
Mitochondrial Metabolism
Bacterial
Reactive Oxygen Species (ROS)
Antibiotic
Topoisomerase
|
/
|
| HY-W767865 | Cyclic GMP sodium-13C5 |
Cyclic GMP sodium-13C5 is the 13C-labeled Cyclic GMP sodium (HY-113469A). Cyclic GMP (cGMP) sodium, an important second messenger, is a major intracellular mediator of extracellular signals such as nitric oxide (NO) and natriuretic peptides (NPs). Effects of Cyclic GMP sodium occur through three main groups of cellular targets: cGMP-dependent protein kinases (PKGs), cGMP-gated cation channels, and PDEs. Cyclic GMP can inhibit both platelet adhesion and aggregation. cGAMP (Cyclic-GMP-AMP) (HY-12512), a conjugate of Cyclic GMP and AMP, can induce IRF3 phosphorylation and nuclear translocation, enhancing antiviral immune responses.
|
|
/
|
| HY-178914 | Copper ionophore I |
Copper ionophore I is an efficient copper ion carrier. Copper ionophore I can regulate various intracellular copper levels to induce cuproptosis, such as 4T1 (IC50 = 0.45 μM) and MDA-MB-231(IC50 = 1.21 μM) cells. Copper ionophore I can induce an increase in ROS and cause mitochondrial dysfunction. Copper ionophore I can reduce the expression of FDX1, DLAT, and LIAS proteins. Copper ionophore I can activate immune related pathways and promote T cell infiltration. Copper ionophore I can be used for cancer research.
|
|
/
|
| HY-W747676 | Glyphosate-13C |
Glyphosate-13C is the 13C-labeled Glyphosate (HY-B0863). Glyphosate, a non-selective systemic biocide with broad-spectrum activity, is an herbicidal derivative of the amino acid glycine. Glyphosate inhibits the enzymatic activity of the 5-endopyruvylshikimate 3-phosphate synthase (EPSPS) in the shikimic acid pathway, preventing the synthesis of the aromatic amino acids tyrosine, phenylalanine, and tryptophan. Glyphosate induces oxidative stress, neuroinflammation, and mitochondrial dysfunction, processes that lead to neuronal death by autophagia, necrosis, or apoptosis, as well as the appearance of behavioral and motor disorders.
|
|
/
|
| HY-119976R | Boscalid (Standard) |
Boscalid (Standard) is the analytical standard of Boscalid. This product is intended for research and analytical applications. Boscalid is a succinate dehydrogenase (SDHI) inhibitor with antifungal activity. Boscalid binds to the ubiquinone-binding site of fungal mitochondrial complex II, blocks ATP production and aerobic respiration, exhibits good control efficacy against a variety of plant fungal diseases including gray mold, sclerotinia rot and powdery mildew, and is widely used for disease control in agriculture. Boscalid induces apoptosis, altered lipid metabolism, mitochondrial dysfunction, respiratory impairment, oxidative stress, ROS accumulation and neurodevelopmental disorders in zebrafish. Boscalid reduces foraging ability, shortens median death time and causes chronic toxicity in exposed honeybees. Boscalid also possesses genotoxicity, cytotoxicity, elevated mitochondrial superoxide levels and early-stage apoptosis.
|
|
/
|
| HY-N0420S3 | Succinic acid-13C2-1 |
Butanedioic acid-13C2 is the 13C labeled Succinic acid[1]. Succinic acid is a potent and orally active anxiolytic agent. Succinic acid is an intermediate product of the tricarboxylic acid cycle. Succinic acid can be used as a precursor of many industrially important chemicals in food, chemical and pharmaceutical industries[2][3].
|
|
/
|
| HY-W688732 | 2-Chloro-4,4,5,5-tetramethyl-1,3,2-dioxaphospholane |
2-Chloro-4,4,5,5-tetramethyl-1,3,2-dioxaphospholane is a biochemical reagent. 2-Chloro-4,4,5,5-tetramethyl-1,3,2-dioxaphospholane serves as a phosphorylation reagent for alcohols and heteroatoms, which is used in the synthesis of glycosyl donors and ligands, and also applied in the analytical research of derivatized lignin samples. 2-Chloro-4,4,5,5-tetramethyl-1,3,2-dioxaphospholane acts as a catalyst in copper oxide/titanium dioxide-catalyzed lignin oxidation studies.
|
|
/
|
| HY-B0158S5 | Cytidine-13C9,15N3 |
Cytidine-13C9,15N3 is the 13C and 15N labeled Cytidine. Cytidine is a pyrimidine nucleoside and acts as a component of RNA. Cytidine is a precursor of uridine. Cytidine controls neuronal-glial glutamate cycling, affecting cerebral phospholipid metabolism, catecholamine synthesis, and mitochondrial function.
|
|
/
|
| HY-123115 | Leucrose |
Leucrose (5-O-α-D-Glucopyranosyl-D-fructose) is an orally active Sucrose (HY-B1779) isomer naturally found in pollen and honey. Leucrose promotes phosphorylation of JAK1 and STAT6, reduces pro-inflammatory mediators and cytokinesas (TNFα, and IL-1β), increases M2 macrophage polarization and suppresses DSS (HY-116282C)-induced colitis. Leucrose suppresses hepatic triglyceride accumulation, improves fasting blood glucose levels, and regulates hepatic lipogenesis and fatty acid β-oxidation in high-fat diet-induced obese mice. Leucrose is slowly hydrolyzed into glucose and fructose by α-glucosidase and acts as as a sugar substitute in diet.
|
|
/
|
| HY-B0572R | Zinc Pyrithione (Standard) |
Zinc Pyrithione (Standard) is the analytical standard of Zinc Pyrithione. This product is intended for research and analytical applications. Zinc Pyrithione is an antifungal and antibacterial agent disrupting membrane transport by blocking the proton pump. Zinc Pyrithione is also a copper ionophore that delivers copper into cells and is a useful tool for studying cuproptosis.
|
|
/
|
| HY-W006398S | Acetic acid-d3 sodium |
Acetic acid-d3 sodium is the deuterium labeled Acetic acid (HY-Y0319). Acetic acid is a carboxylic acid and short-chain fatty acid (SCFAs). Acetic acid activates AMPK, increases ROS, cleaved caspase 9, PPARα, downregulates SREBP-1c, ChREBP expression. Acetic acid exhibits antifungal activity against Saccharomyces cerevisiae W303-1A. Acetic acid regulates energy metabolism. Acetic acid has anticancer activity against gastric cancer. Acetic acid induces writhing reaction and ulcerative colitis. Acetic acid can be used in the researches for gastric cancer, ulcerative colitis, hepatic steatosis, and pain.
|
|
/
|
| HY-W654000 | Cyclic GMP-13C,15N2 |
Cyclic GMP-13C,15N2 is 13C and 15N labeled Cyclic GMP (HY-113469). Cyclic GMP (cGMP), an important second messenger, is a major intracellular mediator of extracellular signals such as nitric oxide (NO) and natriuretic peptides (NPs). Effects of Cyclic GMP occur through three main groups of cellular targets: cGMP-dependent protein kinases (PKGs), cGMP-gated cation channels, and PDEs. Cyclic GMP can inhibit both platelet adhesion and aggregation. cGAMP (Cyclic-GMP-AMP) (HY-12512), a conjugate of Cyclic GMP and AMP, can induce IRF3 phosphorylation and nuclear translocation, enhancing antiviral immune responses.
|
|
/
|
| HY-B1092AS | Gluconate-1-13C sodium |
Gluconate-1-13C (D-Gluconic acid-1-13C) sodium is the 13C labeled Gluconate sodium (HY-B1092A). Gluconate (D-Gluconic acid) sodium is an orally active glucose derivative. Gluconate sodium reduces nitric oxide and inflammatory cytokines (IL-1β and IL-6). Gluconate sodium inhibits ERK phosphorylation. Gluconate sodium has antioxidant and antiplatelet activation activities. Gluconate sodium has antitumor activity against colorectal cancer. Gluconate sodium improves osteoarthritis, intestinal damage and acute lung injury.
|
|
/
|
| HY-119976S | Boscalid-d4 |
Boscalid-d4 is the deuterium labeled Boscalid. Boscalid is a succinate dehydrogenase (SDHI) inhibitor with antifungal activity. Boscalid binds to the ubiquinone-binding site of fungal mitochondrial complex II, blocks ATP production and aerobic respiration, exhibits good control efficacy against a variety of plant fungal diseases including gray mold, sclerotinia rot and powdery mildew, and is widely used for disease control in agriculture. Boscalid induces apoptosis, altered lipid metabolism, mitochondrial dysfunction, respiratory impairment, oxidative stress, ROS accumulation and neurodevelopmental disorders in zebrafish. Boscalid reduces foraging ability, shortens median death time and causes chronic toxicity in exposed honeybees. Boscalid also possesses genotoxicity, cytotoxicity, elevated mitochondrial superoxide levels and early-stage apoptosis.
|
|
/
|
| HY-113081S | 1-Methyladenosine-d3 |
1-Methyl Adenosine-d3 is the deuterium labeled 1-Methyladenosine. 1-Methyladenosine is an RNA modification that can serve as a tumor marker, with elevated levels in the body associated with cancer development. Following 1-methyladenosine methylation, upregulation of PPARδ expression regulates cholesterol metabolism and activates Hedgehog signaling pathway, driving liver tumorigenesis.
|
|
/
|
| HY-142026 | Vitisin A |
Vitisin A ((+)-Vitisin A) is an orally active natural product with multiple pharmacological activities including anti-inflammatory, anti-tumor, anti-oxidant, anti-pathogenic microorganism, hypoglycemic and lipid-regulating, anti-osteoporotic, neuroprotective and cardiovascular protective effects. Vitisin A exhibits inhibitory effects on human AChE and MAO-B with IC50 values of 1.29 µM and 4.94 µM, respectively. Vitisin A inhibits the ERK, MAPK, NF-κB, STAT1, HMGCR and TRAF6 pathways, downregulates the related phosphorylation and protein expression, while activates the Nrf2/HO-1 pathway and upregulates p21 expression. Vitisin A induces tumor cell apoptosis and cell cycle arrest, inhibits adipogenesis and lipid accumulation, while alleviates oxidative stress, suppresses inflammatory responses, blocks hepatic fibrosis, Cuproptosis and cholesterol synthesis, and increases the expression levels of central BDNF and TrkB. Vitisin A can be used in the research of tumors, infectious diseases, metabolic diseases, bone and joint diseases, liver diseases, skin injuries, as well as neurodegenerative and cognitive dysfunction-related diseases.
|
Caspase
ERK
NF-κB
Influenza Virus
PAK
LDLR
PPAR
PCSK9
Androgen Receptor
Keap1-Nrf2
Monoamine Oxidase
Cholinesterase (ChE)
IKK
Wnt
β-catenin
Reactive Oxygen Species (ROS)
Apoptosis
Cuproptosis
|
/
|
| HY-B0158S | Cytidine-d2 |
|
/
|
|
| HY-N6663 | 3-Carene |
3-Carene is an orally active TCA cycle enzyme inhibitor. 3-Carene inhibits succinate dehydrogenase and malate dehydrogenase as well as pyruvate kinase, disrupting energy metabolism. 3-Carene disrupts cell wall and cell membrane integrity, leading to potassium ion leakage, protein leakage, membrane depolarization, ATP depletion, morphological disruption, and cell lysis. 3-Carene interferes with amino acid metabolism, pantothenate and CoA biosynthesis, purine and pyrimidine metabolism, and aminoacyl-tRNA biosynthesis. 3-Carene enhances GABA receptor-mediated synaptic responses. 3-Carene can be used in research on bacterial infections, inflammation, anxiety, and sleep disorders.
|
Mitochondrial Metabolism
Bacterial
GABA Receptor
Succinate Dehydrogenase
Malate Dehydrogenase (MDH)
Pyruvate Kinase
|
/
|
| HY-113081AS | 1-Methyladenosine-d3 hydrochloride |
1-Methyladenosine-d3 hydrochloride is the hydrochloride salt form of deuterium labeled 1-Methyladenosine (HY-113081). 1-Methyladenosine is an RNA modification that can serve as a tumor marker, with elevated levels in the body associated with cancer development. Following 1-methyladenosine methylation, upregulation of PPARδ expression regulates cholesterol metabolism and activates Hedgehog signaling pathway, driving liver tumorigenesis.
|
|
/
|
| HY-B0158S6 | Cytidine-15N3 |
|
/
|
|
| HY-W012382S | N-Acetyl-L-tyrosine-d3 |
N-Acetyl-L-tyrosine-d3 is the deuterated form of N-Acetyl-L-tyrosine (HY-W012382). N-Acetyl-L-tyrosine is an orally active endogenous mitochondrial stress response regulator that can permeate the cell membrane by passive diffusion. N-Acetyl-L-tyrosine induces low-level reactive oxygen species (ROS) generation by transiently perturbing mitochondrial membrane potential, triggering reverse signaling to activate FoxO and Keap1 pathways. As a result, N-Acetyl-L-tyrosine enhances the expression of antioxidant enzyme genes, exerting anti-stress and cytoprotective effects. N-Acetyl-L-tyrosine can improve heat stress tolerance, inhibit tumor growth, and regulate energy metabolism. N-Acetyl-L-tyrosine can be used in the research of aging, metabolic diseases (such as diabetes), and cancer.
|
|
/
|
| HY-114118S1 | Semaglutide-d8 tetraTFA |
Semaglutide-d8 tetraTFA is the deuterium labeled Semaglutide (HY-114118). Semaglutide is a long-acting, selective, competitive GLP-1R agonist that can penetrate the blood-brain barrier. After activating GLP-1R, Semaglutide promotes insulin secretion, inhibits gastric emptying and appetite, and at the same time enhances autophagy, inhibits oxidative stress and apoptosis. Semaglutide also regulates mitochondrial function and lipid metabolism (such as reducing de novo lipogenesis in the liver). Semaglutide has activities such as lowering blood sugar, reducing weight, neuroprotection (such as improving motor function in Parkinson's disease models, reducing α-synuclein aggregation) and improving hepatic steatosis. Semaglutide can be used for the study of neurodegenerative diseases and liver diseases such as type 2 diabetes, obesity, Parkinson's disease, metabolic associated fatty liver disease (MASLD), and cancer.
|
Isotope-Labeled Compounds
GLP Receptor
Insulin Receptor
α-synuclein
Apoptosis
p38 MAPK
Autophagy
Bcl-2 Family
|
/
|
| HY-N7363 | Isolongifolene |
Isolongifolene ((-)-Isolongifolene) is a tricyclic sesquiterpene isolated from Murraya koenigii. Isolongifolene attenuates Rotenone-induced oxidative stress, mitochondrial dysfunction and apoptosis through the regulation of PI3K/AKT/GSK-3β signaling pathways. Isolongifolene has antioxidant, anti-inflammatory, anticancer and neuroprotective properties.
|
|
/
|
| HY-P3003S | Cereulide-13C6 |
Cereulide-13C6 is a deuterated form of Cereulide. Cereulide is an orally active, blood-brain barrier-permeable emetic toxin. Cereulide acts as a potassium ionophore that inserts into membranes, forms complexes with K+, and transports K+ from the cytoplasm into the mitochondrial matrix. Cereulide disrupts the electrochemical gradient of the inner mitochondrial membrane, leading to mitochondrial swelling and dysfunction, uncoupling of oxidative phosphorylation, inhibition of ATP synthesis, ROS accumulation, and ultimately triggering apoptosis and autophagy. Cereulide exhibits multi-organ toxicity and can be used for research on emetic food poisoning.
|
Isotope-Labeled Compounds
Mitochondrial Metabolism
Potassium Channel
Reactive Oxygen Species (ROS)
Apoptosis
Autophagy
Infection
Neurological, Eye or Ear Disease
Inflammation or Immune System Disease
Metabolic or Endocrine Disease
|
/
|
| HY-W015410S | Disodium succinate-13C2 |
Disodium succinate-13C2 is the 13C labeled Disodium succinate. Disodium succinate is the disodium salt of Succinic acid. Succinic acid is an intermediate product of the tricarboxylic acid cycle, as well as one of fermentation products of anaerobic metabolism.
|
|
/
|
| HY-W754527 | Allithiamine |
Allithiamine is a thiamin derivative with absorption characteristics similar to fat-soluble vitamins. Allithiamine acts as a cofactor precursor for thiamin pyrophosphate (TPP), which participates in carbohydrate metabolism by supporting the pyruvate dehydrogenase (PDH) complex to facilitate pyruvate entry into the tricarboxylic acid (TCA) cycle as acetyl CoA. Allithiamine can be used for researching thiamin metabolism.
|
|
/
|
| HY-B1817A | Zinc acetate, 99.99% trace metals basis |
Zinc (Zinc (II)) acetate, 99.99% trace metals basis is a heme oxygenase 1 (HO-1) activator and apoptosis inducer with cytotoxic and anticancer activities. Zinc acetate, 99.99% trace metals basis enhances HO-1 expression, alters the microRNA profile, and increases the level of caspase-cleaved cytokeratin 18. Zinc acetate, 99.99% trace metals basis also regulates the expression of Cdk2/cyclin E and interferes with cell cycle progression. Zinc acetate, 99.99% trace metals basis effectively inhibits cancer cell proliferation and induces their rapid death, with no significant cytotoxicity to non-tumor tissues. Zinc acetate, 99.99% trace metals basis has been widely used in studies related to hepatocellular carcinoma, prostate cancer, and other conditions.
|
|
/
|
| HY-W768336 | Gluconate-13C6 sodium |
Gluconate sodium-13C6 (D-Gluconic acid sodium salt-13C6) is the 13C-labeled Gluconate sodium (HY-B1092A). Gluconate sodium (D-Gluconic acid sodium salt) is an orally active glucose derivative. Gluconate sodium reduces nitric oxide and inflammatory cytokines (IL-1β and IL-6). Gluconate sodium inhibits ERK phosphorylation. Gluconate sodium has antioxidant and antiplatelet activation activities. Gluconate sodium has antitumor activity against colorectal cancer. Gluconate sodium improves osteoarthritis, intestinal damage and acute lung injury.
|
|
/
|
| HY-W015410S2 | Disodium succinate-d4 |
Disodium succinate-d4 is the deuterium labeled Disodium succinate. Disodium succinate is the disodium salt of Succinic acid. Succinic acid is an intermediate product of the tricarboxylic acid cycle, as well as one of fermentation products of anaerobic metabolism.
|
|
/
|
| HY-P3003 | Cereulide |
Cereulide is an orally active, blood-brain barrier-permeable emetic toxin. Cereulide acts as a potassium ionophore that inserts into membranes, forms complexes with K+, and transports K+ from the cytoplasm into the mitochondrial matrix. Cereulide disrupts the electrochemical gradient of the inner mitochondrial membrane, leading to mitochondrial swelling and dysfunction, uncoupling of oxidative phosphorylation, inhibition of ATP synthesis, ROS accumulation, and ultimately triggering apoptosis and autophagy. Cereulide exhibits multi-organ toxicity and can be used for research on emetic food poisoning.
Source: Bacillus cereus |
Neurological, Eye or Ear Disease
Inflammation or Immune System Disease
Metabolic or Endocrine Disease
Fungal Infection
|
/
|
| HY-W339545A | α-Ketoglutaric acid disodium hydrate |
α-Ketoglutaric acid disodium hydrate, an important dicarboxylic acid, is an intermediate in the tricarboxylic acid cycle (TCC) and amino acid metabolism. α-Ketoglutaric acid disodium hydrate can be used as building block chemical for the chemical synthesis of heterocycles, dietary supplement, component of infusion solutions and wound healing compounds, or as main component of new elastomers with a wide range of interesting mechanical and chemical properties.
|
|
/
|
| HY-Y0836S | Diethyl succinate-13C4 |
Diethyl succinate-13C4 is the 13C labeled Diethyl succinate. Diethyl succinate (Diethyl Butanedioate) is used at physiological pH and crosses biological membranes, incorporates into cells in tissue culture and is metabolized by the TCA cycle. Diethyl succinate is known to be non-toxic and used in fragrances and flavoring.
|
|
/
|
| HY-162386 | UM4118 |
UM4118 is a potent copper-selective non-genotoxic copper ionophore that induces cuproptosis in acute myeloid leukemia cells. UM4118 exhibits stronger activity against SF3B1G12C mutant acute myeloid leukemia cells. UM4118 transports extracellular copper into cells, elevates intracellular and mitochondrial copper levels, and triggers lipoylated DLAT aggregation, proteotoxic stress, iron-sulfur cluster protein depletion, reduced lipoylated protein levels, and maximal mitochondrial respiratory damage. UM4118 cytotoxicity can be enhanced by supplementation with extracellular copper, abolished by copper chelation, and shows synthetic lethal effects in the absence of iron-sulfur cluster biosynthesis/transport genes. UM4118 can be used for the study of acute myeloid leukemia.
|
|
/
|
| HY-113081S1 | 1-Methyladenosine-d3 hydriodide |
1-Methyladenosine-d3 hydriodide is the deuterium labeled 1-Methyladenosine (HY-113081). 1-Methyladenosine is an RNA modification that can serve as a tumor marker, with elevated levels in the body associated with cancer development. Following 1-methyladenosine methylation, upregulation of PPARδ expression regulates cholesterol metabolism and activates Hedgehog signaling pathway, driving liver tumorigenesis.
|
|
/
|
| HY-W802699 | α-Ketoglutaric acid disodium dihydrate |
α-Ketoglutaric acid disodium dihydrate, an important dicarboxylic acid, is an intermediate in the tricarboxylic acid cycle (TCC) and amino acid metabolism. α-Ketoglutaric acid disodium dihydrate can be used as building block chemical for the chemical synthesis of heterocycles, dietary supplement, component of infusion solutions and wound healing compounds, or as main component of new elastomers with a wide range of interesting mechanical and chemical properties.
|
|
/
|
| HY-111355S | Cholesterol sulfate-d7 sodium |
Cholesterol sulfate sodium-d7 is the deuterium labeled Cholesterol sulfate sodium. Cholesterol sulfate sodium is a naturally occurring, orally active cholesterol derivative that is widely distributed in various tissues and body fluids. Cholesterol sulfate sodium acts as a DOCK2 inhibitor, with IC50 values of 2 μM and 2.9 μM against mouse and human targets, respectively. Cholesterol sulfate sodium restricts excessive neutrophil infiltration and alleviates intestinal inflammation and damage. Cholesterol sulfate sodium serves as an activator of protein kinase C (PKC), which promotes squamous cell differentiation and inhibits skin carcinogenesis. Cholesterol sulfate sodium regulates cholesterol homeostasis and cellular metabolism by activating the AMPK-Sirt1 pathway. Cholesterol sulfate sodium can be used in research related to actinic keratitis, ulcerative colitis, skin cancer, and other conditions.
|
|
/
|
| HY-N0420S | Succinic acid-d6 |
Succinic acid-d6 is the deuterium labeled Succinic acid. Succinic acid is an intermediate product of the tricarboxylic acid cycle, as well as one of fermentation products of anaerobic metabolism.
|
|
/
|
| HY-114293A | Acetyl coenzyme A trilithium |
Acetyl-coenzyme A (Acetyl-CoA) trilithium is a membrane-impermeant central metabolic intermediate, participates in the TCA cycle and oxidative phosphorylation metabolism. Acetyl-coenzyme A trilithium regulates various cellular mechanisms by providing (sole donor) acetyl groups to target amino acid residues for post-translational acetylation reactions of proteins. Acetyl Coenzyme A trilithium is also a key precursor of lipid synthesis.
|
|
/
|
| HY-B0158S7 | Cytidine-13C9 |
Cytidine-13C9 (Cytosine β-D-riboside-13C9) is 13C labeled Cytidine (HY-B0158). Cytidine is a pyrimidine nucleoside and acts as a component of RNA. Cytidine is a precursor of uridine. Cytidine controls neuronal-glial glutamate cycling, affecting cerebral phospholipid metabolism, catecholamine synthesis, and mitochondrial function.
|
|
/
|
| HY-DY1073 | MitoPerOx (solution) |
MitoPerOx (solution) is a mitochondrial-targeted, lipid peroxidation-indicating fluorescent probe with BODIPY581/591 fluorophores. The triphenylphosphine cation (TPP+) of MitoPerOx can be selectively enriched in mitochondria (depending on membrane potential) and can be used to detect lipid peroxidation in the inner mitochondrial membrane. Under the action of lipid peroxides, the BODIPY581/591 fluorophores of MitoPerOx shift their emission wavelength from 590 nm (reduced state) to 520 nm (oxidized state) , and ratiometric detection can be performed at an excitation wavelength of 488 nm. MitoPerOx can specifically monitor the peroxidation of mitochondrial phospholipids (especially cardiolipin) and is used in the study of oxidative stress-related diseases (such as aging, neurodegenerative diseases, and mitochondrial dysfunction) .
Solvent and concentration: DMSO: 2 mM |
|
/
|
| HY-34740S | Ethylmalonic acid-d3 |
Ethylmalonic acid-d3 is the deuterium labeled Ethylmalonic acid (HY-34740). Ethylmalonic acid is a short-chain organic dicarboxylic acid. Ethylmalonic acid synergistically induces mitochondrial permeability transition (MP) with Ca2+, inhibits Mi-CK, and disrupts mitochondrial energy metabolism. Ethylmalonic acid can be used in the research of SCADD, EE and other genetic metabolic diseases characterized by EMA accumulation.
|
|
/
|
| HY-W016103 | 1-Hydroxy-2-naphthoic acid |
1-Hydroxy-2-naphthoic acid is a ubiquitous bicyclic intermediate metabolite in the microbial degradation process of polycyclic aromatic hydrocarbons (PAHs). 1-Hydroxy-2-naphthoic acid can be converted into 1,2-naphthalenediol, which enters the naphthalene degradation pathway and participates in the tricarboxylic acid (TCA) cycle to achieve complete mineralization.
|
|
/
|
| HY-P6374 | IIQLPEIVVV TFA |
IIQLPEIVVV TFA is a specific inhibitor of Drp1-Mff interaction. IIQLPEIVVV TFA can distinguish physiological from pathological fission and block physiological fission, thus leading to mitochondrial dysfunction. IIQLPEIVVV TFA can be used in the study of Huntington's disease.
|
|
/
|
| HY-W046353 | 2-Methoxycinnamaldehyde |
2-Methoxycinnamaldehyde (o-Methoxycinnamaldehyde) is a natural compound that can be isolated from Cinnamomum cassia. 2-Methoxycinnamaldehyde inhibits topoisomerase-I/II and NF-κB signaling pathway, causes mitochondrial dysfunction, induces lysosomal vesiculation, thereby leading to DNA damage and cell apoptosis. 2-Methoxycinnamaldehyde exhibits antitumor effects.
|
|
/
|
| HY-B2153 | Tetraethylenepentamine pentahydrochloride |
Tetraethylenepentamine pentahydrochloride is an orally active copper chelator and copper mobilizer. Tetraethylenepentamine pentahydrochloride exhibits growth inhibitory and hypolipidemic properties. Tetraethylenepentamine pentahydrochloride significantly increases urinary copper excretion and reduces renal copper accumulation in copper overload models, but does not significantly alter hepatic copper levels. Tetraethylenepentamine pentahydrochloride exerts growth inhibitory effects on Candida albicans and Fluconazole (HY-B0101)-resistant strains, and can be widely used in studies related to Wilson's disease and Candida infections.
|
|
/
|
| HY-113884B | (S)-Coriolic acid |
(S)-Coriolic acid (13(S)-HODE), the product of 15-lipoxygenase (15-LOX) metabolism of linoleic acid, functions as the endogenous ligand to activate PPARγ. (S)-Coriolic acid is an important intracellular signal agent and is involved in cell proliferation and differentiation in various biological systems. (S)-Coriolic acid induces mitochondrial dysfunction and airway epithelial injury.
|
|
/
|
| HY-W015777 | 4-Methoxybenzyl alcohol |
4-Methoxybenzyl alcohol (P-Methoxy-benzyl alcoho; (4-Methoxyphenyl) methanol) is a naturally derived volatile aromatic compound. 4-Methoxybenzyl alcohol upregulates the phosphorylation level of PI3K/Akt pathway proteins, downregulates the expression of pro-inflammatory factors, increases the content of tight junction proteins occludin and claudin-5, and alleviates structural damage to the blood-brain barrier. 4-Methoxybenzyl alcohol improves the decrease in viability and NO level of cerebral microvascular endothelial cells induced by oxygen-glucose deprivation/reperfusion, and reduces the release of lactate dehydrogenase. 4-Methoxybenzyl alcohol serves as a substrate in the two-phase persulfate-mediated electro-oxidation system, where it is directionally oxidized to p-anisaldehyde. 4-Methoxybenzyl alcohol acts as a substrate for wild-type fungal aryl alcohol oxidase. 4-Methoxybenzyl alcohol can be used in studies related to ischemic stroke, as well as in research across various fields such as chemical synthesis, including the synthesis of fragrances and flavorings.
|
|
/
|
| HY-114118CP | Semaglutide (crude) |
Semaglutide (crude) is the crude form of Semaglutide (HY-114118). Semaglutide is a long-acting, selective, competitive GLP-1R agonist that can penetrate the blood-brain barrier. After activating GLP-1R, Semaglutide promotes insulin secretion, inhibits gastric emptying and appetite, and at the same time enhances Autophagy, inhibits oxidative stress and Apoptosis. Semaglutide also regulates mitochondrial function and lipid metabolism (such as reducing de novo lipogenesis in the liver). Semaglutide has activities such as lowering blood sugar, reducing weight, neuroprotection (such as improving motor function in Parkinson's disease models, reducing α-synuclein aggregation) and improving hepatic steatosis. Semaglutide can be used for the study of neurodegenerative diseases and liver diseases such as type 2 diabetes, obesity, Parkinson's disease, metabolic associated fatty liver disease (MASLD), and cancer.
|
|
/
|
| HY-P10409 | SHLP2 |
SHLP2 (Small humanin-like peptide 2) is a small molecule peptide encoded by mitochondrial DNA, belonging to mitochondria derived peptide. SHLP2 has the activity of regulating apoptosis and inhibits cell death. SHLP2 binds to mitochondrial complex 1. SHLP2 improves mitochondrial metabolism by increasing respiration and biogenesis, reducing ROS, and decreasing mtDNA oxidation. SHLP2 also regulated energy homeostasis through the activation of hypothalamic neurons. SHLP2 can be used in the study of diseases related to mitochondrial dysfunction and anti-aging diseases, such as age-related macular degeneration and Parkinson’s disease.
|
|
/
|
| HY-B0762S | Acetyl-L-carnitine-d3 hydrochloride |
Acetyl-L-carnitine-d3 (O-Acetyl-L-carnitine-d3) hydrochloride is the deuterium labeled Acetyl-L-carnitine hydrochloride (HY-B0762). Acetyl-L-carnitine (O-Acetyl-L-carnitine; ALCAR) hydrochloride is an orally active mitochondrial energy metabolism regulator and neuroprotectant that can penetrate the blood-brain barrier. Acetyl-L-carnitine hydrochloride selectively enters cells and the brain through the organic cation transporter OCTN2. Acetyl-L-carnitine hydrochloride can participate in fatty acid β-oxidation, promote acetylcholine synthesis, regulate mitochondrial function and inhibit oxidative stress as an acetyl donor. Acetyl-L-carnitine hydrochloride exerts its activity by enhancing energy metabolism, protecting neurons and improving synaptic plasticity. Acetyl-L-carnitine hydrochloride is mainly used in the study of neurodegenerative diseases and metabolic disorder-related diseases such as neonatal hypoxic-ischemic brain damage, Alzheimer's disease, and depression.
|
|
/
|
| HY-P10586A | Macrophage-activating lipopeptide 2 TFA |
Macrophage-activating lipopeptide 2 TFA is an agonist of Toll like receptors TLR-2/TLR-6. Macrophage-activating lipopeptide-2 enhances endothelial nitric oxide synthase (eNOS) phosphorylation and endothelial cell release of NO, thereby improving vasodilation. Macrophage-activating lipopeptide-2 enhances endothelial adhesion of white blood cells and improve perfusion recovery and collateral growth in the hind limbs of hypercholesterolemic Apoe deficient mice undergoing experimental femoral artery ligation (FAL).
|
|
/
|
| HY-B0762S1 | Acetyl-L-carnitine-d3-1 hydrochloride |
Acetyl-L-carnitine-d3-1 (O-Acetyl-L-carnitine-d3-1) hydrochloride is the deuterium labeled Acetyl-L-carnitine hydrochloride (HY-B0762). Acetyl-L-carnitine (O-Acetyl-L-carnitine; ALCAR) hydrochloride is an orally active mitochondrial energy metabolism regulator and neuroprotectant that can penetrate the blood-brain barrier. Acetyl-L-carnitine hydrochloride selectively enters cells and the brain through the organic cation transporter OCTN2. Acetyl-L-carnitine hydrochloride can participate in fatty acid β-oxidation, promote acetylcholine synthesis, regulate mitochondrial function and inhibit oxidative stress as an acetyl donor. Acetyl-L-carnitine hydrochloride exerts its activity by enhancing energy metabolism, protecting neurons and improving synaptic plasticity. Acetyl-L-carnitine hydrochloride is mainly used in the study of neurodegenerative diseases and metabolic disorder-related diseases such as neonatal hypoxic-ischemic brain damage, Alzheimer's disease, and depression.
|
|
/
|
| HY-N0660 | Jujuboside B |
Jujuboside B is a bioactive saponin component isolated from Ziziphi Spinosae Semen (sour jujube seed), with oral efficacy and blood-brain barrier permeability. Jujuboside B induces acute leukemia cell death and drives necroptosis apoptosis by activating the RIPK1/RIPK3/MLKL pathway. Jujuboside B upregulates the expression of NOXA, PARP and caspase-3, activates AMPK, inhibits the proliferation of breast cancer cells, and induces cell apoptosis and autophagy. Jujuboside B inhibits angiogenesis and tumor growth by blocking the VEGFR-2 signaling pathway. Jujuboside B alleviates liver injury in mice by regulating the Nrf2-STING signaling pathway. Jujuboside B alleviates liver injury by regulating anti-inflammatory responses and downregulating the expression of 11β-HSD2. Jujuboside B induces ferroptosis and overcomes radioresistance in non-small cell lung cancer via the PPARγ-ATF3-Gpx4 signaling pathway. Jujuboside B exerts inhibitory effects on platelet aggregation. Jujuboside B inhibits febrile seizures by suppressing the activity of AMPA receptors. Jujuboside B reverses chronic unpredictable mild stress-promoted tumor progression by blocking the PI3K/Akt and MAPK/ERK pathways and dephosphorylating CREB signaling. Jujuboside B is applicable to related studies on acute leukemia, breast cancer, PM2.5-induced lung injury, hepatotoxicity, liver injury, colorectal cancer, non-small cell lung cancer, thromboembolic diseases, cardiovascular diseases associated with high platelet aggregation, febrile seizures, and depressive-like phenotypes.
|
Apoptosis
PARP
Caspase
AMPK
Autophagy
VEGFR
Keap1-Nrf2
STING
11β-HSD
Ferroptosis
PI3K
Akt
p38 MAPK
ERK
Inflammation or Immune System Disease
Metabolic or Endocrine Disease
Breast Cancer
Colorectal Cancer
Leukemia/Lymphoma/Myeloma
Depression
Non-Small Cell Lung Cancer
|
/
|
| HY-16739 | Emeramide |
Emeramide is a thiol-redox antioxidant and heavy metal chelator.
|
|
/
|
| HY-B1092A | Gluconate sodium |
Gluconate sodium (D-Gluconic acid sodium salt) is an orally active glucose derivative. Gluconate sodium reduces nitric oxide and inflammatory cytokines (IL-1β and IL-6). Gluconate sodium inhibits ERK phosphorylation. Gluconate sodium has antioxidant and antiplatelet activation activities. Gluconate sodium has antitumor activity against colorectal cancer. Gluconate sodium improves osteoarthritis, intestinal damage and acute lung injury.
|
Breast Cancer
Colorectal Cancer
Prostate Cancer
Liver Cancer
Depression
Pain
Autoimmune Disease
Digestive System Inflammation
Cardiovascular Disease
SARS-CoV-2 Infection
Staphylococcus Aureus Infection
Clostridium Difficile Infection
Obesity
|
/
|
| HY-W012382 | N-Acetyl-L-tyrosine |
N-Acetyl-L-tyrosine is an orally active endogenous mitochondrial stress response regulator that can permeate the cell membrane by passive diffusion. N-Acetyl-L-tyrosine induces low-level reactive oxygen species (ROS) generation by transiently perturbing mitochondrial membrane potential, triggering reverse signaling to activate FoxO and Keap1 pathways. As a result, N-Acetyl-L-tyrosine enhances the expression of antioxidant enzyme genes, exerting anti-stress and cytoprotective effects. N-Acetyl-L-tyrosine can improve heat stress tolerance, inhibit tumor growth, and regulate energy metabolism. N-Acetyl-L-tyrosine can be used in the research of aging, metabolic diseases (such as diabetes), and cancer.
|
|
/
|
| HY-N0420R | Succinic acid (Standard) |
Succinic acid (Standard) is the analytical standard of Succinic acid. This product is intended for research and analytical applications. Succinic acid is an anti-anxiety agent with oral activity. Disodium succinate is the salt form of Succinic acid. Succinic acid is an intermediate product of the tricarboxylic acid cycle. Succinic acid is an important platform chemical. Succinic acid can be used as surfactant, additive, ion chelating agent, flavoring agent and other applications in chemical, pharmaceutical and food fields.
Source: Human Blood, Breast Milk, Cerebrospinal Fluid (CSF |
|
/
|
| HY-Y0396 | N-Hydroxyphthalimide |
N-Hydroxyphthalimide is a blocking agent and catalyst. N-Hydroxyphthalimide promotes oxidation reactions by generating PINO free radicals and activating hydrogen atom transfer processes. N-Hydroxyphthalimide reduces the expression of anti-apoptotic proteins Survivin and Bcl-xL and activates caspase 9 and caspase 3. N-Hydroxyphthalimide induces Apoptosis. N-Hydroxyphthalimide inhibits the phosphorylation of mTOR (Ser2448, Ser2481) and Akt (Ser473). N-Hydroxyphthalimide has anticancer effects against breast and colon cancer.
|
|
/
|
| HY-Y0319G | Magnesium acetate tetrahydrate |
Magnesium acetate tetrahydrate is a carboxylic acid and short-chain fatty acid (SCFAs). Magnesium acetate tetrahydrate activates AMPK, increases ROS, cleaved caspase 9, PPARα, downregulates SREBP-1c, ChREBP expression. Magnesium acetate tetrahydrate exhibits antifungal activity against Saccharomyces cerevisiae W303-1A. Magnesium acetate tetrahydrate regulates energy metabolism. Magnesium acetate tetrahydrate has anticancer activity against gastric cancer. Magnesium acetate tetrahydrate induces writhing reaction and ulcerative colitis. Magnesium acetate tetrahydrate can be used in the researches for gastric cancer, ulcerative colitis, hepatic steatosis, and pain.
|
Infection
Neurological, Eye or Ear Disease
Inflammation or Immune System Disease
Metabolic or Endocrine Disease
|
/
|
| HY-126358 | Acetylcarnitine |
Acetylcarnitine is a CNS-penetrant endogenous metabolite. Acetylcarnitine shuttling links mitochondrial metabolism to histone acetylation and lipogenesis. Acetylcarnitine attenuates oxidative stress and neuroinflammation. Acetylcarnitine can be used for fatigue-associated diseases research. Acetylcarnitine can be used as a candidate diagnostic and prognostic biomarker of hepatocellular carcinoma.
|
|
/
|
| HY-B0240R | Disulfiram (Standard) |
Disulfiram (Standard) is the analytical standard of Disulfiram. This product is intended for research and analytical applications. Disulfiram (Tetraethylthiuram disulfide) is a specific inhibitor of aldehyde-dehydrogenase (ALDH1), used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells. Disulfiram + Cu2+ increases intracellular ROS levels triggering apoptosis of ovarian cancer stem cells.
|
Reference Standards
Aldehyde Dehydrogenase (ALDH)
Interleukin Related
Pyroptosis
Apoptosis
Cuproptosis
|
/
|
| HY-N0420S2 | Succinic acid-13C4 |
Succinic acid-13C4 is the 13C labeled Succinic acid. Succinic acid is a potent and orally active anxiolytic agent. Succinic acid is an intermediate product of the tricarboxylic acid cycle. Succinic acid can be used as a precursor of many industrially important chemicals in food, chemical and pharmaceutical industries.
|
|
/
|
| HY-Y1325I | Sodium acetate trihydrate, 99.5% |
Sodium acetate trihydrate, 99.5% is a carboxylic acid and short-chain fatty acid (SCFAs). Sodium acetate trihydrate activates AMPK, increases ROS, cleaved caspase 9, PPARα, downregulates SREBP-1c, ChREBP expression. Sodium acetate trihydrate exhibits antifungal activity against Saccharomyces cerevisiae W303-1A. Sodium acetate trihydrate regulates energy metabolism. Sodium acetate trihydrate has anticancer activity against gastric cancer. Sodium acetate trihydrate induces writhing reaction and ulcerative colitis. Sodium acetate trihydrate can be used in the researches for gastric cancer, ulcerative colitis, hepatic steatosis, and pain.
|
|
/
|
| HY-100355 | C18-Ceramide (d18:1/18:0) |
C18-Ceramide (d18:1/18:0) is a bioactive molecule with multiple functions in cells, not a traditional agonist or inhibitor targeting a single site. It can act on multiple cellular targets, such as proteins related to endoplasmic reticulum stress (e.g., ATF-4, XBP-1, CHOP), proteins in the PI3K/AKT signaling pathway, and SNARE complex proteins. It exerts activities like inducing cell death, promoting autophagy, and regulating exocytosis through mechanisms such as activating endoplasmic reticulum stress, inhibiting the PI3K/AKT signaling pathway, and affecting lipid raft - related functions. It can be used in research on the mechanism of neuronal injury in the field of neuroscience and in the treatment research of cancers such as glioma in the field of oncology.
|
|
/
|
| HY-P75286 | DLAT Protein, Human (sf9, His) |
DLAT protein is an important component of the pyruvate dehydrogenase complex, which mainly promotes the conversion of pyruvate into acetyl-CoA and CO2. This enzymatic step establishes a critical link between glycolysis and the tricarboxylic acid (TCA) cycle. DLAT Protein, Human (sf9, His) is the recombinant human-derived DLAT protein, expressed by Sf9 insect cells , with N-His labeled tag.
Species: Human; Source: Sf9 insect cells |
|
/
|
| HY-P70821 | TRAIL R2/TNFRSF10B Protein, Mouse (HEK293, hFc) |
TRAIL R2/TNFRSF10B protein is the receptor of TNFSF10/TRAIL and activates apoptosis through FADD-mediated recruitment of caspase-8 to form death-inducing signaling complex (DISC).It initiates caspase cascade-mediated apoptosis and promotes NF-kappa-B activation, which is critical for ER stress-induced apoptosis.TRAIL R2/TNFRSF10B Protein, Mouse (HEK293, hFc) is the recombinant mouse-derived TRAIL R2/TNFRSF10B protein, expressed by HEK293 , with C-hFc labeled tag.
Species: Mouse; Source: HEK293 |
|
/
|
| HY-P7307 | TRAIL R2/TNFRSF10B Protein, Human (HEK293) |
TRAIL R2/TNFRSF10B Protein, Human (HEK293) is a cell surface receptor of the TNF-receptor superfamily that binds TRAIL and mediates apoptosis.
Species: Human; Source: HEK293 |
|
/
|
| HY-P75316 | CUTC Protein, Human (His) |
CUTC proteins potentially regulate copper homeostasis by binding Cu(1+) of each subunit, suggesting a role in the control of cellular copper levels. As a homotetramer, the tetrameric arrangement of CUTC suggests cooperative behavior in managing copper ions. CUTC Protein, Human (His) is the recombinant human-derived CUTC protein, expressed by E. coli , with N-His labeled tag.
Species: Human; Source: E. coli |
|
/
|
| HY-P705478 | Ferredoxin-1 Protein, Human (His, Myc) |
Species: Human; Source: E. coli |
|
/
|
| HY-P74497 | TRAIL R2/TNFRSF10B Protein, Human (HEK293, hFc) |
TRAIL R2/TNFRSF10B protein is the receptor of TNFSF10/TRAIL and recruits caspase-8 through FADD to initiate cell apoptosis. It forms the death-inducing signaling complex (DISC), activates caspases and mediates apoptosis. TRAIL R2/TNFRSF10B Protein, Human (HEK293, hFc) is the recombinant human-derived TRAIL R2/TNFRSF10B protein, expressed by HEK293 , with C-hFc labeled tag.
Species: Human; Source: HEK293 |
|
/
|
| HY-P78220 | TRAIL R2/TNFRSF10B Protein, Human (Biotinylated, HEK293, His-Avi) |
TRAIL R2/TNFRSF10B protein is the receptor of TNFSF10/TRAIL and recruits caspase-8 through FADD to initiate cell apoptosis. It forms the death-inducing signaling complex (DISC), activates caspases and mediates apoptosis. TRAIL R2/TNFRSF10B Protein, Human (Biotinylated, HEK293, His-Avi) is the recombinant human-derived TRAIL R2/TNFRSF10B protein, expressed by HEK293 , with C-Avi, C-His labeled tag.
Species: Human; Source: HEK293 |
|
/
|
| HY-P78530 | TRAIL R2/TNFRSF10B Protein, Human (HEK293, His-Avi) |
TRAIL R2/TNFRSF10B protein is the receptor of TNFSF10/TRAIL and recruits caspase-8 through FADD to initiate cell apoptosis. It forms the death-inducing signaling complex (DISC), activates caspases and mediates apoptosis. TRAIL R2/TNFRSF10B Protein, Human (HEK293, His-Avi) is the recombinant human-derived TRAIL R2/TNFRSF10B protein, expressed by HEK293 , with C-Avi, C-His labeled tag.
Species: Human; Source: HEK293 |
|
/
|
| HY-P72977 | TRAIL R2/TNFRSF10B Protein, Mouse (HEK293, His-Fc) |
TRAIL R2/TNFRSF10B protein is the receptor of TNFSF10/TRAIL and activates apoptosis through FADD-mediated recruitment of caspase-8 to form death-inducing signaling complex (DISC).It initiates caspase cascade-mediated apoptosis and promotes NF-kappa-B activation, which is critical for ER stress-induced apoptosis.TRAIL R2/TNFRSF10B Protein, Mouse (HEK293, His-Fc) is the recombinant mouse-derived TRAIL R2/TNFRSF10B protein, expressed by HEK293 , with C-hFc, C-His labeled tag.
Species: Mouse; Source: HEK293 |
|
/
|
| HY-P78363 | TRAIL R2/TNFRSF10B Protein, Mouse (HEK293, His) |
TRAIL R2/TNFRSF10B protein is the receptor of TNFSF10/TRAIL and activates apoptosis through FADD-mediated recruitment of caspase-8 to form death-inducing signaling complex (DISC).It initiates caspase cascade-mediated apoptosis and promotes NF-kappa-B activation, which is critical for ER stress-induced apoptosis.TRAIL R2/TNFRSF10B Protein, Mouse (HEK293, His) TRAIL R2/TNFRSF10B Protein, Mouse (HEK293, His) is the recombinant mouse-derived TRAIL R2/TNFRSF10B protein, expressed by HEK293 , with C-His labeled tag.
Species: Mouse; Source: HEK293 |
|
/
|
| HY-P78567 | TRAIL R2/TNFRSF10B Protein, Cynomolgus (HEK293, His) |
TRAIL R2/TNFRSF10B Protein serves as a receptor for the cytotoxic ligand TNFSF10/TRAIL. Upon ligand binding, the adapter molecule FADD recruits caspase-8 to the activated receptor, forming the death-inducing signaling complex (DISC). This activation leads to a cascade of caspases, mediating apoptosis. TRAIL R2/TNFRSF10B lacks conserved residue(s) crucial for feature annotation propagation. TRAIL R2/TNFRSF10B Protein, Cynomolgus (HEK293, His) is the recombinant cynomolgus-derived TRAIL R2/TNFRSF10B protein, expressed by HEK293 , with C-His labeled tag.
Species: Cynomolgus; Source: HEK293 |
|
/
|
| HY-P74498 | TRAIL R2/TNFRSF10B Protein, Human (Biotinylated, HEK293, His) |
TRAIL R2/TNFRSF10B protein is the receptor of TNFSF10/TRAIL and recruits caspase-8 through FADD to initiate cell apoptosis. It forms the death-inducing signaling complex (DISC), activates caspases and mediates apoptosis. TRAIL R2/TNFRSF10B Protein, Human (Biotinylated, HEK293, His) is the recombinant human-derived TRAIL R2/TNFRSF10B protein, expressed by HEK293 , with C-His labeled tag.
Species: Human; Source: HEK293 |
|
/
|
| HY-P71378 | TRAIL R2/TNFRSF10B Protein, Mouse (HEK293, Avi-His) |
TRAIL R2/TNFRSF10B protein is the receptor of TNFSF10/TRAIL and activates apoptosis through FADD-mediated recruitment of caspase-8 to form death-inducing signaling complex (DISC).It initiates caspase cascade-mediated apoptosis and promotes NF-kappa-B activation, which is critical for ER stress-induced apoptosis.TRAIL R2/TNFRSF10B Protein, Mouse (HEK293, Avi-His) is the recombinant mouse-derived TRAIL R2/TNFRSF10B protein, expressed by HEK293 , with C-Avi, C-6*His labeled tag.
Species: Mouse; Source: HEK293 |
|
/
|
| HY-P87493 | ADX/FDX1 Antibody (YA7180) |
ADX/FDX1 Antibody (YA7180) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to ADX/FDX1.
Host: Rabbit; Reactivity: Human, Mouse, Rat |
|
/
|
| HY-P80292 | Pyruvate Dehydrogenase E2 Antibody (YA113) |
Pyruvate Dehydrogenase E2 Antibody (YA113) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to Pyruvate Dehydrogenase E2.
Host: Rabbit; Reactivity: Human, Mouse, Rat |
|
/
|
| HY-P82260A | ADX/FDX1 Antibody (YA2005)(PBS only) |
ADX/FDX1 Antibody (YA2005) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to ADX.
Host: Rabbit; Reactivity: Human, Mouse |
|
/
|
| HY-P81070A | Pyruvate Dehydrogenase E2 Antibody (YA912)(PBS only) |
Pyruvate Dehydrogenase E2 Antibody (YA912) is a Mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to Pyruvate Dehydrogenase E2.
Host: Mouse; Reactivity: Human, Mouse |
|
/
|
| HY-P85448 | Pyruvate Dehydrogenase E2 Antibody (YA5140) |
Pyruvate Dehydrogenase E2 Antibody (YA5140) is a Mouse-derived and non-conjugated monoclonal antibody, targeting to Pyruvate Dehydrogenase E2.
Host: Mouse; Reactivity: Human, Rabbit |
|
/
|
| HY-P85556 | Pyruvate Dehydrogenase E2 Antibody (YA5248) |
Pyruvate Dehydrogenase E2 Antibody (YA5248) is a Mouse-derived and non-conjugated monoclonal antibody, targeting to Pyruvate Dehydrogenase E2.
Host: Mouse; Reactivity: Human, Mouse |
|
/
|
| HY-P85577 | DR5 Antibody (YA5269) |
DR5 Antibody (YA5269) is a Mouse-derived and non-conjugated monoclonal antibody, targeting to DR5.
Host: Mouse; Reactivity: Human, Mouse |
|
/
|
Targets/Pathways
























































.jpg)































































































































































































































































































































































































































































































































































































































































































































































































































































