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.
-
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. -
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.
-
TME (Tumor microenvironment) is considered as a complex integrated system, composed of cellular components such as tumor cells and immune cells, as well as non-cellular components such as ECM and cytokines. According to the spatial distribution of immune cells in TME, "hot" and "cold" TME will be explained in this article.
-
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.
-
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! -
HLA-E, A Novel Immune Checkpoint
2023-06-29
Immune checkpoints have immunosuppressive functions. It can be used in the research of tumor immunotherapy. In this article, we introduce a new paper entitled "Immune checkpoint HLA-E: CD94 - NKG2Amediates evasion of circulating tumor cells from NK cell surveillance "research paper. -
How to Perform Western Blot?
2023-07-13
Western blot is one of the most frequently performed experiments in molecular biology, biochemistry and immunology. This article describes in detail how to do WB. -
Organoid Culture: Questions & Answers
2023-07-26
In the last issue, we conducted a live lecture on the theme of organoid culture. Today, we have a special topic to solve your doubts in the last live class! -
WHO's Q2 drug list has been updated. Let's take you through the list of the most noteworthy small molecule drugs that we should pay attention to.
-
FDA Approved Drug List!
2023-09-14
In the first half of 2023 (as of June 27), the FDA approved 26 new drugs, let's take you learn about it through the article. -
IHC is an indispensable technique for studying tissue morphology and in situ antigen expression, but usually only one or two antigens in tissues can be stained for analysis. It cannot judge the results more intuitively. Today, Little M will introduce you to the upgraded version mlHC.
-
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?
-
Katalin Karikó and Drew Weissman were awarded the Nobel Prize in Physiology or Medicine in 2023 for their groundbreaking work in nucleoside modification, which paved the way for the creation of successful mRNA vaccines to fight against COVID-19. Let's now delve into the complete process of mRNA vaccine development.
-
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.
-
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.
-
Antibodies!
2024-07-26
Today, We introduce antibodies for everyone! -
Streptavidin-Biotin System
2024-08-03
Streptavidin strongly binding small molecule biotin is one of the most popular non-covalent coupling methods. Streptavidin can be coupled to various carriers such as magnetic beads and agarose matrix, and become a highly specific affinity medium to capture various biotin-labeled ligands. -
What Are Popular Anti-tumor Drug Targets?
2024-08-20
The rapid development of targeted anti-cancer drugs has spurred diverse research across various modalities. These include small molecules, monoclonal antibodies (mAbs), cell immunotherapies, antibody-drug conjugates (ADCs), and PROTACs (proteolysis targeting chimeras). -
Cuproptosis, How much do you know?
2024-08-22
Cells die in a variety of ways, including apoptosis, pyroptosis, necrosis, and ferroptosis......And, of course, cuproptosis. So, how much do you know about cuproptosis? -
Virtual Screening and New Uses for Old Drugs
2024-09-17
With the advancement of medical science, drug screening against various disease targets has become the fundamental strategy for drug development. Currently, computer-based virtual screening techniques are emerging in the field of new drug research due to their efficiency and low cost. Let's explore it today! -
Recently, Mol Cell reported the discovery of the first ferroptosis marker, Hyperoxidized PRDX3! Let’s take a look together~
-
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!
-
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.
-
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.
-
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.
-
This detailed guide outlines the standardized experimental protocols for multiplex immunohistochemistry (mIHC), systematically summarizes common technical issues encountered during sample preparation, staining and imaging processes, and provides practical troubleshooting solutions to ensure reliable and reproducible results in biomedical research and clinical sample analysis.
-
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.
-
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.
-
This paper elaborates on cytokines for culturing major immune cells, their regulatory roles, recombinant cytokines' merits and MCE’s related high-quality products.
-
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.
-
This review critically examines the role of the JAK-STAT pathway in immunity and autoimmune diseases, reviews current clinical applications of targeted therapies, and highlights emerging trends in autoimmune drug development.
-
This review summarizes the mechanisms of DSS-induced colitis, commonly used modeling approaches, and key considerations related to DSS molecular weight.
-
This review discusses β-cell dysfunction driven by mitochondrial impairment, outlines mitochondrial quality control networks, and summarizes strategies to restore mitochondrial function.
-
Review mitophagy regulation, disease mechanisms, and therapeutic advances to guide future research and drug development.
-
Review the mechanisms, mitochondrial regulation, disease relevance, and translational opportunities of the NLRP3–STING axis in neuroinflammation.
-
Explore the mechanisms driving immune tolerance breakdown in autoimmune diseases and emerging tolerance-restoring strategies, with a focus on IL-2-based immune modulation.
-
Explore how mitochondrial quality control, inflammatory signaling, and metabolic–epigenetic reprogramming regulate cellular senescence and the SASP, along with strategies to restore mitochondrial homeostasis.
-
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. -
Multiple Tyrosine Kinases Inhibitor TAS-115
2019-04-19
TAS-115 is a potent VEGFR and c-Met/HGFR-targeted kinase inhibitor with IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively. -
Y06036 is a potent and selective BET inhibitor for potential treatment of castration-resistant prostate cancer. With nanomolar inhibition.
-
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.
-
TAK-828F is a potent, selective and orally active retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist. TAK-828F inhibits IL-17A cytokine expression and reduces symptoms of autoimmune encephalomyelitis mice.
-
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.
-
S18-000003 is a potent, selective and orally active inhibitor of retinoic acid receptor-related orphan receptor-gamma-t (RORγt). S18-000003 ameliorates psoriasis-like lesions in vivo. S18-000003 can be used for the research of skin inflammatory diseases.
-
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.
-
BI-167107 is a high affinity, full agonist that binds to the β2 adrenergic receptor (β2AR) with a dissociation constant Kd of 84 pM.
-
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.
-
ADH-503 is an orally active and allosteric CD11b agonist and leads to the repolarization of tumor-associated macrophages.
-
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.
-
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.
-
AUTAC4 is a mitochondria-targeting autophagy-targeting chimera, which can be used for the study of mitochondrial dysfunction.
-
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.
-
Trolox is an analogue of vitamin E with a powerful antioxidant effect. Trolox is also a powerful inhibitor of membrane damage.
-
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. -
CL097 is a TLR7/8 agonist. CL097 induces pro-nflammatory cytokines. CL097 induces NADPH oxidase priming and efficient diabetogenic cytotoxic T lymphocyte (CTL) function in NOD mice.
-
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.
-
BM213 is a selective C5aR1 agonist. It’s a useful research tool to study C5aR1 function
-
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.
-
Pelecopan is a potent, selective, and orally active complement factor D inhibitor, possessing the potential to study paroxysmal nocturnal hemoglobinuria (PNH).
-
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
-
Etrolizumab is a Gut-selective, Anti-β7 Integrin McAb for Inflammatory Bowel Disease (IBD) Research
2022-11-05
Etrolizumab is a gut-selective, anti-β7 integrin monoclonal antibody and has the potential for the research of inflammatory bowel disease. -
JNJ-9350 is an inhibitor of spermine oxidase (SMOX). JNJ-9350 also inhibits polyamine oxidase (PAO). JNJ-9350 has anti-cancer activity.
-
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
-
Kits
-
Inhibitory Antibodies
-
Reference Standards
-
Induced Disease Models Products
-
GMP Small Molecules
-
Enzyme
-
Biochemical Assay Reagents
-
Natural Products
| Cat. No. | Product Name | Information | Application | Publication |
|---|---|---|---|---|
| HY-100523 | ML385 |
ML385 is a potent and selective Nrf2 inhibitor with an IC50 of 1.9 μM. ML385 directly binds to the Neh1 domain of NRF2, interferes with the binding of the MAFG-NRF2 protein complex to the antioxidant response element (ARE) DNA sequence, thereby blocking the expression of downstream target genes of NRF2. ML385 can be used in studies related to adult T-cell leukemia, breast cancer, myocardial ischemia/reperfusion injury, non-small cell lung cancer, esophageal squamous cell carcinoma, head and neck squamous cell carcinoma, and lung squamous cell carcinoma.
|
Breast Cancer
Colorectal Cancer
Cardiovascular Disease
Non-Small Cell Lung Cancer
Lung Squamous Cell Carcinoma
Squamous Cell Carcinoma
Esophageal Cancer
|
644
|
| HY-A0281 | 4-Phenylbutyric acid |
Lung Cancer
Breast Cancer
Liver Cancer
Leukemia/Lymphoma/Myeloma
Pancreatic Cancer
Viral Infection
SARS-CoV-2 Infection
|
262
|
|
| HY-15144 | Trichostatin A |
|
201
|
|
| HY-A0004 | Decitabine |
Decitabine (NSC 127716) is an orally active deoxycytidine analogue antimetabolite and DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell Apoptosis. Decitabine has potent anticancer activity.
|
Pancreatic Cancer
Viral Infection
Digestive System Inflammation
Urogenital Cancer
Non-Small Cell Lung Cancer
Acute Myeloid Leukemia
SARS-CoV-2 Infection
Rheumatoid Arthritis
|
183
|
| HY-10221 | Vorinostat |
Vorinostat (SAHA) is a potent and orally active pan-inhibitor of HDAC1, HDAC2 and HDAC3 (Class I), HDAC6 and HDAC7 (Class II) and HDAC11 (Class IV), with ID50 values of 10 nM and 20 nM for HDAC1 and HDAC3, respectively. Vorinostat induces cell apoptosis. Vorinostat is also an effective inhibitor of human papillomaviruse (HPV)-18 DNA amplification.
|
Neurological, Eye or Ear Disease
Breast Cancer
Prostate Cancer
Liver Cancer
Leukemia/Lymphoma/Myeloma
Pancreatic Cancer
Viral Infection
Digestive System Inflammation
Lung Fibrosis
|
175
|
| HY-16561 | Resveratrol |
Resveratrol (trans-Resveratrol; SRT501) is a CNS-penetrant natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator. Resveratrol is a potent pregnane X receptor (PXR) inhibitor. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model. Resveratrol increases production of NO in endothelial cells.
|
Neurological, Eye or Ear Disease
Prostate Cancer
Liver Cancer
Bacterial Infection
Fungal Infection
Digestive System Inflammation
Glucose Metabolism
SARS-CoV-2 Infection
Obesity
Lung Fibrosis
|
174
|
| HY-B0075 | Melatonin |
Melatonin is a hormone made by the pineal gland that can activate melatonin receptor and inhibit PANoptosis. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties. Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation. Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress.
|
Melatonin Receptor
Autophagy
Mitophagy
Endogenous Metabolite
Apoptosis
PANoptosis
Ligands for Target Protein for PROTAC
Histone Acetyltransferase
Lung Cancer
Breast Cancer
Prostate Cancer
Liver Cancer
Viral Infection
Neurodegenerative Disease
Digestive System Inflammation
SARS-CoV-2 Infection
|
149
|
| HY-100573 | Necrosulfonamide |
Necrosulfonamide is a MLKL and Gasdermin D (GSDMD) inhibitor, capable of separately inhibiting necroptosis and pyroptosis of cells. Necrosulfonamide does not affect the activation of upstream signals, but specifically inhibits the downstream executor oligomerization step. Necrosulfonamide reduces the expression of the key kinases NLRP3 and caspase-1 involved in necroptosis and pyroptosis, activate the Nrf2 pathway and the downstream antioxidant enzymes, and also downregulates a variety of inflammatory factors. Necrosulfonamide plays significant roles in various diseases such as neurodegenerative diseases (such as Parkinson’s disease), tissue damage and ischemia-reperfusion injury, inflammatory bowel disease, osteoarthritis and fracture repair, and hair loss by regulating two important programmed necrosis pathways.
|
Mixed Lineage Kinase
Necroptosis
Pyroptosis
Caspase
NOD-like Receptor (NLR)
Keap1-Nrf2
TNF Receptor
Interleukin Related
NO Synthase
Heme Oxygenase (HO)
Digestive System Disease
Prostate Cancer
Leukemia/Lymphoma/Myeloma
Depression
Digestive System Inflammation
Cardiovascular Disease
Parkinson's Disease
Obesity
Lung Fibrosis
Rheumatoid Arthritis
|
147
|
| HY-10586 | 5-Azacytidine |
Lung Cancer
Prostate Cancer
Leukemia/Lymphoma/Myeloma
Pancreatic Cancer
Bacterial Infection
SARS-CoV-2 Infection
Rheumatoid Arthritis
|
142
|
|
| HY-N0005 | Curcumin |
Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin is a photosensitizer against microorganisms. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
|
Histone Acetyltransferase
Epigenetic Reader Domain
Keap1-Nrf2
Autophagy
Mitophagy
Influenza Virus
Ferroptosis
Apoptosis
Prostate Cancer
Leukemia/Lymphoma/Myeloma
Pancreatic Cancer
Viral Infection
Pain
Digestive System Inflammation
Glucose Metabolism
Metastatic Breast Cancer
SARS-CoV-2 Infection
Obesity
Lung Fibrosis
|
138
|
| HY-100489 | TBHQ |
|
131
|
|
| HY-107455 | A-485 |
A-485, a chemical probe, is a potent and selective catalytic inhibitor of p300/CBP with IC50s of 9.8 nM and 2.6 nM for p300 and CBP histone acetyltransferase (HAT), respectively.
|
|
114
|
| HY-L005 | Epigenetics Compound Library |
Epigenetics refers to changes in phenotype that are not rooted in DNA sequence. Many types of epigenetic processes have been identified, including DNA methylation, alteration in the structure of histone proteins and gene regulation by small noncoding microRNAs. Modification of DNA, protein, or RNA, resulting in changes to the function and/or regulation of these molecules, without altering their primary sequences, reveals the complexities of cellular differentiation, embryology, the regulation of gene expression, aging, cancer, and other diseases.
MCE provide a unique collection of 2,031 epigenetics-related compounds that can be used in the research of the related diseases.
|
|
102
|
| HY-13823 | C646 |
C646 is a selective and competitive histone acetyltransferase p300 inhibitor with Ki of 400 nM, and is less potent for other acetyltransferases.
|
|
98
|
| HY-112675 | 4-Octyl itaconate |
4-Octyl Itaconate is a cell-permeable Itaconate derivative. Itaconate is an anti-inflammatory metabolite that activates Nrf2 via alkylation of KEAP1.
|
|
98
|
| HY-N0162 | Luteolin |
Luteolin (Luteoline), a flavanoid compound, is a potent Nrf2 inhibitor. Luteolin has anti-inflammatory, anti-cancer properties, including the induction of apoptosis and cell cycle arrest, and the inhibition of metastasis and angiogenesis, in several cancer cell lines, including human non-small lung cancer cells.
|
Lung Cancer
Colorectal Cancer
Ovarian Cancer
Digestive System Inflammation
Glucose Metabolism
Obesity
|
96
|
| HY-12163 | Entinostat |
|
95
|
|
| HY-10224 | Panobinostat |
Panobinostat (LBH589; NVP-LBH589) is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities. Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells. Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma.
|
Prostate Cancer
Liver Cancer
Leukemia/Lymphoma/Myeloma
Pancreatic Cancer
Viral Infection
Digestive System Inflammation
Small Cell Lung Cancer
Non-Small Cell Lung Cancer
HER-2 Positive Breast Cancer
Metastatic Breast Cancer
SARS-CoV-2 Infection
Lung Fibrosis
|
90
|
| HY-L024 | Histone Modification Research Compound Library |
A histone modification, a covalent post-translational modification (PTM) to histone proteins, includes methylation, phosphorylation, acetylation, ubiquitylation, and sumoylation, etc. In general, histone modifications are catalyzed by specific enzymes that act predominantly at the histone N-terminal tails involving amino acids such as lysine or arginine, as well as serine, threonine, tyrosine, etc. The PTMs made to histones can impact gene expression by altering chromatin structure or recruiting histone modifiers. Histone modifications act in diverse biological processes such as transcriptional activation/inactivation, chromosome packaging, and DNA damage/repair. Deregulation of histone modification contributes to many diseases, including cancer and autoimmune diseases.
MCE owns a unique collection of 931 bioactive compounds targeting Epigenetic Reader Domain, HDAC, Histone Acetyltransferase, Histone Demethylase, Histone Methyltransferase, Sirtuin, etc. Histone Modification Research Compound Library is a useful tool for histone modification research and drug screening.
|
|
85
|
| HY-L123 | Human Metabolite Library |
Human metabolism is an integral part of cellular function that reflects individual differences in health, disease, diet, and lifestyle. Many health conditions such as obesity, diabetes, hypertension, heart disease, and cancer are associated with abnormal metabolic states. In the pathological state of the human body, metabolic pathways are significantly altered, resulting in aberrant levels of intermediates or end-products that can be viewed as potential diagnostic biomarkers or even therapeutic targets. Therefore, detection, identification and quantification of human metabolites are very important for drug metabolism research in drug development.
MCE offers a unique collection of 6,767 human metabolites, including endogenous metabolites and exogenous metabolites, covering multiple structure types, such as lipids, amino acids, nucleic acids, carbohydrates, organic acids, biogenic amines, vitamins,. MCE Human Metabolites Library is a helpful tool for studying the relationship between diseases and metabolism.
|
|
85
|
| HY-L046 | Anti-Cardiovascular Disease Compound Library |
Cardiovascular diseases (CVDs) are a group of disorders of the heart and blood vessels which include coronary heart disease, cerebrovascular disease, peripheral arterial disease, rheumatic heart disease, etc. CVDs are the number 1 cause of death globally. Smoking, unhealthy nutrition, aging population, lack of physical activity, arterial hypertension, or diabetes can promote cardiovascular disease like myocardial infarction or stroke. It is multifactorial and encompasses a multitude of mechanisms, such as eNOS uncoupling, reactive oxygen species formation, chronic inflammatory disorders and abnormal calcium homeostasis. Antioxidant, anti-inflammatory and anti-diabetes agents may reduce the cardiovascular disease risk.
MCE supplies a unique collection of 2,468 compounds with confirmed anti-cardiovascular activity. These compounds mainly target metabolic enzyme, membrane transporter, ion channel, inflammation related signaling pathways. MCE Anti-Cardiovascular Disease Compound Library can be used for cardiovascular diseases related research and high throughput and high content screening for new drugs.
|
|
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-L005M | Epigenetics Compound Library Mini |
Epigenetics involves heritable phenotypic changes that occur without alterations to the underlying DNA sequence. Key mechanisms include DNA methylation, histone modifications, and regulation by small non-coding RNAs such as microRNAs. By modifying DNA, histones, or RNA—while leaving their primary sequences intact—these processes influence molecular function and regulation, thereby playing critical roles in cellular differentiation, embryonic development, gene expression control, aging, and diseases such as cancer.
MCE provide a unique collection of 295 epigenetics-related compounds. For each regulatory target and its subtype, 3 to 5 highly specific representative compounds have been retained, which can be used in epigenetic and related disease research.
|
|
83
|
| HY-L118 | Sodium Channel Blocker Library |
Sodium channels conduct sodium ions (Na+) through a cell's plasma membrane that are the source of excitatory currents for the nervous system and muscle. Na channels are classified according to the trigger that opens the channel for such ions, i.e. either a voltage-change (Voltage-gated, voltage-sensitive, or voltage-dependent sodium channel also called VGSCs or Nav channel) or a binding of a substance (a ligand) to the channel (ligand-gated sodium channels). Dysfunction in voltage-gated sodium channels correlates with neurological and cardiac diseases, including epilepsy, myopathies, pain and cardiac arrhythmias. Sodium channel blockers are used in the treatment of cardiac arrhythmia, pain and convulsion.
MCE offers a unique collection of 199 sodium channel blocker and antagonists, all of which have the identified inhibitory effect on sodium channels. MCE Sodium Channel Blocker Library can be used for neurological and cardiac diseases drug discovery and sodium channel research.
|
|
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-L197 | Vitamin Compound Library |
Vitamins are a category of trace organic compounds essential for maintaining normal physiological functions in living organisms. They are classified into fat-soluble and water-soluble vitamins. Fat-soluble vitamins play a role in maintaining vision, bone health, reproductive functions, and blood coagulation. Water-soluble vitamins are involved in energy metabolism, nervous system function, and cellular repair processes. Most vitamins cannot be synthesized by the organism and must be obtained through diet. In recent years, vitamins and their derivatives have become increasingly important in the field of drug development due to their extensive physiological activities. Additionally, vitamins and their derivatives can be used to construct research platforms for vitamin metabolism, which helps to delve into the metabolic pathways and dynamic changes of vitamins within the body and aids in identifying new biomarkers for certain diseases.
MCE included 136 vitamins and their derivatives, including Vitamin A, Vitamin B, Vitamin D, etc., which is a good tool for studying vitamin metabolism.
|
|
83
|
| HY-L203 | Methylation Compound Library |
Methylation is an epigenetic modification mechanism that involves adding methyl groups to molecules such as DNA and histones, which can alter gene expression without changing the DNA sequence. This process is catalyzed by enzymes such as DNA methyltransferases (DNMTs) and histone methyltransferases (HMTs), and can be reversed by demethylases.
The balance of methylation and demethylation is crucial for maintaining cellular function and genomic stability. Abnormal regulation of methylation may lead to a variety of diseases, including cancer, neurological disorders, and developmental abnormalities. A deep understanding of the molecular mechanisms of methylation metabolism is essential for developing therapeutic strategies for diseases associated with methylation dysregulation.
MCE contains 351 compounds targeting methylation/demethylation enzymes, which is of significant value for studying the pathways of methylation metabolism and exploring their mechanisms of action in diseases.
|
|
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-L208 | Bile Acids Library |
Bile acids are a class of amphiphilic molecules derived from the metabolic breakdown of cholesterol, primarily synthesized in the liver, and play a crucial role in the intestines. Based on their structural characteristics, bile acids are mainly divided into two categories: free bile acids (including Cholic acid, Deoxycholic acid, Chenodeoxycholic acid) and conjugated bile acids (including Glycocholic acid, Glycochenodeoxycholic acid, Taurocholic acid, etc.). Bile acids play a significant role in the pathophysiological research of liver and gastrointestinal diseases and are closely associated with the occurrence of metabolic diseases such as obesity, type II diabetes, non-alcoholic fatty liver disease, and atherosclerosis. Bile acids maintain metabolic balance within the body by regulating sugar metabolism, lipid metabolism, and amino acid metabolism, and they influence the activity of metabolism-related enzymes and transporters. In addition, Bile acids can also be used to construct a bile acid metabolism research platform, which helps to delve into the metabolic pathways and dynamic changes of bile acids in living organisms and aids in identifying new biomarkers for certain diseases.
MCE included 62 bile acids, including Cholic acid, Deoxycholic acid, Glycocholic acid, etc., which are effective tools for the study of liver and gallbladder diseases.
|
|
83
|
| HY-L225 | Cardiotoxic Compound Library |
Drug development is both expensive and time-consuming, with approximately one-third of drug discontinuations caused by severe adverse drug reactions (ADRs). Among these, drug-induced cardiotoxicity (DICT) is one of the primary reasons for late-stage clinical drug failures and market withdrawals. To date, cardiotoxicity has been observed in multiple drug classes, such as anticancer drugs, antipsychotics, antidepressants, antibiotics, and neurodegenerative disease medications. To reduce cardiac ADRs, it is crucial to determine the clinical relevance of DICT to treatment, elucidate the underlying molecular mechanisms, identify reliable biomarkers, and develop new diagnostic and therapeutic approaches.
MCE offers 260 cardiotoxicity compounds, including some FDA-approved drugs as well as inhibitors/blockers of the hERG potassium channel.
|
|
83
|
| HY-L229 | Nephrotoxicity Compound Library |
Kidneys are one of the vital organs in the human body. Due to their exposure to higher concentrations of circulating drugs or metabolites, they are highly susceptible to drug-induced renal injury (DIRI). According to statistics, drug-induced kidney injury accounts for approximately 20% of nephrotoxicity reports and can lead to acute kidney injury (AKI), chronic kidney disease (CKD), or even end-stage renal disease (ESRD). Early detection of drug nephrotoxicity is crucial for preventing irreversible kidney damage. Research into its mechanisms can help optimize clinical medication by adjusting dosages or avoiding combinations of nephrotoxic drugs. Additionally, predicting drug-induced nephrotoxicity in early drug development can reduce the risk of late-stage R&D failure.
MCE offers 160 nephrotoxicity compounds that have been clearly reported by the FDA to be associated with kidney injury. This library can be used for studying molecular mechanisms of nephrotoxicity or developing novel biomarkers.
|
|
83
|
| HY-L249 | Lactylation Compound Library |
Protein lactylation, an emerging post-translational modification identified in recent years, plays a critical role in linking cellular metabolic reprogramming, epigenetic regulation, and signaling networks. Based on a systematic framework encompassing lactate metabolism, lactylation, and downstream signaling pathways, this compound library comprehensively targets multiple regulatory layers, including histone modification enzymes (such as p300 and HDACs), key glycolytic enzymes (such as PKM2, LDHA, and GAPDH), transcriptional regulators (such as STAT3, HMGB1, and p53), as well as central signaling pathway nodes including HIF-1α, NF-κB, and PI3K-AKT-mTOR. This integrated design enables a comprehensive representation of the regulatory roles of lactylation across the “metabolism–epigenetics–signaling” axis.
MCE has assembled a collection of 6,182 known bioactive compounds and potential functional molecules, making this library suitable for a wide range of applications, including high-throughput drug screening, inhibitor identification, and mechanistic studies. It can be used to systematically evaluate the functional roles of lactylation in biological processes such as tumor metabolism, immune regulation, and inflammatory responses, and to efficiently identify small-molecule candidates with regulatory potential, thereby facilitating the development of innovative therapeutics targeting the interplay between metabolism and epigenetic regulation.
|
|
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-L253 | Fungal-Sourced Compound Library |
For thousands of years, natural products have always been an important source for drug discovery. Fungi, due to their unique and diverse secondary metabolic capabilities, have become a valuable resource for natural active molecules. Since the discovery of penicillin, natural products derived from fungi have demonstrated significant application value in areas such as anti-infection, anti-tumor, immune regulation, and metabolic disease research. A large number of clinical drugs, such as antibiotics, immunosuppressants, and lipid-lowering drugs, are derived from fungal metabolites or their structurally optimized derivatives.
MCE fungal-derived compound library contains 91 structurally diverse and bioactive fungal natural products and their derivatives. It can be widely applied in various research fields such as antibacterial, anti-tumor, anti-inflammatory, immune regulation, epigenetics, and cell signaling pathways, providing high-quality tools for natural product drug development and high-throughput screening.
|
|
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-L923 | Ion Channel Lead-like Compound Library |
Ion channels are key proteins on the cell membrane that regulate the flow of ions across membranes. They participate in nearly all physiological processes, including nerve conduction, muscle contraction, heart rhythm, and pain perception. Abnormalities in their function can lead to various serious diseases such as arrhythmia, epilepsy, hypertension, neuropathic pain, and cancer. Therefore, ion channels are highly valuable drug targets—over 15% of approved drugs target ion channels currently, demonstrating their irreplaceable therapeutic value in cardiovascular, neurological, and analgesic fields.
MCE has collected a library of over 5,000 reported ion channel-related bioactive compounds targeting major sites such as Na+ channels, K+ channels, Ca2+ channels, GABA receptors, iGluRs, and others. Using AI models, these compounds are characterized through both 2D representations (molecular fingerprints, pharmacophores) and 3D representations (3D conformation) to screen for a collection of lead-like compounds highly similar to known active molecules. Additionally, an hERG channel prediction algorithm integrating XGB and ISE mapping strategy is employed to assess and exclude potential cardiotoxicity in the library.. This step significantly reduces safety risks in subsequent screenings, particularly for ion channel drug development related to cardiovascular systems (e.g., Nav1.5, Cav1.2), effectively minimizing failures due to hERG inhibition and serving as a valuable tool for ion channel drug screening.
|
|
83
|
| HY-13755 | Sulforaphane |
Sulforaphane is an orally active inducer of the Keap1/Nrf2/ARE pathway. Sulforaphane promotes the transcription of tumor-suppressing proteins and effectively inhibits the activity of HDACs. Through the activation of the Keap1/Nrf2/ARE pathway and further induction of HO-1 expression, Sulforaphane protects the heart. Sulforaphane suppresses high glucose-induced pancreatic cancer through AMPK-dependent signal transmission. Sulforaphane exhibits both anticancer and anti-inflammatory properties.
|
|
79
|
| HY-66005 | Acetaminophen |
Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic agent.. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor. Acetaminophen induces ferroptosis and leads to acute liver injury in mice model.
|
Environmental Pollutants
Histone Acetyltransferase
Ferroptosis
COX
Bacterial
Endogenous Metabolite
Parasite
|
76
|
| HY-15149 | Romidepsin |
Romidepsin (FK 228) is a Histone deacetylase (HDAC) inhibitor with anti-tumor activities. Romidepsin (FK 228) inhibits HDAC1, HDAC2, HDAC4, and HDAC6 with IC50s of 36 nM, 47 nM, 510 nM and 1.4 μM, respectively. Romidepsin (FK 228) is produced by Chromobacterium violaceum, induces cell G2/M phase arrest and apoptosis.
|
|
75
|
| HY-10585A | Valproic acid sodium |
Valproic acid (Sodium Valproate) sodium is an orally active HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium is used in the treatment of epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches.
|
|
70
|
| HY-10585 | Valproic acid |
Valproic acid (VPA) is an orally active HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM. Valproic acid inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid is used in the epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches.
|
Infection
Neurological, Eye or Ear Disease
Metabolic or Endocrine Disease
Respiratory Disease
Small Cell Lung Cancer
|
70
|
| HY-B2227 | Lactic acid |
Lactic acid (DL-Lactic acid) is a hydroxycarboxylic acid receptor 1 (HCAR1) activator and an epigenetic modulator inducing lysine residues lactylation. Lactic acid is a glycolysis end-product, bridging the gap between glycolysis and oxidative phosphorylation. Lactic acid is an oncometabolite and has immune protective role of lactate in anti-tumor immunity. Lactic acid also has antimicrobial activity, which can be used as a food preservative.
|
|
67
|
| HY-17363 | Dimethyl fumarate |
Dimethyl fumarate (DMF) is an orally active and brain-penetrant Nrf2 activator and induces upregulation of antioxidant gene expression. Dimethyl fumarate induces necroptosis in colon cancer cells through GSH depletion/ROS increase/MAPKs activation pathway, and also induces cell autophagy. Dimethyl fumarate can be used for multiple sclerosis research.
|
Neurological, Eye or Ear Disease
Inflammation or Immune System Disease
Colorectal Cancer
Viral Infection
Obesity
Lung Fibrosis
|
65
|
| HY-Y1269C | Ammonium chloride, for cell culture |
Ammonium chloride, for cell culture (Salmiac, for cell culture) is a reagent that can be used in cell culture to provide a source of nitrogen. Ammonium chloride can be used as a heteropolar compound to regulate pH value, which can cause intracellular alkalination and metabolic acidosis, thus affecting the activity of enzymes and affecting the process of biological systems. Ammonium chloride acts as an autophagy inhibitor.Ammonium chloride is also a lysosome inhibitor.
|
|
62
|
| HY-Y1269 | Ammonium chloride, AR, 99.5% |
Ammonium chloride, as a heteropolar compound with pH value regulation, can cause intracellular alkalization and metabolic acidosis thus effecting enzymatic activity and influencing the process of biological system. Ammonium chloride is an autophagy inhibitor. Ammonium chloride is also a lysosome inhibitor.
|
|
62
|
| HY-108841 | Raleukin |
Raleukin (Kineret) is a recombinant, nonglycosylated human interleukin-1 receptor (IL-1R) antagonist. Raleukin significantly reduces neutrophil accumulation in blood vessels and brain infarct volume as well as improves motor coordination performance in ischemic stroke mice model. Anakinra can be used to study chronic inflammatory disorders like rheumatoid arthritis and cardiovascular recurrence post-myocardial infarction.
Species: Human |
|
57
|
| HY-D0711 | Indocyanine green |
Indocyanine green (Foxgreen) is a low toxicic fluorescent agent that has been widely used in medical diagnostics, such as determining cardiac output, hepatic function, and liver blood flow, and for ophthalmic angiography (Ex/Em = 785/813 nm).
|
|
49
|
| HY-112288 | C188-9 |
C188-9 (TTI-101) is a STAT3 inhibitor with a Kd value of 4.7 nM. C188-9 targets the SH2 domain of STAT3, blocks the processes of STAT3 ligand binding, receptor recruitment, homodimerization and phosphorylation, and regulates STAT3-mediated genes associated with tumorigenesis and radioresistance. C188-9 regulates STAT1-mediated genes related to radioresistance and reduces the activation level of STAT1. C188-9 downregulates the expression of DNMT1, enhances DAC-induced demethylation and re-expression of RASSF1A, and simultaneously potentiates the anti-tumor effect of DAC on pancreatic cancer cells. C188-9 inhibits both anchorage-dependent and anchorage-independent growth of cancer cells, induces Apoptosis, blocks the growth of tumor xenografts, and suppresses muscle atrophy. C188-9 maintains muscle mass, increases body weight and improves grip strength in tumor-bearing mice. C188-9 can be used in research related to head and neck squamous cell carcinoma, pancreatic cancer, sepsis-related skeletal muscle wasting, non-small cell lung cancer, acute myeloid leukemia and cancer cachexia.
|
Lung Cancer
Breast Cancer
Prostate Cancer
Liver Cancer
Leukemia/Lymphoma/Myeloma
Pancreatic Cancer
Digestive System Inflammation
Obesity
|
37
|
| HY-111558A | Bobcat339 hydrochloride |
Bobcat339 hydrochloride is a potent and selective cytosine-based inhibitor of TET enzyme, with the IC50s of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 hydrochloride is useful to the field of epigenetics and serves as a starting point for new therapeutics that target DNA methylation and gene transcription.
|
|
29
|
| HY-111558 | Bobcat339 |
Bobcat339 is a potent and selective cytosine-based inhibitor of TET enzyme, with IC50s of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 is useful to the field of epigenetics and serves as a starting point for new therapeutics that target DNA methylation and gene transcription.
|
|
29
|
| HY-B0350A | Sodium butyrate |
Sodium butyrate ((Butanoic acid; Butyric acid) sodium) is an orally active HDAC inhibitor. Sodium butyrate induces hyperacetylation of core histones and affects phosphorylation of H1/H2A, thereby altering chromatin structure and regulating gene expression. Sodium butyrate can be used in research related to various cancers, inflammatory bowel disease, and sickle cell anemia.
|
|
28
|
| HY-135146 | GSK-3484862 |
GSK-3484862 is a highly potent non-covalent inhibitor and demethylating agent of DNMT1. GSK-3484862 induces genome-wide DNA demethylation, including the regulatory elements of DNMT3B and the promoter region of TERT, and significantly inhibits cell viability, growth, proliferation and self-renewal. GSK-3484862 blocks the transformation of young AT2 cells, induces apoptosis, and generates transcriptomic features similar to those of senescent cells. GSK-3484862 is widely used in studies related to lung cancer, oral squamous cell carcinoma and lung adenocarcinoma.
|
|
26
|
| HY-12212 | Omaveloxolone |
|
26
|
|
| HY-15826 | SGC-CBP30 |
SGC-CBP30, a chemical probe, is a potent and highly selective CBP/p300 bromodomain (Kds of 21 nM and 32 nM for CBP and p300, respectively) inhibitor, displaying 40-fold selectivity over the first bromodomain of BRD4 [BRD4(1)] bound. SGC-CBP30 strongly reduces secretion of IL-17A in Th17 cells and has anti-inflammatory effects.
|
|
24
|
| HY-16706 | Remodelin |
Remodelin is an orally active and selective inhibitor of acetyltransferase NAT10. Remodelin inhibits NAT10 activitity and slows DNA replication and suppresses growth of prostate cancer cells. Remodelin inhibits the growth of prostate cancer and hepatocellular carcinoma in xenograft model. Remodelin enhances the healthspan in hutchinson-gilford progeria syndrome (HGPS) mouse model.
|
|
24
|
| 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-13962 | SGI-1027 |
SGI-1027 is a DNA methyltransferase (DNMT) inhibitor, with IC50s of 7.5 μM, 8 μM, and 12.5 μM for DNMT3B, DNMT3A, and DNMT1 with poly(dI-dC) as substrate.
|
Digestive System Disease
Leukemia/Lymphoma/Myeloma
Digestive System Inflammation
Rheumatoid Arthritis
|
20
|
| HY-113466 | 4-Hydroxynonenal |
4-Hydroxynonenal (4-HNE) is an α,β unsaturated hydroxyalkenal and an oxidative/nitrosative stress biomarker. 4-Hydroxynonenal is a substrate and an inhibitor of acetaldehyde dehydrogenase 2 (ALDH2). 4-Hydroxynonenal can modulate a number of signaling processes mainly through forming covalent adducts with nucleophilic functional groups in proteins, nucleic acids, and membrane lipids. 4-Hydroxynonenal plays an important role in cancer through mitochondria.
|
|
18
|
| HY-13642 | RG108 |
RG108 (N-Phthalyl-L-tryptophan) is a non-nucleoside DNA methyltransferases (DNMTs) inhibitor (IC50=115 nM) that blocks the DNMTs active site. RG108 (N-Phthalyl-L-tryptophan) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences.
|
|
15
|
| HY-139664 | GSK-3685032 |
|
15
|
|
| HY-13765 | 6-Thioguanine |
6-Thioguanine (Thioguanine; 2-Amino-6-purinethiol) is an anti-leukemia and immunosuppressant agent, acts as an inhibitor of SARS and MERS coronavirus papain-like proteases (PLpros) and also potently inhibits USP2 activity, with IC50s of 25 μM and 40 μM for Plpros and recombinant human USP2, respectively.
|
Digestive System Disease
Leukemia/Lymphoma/Myeloma
Viral Infection
Digestive System Inflammation
SARS-CoV-2 Infection
Rheumatoid Arthritis
|
14
|
| HY-111784 | Inobrodib |
Inobrodib (CCS1477) is an orally active, potent, and selective inhibitor of the p300/CBP bromodomain. Inobrodib binds to p300 and CBP with Kd values of 1.3 and 1.7 nM, respectively, and with 170/130-fold selectivity compared with BRD4 with a Kd of 222 nM. CCS1477 inhibits cell proliferation in prostate cancer cell lines and decreases androgen receptor (AR)- and C-MYC-regulated gene expression.
|
Leukemia/Lymphoma/Myeloma
Non-Small Cell Lung Cancer
Metastatic Breast Cancer
Metastatic Prostate Cancer
|
13
|
| HY-N2037 | Higenamine |
Higenamine (Norcoclaurine), a β2-AR agonist with antioxidant capability, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries. Higenamine is also a α1-adrenergic receptor antagonist with hypotensive effect. is a selective LSD1 inhibitor (IC50=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine protects myocyte Apoptosis and ischemia/reperfusion (I/R) injury through selective activation of beta2-adrenergic receptor (β2-AR). Higenamine also reduces I/R-induced myocardial infarction in mice. Higenamine can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine can be used to study cancer, inflammation, cardiorenal syndrome and other diseases.
|
Leukemia/Lymphoma/Myeloma
Pancreatic Cancer
Bacterial Infection
Depression
Pain
Digestive System Inflammation
Cardiovascular Disease
Obesity
|
12
|
| HY-N0935 | Ligustrazine hydrochloride |
Ligustrazine hydrochloride (Chuanxiongzine hydrochloride) is an orally active, blood-brain barrier-permeable alkaloid. It can be isolated from Ligusticum striatum DC. Ligustrazine hydrochloride reduces ROS, upregulates the levels of p-Akt/Akt and p-eNOS/eNOS, and decreases ALT and AST. It inhibits glutamate excitotoxicity, calcium overload, oxidative stress, ischemia-reperfusion injury and atherosclerotic plaque progression, enhances synaptic plasticity, and improves neurological function, cerebral infarct volume and brain water content. Ligustrazine hydrochloride possesses anti-inflammatory, antioxidant, lipid-lowering, endothelial protective and hepatoprotective activities. It can be used in studies related to ischemic stroke, cerebral ischemia-reperfusion injury and atherosclerosis.
|
Cerebrovascular Disease
Lipid Metabolism
Ischemia-Reperfusion Injury
Atherosclerosis and Inflammation
|
11
|
| HY-N0264 | Ligustrazine |
Ligustrazine (Chuanxiongzine) is an orally active, blood-brain barrier-permeable alkaloid. It can be isolated from Ligusticum striatum DC. Ligustrazine reduces ROS, upregulates the levels of p-Akt/Akt and p-eNOS/eNOS, and decreases ALT and AST. It inhibits glutamate excitotoxicity, calcium overload, oxidative stress, ischemia-reperfusion injury and atherosclerotic plaque progression, enhances synaptic plasticity, and improves neurological function, cerebral infarct volume and brain water content. Ligustrazine possesses anti-inflammatory, antioxidant, lipid-lowering, endothelial protective and hepatoprotective activities. It can be used in studies related to ischemic stroke, cerebral ischemia-reperfusion injury and atherosclerosis.
|
Cerebrovascular Disease
Lipid Metabolism
Ischemia-Reperfusion Injury
Atherosclerosis and Inflammation
|
11
|
| HY-134901 | WM-3835 |
WM-3835 is a potent and high-specific HBO1 (KAT7 or MYST2) inhibitor and binds directly to the acetyl-CoA binding site of HBO1. WM-3835 activates apoptosis while inhibits osteosarcoma (OS) cell proliferation, migration and invasion. WM-3835 has antitumor activity and potently inhibits pOS-1 xenograft growth in mice.
|
|
11
|
| HY-W396714 | Succinic acid sodium |
Succinic acid sodium is a potent and orally active anxiolytic agent. Succinic acid sodium shows inhibitory effects on colonic epithelial cell proliferation in vivo. Succinic acid sodium can down-regulate the expression of KCNMB1 (potassium channel subunit β1) and TET1 (ten?eleven translocation 1). Succinic acid sodium can be used for gestational hypertension research.
|
|
7
|
| HY-N0739 | Betaine chloride |
Betaine chloride is a natural compound found in many foods and also an active methyl-donor which can maintain normal DNA methylation patterns.
|
|
7
|
| HY-W011540 | 8-Hydroxy-2'-deoxyguanosine |
8-Hydroxy-2'-deoxyguanosine is a critical biomarker of oxidative stress and carcinogenesis.
|
|
7
|
| HY-B0710 | Betaine |
Betaine (Trimethylglycine) is a natural compound found in many foods and also an active methyl-donor which can maintain normal DNA methylation patterns. Betaine is found ubiquitously in plants, animals, microorganisms, and rich dietary sources including seafood, spinach, and wheat bran. Betaine also acts as an osmolyte, to maintain the avian’s cellular water and ion balance to improve the avian’s capacity against heat stress via preventing dehydration and osmotic inactivation. It helps in maintaining the protective osmolytic activity, especially in heat-stressed birds. Betaine may promote various intestinal microbes against osmotic variations and thus improve microbial fermentation activity.
Source: Widespread |
|
7
|
| HY-D0098 | Fluorescein-5-maleimide |
Fluorescein-5-maleimide (N-(5-Fluoresceinyl)maleimide) is a fluorescent dye. Fluorescein-5-maleimide can be used to detect the redox state of thiols in eukaryotic cells. Fluorescein-5-maleimide can label peptides and is used to detect negatively charged nanoparticles. Fluorescein-5-maleimide can also label actin to explore its interaction with cardiac myosin-binding protein C (cMyBP-C), which helps in developing small molecule modulators for heart failure. Fluorescein-5-maleimide can screen mutant proteins that contain cysteine residues. The excitation wavelength of Fluorescein-5-maleimide is 494 nm, and the emission wavelength is 519 nm.
|
|
5
|
| HY-132283 | PF-9363 |
PF-9363 (CTx-648) is a first-in-class potent and high selective KAT6A/KAT6B inhibitor. PF-9363 can be used for the research of cancer.
|
|
5
|
| HY-101410A | SDMA (p-hydroxyazobenzene-p′-sulfonate) |
SDMA p-hydroxyazobenzene-p′-sulfonate is the p-hydroxyazobenzene-p′-sulfonate salt form of SDMA (HY-101410). SDMA p-hydroxyazobenzene-p′-sulfonate is an endogenous inhibitor of nitric oxide synthase (NO synthase) activity. SDMA p-hydroxyazobenzene-p′-sulfonate is an activator for NF-κB, and promotes the expression of IL-6 and TNF-α. SDMA p-hydroxyazobenzene-p′-sulfonate is stable in serum and plasma, and can be used as a kidney biomarker of hepatic and renal dysfunction.
|
|
4
|
| HY-106262 | Delcasertib |
Delcasertib (KAI-9803) is a potent and selective δ-protein kinase C (δPKC) inhibitor. Delcasertib (KAI-9803) could ameliorate injury associated with ischemia and reperfusion in animal models of acute myocardial infarction (MI).
|
|
4
|
| HY-N1910 | 4'-O-Methylbavachalcone |
4'-O-Methylbavachalcone is an orally active prenylated flavonoid that inhibits the activity of SARS-CoV papain-like protease (PLpro), with an IC50 of 10.1 μM and a Ki of 4.6 μM. 4'-O-Methylbavachalcone inhibits poly (ADP-ribose) polymerase-mediated cell death (parthanatos), reduces cerebral infarct volume, binds to the orthosteric site of SUCNR1, blocks the interaction between succinate and SUCNR1, inhibits SUCNR1 activity, blocks the nuclear translocation of NFATc4, suppresses the activation of the ERK1/2 signaling pathway, inhibits cardiomyocyte hypertrophy and restores the expression of α-actinin. 4'-O-Methylbavachalcone can be used in studies related to ischemic stroke, SARS-CoV and cardiomyocyte hypertrophy.
|
|
4
|
| HY-106262B | Delcasertib hydrochloride |
Delcasertib (KAI-9803) hydrochloride is a potent and selective δ-protein kinase C (δPKC) inhibitor. Delcasertib (KAI-9803) hydrochloride could ameliorate injury associated with ischemia and reperfusion in animal models of acute myocardial infarction (MI).
|
|
4
|
| HY-W008253 | 5-Hydroxyindole-3-acetic acid |
5-Hydroxyindole-3-acetic acid is the main metabolite of serotonin or metanephrines, which can be used as a biomarker of neuroendocrine tumors.
|
|
4
|
| HY-76082A | L-Pyroglutamic acid sodium |
L-Pyroglutamic acid sodium is the levo-isomer of Pyroglutamic acid. L-Pyroglutamic acid sodium is the biologically active enantiomer in humans. Pyroglutamic acid is an intermediate in glutathione metabolism. L-Pyroglutamic acid sodium can be used as a biomarker for systemic lupus erythematosus (SLE).
|
|
3
|
| HY-N0385 | Gomisin J |
Gomisin J is a Schisandra chinensis-derived lignan that can inhibit multiple targets such as eNOS, AMPK (LKB1, CaMKIIβ), fetuin-A, NF-κB, Nrf2/HO-1, and can pass through the blood-brain barrier. Gomisin J increases NO bioavailability by activating eNOS, regulates lipid metabolism by activating the AMPK pathway, inhibits fetuin-A and NF-κB to exert anti-inflammatory effects, and activates Nrf2/HO-1 to enhance antioxidant capacity. Gomisin J has the activities of anti-hypertension, regulating liver lipid metabolism, and reducing cerebral ischemia-reperfusion injury, and can be used for research on hypertension, non-alcoholic fatty liver disease, cerebral ischemia-reperfusion injury, etc.
|
Breast Cancer
Prostate Cancer
Liver Cancer
Leukemia/Lymphoma/Myeloma
Pancreatic Cancer
Ovarian Cancer
Depression
Pain
Ischemia-Reperfusion Injury
Nonalcoholic Steatohepatitis
Hypertension
Obesity
Lung Fibrosis
|
3
|
| HY-112175 | N-Acetylhistamine |
N-Acetylhistamine is a histamine metabolite. N-acetylhistamine can be used as a potential biomarker of histidine metabolism for anaphylactoid reactions.
|
|
3
|
| HY-W017386 | 3-Methyl-2-oxovaleric acid sodium |
3-Methyl-2-oxovaleric acid sodium is a degradation product from Isoleucine. 3-Methyl-2-oxovaleric acid sodium is a biomarker of mustard airway diseases (MADs) and uric acid stone.
|
|
3
|
| HY-W012078 | 5-Methyl-2'-deoxycytidine |
5-Methyl-2'-deoxycytidine (5mdC) is an endogenous substrate of DNA methyltransferases (such as mammalian 5-C-MTase) and binds to DNA dependent on the formation of DNA stem-loop structures. 5-Methyl-2'-deoxycytidine guides de novo DNA methylation by acting as a methylation mark and activates the methylation of adjacent CpG sites in single-stranded DNA through cis action. 5-Methyl-2'-deoxycytidine regulates DNA methylation patterns by recruiting methyltransferases to specific chromatin regions, affecting chromatin condensation and gene expression. Its distribution in plant cells is related to cell proliferation and differentiation stages. The methylation level of 5-Methyl-2'-deoxycytidine is low in proliferating cells and high in differentiated cells.
|
|
3
|
| HY-I0626 | Cytosine |
|
3
|
|
| HY-P4911 | SDF-1α (human) |
SDF-1α (human) is a mononuclear cells chemoattractant that can bind to CXCR4. SDF-1α plays a central role in stem cell homing, retention, survival, proliferation, cardiomyocyte repair, angiogenesis and ventricular remodelling following myocardial infarction. SDF-1α (human) can be used in cardiovascular disease research.
|
|
2
|
| HY-W008091R | 5-Methylcytosine (Standard) |
5-Methylcytosine (Standard) is the analytical standard of 5-Methylcytosine (HY-W008091). This product is intended for research and analytical applications. 5-Methylcytosine is a well-characterized DNA modification in prokaryotes and eukaryotes. 5-Methylcytosine forms symmetrical methylation on CpG dinucleotides in DNA, stabilizes tRNA/rRNA structure in RNA, and affects mRNA translation. 5-Methylcytosine can be oxidized to generate 5hmC, 5fC, and 5caC. 5-Methylcytosine can be used in epigenetics, developmental biology, and the study of diseases such as colorectal cancer and hepatocellular carcinoma.
|
|
2
|
| HY-P4911A | SDF-1α (human) TFA |
SDF-1α (human) TFA is a mononuclear cells chemoattractant that can bind to CXCR4. SDF-1α plays a central role in stem cell homing, retention, survival, proliferation, cardiomyocyte repair, angiogenesis and ventricular remodelling following myocardial infarction. SDF-1α (human) TFA can be used in cardiovascular disease research.
|
|
2
|
| HY-113447 | 11-Dehydrocorticosterone |
11-Dehydrocorticosterone is a endogenous corticosteroid. 11-Dehydrocorticosterone can be a source of transcriptionally active glucocorticoid in cardiac myocytes and fibroblasts. 11-Dehydrocorticosterone can increase SGK mRNA expression in cardiac fibroblast.
|
|
2
|
| HY-N0745 | Senkyunolide I |
Senkyunolide I is an orally active, blood-brain barrier-permeable metabolite of Z-ligustilide (HY-N0401A). Senkyunolide I is isolated from Ligusticum chuanxiong. Senkyunolide I upregulates p-Erk1/2 and Nrf2/HO-1, and inhibits Caspase 3. Senkyunolide I alleviates Apoptosis. Senkyunolide I increases the pain threshold in mice and reduces acetic acid-induced writhing responses in mice. Senkyunolide I improves neurological deficits, reduces infarct volume and alleviates cerebral edema in rats with focal cerebral ischemia-reperfusion injury. Senkyunolide I protects renal function and structural integrity in a mouse model of renal ischemia-reperfusion injury. Senkyunolide I is applicable to research related to focal cerebral ischemia-reperfusion injury, migraine, and renal ischemia-reperfusion injury.
|
|
2
|
| HY-114252 | Strophanthidin |
Strophanthidin is a naturally available cardiac glycoside. Strophanthidin 0.1 and 1 nmol/L increases and 1~100 μmol/L inhibits the Na+/K+-ATPase activities, but Strophanthidin 10 and 100 nmol/L does not affect Na+/K+-ATPase activities in cardiac sarcolemmal. Strophanthidin increases both diastolic and systolic intracellular Ca2+ concentration.
|
|
2
|
| HY-W008091 | 5-Methylcytosine |
5-Methylcytosine is a well-characterized DNA modification in prokaryotes and eukaryotes. 5-Methylcytosine forms symmetrical methylation on CpG dinucleotides in DNA, stabilizes tRNA/rRNA structure in RNA, and affects mRNA translation. 5-Methylcytosine can be oxidized to generate 5hmC, 5fC, and 5caC. 5-Methylcytosine can be used in epigenetics, developmental biology, and the study of diseases such as colorectal cancer and hepatocellular carcinoma.
Source: prokaryotes and eukaryotes |
|
2
|
| HY-P4094 | CTP |
CTP (cardiac targeting peptide) can transduce cardiomyocytes in vitro. CTP leads to efficient and specific transduction of heart tissue in mice model. CTP can be reversibly linked (e.g. via enolases, thiol groups) to cargo (e.g. miRNAs) for delivery specifically to cardiomyocytes over all other organs.
|
|
2
|
| HY-158301 | MY-1B |
MY-1B is a covalent inhibitor of the RNA Methyltransferase NSUN2 (IC50: 1.3 μM). MY-1B stereoselectively ligands active-site cysteine residues (C271) of NSUN2. MY-1B can stereoselectively and covalently bind to PSME1, disrupting the proteasome regulatory complex and downregulating the presentation of specific MHC-I subtypes.
|
|
2
|
| HY-13315S | Montelukast-d6 |
Montelukast-d6 is the deuterium labeled Montelukast (sodium). Montelukast sodium is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (Cysltr1). Montelukast sodium can be used for the reseach of asthma and liver injury. Montelukast sodium also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage.
|
|
1
|
| HY-106150 | Eniporide |
Eniporide (EMD 96785) is a Na(+)/H(+) exchange (NHE) inhibitor. Eniporide specifically inhibits the NHE-1 isoform. Eniporide improves cardiac performance inhibition associated with myocardial ischemia/reperfusion in animals, and limits infarct size in experimental models. Eniporide regulates cardiac performance and high-energy phosphate content in clinically relevant pig models of CPB and cardiac arrest.
|
|
1
|
| HY-13315S1 | Montelukast-d6 sodium |
Montelukast-d6 (sodium) is the deuterium labeled Montelukast (sodium). Montelukast sodium is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (Cysltr1). Montelukast sodium can be used for the reseach of asthma and liver injury. Montelukast sodium also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage.
|
|
1
|
| HY-P2196 | ELA-32(human) |
ELA-32 (human) is a potent critical cardiac developmental peptide that acts through the G-protein–coupled apelin receptor.
|
|
1
|
| HY-120395 | UC-514321 |
UC-514321, a structural analog of NSC370284 with higher activity, directly targets STAT3/5 and represses TET1 expression, but not TET2 or TET3. UC-514321 has the potential to treat acute myeloid leukemia (AML) both in vitro and in vivo, with low toxicity.
|
Lung Cancer
Breast Cancer
Prostate Cancer
Liver Cancer
Leukemia/Lymphoma/Myeloma
Pancreatic Cancer
Digestive System Inflammation
Obesity
|
1
|
| HY-P99891 | Rovelizumab |
Rovelizumab is a humanized monoclonal leukointegrin antibody. Rovelizumab is a monoclonal antibody directed against the CD11/CD18 cell adhesion proteins. Rovelizumab can be used for research of multiple sclerosis (MS), hemorrhagic shock, myocardial infarction (MI) and stroke.
Species: Human |
|
1
|
| HY-13912G | IWP-2 (GMP) |
IWP-2 (GMP) is >IWP-2 (HY-13912) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. IWP-2 is an inhibitor of Wnt processing and secretion with an IC50 of 27 nM. IWP-2 targets the membrane-bound O-acyltransferase porcupine (Porcn) and blocks Wnt ligand palmitoylation.
|
|
1
|
| HY-P99121 | Anti-Mouse/Human CD11b Antibody (M1/70) |
Anti-Mouse/Human CD11b Antibody (M1/70) is an anti-mouse CD11b IgG2b monoclonal antibody. Anti-Mouse/Human CD11b Antibody (M1/70) can significantly inhibit the adhesion between dendritic cells (DCs) and platelets. Anti-Mouse/Human CD11b Antibody (M1/70) can kill ovarian cancer cells and inhibit their migration. Anti-Mouse/Human CD11b Antibody (M1/70) can alleviate renal fibrosis and inflammation. Anti-Mouse/Human CD11b Antibody (M1/70) can be used for researches on inflammation conditions and cancer such as ischemia-reperfusion injury (IRI), thrombotic inflammatory conditions and ovarian cancer.
Species: Mouse |
|
1
|
| HY-160638 | NSC-311068 |
|
1
|
|
| HY-P990209 | Anti-Mouse IL-7Rα/CD127 Antibody (A7R34) |
Anti-Mouse IL-7Rα/CD127 Antibody (A7R34) is a rat-derived IgG2a κ type antibody inhibitor, targeting to mouse IL-7Rα/CD127. Anti-Mouse IL-7Rα/CD127 Antibody (A7R34) blocks IL-7 signaling. Anti-Mouse IL-7Rα/CD127 Antibody (A7R34) can be used for the researches of cancer,infection, inflammation, immunology, cardiovascular and metabolic disease, such as abdominal aortic aneurysms, helicobacter felis-induced gastritis and diabetes.
Species: Mouse |
Cancer
Infection
Inflammation or Immune System Disease
Blood or Cardio-cerebrovascular Disease
Metabolic or Endocrine Disease
|
1
|
| HY-143711S | Trimethyllysine-d9 |
Trimethyllysine-d9 is the deuterium labeled Trimethyllysine (HY-143711). Trimethyllysine is an important post-translationally modified amino acid, involving in carnitine biosynthesis and epigenetic processes.
|
|
1
|
| HY-15108G | Purmorphamine (GMP) |
Purmorphamine (GMP) is Purmorphamine (HY-15108) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Purmorphamine is a smoothened/Smo receptor agonist with an EC50 of 1 μM.
|
|
1
|
| HY-N4252 | Periplocymarin |
Periplocymarin, a cardiac glycoside isolated from Periploca sepium and Periploca graeca, is a potential anti-cancer compound.
|
|
1
|
| HY-P1108 | Astressin 2B |
Astressin 2B is a blood-brain barrier-impermeable, highly selective CRFR2 antagonist (rCRFR2, IC50=0.57 nM). Astressin 2B blocks the protective effects mediated by CRFR2, thereby exacerbating indomethacin (HY-14397)-induced hemorrhagic intestinal injury in rats. Astressin 2B reverses the protective effects of Urocortin 1 against intestinal hypermotility, bacterial invasion and upregulation of inflammatory mediators. Astressin 2B also blocks the anxiogenic effect of Urocortin 2 and attenuates stress-induced anxiety-related behaviors. In the Clostridioides difficile toxin A (C. difficile toxin A)-mediated enteritis model, Astressin 2B mimics the phenotype of CRFR2-deficient mice, significantly exacerbating intestinal epithelial damage, edema, neutrophil migration and the expression of multiple proinflammatory cytokines. Astressin 2B is an important tool molecule for investigating the intestinal protective mechanisms of CRFR2.
|
|
1
|
| HY-A0248A | Polymyxin B1 |
Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment.
Source: Bacilus polymyxa |
|
1
|
| HY-W329357 | 15:0 Lyso PC |
15:0 Lyso PC is a lysophosphatidylcholine (Lyso PC), a product of phospholipase A2 (PLA2) hydrolysis of phosphatidylcholine (PC) and is involved in cell membrane remodeling and inflammatory signaling. 15:0 Lyso PC demonstrates significant lipid metabolism disturbances in the serum with ischemic heart disease (IHD) and ischemic cardiomyopathy (ICM). 15:0 Lyso PC can be used as a lipid biomarker for cardiovascular disease.
|
|
1
|
| HY-122258 | NSC-370284 |
Lung Cancer
Breast Cancer
Prostate Cancer
Liver Cancer
Leukemia/Lymphoma/Myeloma
Pancreatic Cancer
Obesity
|
1
|
|
| HY-P1108A | Astressin 2B TFA |
Astressin 2B TFA is a blood-brain barrier-impermeable, highly selective CRFR2 antagonist (rCRFR2, IC50=0.57 nM). Astressin 2B TFA blocks the protective effects mediated by CRFR2, thereby exacerbating indomethacin (HY-14397)-induced hemorrhagic intestinal injury in rats. Astressin 2B TFA reverses the protective effects of Urocortin 1 against intestinal hypermotility, bacterial invasion and upregulation of inflammatory mediators. Astressin 2B TFA also blocks the anxiogenic effect of Urocortin 2 and attenuates stress-induced anxiety-related behaviors. In the Clostridioides difficile toxin A (C. difficile toxin A)-mediated enteritis model, Astressin 2B TFA mimics the phenotype of CRFR2-deficient mice, significantly exacerbating intestinal epithelial damage, edema, neutrophil migration and the expression of multiple proinflammatory cytokines. Astressin 2B TFA is an important tool molecule for investigating the intestinal protective mechanisms of CRFR2.
|
|
1
|
| HY-W018499 | (S)-2-Hydroxybutanoic acid |
(S)-2-Hydroxybutanoic acid is the S-enantiomer of 2-Hydroxybutanoic acid. 2-Hydroxybutanoic acid, a coproduct of protein metabolism, is an insulin resistance (IR) biomarker.
|
|
1
|
| HY-12303 | OAC1 |
OAC1 is a potent Oct4 activator. OAC1 activates Oct4 and Nanog promoters and enhances induced pluripotent stem cells (iPSC) formation. OAC1 activates OCT4 through upregulation of HOXB4 expression. OAC1 increases transcription of the Oct4-Nanog-Sox2 triad and TET1. OAC1 facilitates the reprogramming of cells by enhancing efficiency and shortening the reprogramming time.
|
|
1
|
| HY-108750 | Soybean oil |
Soybean oil (VT 18 (oil); Vegetoil; Wesson) is an edible vegetable oil. Soybean oil reduces circulating blood cholesterol levels when it replaces dietary saturated fats. Soybean oil does not affect inflammatory biomarkers or increase oxidative stress. Soybean oil contains γ-tocopherol and δ-tocopherol, which possess antioxidant properties. Soybean oil can be used in research related to coronary heart disease.
|
|
1
|
| HY-113202 | Stearoylcarnitine |
Stearoylcarnitine, a fatty ester lipid molecule, is an endogenous metabolite. Stearoylcarnitine can be used as PKC inhibitor. Stearoylcarnitine accumulates in β cells, leading to arrest of insulin synthesis and energy deficiency in type 2 diabetes mouse. Stearoylcarnitine inhibits lecithin cholesterol acyltransferase (LCAT) in rat and rabbits plasma. Stearoylcarnitine acts as a metabolomics biomarker for Parkinson’s disease. Stearoylcarnitine is a less potent inhibitor of GlyT2.
|
|
1
|
| HY-W250116 | Co(III) protoporphyrin IX chloride |
Co(III) protoporphyrin IX chloride (Protoporphyrin IX cobaltic chloride) is an inducer of HO-1. Co(III) protoporphyrin IX chloride has activities such as anti-inflammation and antibacterial properties. Co(III) protoporphyrin IX chloride can also be used in the research of ischemia-reperfusion injury models.
|
|
1
|
| HY-W015061 | Phenylacetylglycine |
Phenylacetylglycine is a gut microbial metabolite that can activate β2AR. Phenylacetylglycine protects against cardiac injury caused by ischemia/reperfusion.
|
|
1
|
| HY-402410 | TETi76 |
TETi76 is an orally active TET family inhibitor with IC50 values ??of 1.5, 9.4 and 8.8 μM for TET1, TET2 and TET3, respectively. TETi76 competitively binds to the active site of TET enzymes, reduces cytosine hydroxymethylation and restricts clonal growth of TET2 mutants in vitro and in vivo, but does not affect the growth of normal hematopoietic precursor cells. TETi76 can be used for leukemia research.
|
|
1
|
| HY-134124 | Glutathione ethyl ester |
Glutathione ethyl ester is a cell-permeable GSH donor and provides an efficient supply of GSH to the oocyte. Glutathione ethyl ester shows positive effect on the in vitro production of embryos by enhancement of the antioxidative defense.
|
|
1
|
| HY-P990006 | Duvakitug |
Duvakitug (TEV-48574) is a humanized IgG1-λ2 monoclonal antibody targeting to TNFSF15/TL1A. Duvakitug' main expression system is CHOK1SV cells endogenously expressing glutamine synthetase (GS). Duvakitug can be used in the study of Crohn's Disease (CD).
Species: Human |
|
1
|
| HY-P2473 | Neurogranin (48-76), human |
Neurogranin (48-76), human is a dominant endogenous peptide in Alzheimer's disease (AD) brain tissue. Neurogranin (48-76) is a potential biomarker for synaptic function in AD.
|
|
/
|
| HY-D1317A | Cyanine7.5 carboxylic |
Cyanine7.5 carboxylic is a dye derivative of Cyanine 7.5 (Cy7.5) (HY-D0926) with carboxylic acid functional groups. Cy7.5 is a near-infrared fluorescent dye commonly used in biomedical research areas such as biomarkers and cell imaging. Cyanine7.5 carboxylic can be covalently bound to some biological molecules (especially antibodies, proteins, etc.) to track their location and dynamic changes in biological samples.
|
|
/
|
| HY-P5007 | Copeptin (human) |
Copeptin (human) is a peptide biochemical reagent corresponding to the 39 amino acid sequence at the C-terminus of human pre-provasopressin, which serves as a stable surrogate biomarker reflecting the secretion of arginine vasopressin (AVP). Copeptin (human) can be used in studies related to AVP secretion, fluid and osmotic homeostasis, stress responses, and cardiovascular biomarkers.
|
|
/
|
| HY-113266S | Valerylcarnitine-d9 |
Valerylcarnitine-d9 (C5:0 L-carnitine-d9) is the deuterium labeled Valerylcarnitine (HY-113266). Valerylcarnitine is an endogenous metabolite, belonging to the short-chain acylcarnitines. Valerylcarnitine acts as a metabolomic biomarker for ionizing radiation exposure in nonhuman primates. Valerylcarnitine can be used for the research of type 1 diabetes.
|
|
/
|
| HY-N16650 | Bisadinrone A |
Bisadinrone A is a sesquiterpene found in Curcuma longa. Bisadinrone A can inhibit LDH release and shows significant anti-myocardial ischemia-reperfusion injury activity. Bisadinrone A can be used for the research of cardiovascular disease, such as ischemic heart disease.
|
|
/
|
| HY-D3002 | ONOO-/O2- tracker probe |
ONOO-/O2- tracker probe is a dual-responsive near-infrared fluorescent probe. ONOO-/O2- tracker probe will only emit a strong fluorescence signal when both peroxynitrite (ONOO⁻) and superoxide anion (O₂•⁻), the two key reactive oxygen/nitrogen species, are present simultaneously. ONOO-/O2- tracker probe can be used as a biomarker detection tool for drug-induced liver injury (DILI).
|
|
/
|
| HY-D3000 | NIR-RED ROS-H2O2 Probe |
NIR-RED ROS-H2O2 Probe is a near-infrared fluorescent probe used for detecting hydrogen peroxide (H₂O₂) and featuring dual-modal fluorescence/photoacoustic imaging capabilities. NIR-RED ROS-H2O2 Probe successfully detects the upregulated fluorescence signal of H₂O₂ in HepG2 cells and a mouse liver injury model. NIR-RED ROS-H2O2 Probe can be used as a biomarker detection tool for drug-induced liver injury (DILI).
|
|
/
|
| HY-158498 | FA2 glycan (G0F) |
FA2 glycan (G0F) (FA2 N-linked oligosaccharide; F(6)A2 glycan) is a core-fucosylated biantennary N-linked oligosaccharide that serves as a prostate cancer biomarker. The level of FA2 glycan (G0F) is higher in prostate cancer than in benign prostatic hyperplasia, and it is further elevated in advanced prostate cancer with a Gleason score ≥8 compared with both benign prostatic hyperplasia and low-/intermediate-risk prostate cancer. FA2 glycan (G0F) can be used in prostate cancer research.
|
|
/
|
| HY-P5044 | α-Synuclein (45-54) (human) |
α-Synuclein (45-54) (human) is the 45-54 fragment of α-Synuclein. α-Synuclein is an abundant neuronal protein that is highly abundant in presynaptic nerve terminals. α-Synuclein is a biomarker for Parkinson's disease (PD).
|
|
/
|
| HY-P990194 | Anti-Mouse MHC Class I (H-2Kd) Antibody (HB-159) |
Anti-Mouse MHC Class I (H-2Kd) Antibody (HB-159) is a mouse-derived IgG2a κ type antibody inhibitor, targeting to mouse MHC Class I. Anti-Mouse MHC Class I (H-2Kd) Antibody (HB-159) reacts with the mouse H-2Kd MHC class I alloantigen. Anti-Mouse MHC Class I (H-2Kd) Antibody (HB-159) can be used for immunology research, such as cardiac graft.
Species: Mouse |
|
/
|
| HY-P1556 | Vasonatrin Peptide (VNP) |
Vasonatrin Peptide (VNP) is a chimera of atrial natriuretic peptide (ANP) and C-type natriuretic peptide (CNP). Vasonatrin peptide possesses the venodilating actions of CNP, the natriuretic actions of ANP, and unique arterial vasodilating actions not associated with either ANP or CNP. Vasonatrin Peptide protects the diabetic heart against ischemia-reperfusion injury by inhibiting ER stress via the cGMP-PKG signaling pathway.
|
|
/
|
| HY-B0932S1 | Levocarnitine propionate-d5 hydrochloride |
Levocarnitine propionate-d5 (hydrochloride) is the deuterium labeled Levocarnitine propionate hydrochloride. Levocarnitine propionate hydrochloride (L-Propionylcarnitine chloride; ST-261) is a ligand of carnitine acetyltransferase (CAT) with high enzyme affinity. Levocarnitine propionate hydrochloride possesses antioxidant activity. Levocarnitine propionate hydrochloride increases intracellular L-carnitine reserves. Levocarnitine propionate hydrochloride exerts a protective effect against myocardial ischemia-reperfusion injury. Levocarnitine propionate hydrochloride can be used in research related to myocardial ischemia-reperfusion injury and chronic ischemic heart disease.
|
|
/
|
| HY-P11739 | ZD2 peptide |
ZD2 peptide is an EDB-FN-binding peptide with a Kd value of 11 μM. ZD2 peptide binds specifically to the EDB protein fragment of extradomain B fibronectin, a tumor microenvironment biomarker. ZD2 peptide can be conjugated to imaging agents. ZD2 peptide can be used for the research of cancer.
|
|
/
|
| HY-114346A | BODIPY FL EDA free base |
ODIPY FL EDA free base is an amine-based, green fluorescent probe. The R-NH2 of ODIPY FL EDA free base can be coupled with aldehydes or ketones to form reversible Schiff base products. Convert to stable amine derivatives using reducing agents such as sodium borohydride or sodium cyanoborohydride. ODIPY FL EDA free base can be used to detect modified or normal deoxynucleotides and demonstrate DNA damage and genomic DNA methylation.
|
|
/
|
| HY-P4898 | Anthopleurin-A |
Anthopleurin-A is a soidum channel toxin. Anthopleurin-A is selective for cardiac channels and has cardiotonic effect. Anthopleurin-A can be isolated from the sea anemone.
|
|
/
|
| HY-P10821 | Myr-Tat-PKCβII |
Myr-Tat-PKCβII is a cell permeable protein kinase C β II peptide inhibitor. Myr-Tat-PKCβII mitigates the generation of reactive oxygen species in rat ex-vivo and porcine in-vivo ischemia-reperfusion injury.
|
|
/
|
| HY-P5046 | α-Synuclein (71-82) (human) |
α-Synuclein (71-82) (human) is the 71-82 fragment of α-Synuclein. α-Synuclein is an abundant neuronal protein that is highly abundant in presynaptic nerve terminals. α-Synuclein is a biomarker for Parkinson's disease (PD).
|
|
/
|
| HY-135146G | GSK-3484862 (GMP) |
GSK-3484862 GMP is GSK-3484862 (HY-135146) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. GSK-3484862 is a highly potent non-covalent inhibitor and demethylating agent of DNMT1. GSK-3484862 induces genome-wide DNA demethylation, including the regulatory elements of DNMT3B and the promoter region of TERT, and significantly inhibits cell viability, growth, proliferation and self-renewal. GSK-3484862 blocks the transformation of young AT2 cells, induces apoptosis, and generates transcriptomic features similar to those of senescent cells. GSK-3484862 is widely used in studies related to lung cancer, oral squamous cell carcinoma and lung adenocarcinoma.
|
|
/
|
| HY-P991921 | TNX-1500 |
TNX-1500 is a crystallizable fragment-modified anti-CD154 antibody. TNX-1500 contains the hu5c8 fragment antigen-binding (Fab) domain from Ruplizumab (HY-P99315) and an IgG4 Fc region engineered to reduce FcγRIIa binding. TNX-1500 has significantly weaker binding affinity to FcγRI, FcγRIIaH, FcγRIIbF, FcγRIIIaF, and FcγRIIIaV compared to hu5c8 (Kd values: 8.7 nM, 7100 nM, 4900 nM, 8000 nM, 6000 nM respectively). TNX-1500 prolongs nonhuman primate renal allograft survival, prolongs nonhuman primate cardiac allograft survival. TNX-1500 can be used for the research of allograft rejection[1].
Species: Human |
|
/
|
| HY-B0203BS2 | (Rac)-Nebivolol-d2,15N |
(Rac)-Nebivolol-d2,15N is 15N and deuterated labeled (Rac)-Nebivolol (HY-B0203B). (Rac)-Nebivolol ((Rac)-R 065824) is a racemic isomer of Nebivolol. Nebivolol is a selective β1-adrenergic receptor antagonist with an IC50 value of 0.8 nM. Nebivolol can prevent up-regulation of Nox2/NADPH oxidase and lipoperoxidation in the early stages of ethanol-induced cardiac toxicity. Vasodilatory activity.
|
|
/
|
| HY-P10563 | Noraramtide |
Noraramtide (BHV-1100) is an antibody-recruiting molecule. Noraramtide binds to CD38 and recruits natural killer (NK) cells to mediate antibody-dependent cellular cytotoxicity. Noraramtide enhances the capacity of autologous cytokine-induced memory-like (CIML) NK cells to produce IFNγ and CD107a, thereby improving their cytotoxicity against multiple myeloma cells. Noraramtide can be used in the research of multiple myeloma.
|
|
/
|
| HY-P1306 | Obestatin(rat) |
Obestatin(rat), encoded by the Ghrelin gene, is a cpeptide, comprised of 23 amino acids. Obestatin(rat) suppresses food intake, inhibits jejunal contraction, and decreases body-weight gain. Obestatin is an endogenous ligand of G-protein coupled receptor 39 (GPR39). Obestatin(rat) has anti-inflammatory, anti-myocardial infarction and antioxidant activities.
|
|
/
|
| HY-174935B | DBCO-PEG3400-NHS |
DBCO-PEG3400-NHS is a dibenzocyclooctyne-conjugated polyethylene glycol derivative bearing an NHS group. DBCO-PEG-NHS forms a stable covalent linkage with the amino group of target molecules via the NHS ester at one end, while introducing a DBCO group at the other end, thus preparing for subsequent click chemical conjugation with any azide-bearing molecule or material.
|
|
/
|
| HY-P1219 | Jingzhaotoxin-III |
Jingzhaotoxin-III is a potent and selective blocker of Nav1.5 channels, with an IC50 of 348 nM, and shows no effect on other sodium channel isoforms. Jingzhaotoxin-III can selectively inhibit the activation of cardiac sodium channel but not neuronal subtypes, and hopefully represents an important ligand for discriminating cardiac VGSC subtype.
|
|
/
|
| HY-D1864 | Sulfo-Cy7.5 dicarboxylic acid |
Sulfo-Cy7.5 dicarboxylic acid is a dye derivative of Cyanine 7.5 (Cy7.5) (HY-D0926) with carboxylic acid and sulfonate functional groups. The sulfonate ion increases the water solubility of the compound, making it suitable for use in aqueous solutions. Cy7.5 is a near-infrared fluorescent dye commonly used in biomedical research areas such as biomarkers and cell imaging. Sulfo-Cy7.5 dicarboxylic acid can be covalently bound to some biomolecules (especially antibodies, proteins, etc.) to track their location and dynamic changes in biological samples.
|
|
/
|
| HY-N15743 | Anti-Heart Failure Agent 2 |
Anti-Heart Failure Agent 2 (Compound 1) is an anti-heart failure agent with anti-inflammatory activity found in processed Cornus officinalis. Anti-Heart Failure Agent 2 inhibits NO release in LPS-induced RAW264.7 cells. Anti-Heart Failure Agent 2 alleviates myocardial ischemia-reperfusion injury, reduces myocardial infarction size, and improves myocardial histopathological changes. Anti-Heart Failure Agent 2 is promising for research of heart failure.
|
|
/
|
| HY-W744298 | Trandolapril-d3 |
Trandolapril-d3 is the deuterium labeled Trandolapril (HY-B0592). Trandolapril (RU44570) is a nonsulfhydryl proagent that is hydrolysed to the active diacid Trandolaprilat. Trandolapril is an orally administered angiotensin converting enzyme (ACE) inhibitor that has been used in the treatment of hypertension and congestive heart failure (CHF), and after myocardial infarction (MI).
|
|
/
|
| HY-P992516 | DNL-919 (ATV) |
DNL-919 ATV is a brain-penetrant TREM2 agonist. DNL-919 ATV induces responsive microglial cell state changes and modulates microglial biomarkers. DNL-919 ATV can be used for the research of Alzheimer's disease.
|
|
/
|
| HY-D1866 | Sulfo-Cy7.5 carboxylic acid |
Sulfo-Cy7.5 carboxylic acid is a dye derivative of Cyanine 7.5 (Cy7.5) (HY-D0926) with carboxylic acid and sulfonate ion (sulfonate) functional groups. The sulfonate ion increases the water solubility of the compound, making it suitable for use in aqueous solutions. Cy7.5 is a near-infrared fluorescent dye commonly used in biomedical research areas such as biomarkers and cell imaging. Sulfo-Cy7.5 carboxylic acid can be covalently bound to some biomolecules (especially antibodies, proteins, etc.) to track their location and dynamic changes in biological samples.
|
|
/
|
| HY-17380S | (S)-Timolol-d9 maleate |
(S)-Timolol-d9 (maleate) is deuterium labeled (S)-Timolol (Maleate). (S)-Timolol Maleate (L-714,465 Maleate) is a non-cardioselective hydrophilic β-adrenoceptor blocker. (S)-Timolol Maleate is widely used as standard medication for intraocular pressure (glaucoma) by preventing the production of aqueous humor. (S)-Timolol Maleate can be used for hypertension, angina pectoris and myocardial infarction.
|
|
/
|
| HY-P3054 | S6 peptide |
S6 peptide is a potentially important lamin kinase. S6 peptide is involved in the process of cardiac hypertrophy induced by mechanical loading. S6 peptide can be activated by many kinds of growth factors.
|
|
/
|
| HY-P3631 | SALMF amide 2 |
SALMF amide 2, a neuropeptide S2 from the starfish Asterias rubens, is involved in the regulation of eversion of the cardiac stomach in starfish.
|
|
/
|
| HY-12515AS2 | Nicardipine-d4 hydrochloride |
Nicardipine-d4 hydrochloride is deuterated labeled Nicardipine hydrochloride (HY-12515A). Nicardipine hydrochloride (YC-93) is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine hydrochloride acts as an agent for chronic stable angina and for controlling blood pressure.
|
|
/
|
| HY-N20270 | Trichosanthis fructus extract |
Trichosanthis fructus extract is an extract of Trichosanthis fructus that can be used in research on angina pectoris, heart failure, myocardial infarction, pulmonary heart disease, and cerebral ischemia.
|
|
/
|
| HY-N19029 | Vernodalin |
Vernodalin is an orally active, cytotoxic sesquiterpene lactone with a Kd value of 9.55 μM for p38 MAPK. Vernodalin downregulates the expression of phosphorylated ERK, JNK, AKT, PI3K, mTOR, p38MAPK, FAK, MMP-2, MMP-9, and uPA, while upregulates the expression of TIMP-1 and TIMP-2. Vernodalin increases ROS production, upregulates the expression of Bax and caspase 3, downregulates the expression of Bcl-2, and induces apoptosis (apoptosis), oxidative stress response and cell cycle arrest. Vernodalin inhibits the proliferation, adhesion and metastasis of cancer cells. Vernodalin enhances the activity of VEGF-B, AMPK and eNOS signaling pathways. Vernodalin alleviates myocardial injury and restores hemodynamic parameters. Vernodalin inhibits the growth of Trypanosoma brucei rhodesiense. Vernodalin can be used in research related to various cancers including gastric cancer, colorectal cancer and lung cancer, as well as African human trypanosomiasis and myocardial infarction.
|
p38 MAPK
PERK
JNK
Akt
PI3K
mTOR
FAK
MMP
PAI-1
Reactive Oxygen Species (ROS)
Caspase
Bcl-2 Family
Apoptosis
VEGFR
AMPK
Parasite
|
/
|
| HY-DY1027 | Indocyanine green (solution) |
Indocyanine green (Foxgreen) (solution) is a low toxicic fluorescent agent that has been widely used in medical diagnostics, such as determining cardiac output, hepatic function, and liver blood flow, and for ophthalmic angiography (Ex/Em = 785/813 nm) .
Solvent and concentration: DMSO: 10 mM |
|
/
|
| HY-P99553 | Torapsel |
Torapsel (42-89-glycoprotein; WAY164339) is a fusion protein with immunoglobiln. Torapsel can be used to research the prevention of ischemia reperfusion injury.
Species: Human |
|
/
|
| HY-B1505G | Acefylline (GMP) |
Acefylline (Theophyllineacetic acid) (GMP), a xanthine derivative, is an Adenosine Receptor antagonist. Acefylline (GMP) is a peptidylarginine deiminase (PAD) activator. Acefylline (GMP) is also a bronchodilator and cardiac stimulant that inhibits rat lung cAMP phosphodiesterase isoenzymes. Acefylline (GMP) can be used in asthma research.
|
Neurological, Eye or Ear Disease
Inflammation or Immune System Disease
Blood or Cardio-cerebrovascular Disease
|
/
|
| HY-A0144AR | Etilefrine hydrochloride (Standard) |
Etilefrine hydrochloride (Standard) is the analytical standard of Etilefrine hydrochloride (HY-A0144A). This product is intended for research and analytical applications. Etilefrine hydrochloride is a sympathetic nerve agonist and AMPK activator that selectively targets α1/β1 adrenergic receptors. Etilefrine hydrochloride stimulates α1 adrenergic receptors, leading to contraction of vascular smooth muscle and increased peripheral resistance. Etilefrine hydrochloride also stimulates β1 receptors to enhance myocardial contractility and increase heart rate, thereby increasing blood pressure and improving cardiac output. Etilefrine hydrochloride also bidirectionally regulates the AMPK/Akt pathway and modulates the phosphorylation levels. Etilefrine hydrochloride can be used in cardiovascular research, such as postural hypotension, chylothorax, and improving low cardiac output.
|
|
/
|
| HY-P10828 | MAPI |
|
/
|
|
| HY-N15744 | Anti-Heart Failure Agent 3 |
Anti-Heart Failure Agent 3 (Compound 2) is an anti-heart failure agent with anti-inflammatory activity found in processed Cornus officinalis. Anti-Heart Failure Agent 3 inhibits NO release in LPS-induced RAW264.7 cells. Anti-Heart Failure Agent 3 alleviates myocardial ischemia-reperfusion injury, reduces myocardial infarction size, and improves myocardial histopathological changes. Anti-Heart Failure Agent 3 is promising for research of heart failure.
|
|
/
|
| HY-B0251S | Eplerenone-d3 |
Eplerenone-d3 is the deuterium labeled Eplerenone. Eplerenone (Epoxymexrenone) is a selective, competitive and oreally active aldosterone antagonist with an IC50 of 138 nM. Eplerenone has low affinity for progesterone, androgen, estrogen and glucocorticoid receptors. Eplerenone can be used for hypertension and heart failure after myocardial infarction reserch.
|
|
/
|
| HY-P991572 | MM-151 |
MM-151 is a humanized IgG1 monoclonal antibody targeting EGFR. MM-151 binds multiple regions of the EGFR extracellular domain (ECD) and reduces its mutations in circulating cell-free tumor DNA with EGFR resistance. MM-151 significantly inhibits EGFR signaling and cell growth. MM-151 can be used for drug-resistant cancers research, such as colorectal, non-small cell lung and triple negative breast cancer.
Species: Human |
|
/
|
| HY-P992212 | Anti-CD62L Antibody (DREG-200) |
Anti-CD62L Antibody (DREG-200) is a human monoclonal antibody targeting CD62L/L-selectin. Anti-CD62L Antibody (DREG-200) binds to residues 45, 46 and 47 of L-selectin, and blocks L-selectin-mediated interactions, neutrophil rolling, adhesion, aggregation, secondary anchoring, as well as leukocyte rolling on ligands. Anti-CD62L Antibody (DREG-200) reduces myocardial necrosis, coronary endothelial dysfunction, and neutrophil migration driven by neutrophil microparticles. Anti-CD62L Antibody (DREG-200) exerts cardioprotective effects in feline models. Anti-CD62L Antibody (DREG-200) can be used in studies related to myocardial ischemia-reperfusion injury. The recommended isotype control is Mouse IgG1 kappa (HY-P99977).
Species: Human |
|
/
|
| HY-B0252S3 | Hydrochlorothiazide-15N2,13C,d2 |
Hydrochlorothiazide-15N2,13C,d2 is 15N and deuterated labeled Hydrochlorothiazide (HY-B0252). Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect.
|
|
/
|
| HY-P991895 | PLG-101 |
PLG-101 is a human anti-CD8 antibody. PLG-101 can be used in research on acute myocardial infarction .
Species: Human |
|
/
|
| HY-N15745 | Anti-Heart Failure Agent 4 |
Anti-Heart Failure Agent 4 (Compound 3) is an anti-heart failure agent with anti-inflammatory activity found in processed Cornus officinalis. Anti-Heart Failure Agent 4 inhibits NO release in LPS-induced RAW264.7 cells. Anti-Heart Failure Agent 4 alleviates myocardial ischemia-reperfusion injury, reduces myocardial infarction size, and improves myocardial histopathological changes. Anti-Heart Failure Agent 4 is promising for research of heart failure.
|
|
/
|
| HY-174935C | DBCO-PEG5000-NHS |
DBCO-PEG5000-NHS is a dibenzocyclooctyne-conjugated polyethylene glycol derivative bearing an NHS group. DBCO-PEG-NHS forms a stable covalent linkage with the amino group of target molecules via the NHS ester at one end, while introducing a DBCO group at the other end, thus preparing for subsequent click chemical conjugation with any azide-bearing molecule or material.
|
|
/
|
| HY-13642G | RG108 (GMP) |
RG108 (GMP) is RG108 (HY-13642) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. RG108 (N-Phthalyl-L-tryptophan) is a non-nucleoside DNA methyltransferases (DNMTs) inhibitor (IC50=115 nM) that blocks the DNMTs active site. RG108 (N-Phthalyl-L-tryptophan) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences.
|
|
/
|
| HY-174935D | DBCO-PEG10000-NHS |
DBCO-PEG10000-NHS is a dibenzocyclooctyne-conjugated polyethylene glycol derivative bearing an NHS group. DBCO-PEG-NHS forms a stable covalent linkage with the amino group of target molecules via the NHS ester at one end, while introducing a DBCO group at the other end, thus preparing for subsequent click chemical conjugation with any azide-bearing molecule or material.
|
|
/
|
| HY-16910G | WIKI4 (GMP) |
|
/
|
|
| HY-NP002I | SSA Protein |
SSA Protein (Sheep Serum Albumin) is a plasma protein derived from sheep. Sheep serum albumin is a 583 amino acid residues long multidomain monomeric protein which is rich in cysteine and low in tryptophan content. SSA Protein can be used as a potential biomarker of age-related decline.
|
|
/
|
| HY-136490S1 | Psychosine-d7 |
Psychosine-d7 is deuterium labeled Psychosine. Psychosine, a substrate of the galactocerebrosidase (GALC) enzyme, is a potential biomarker for Krabbe disease. Psychosine is a highly cytotoxic lipid, capable of inducing cell death in a wide variety of cell
|
|
/
|
| HY-P3759 | BNP (22-46), Pro (Human) |
BNP (22-46), Pro (Human) is an peptide . BNP (22-46), Pro (Human) can be used for the research of cardiac dysfunction.
|
|
/
|
| HY-P12125 | TAT-Epsilon-V1-2 TFA |
TAT-Epsilon-V1-2 TFA is a cell-permeable PKCε peptide inhibitor. TAT-Epsilon-V1-2 TFA reduces chronic immune responses after heart transplantation. TAT-Epsilon-V1-2 TFA is applicable to research related to delayed graft function and acute kidney injury caused by renal ischemia-reperfusion injury.
|
|
/
|
| HY-P5142 | ω-Hexatoxin-Hv1a |
ω-Hexatoxin-Hv1a (ω-ACTX-Hv1; ω-Atracotoxin-HV1) is an orally active insecticidal neurotoxin containing an inhibitor cystine knot motif and a selective calcium channel inhibitor. ω-Hexatoxin-Hv1a blocks L-type voltage-dependent Ca2+ channels and reduces intracellular calcium ion concentration, thereby decreasing apoptosis, necroptosis and oxidative stress, and promoting cell recovery and energy level elevation. ω-Hexatoxin-Hv1a causes larval paralysis and death by impairing neurotransmission in the central nervous system of insects. It shows high injectable toxicity against insects of multiple orders, but exhibits weak oral toxicity. ω-Hexatoxin-Hv1a is widely applicable to studies related to ischemia-reperfusion injury, atopic dermatitis, and ischemic injury of cardiomyocytes and neurons.
|
|
/
|
| HY-113352S | 7-Methylguanine-d3 |
7-Methylguanine-d3 is the deuterium labeled 7-Methylguanine. 7-Methylguanine is a metabolite of DNA methylation. It can be generated by methylating agents, and used as a probe of protein–DNA interactions and a key component of DNA sequencing method.
|
|
/
|
| HY-D2999 | NIR-RED ATP Probe |
NIR-RED ATP Probe is a NIR-II fluorescent probe. NIR-RED ATP Probe exhibits high affinity and selectivity for ATP and can non-invasively and with high contrast detect changes in ATP concentration at the cellular level, with minimal interference to the abundant biomolecules within the cells. NIR-RED ATP Probe can be used as a biomarker detection tool for drug-induced liver injury (DILI).
|
|
/
|
| HY-W701252 | Methyl paraben-d3 |
Methyl paraben-d3 (Methyl 4-hydroxybenzoate-d3) is the deuterium labeled Methyl paraben (HY-N0349). Methyl Paraben is a standardized methyl paraben allergen isolated from Yunnan hemlock (Tsuga dumosa). Methyl Paraben is commonly used as a stable, non-volatile preservative. Methyl Paraben increases histamine release and cellular regulation of immunity, blocks sodium channels, and prevents ischemia-reperfusion injury.
|
|
/
|
| HY-P5043 | α-Synuclein (67-78) (human) |
α-Synuclein (67-78) (human) is the 67-78 fragment of α-Synuclein. α-Synuclein (67-78) (human) promotes network activity drive and blocks KCl-induced syt1L-ab uptake.
|
|
/
|
| HY-P992465 | SIWA318H |
SIWA318H is an adbanvced glycation end product (AGE) specific antibody. SIWA318H selectively binds to advanced glycation end product biomarkers, human FcγRIIIa, and pancreatic cancer cells, and cancer-associated fibroblasts. SIWA318H suppresses tumor growth in mouse PSN1 xenografts. SIWA318H can be used for the research of pancreatic cancer.
Species: Human |
|
/
|
| HY-E70188 | N-Acetylgalactosamine-6-Sulfatase |
N-Acetylgalactosamine-6-Sulfatase (GALNS) is a potential general biomarker for multiple malignancies (such as lung cancer, breast cancer, head and neck cancer, etc.). N-Acetylgalactosamine-6-Sulfatase deficiency causes mucopolysaccharidosis type IVA (MPS IVA), also known as Morquio A syndrome. N-Acetylgalactosamine-6-Sulfatase can be used in MPS IVA as well as cancer research.
|
|
/
|
| HY-N21583 | Dracoflavan B2 |
Dracoflavan B2 is an allosteric activator of pyruvate carboxylase (PC) that enhances Oxaloacetic acid (HY-W010382) production by inducing conformational changes in the BCCP domain, restores mitochondrial function, and improves metabolism, while also exhibiting anti-inflammatory activity. Dracoflavan B2 can be used for research on myocardial infarction.
|
|
/
|
| HY-P2632 | RAD16-I |
RAD16-I (RADA16) is a non-directed self-assembling peptide hydrogel. Under physiological conditions, RAD16-I spontaneously forms a three-dimensional nanofiber network that mimics the extracellular matrix, and possesses excellent properties such as high water content, biocompatibility and degradability. RAD16-I serves as an ideal scaffold for three-dimensional cell culture. RAD16-I not only maintains cell viability and induces self-organization, but also supports cell adhesion, proliferation, differentiation and insulin secretion, effectively stabilizes islet clusters and promotes directed differentiation of the cardiac lineage. RAD16-I can construct a cell-friendly nano-microenvironment for research related to diseases such as myocardial infarction and diabetes.
|
|
/
|
| HY-P4654 | H-Tyr-Lys-OH |
H-Tyr-Lys-OH is a dipeptide that can be used as a biomarker for AJH-1. H-Tyr-Lys-OH has a good binding affinity to angiotensin converting enzyme (ACE).
|
|
/
|
| HY-13689G | Go 6983 (GMP) |
Go 6983 GMP is Go 6983 (HY-13689) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Go 6983 is a dual inhibitor targeting Suv39h1/2 (KMT1A/KMT1B) and PKC, as well as a transcriptional activator capable of inducing DNA hypomethylation. Go 6983 stimulates the transcription of Prdm14 by reducing Suv39h1/2 protein levels, decreasing histone modifications in the Prdm14 promoter region, and increasing the recruitment of RNA polymerase II. Go 6983 induces genome-wide DNA hypomethylation by inhibiting de novo methyltransferase expression and increasing Tet1/Tet2 levels, thereby promoting self-renewal and pluripotency maintenance of stem cells. Meanwhile, Go 6983 can block PKC-mediated signaling pathways to reduce the expression of EMT-related genes and eliminate the upregulation of antioxidant genes downstream of NRF2. Go 6983 is mainly used in mechanism studies related to myocardial ischemia/reperfusion injury.
|
|
/
|
| HY-W744986 | L-2-Hydroxyglutaric acid-d5 disodium |
L-2-Hydroxyglutaric acid-d5 disodium ((2S)-2-Hydroxyglutaric acid-d5 disodium) is the deuterium labeled L-2-Hydroxyglutaric acid disodium (HY-W015114). L-2-Hydroxyglutaric acid disodium is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid disodium can inhibit histone demethylases and hence promote histone methylation. L-2-Hydroxyglutaric acid inhibits mitochondrial creatine kinase (Mi-CK) activity with Km and Ki of 2.52 mM and 11.13 mM, respectively.
|
|
/
|
| HY-P991657 | MEDI7814 |
MEDI7814 is a humanized monoclonal antibody inhibitor targeting C5a and C5adesArg. MEDI7814 binds to recombinant human C5a and serum purified human C5a with affinities of 14 pM and 8 pM, respectively. MEDI7814 is acute inflammatory diseases such as sepsis and renal ischemia-reperfusion injury.
Species: Human |
|
/
|
| HY-W738852 | Hydroxylysylpyridinoline-d6 |
Hydroxylysylpyridinoline-d6 is deuterium labeled Pyridinoline. Pyridinoline, a fluorescent material, is a bone resorption biomarker. Pyridinoline also is a type crosslink of collagen.
|
|
/
|
| HY-109037S | Mavacamten-d6 |
Mavacamten-d6 (MYK461-d6; SAR439152-d6) is deuterium labeled Mavacamten (HY-109037). Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
|
|
/
|
| HY-17494S1 | Timolol-d9 maleate |
Timolol-d9 (maleate) is deuterium labeled Timolol. Timolol is a β-blocker available for both topical and systemic administration. Topical Timolol is primarily used to reduce intraocular pressure with open-angle glaucoma and ocular hypertension. Timolol can also be used for the research of infantile hemangiomas, hypertension, myocardial infarction, migraine prophylaxis, and atrial fibrillation.Timolol also has cardioprotective effect.
|
|
/
|
| HY-W653970 | 5-Azacytidine-15N4 |
5-Azacytidine-15N4 is 13C and 15N labeled 5-Azacytidine. 5-Azacytidine (Azacitidine; 5-AzaC; Ladakamycin) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation. 5-Azacytidine is incorporated into DNA to covalently trap DNA methyltransferases and contributes to reverse epigenetic changes. 5-Azacytidine induces cell autophagy.
|
Isotope-Labeled Compounds
Organoid
Bacterial
DNA Methyltransferase
Nucleoside Antimetabolite/Analog
Antibiotic
Autophagy
|
/
|
| HY-P992108 | Efadirelaxin alfa |
Efadirelaxin alfa (RELAX10) is a highly selective agonist of relaxin/insulin-like family peptide receptor RXFP1. After subcutaneous administration in animal experiments, Efadirelaxin alfa exhibits a significantly prolonged terminal half-life (7 days in mice, 3.75 days in rats), and shows no activity against related receptors such as RXFP2 and RXFP3. Efadirelaxin alfa has significant anti-cardiac hypertrophy and anti-fibrotic effects. Efadirelaxin alfa effectively attenuates and reverses cardiac hypertrophy and collagen deposition by regulating the TGF-β1/Smad2 and AKT/eNOS signaling pathways. Efadirelaxin alfa improves cardiac systolic function without causing fluctuations in blood pressure or heart rate, demonstrating favorable safety. Efadirelaxin alfa is currently mainly used in studies related to heart failure.
Species: Human |
|
/
|
| HY-N2037R | Higenamine (Standard) |
Higenamine (Norcoclaurine), a β2-AR agonist with antioxidant capability, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries. Higenamine is also a α1-adrenergic receptor antagonist with hypotensive effect. is a selective LSD1 inhibitor (IC50=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine protects myocyte Apoptosis and ischemia/reperfusion (I/R) injury through selective activation of beta2-adrenergic receptor (β2-AR). Higenamine also reduces I/R-induced myocardial infarction in mice. Higenamine can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine can be used to study cancer, inflammation, cardiorenal syndrome and other diseases.
|
|
/
|
| HY-13599S2 | Cladribine-15N |
Cladribine-15N (2-Chloro-2′-deoxyadenosine-15N) is 15N labeled Cladribine. Cladribine (2-Chloro-2′-deoxyadenosine), a purine nucleoside analog, is an orally active adenosine deaminase inhibitor. Cladribine functions as an inhibitor of DNA synthesis to block the repair of the damaged DNA. Cladribine can inhibit DNA methylation. Cladribine has anti-lymphoma activity. Cladribine can be used for the research of several hematologic malignancies and multiple sclerosis.
|
|
/
|
| HY-100713S | Temocapril-d5 |
Temocapril-d5 is the deuterium labeled Temocapril. Temocapril is an angiotensin-converting enzyme (ACE) inhibitor. Temocapril hydrochloride can be used for the research of hypertension, congestive heart failure, acute myocardial infarction, insulin resistance, and renal diseases.
|
|
/
|
| HY-109037S2 | Mavacamten-d1 |
Mavacamten-d1 (MYK461-d1; SAR439152-d1) is deuterium labeled Mavacamten (HY-109037). Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
|
|
/
|
| HY-116486 | Aureusimine B |
Aureusimine B (Phevalin) is a cyclic dipeptide. Aureusimine B can be produced by Staphylococcus aureus biofilms. Aureusimine B may be exploited as potential biomarker for chronic, S. aureus biofilm-based infections.
Source: Streptomyces coelicolor M1146 |
|
/
|
| HY-174935 | DBCO-PEG1000-NHS |
DBCO-PEG1000-NHS is a dibenzocyclooctyne-conjugated polyethylene glycol derivative bearing an NHS group. DBCO-PEG-NHS forms a stable covalent linkage with the amino group of target molecules via the NHS ester at one end, while introducing a DBCO group at the other end, thus preparing for subsequent click chemical conjugation with any azide-bearing molecule or material.
|
|
/
|
| HY-13599S | Cladribine-d4 |
Cladribine-d4 (2-Chloro-2′-deoxyadenosine-d4) is deuterium labeled Cladribine. Cladribine (2-Chloro-2′-deoxyadenosine), a purine nucleoside analog, is an orally active adenosine deaminase inhibitor. Cladribine functions as an inhibitor of DNA synthesis to block the repair of the damaged DNA. Cladribine can inhibit DNA methylation. Cladribine has anti-lymphoma activity. Cladribine can be used for the research of several hematologic malignancies and multiple sclerosis.
|
|
/
|
| HY-113202S | Stearoyl-L-carnitine-d3 |
Stearoyl-L-carnitine-d3 is the deuterium labeled Stearoylcarnitine. Stearoylcarnitine, a fatty ester lipid molecule, is an endogenous metabolite. Stearoylcarnitine can be used as PKC inhibitor. Stearoylcarnitine accumulates in β cells, leading to arrest of insulin synthesis and energy deficiency in type 2 diabetes mouse. Stearoylcarnitine inhibits lecithin cholesterol acyltransferase (LCAT) in rat and rabbits plasma. Stearoylcarnitine acts as a metabolomics biomarker for Parkinson’s disease. Stearoylcarnitine is a less potent inhibitor of GlyT2.
|
|
/
|
| HY-B0419S | Manidipine-d4 |
Manidipine-d4 is the deuterium labeled Manidipine (HY-B0419). Manidipine is an orally active calcium channel antagonist. Manidipine regulates the expression of cytokines (IL-1β, IL-6). Manidipine has a hypotensive effect. Manidipine can be used in the study of cardiovascular diseases (such as hypertension, myocardial ischemia-reperfusion injury, ventricular hypertrophy), kidney diseases (such as glomerular diseases), and epilepsy.
|
|
/
|
| HY-P3199 | PKCβII Peptide Inhibitor I |
PKCβII Peptide Inhibitor I is a PKCβII inhibitor. PKCβII Peptide Inhibitor I shows cardioprotective effects in rat cardiac Ischemia/reperfusion injury model. PKCβII Peptide Inhibitor I also prevents vascular endothelial dysfunction.
|
|
/
|
| HY-D2443 | AF594 DBCO |
AF594 DBCO is an AlexaFluor 594-conjugated DBCO click chemistry probe for fluorescent labeling of azido-modified cholesterol probes. DBCO is a commonly used chemical biomarker group. AF594 DBCO (Excitation wavelength about 590 nm, emission wavelength about 617 nm) can be used to label proteins, cells and other biomolecules for fluorescence imaging and flow cytometry detection.
|
|
/
|
| HY-W018324S | 5-Hydroxymethylcytosine-13C,d2 |
5-Hydroxymethylcytosine-13C,d2 is the 13C and deuterium labeled 5-Hydroxymethylcytosine (HY-W018324). 5-Hydroxymethylcytosine (5hmC) is an oxidized forms of 5-methylcytosine (5mC) in mammalian DNA. 5-Hydroxymethylcytosine is produced from 5mC in an enzymatic pathway involving three 5mC oxidases, Ten-eleven translocation (TET)1, TET2, and TET3. The conversion of 5mC into 5hmC can be the first step in a pathway leading towards DNA demethylation. 5-Hydroxymethylcytosine is associated with gene transcription and frequently used as a mark to investigate dynamic DNA methylation conversion during mammalian development. 5-Hydroxymethylcytosine can be used for the study of non-small cell lung cancer (NSCLC), neurodegenerative diseases (Alzheimer’s, Parkinson’s) and hematological malignancies (acute myeloid leukemia, myelodysplastic syndromes).
|
|
/
|
| HY-13599S1 | Cladribine-13C5,15N2 |
Cladribine-13C5,15N2 (2-Chloro-2′-deoxyadenosine-13C5,15N2) is 13C and 15N labeled Cladribine. Cladribine (2-Chloro-2′-deoxyadenosine), a purine nucleoside analog, is an orally active adenosine deaminase inhibitor. Cladribine functions as an inhibitor of DNA synthesis to block the repair of the damaged DNA. Cladribine can inhibit DNA methylation. Cladribine has anti-lymphoma activity. Cladribine can be used for the research of several hematologic malignancies and multiple sclerosis.
|
|
/
|
| HY-B0592S2 | rac-Trandolapril-d5 |
rac-Trandolapril-d5 (rac-RU44570-d5) is deuterium labeled Trandolapril. Trandolapril (RU44570) is a nonsulfhydryl proagent that is hydrolysed to the active diacid Trandolaprilat. Trandolapril is an orally administered angiotensin converting enzyme (ACE) inhibitor that has been used in the treatment of hypertension and congestive heart failure (CHF), and after myocardial infarction (MI).
|
|
/
|
| HY-P9S0124 | Anti-CD33 Antibody (OR000283) |
Anti-CD33 Antibody (OR000283) (ORM-6151 Antibody; BMS-986497 Antibody) is an antibody targeting CD33. It is generated by grafting the FAb (H&L) sequence of Gemtuzumab (HY-P99971) onto an IgG1 Fc carrying the N297A mutation, which inhibits Fc-γR binding. Anti-CD33 Antibody (OR000283) can be used to construct degrader-antibody conjugates (DACs), such as ORM-6151 (HY-171792).
Species: Human |
|
/
|
| HY-W010708S | Cholesteryl palmitate-d9 |
Cholesteryl palmitate-d9 is the deuterium labeled Cholesteryl palmitate. Cholesteryl palmitate is a useful prognostic biomarker for chronic interstitial pneumonia (CIP).
|
|
/
|
| HY-B0932S2 | Levocarnitine propionate-d9 hydrochloride |
Levocarnitine propionate-d9 hydrochloride (L-Propionylcarnitine-d9 chloride) is deuterium labeled Levocarnitine propionate hydrochloride. Levocarnitine propionate hydrochloride (L-Propionylcarnitine chloride; ST-261) is a ligand of carnitine acetyltransferase (CAT) with high enzyme affinity. Levocarnitine propionate hydrochloride possesses antioxidant activity. Levocarnitine propionate hydrochloride increases intracellular L-carnitine reserves. Levocarnitine propionate hydrochloride exerts a protective effect against myocardial ischemia-reperfusion injury. Levocarnitine propionate hydrochloride can be used in research related to myocardial ischemia-reperfusion injury and chronic ischemic heart disease.
|
|
/
|
| HY-P11094 | Tet1-Cys peptide |
Tet1-Cys peptide is a peptide with the sequence HLNILSTLWKYRC. Tet1 (HLNILSTLWKYR) (HY-P10998) can specifically bind to the neuronal ganglioside receptor GT1b, possessing neuronal targeting capabilities. The Tet1-Cys peptide sequence has an added Cys, which can be used for drug conjugation for research on drug delivery.
|
|
/
|
| HY-P99886 | Pexelizumab |
Pexelizumab (h5G1. 1-SC) is a humanized scFv monoclonal antibody directed against the C5 complement component. Pexelizumab inhibits apoptosis and leukocyte infiltration. Pexelizumab can be used for the research of cerebral IR injury and myocardial infarction.
Species: Human |
|
/
|
| HY-174935A | DBCO-PEG2000-NHS |
DBCO-PEG2000-NHS is a dibenzocyclooctyne-conjugated polyethylene glycol derivative bearing an NHS group. DBCO-PEG-NHS forms a stable covalent linkage with the amino group of target molecules via the NHS ester at one end, while introducing a DBCO group at the other end, thus preparing for subsequent click chemical conjugation with any azide-bearing molecule or material.
|
|
/
|
| HY-P4898A | Anthopleurin-A TFA |
Anthopleurin-A TFA is a soidum channel toxin. Anthopleurin-A TFA is selective for cardiac channels and has cardiotonic effect. Anthopleurin-A TFA can be isolated from the sea anemone.
|
|
/
|
| HY-N0739R | Betaine chloride (Standard) |
Betaine (chloride) (Standard) is the analytical standard of Betaine (chloride). This product is intended for research and analytical applications. Betaine hydrochloride is a natural compound found in many foods and also an active methyl-donor which can maintain normal DNA methylation patterns.
|
|
/
|
| HY-P10998 | Tet1 peptide |
Tet1 peptide is a peptide that specifically binds to neurons. Tet1 peptide binds to GT1B ganglioside and trisialoganglioside clostridial toxin receptor on the surface of neuronal cells, and can be used in peptide conjugation and drug delivery research.
|
|
/
|
| HY-W015061S | N-(Phenylacetyl-d5)glycine |
N-(Phenylacetyl-d5)glycine is the deuterium labeled Phenylacetylglycine. Phenylacetylglycine is a gut microbial metabolite that can activate β2AR. Phenylacetylglycine protects against cardiac injury caused by ischemia/reperfusion.
|
|
/
|
| HY-P11797 | EP9 |
EP9 is a peptide targeting CD63. EP9 binds specifically to the extracellular region of CD63, including a groove in the large extracellular loop (EC2) or the extracellular end of CD63’s central cavity, triggering endocytosis of decorated nanoemulsions/liposomes into cells. EP9 promotes cellular uptake of decorated nanoemulsions/liposomes into activated cardiac fibroblasts and epicardial stromal cells via caveolae and/or clathrin-coated pits. EP9 can be used for the research of myocardial infarction, cardiac fibrosis.
|
|
/
|
| HY-105168 | TAK 044 |
TAK 044 is an antagonist of Endothelin Receptor. TAK 044 strongly inhibits ET-induced deterioration in various animal models. TAK 044 can be used in study ET-related diseases such as acute myocardial infarction,acute renal failure, acute hepatic malfunction, and subarachnoid hemorrhage.
|
|
/
|
| HY-P3066 | SKF 100398 |
SKF 100398 (d(CH2)5Tyr(Et)VAVP), an arginine vasopressin (AVP) analogue, is a specific antagonist of the antidiuretic effect of exogenous and endogenous AVP.
|
|
/
|
| HY-12515AS | Nicardipine-d3 hydrochloride |
Nicardipine-d3 hydrochloride (YC-93 D3) is the deuterium labeled Nicardipine hydrochloride. Nicardipine hydrochloride is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine hydrochloride acts as an agent for chronic stable angina and for controlling blood pressure.
|
|
/
|
| HY-P1556A | Vasonatrin Peptide (VNP) TFA |
Vasonatrin Peptide (VNP) TFA is a chimera of atrial natriuretic peptide (ANP) and C-type natriuretic peptide (CNP). Vasonatrin peptide TFA possesses the venodilating actions of CNP, the natriuretic actions of ANP, and unique arterial vasodilating actions not associated with either ANP or CNP. Vasonatrin Peptide TFA protects the diabetic heart against ischemia-reperfusion injury by inhibiting ER stress via the cGMP-PKG signaling pathway.
|
|
/
|
| HY-W250148 | Solvent black 5 |
Solvent black 5 (Spirit nigrosine) is a synthetic dye belonging to the family of azo dyes. Also known as oil black or naphthol black, it is dark blue-black and has excellent solubility in organic solvents. Solvent black 5 is commonly used as a colorant in various industrial applications such as printing inks, coatings and plastics. It can also be used as an indicator dye to detect the presence of metals in solution. Furthermore, due to its high absorption and emission properties in the near-infrared region, it has been used in scientific research as a fluorescent biomarker for tissues and cells. However, Solvent black 5 has been reported to have potentially toxic effects on human health and the environment and its use is therefore regulated in some countries.
|
|
/
|
| HY-B1409S | Isosorbide dinitrate-13C6 |
Isosorbide dinitrate-13C6 is the 13C labeled Isosorbide dinitrate. Isosorbide dinitrate (ISDN) is an NO donor that prevents LV remodeling and degradation of cardiac function following myocardial infarction (MI).
|
|
/
|
| HY-17494S | (Rac)-Timolol-d5 maleate |
rac Timolol-d5 (maleate) is a labelled racemic (S)-Timolol maleate. (S)-Timolol Maleate (L-714,465 Maleate) is a non-cardioselective hydrophilic β-adrenoceptor blocker. (S)-Timolol Maleate is widely used as standard medication for intraocular pressure (glaucoma) by preventing the production of aqueous humor. (S)-Timolol Maleate can be used for hypertension, angina pectoris and myocardial infarction.
|
|
/
|
| HY-A0248AS | Polymyxin B1-d7 TFA |
Polymyxin B1-d7 TFA is the deuterium labeled Polymyxin B1 TFA (HY-A0248A). Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment.
Source: Bacilus polymyxa |
|
/
|
| HY-P990791 | Anti-Mouse CD71/TfR1 Antibody (R17 217.1.3) |
Anti-Mouse CD71/TfR1 Antibody (R17 217.1.3) is a rat-derived IgG2a κ type antibody inhibitor, targeting to mouse CD71/TfR1. Anti-Mouse CD71/TfR1 Antibody (R17 217.1.3) can deplete CD71+ cells and inhibit transferrin receptor. Anti-Mouse CD71/TfR1 Antibody (R17 217.1.3) can be used for the researches of cancer, infection, inflammation and immunology, such as lung cancer, lymphocytic choriomeningitis virus (LCMV) infection and Cardiac allograft.
Species: Mouse |
|
/
|
| HY-P990264 | Anti-Mouse CD70 Antibody (FR70) |
Anti-Mouse CD70 Antibody (FR70) is a rat-derived ant-mouse CD70 IgG2b κ type antibody inhibitor. Anti-Mouse CD70 Antibody (FR70) decreases CD4+, CD8+ T cells and eosinophils. Anti-Mouse CD70 Antibody (FR70) shows potent anti-inflammatory and anti-immune effects on allergic lung inflammation and cardiac transplant mice models.
Species: Mouse |
|
/
|
| HY-P5142A | ω-Hexatoxin-Hv1a TFA |
ω-Hexatoxin-Hv1a (ω-ACTX-Hv1; ω-Atracotoxin-HV1) TFA is an orally active insecticidal neurotoxin containing an inhibitor cystine knot motif and a selective calcium channel inhibitor. ω-Hexatoxin-Hv1a TFA blocks L-type voltage-dependent Ca2+ channels and reduces intracellular calcium ion concentration, thereby decreasing apoptosis, necroptosis and oxidative stress, and promoting cell recovery and energy level elevation. ω-Hexatoxin-Hv1a TFA causes larval paralysis and death by impairing neurotransmission in the central nervous system of insects. It shows high injectable toxicity against insects of multiple orders, but exhibits weak oral toxicity. ω-Hexatoxin-Hv1a TFA is widely applicable to studies related to ischemia-reperfusion injury, atopic dermatitis, and ischemic injury of cardiomyocytes and neurons.
|
|
/
|
| HY-P3678 | Neuropeptide Y (18-36) (porcine) |
Neuropeptide Y (18-36) (porcine) is a competitive neuropeptide Y (NPY) cardiac receptor antagonist. Neuropeptide Y (18-36) (porcine) inhibits the binding of I-NPY to cardiac ventricular membranes in a concentration-dependent manner with an IC50 value of 158 nM and an Ki value of 140 nM. Neuropeptide Y (18-36) (porcine) can be used for the research of congestive heart failure.
|
|
/
|
| HY-N1923 | Hypaconine |
Hypaconine is a C19-diterpenoid alkaloid isolated from Aconitum and Delphinium spp. Hypaconine exhibits strong cardiac activity.
|
|
/
|
| HY-136490S | Psychosine-d5 |
Psychosine-d5 is deuterium labeled Psychosine. Psychosine, a substrate of the galactocerebrosidase (GALC) enzyme, is a potential biomarker for Krabbe disease. Psychosine is a highly cytotoxic lipid, capable of inducing cell death in a wide variety of cell.
|
|
/
|
| HY-P6437A | Drp1 peptide inhibitor P110 TFA |
Drp1 peptide inhibitor P110 (Compound P110) TFA is a selective Drp1 peptide inhibitor with neuroprotective properties. Drp1 peptide inhibitor P110 TFA can inhibit the activation of Drp1, prevent MPTP (HY-15608)-induced Drp1 mitochondrial translocation, and alleviate MPTP-induced dopaminergic neuron loss, dopaminergic nerve terminal damage, and behavioral deficits, and can be used in the study of Alzheimer's disease. Additionally, Drp1 peptide inhibitor P110 TFA can reduce mitochondrial damage and organ injury in animal models of Huntington's disease, cerebral ischemic injury, and myocardial infarction.
|
|
/
|
| HY-W740027 | 5-Methyl-2'-deoxycytidine-d3 |
5-Methyl-2'-deoxycytidine-d3 (5-Methyldeoxycytidine-d3) is the deuterium labeled Methyl-2'-deoxycytidine (HY-W012078). 5-Methyl-2'-deoxycytidine (5mdC) is an endogenous substrate of DNA methyltransferases (such as mammalian 5-C-MTase) and binds to DNA dependent on the formation of DNA stem-loop structures. 5-Methyl-2'-deoxycytidine guides de novo DNA methylation by acting as a methylation mark and activates the methylation of adjacent CpG sites in single-stranded DNA through cis action. 5-Methyl-2'-deoxycytidine regulates DNA methylation patterns by recruiting methyltransferases to specific chromatin regions, affecting chromatin condensation and gene expression. Its distribution in plant cells is related to cell proliferation and differentiation stages. The methylation level of 5-Methyl-2'-deoxycytidine is low in proliferating cells and high in differentiated cells.
|
|
/
|
| HY-N7177 | Hydroxytanshinone IIA |
Hydroxytanshinone IIA is a hydrolytic metabolite of Tanshinone IIA (HY-N0135). Tanshinone IIA inhibits angiogenesis by targeting the protein kinase domain of VEGF/VEGFR2. Hydroxytanshinone IIA exhibits antioxidant and anti-inflammatory activities. Hydroxytanshinone IIA can be used in studies of angina pectoris and myocardial infarction.
|
|
/
|
| HY-P99645 | Goflikicept |
Goflikicept (RPH 104) is a fusion protein that selectively binds and inactivates both circulating IL-1β and IL-1α. Goflikicept has the potential for the research of ST-segment elevation myocardial infarction (STEMI).
|
|
/
|
| HY-B0573BS | Propranolol-d7 |
Propranolol-d7 is the deuterium labeled Propranolol. Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM. Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.
|
Neurological, Eye or Ear Disease
Blood or Cardio-cerebrovascular Disease
Metabolic or Endocrine Disease
|
/
|
| HY-P99946 | Erlizumab |
Erlizumab (rhuMAb) is a monoclonal antibody against the Integrin b2/ITGB2/CD18 subunit of the Mac-1 receptor. Erlizumab can reduce reperfusion injury in myocardial infarction.
Species: Human |
|
/
|
| HY-N2439 | Methyl isoeugenol |
Methyl isoeugenol is an orally active, blood-brain barrier-permeable isoeugenol-type eugenol analog. Methyl isoeugenol promotes the nuclear translocation of Nrf2, upregulates the expressions of HO-1, NQO1 and SOD, and reduces the expression level of MDA. Methyl isoeugenol decreases the nuclear translocation of NF-κB. Methyl isoeugenol inhibits NLRP3 inflammasome-mediated pyroptosis. Methyl isoeugenol reduces cerebral infarction volume and regulates the M1/M2 phenotypic balance of microglia. Methyl isoeugenol can be used for the research of cerebral ischemia-reperfusion injury.
|
|
/
|
| HY-P6437 | Drp1 peptide inhibitor P110 |
Drp1 peptide inhibitor P110 (Compound P110) is a selective Drp1 peptide inhibitor with neuroprotective properties. Drp1 peptide inhibitor P110 can inhibit the activation of Drp1, prevent MPTP-induced Drp1 mitochondrial translocation, and alleviate MPTP-induced dopaminergic neuron loss, dopaminergic nerve terminal damage, and behavioral deficits, and can be used in the study of Alzheimer's disease. Additionally, Drp1 peptide inhibitor P110 can reduce mitochondrial damage and organ injury in animal models of Huntington's disease, cerebral ischemic injury, and myocardial infarction.
|
|
/
|
| HY-P10143 | MMP-2/MMP-9 Substrate |
MMP-2/MMP-9 Substrate (Ac-Pro-Leu-Gly-[(S)-2-mercapto-4-methyl-pentanoyl]-Leu-Gly-OEt) is a synthetic chromogenic polypeptide substrate whose core structure mimics the cleavage sites of MMP-2 and MMP-9 (gelatinase A and B) in collagen. After being hydrolyzed by collagenase, MMP-2/MMP-9 Substrate reacts with 4,4'-dithiodipyridine or Ellman's Reagent via its thiol fragment to produce a product with ultraviolet absorption properties.
|
|
/
|
| HY-113248S | 3-Nitro-L-tyrosine-d3 |
3-Nitro-L-tyrosine-d3 is the deuterium labeled 3-Nitro-L-tyrosine (HY-113248). 3-Nitro-L-tyrosine serves as a biomarker of oxidative stress. 3-Nitro-L-tyrosine attenuates the pressor and vasoconstrictive effects of angiotensin II by inhibiting the α1-adrenergic receptor-mediated signaling pathway, and participates in hemodynamic regulation under pathological conditions such as inflammation and ischemia. 3-Nitro-L-tyrosine can be used in studies related to atherosclerosis, ischemia-reperfusion and sepsis.
|
|
/
|
| HY-W014075S | 1-Hydroxypyrene-d9 |
1-Hydroxypyrene-d9 is the deuterium labeled 1-Hydroxypyrene (HY-W014075). 1-Hydroxypyrene, a biomarker of exposure to polycyclic aromatic hydrocarbons (PAHs), is analyzed in urine samples. 1-Hydroxypyrene is the major biomarker of exposure to pyrenes. 1-Hydroxypyrene is the orally active agonist for aryl hydrocarbon receptor (AhR) and can lead to renal fibrosis.
|
|
/
|
| HY-P11315 | MG1 peptide |
MG1 peptide is an M1 microglia-targeting peptide with blood-brain barrier permeability. MG1 peptide can be used in studies related to ischemic stroke and cerebral ischemia-reperfusion injury.
|
|
/
|
| HY-W010708S1 | Cholesteryl palmitate-d7 |
Cholesteryl palmitate-d7 is deuterium labeled Cholesteryl palmitate. Cholesteryl palmitate is a useful prognostic biomarker for chronic interstitial pneumonia (CIP).
|
|
/
|
| HY-106275 | FX-06 |
FX-06 (Fibrin-derived peptide Bβ15-42) is a fibrin Bbeta chain-derived peptide. FX-06 binds to VE-cadherin and inhibits leukocyte transmigration and initiates VE-cadherin-mediated signaling. FX-06 can be used in the research of ischemia/reperfusion injury, Dengue shock syndrome (DSS).
|
|
/
|
| HY-P10728 | B7-33 |
B7-33 is a single-chain relaxin mimetic and a selective relaxin receptor 1 (RXFP1) agonist. B7-33 phosphorylates ERK1/2 without inducing activation of the cAMP signaling pathway. B7-33 exhibits anti-fibrotic and cardioprotective activities. B7-33 can be used in the research of vascular diseases such as cardiomyopathy, myocardial infarction and fibrosis.
|
|
/
|
| HY-113247S | trans-trans-Muconic acid-d4 |
trans-trans-Muconic acid-d4 is the deuterium labeled trans-trans-Muconic acid. trans-trans-Muconic acid is a urinary metabolite of benzene and has been used as a biomarker of exposure to benzene in human.
|
|
/
|
| HY-109037S4 | Mavacamten-d7 |
Mavacamten-d7 (MYK461-d7) is deuterium labeled Mavacamten. Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
|
|
/
|
| HY-N11222 | Nonanoylcarnitine |
Nonanoylcarnitine is a metabolite associated with chronic environmental exposure to polycyclic aromatic hydrocarbons (PAH) and fragmented QRS waves in acute myocardial infarction. Nonanoylcarnitine can be used as a potential biomarker for the metabolic outcome of PAH exposure and the prognosis of acute myocardial infarction.
|
|
/
|
| HY-130189R | S-Phenylmercapturic acid (Standard) |
S-Phenylmercapturic acid (Standard) is the analytical standard of S-Phenylmercapturic acid. This product is intended for research and analytical applications. S-Phenylmercapturic acid, a metabolite of benzene, can be used as a biomarker, identified by GC, HPLC (UV or fluorescence detection), GC-MS, LC-MS/MS or immunoassay.
|
|
/
|
| HY-W015114R | L-2-Hydroxyglutaric acid disodium (Standard) |
L-2-Hydroxyglutaric acid (disodium) (Standard) is the analytical standard of L-2-Hydroxyglutaric acid (disodium). This product is intended for research and analytical applications. L-2-Hydroxyglutaric acid disodium is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid disodium can inhibit histone demethylases and hence promote histone methylation. L-2-Hydroxyglutaric acid inhibits mitochondrial creatine kinase (Mi-CK) activity with Km and Ki of 2.52 mM and 11.13 mM, respectively.
|
|
/
|
| HY-B0573S | Propranolol-d7 hydrochloride |
Propranolol-d7 (hydrochloride) is a deuterium labeled Propranolol hydrochloride. Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol hydrochloride inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM. Propranolol hydrochloride is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.
|
Neurological, Eye or Ear Disease
Blood or Cardio-cerebrovascular Disease
Metabolic or Endocrine Disease
|
/
|
| HY-W016733 | D-Citrulline |
D-Citrulline (H-D-Cit-OH) is a stereoisomer of L-citrulline (HY-N0391). D-Citrulline significantly attenuates polymorphonuclear leukocyte (PMN)-induced cardiac contractile dysfunction in the isolated perfused rat heart subjected to ischemia/reperfusion via a non-NO-mediated mechanism.
|
|
/
|
| HY-W008091S | 5-Methylcytosine-d4 |
5-Methylcytosine-d4 is the deuterium labeled 5-Methylcytosine (HY-W008091). 5-Methylcytosine is a well-characterized DNA modification in prokaryotes and eukaryotes. 5-Methylcytosine forms symmetrical methylation on CpG dinucleotides in DNA, stabilizes tRNA/rRNA structure in RNA, and affects mRNA translation. 5-Methylcytosine can be oxidized to generate 5hmC, 5fC, and 5caC. 5-Methylcytosine can be used in epigenetics, developmental biology, and the study of diseases such as colorectal cancer and hepatocellular carcinoma.
|
|
/
|
| HY-B0710S | Betaine-13C3 |
Betaine-13C3 (Trimethylglycine-13C3) is the 13C labeled isotope of Betaine (HY-B0710). Betaine (Trimethylglycine) is a natural compound found in many foods and also an active methyl-donor which can maintain normal DNA methylation patterns. Betaine is found ubiquitously in plants, animals, microorganisms, and rich dietary sources including seafood, spinach, and wheat bran. Betaine also acts as an osmolyte, to maintain the avian’s cellular water and ion balance to improve the avian’s capacity against heat stress via preventing dehydration and osmotic inactivation. It helps in maintaining the protective osmolytic activity, especially in heat-stressed birds. Betaine may promote various intestinal microbes against osmotic variations and thus improve microbial fermentation activity.
|
|
/
|
| HY-P991222 | AMG-529 |
AMG-529 is a humanized monoclonal antibody against ASGR1 that binds to ASGR1, blocks ligand binding, and causes a dose-dependent increase in ALP (a biomarker of ASGR1 inhibition). AMG-529 can be used for the research of cardiovascular diseases.
Species: Human |
|
/
|
| HY-A0144A | Etilefrine hydrochloride |
Etilefrine hydrochloride is a sympathetic nerve agonist and AMPK activator that selectively targets α1/β1 adrenergic receptors. Etilefrine hydrochloride stimulates α1 adrenergic receptors, leading to contraction of vascular smooth muscle and increased peripheral resistance. Etilefrine hydrochloride also stimulates β1 receptors to enhance myocardial contractility and increase heart rate, thereby increasing blood pressure and improving cardiac output. Etilefrine hydrochloride also bidirectionally regulates the AMPK/Akt pathway and modulates the phosphorylation levels. Etilefrine hydrochloride can be used in cardiovascular research, such as postural hypotension, chylothorax, and improving low cardiac output.
|
Lung Cancer
Breast Cancer
Colorectal Cancer
Prostate Cancer
Gastric Cancer
Liver Cancer
Leukemia/Lymphoma/Myeloma
Pancreatic Cancer
Ovarian Cancer
Depression
Pain
Digestive System Inflammation
Cardiovascular Disease
Obesity
Lung Fibrosis
|
/
|
| HY-P6442 | Chemerin15 |
Chemerin15 is an anti-inflammatory peptide derived from Chemerin. Chemerin15 binds to ChemR23. Chemerin15 inhibits TNFα-induced activation of Syk, ERK and Src kinases. Chemerin15 increases the expression of p-p38 mRNA and protein. Chemerin15 mediates phagocytosis, resolution of inflammation, CD62L shedding and downregulation of PSGL-1 expression in macrophages and microglia. Chemerin15 inhibits neutrophil-mediated vascular inflammation and myocardial ischemia-reperfusion injury via ChemR23. Chemerin15 enhances microglial phagocytosis, thereby alleviating cerebral ischemia-reperfusion injury.
|
|
/
|
| HY-NP192 | Sericin |
Sericin is an orally active globular protein produced by silkworm cocoons. Sericin inhibits the expression of COX2, iNOS, TLR4, MAPK and NF-κB; reduces the levels of IL-18, IL-1 and CCL2; antagonizes the activity of AChE; and downregulates the expression of Bcl-2. Sericin enhances the PI3K/AKT-mediated insulin signaling pathway. Sericin inhibits the activity of tyrosinase (Tyrosinase), scavenges ROS, chelates metal ions, and increases the levels of antioxidant enzymes. Sericin induces apoptosis and arrests the cell cycle. Sericin exhibits antibacterial, moisturizing, cardioprotective and anticoagulant properties. Sericin can be used in research related to type 2 diabetes, hyperlipidemia, obesity, Alzheimer's disease, colon cancer, peripheral nerve injury and ischemic myocardial infarction.
|
Reactive Oxygen Species (ROS)
Bacterial
COX
NO Synthase
Toll-like Receptor (TLR)
p38 MAPK
NF-κB
Interleukin Related
Cholinesterase (ChE)
Bcl-2 Family
Tyrosinase
PI3K
Akt
Cancer
Infection
Neurological, Eye or Ear Disease
Inflammation or Immune System Disease
Metabolic or Endocrine Disease
|
/
|
| HY-143368S | L-Phenylmercapturic acid-d5 |
L-Phenylmercapturic acid-d5 is the deuterium labeled L-Phenylmercapturic acid (HY-143368). L-Phenylmercapturic acid is often used as a biomarker for exposure to aniline compounds such as aniline and xylene.
|
|
/
|
| HY-P4511 | Serylleucine |
Serylleucine (H-Ser-Leu-OH) is a dipeptide. Serylleucine's core 1 o-glycosylated peptide (SLC1G) can be detected in urine as a metabolite and is a biomarker in TB studies.
|
|
/
|
| HY-119152 | CMX-2043 |
CMX-2043 is a novel analogue of α-Lipoic Acid (HY-N0492). CMX-2043 is effective in antioxidant effect, activation of insulin receptor kinase, soluble tyrosine kinase, and Akt phosphorylation. CMX-2043 shows protection against ischemia-reperfusion injury (IRI) in rat model.
|
|
/
|
| HY-D1603 | BODIPY FL-EDA |
BODIPY FL-EDA is a widely used fluorescent dye for quantitative analysis of nucleotides. BODIPY FL-EDA is an aliphatic amine analog that can react with aldehydes and ketones. BODIPY FL-EDA can be used to detect both modified and unmodified deoxynucleotides and to determine DNA damage and genomic DNA methylation through capillary electrophoresis with laser-induced fluorescence (CE-LIF). Additionally, it can be used for quantifying intracellular ATP levels. The excitation wavelength is 500 nm, and the emission wavelength is 510 nm.
|
|
/
|
| HY-113039 | L-2-Hydroxyglutaric acid |
L-2-Hydroxyglutaric acid is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid can inhibit histone demethylases and hence promote histone methylation. L-2-Hydroxyglutaric acid inhibits mitochondrial creatine kinase (Mi-CK) activity with Km and Ki of 2.52 mM and 11.13 mM, respectively.
|
|
/
|
| HY-113151 | 18-Oxocortisol |
18-Oxocortisol is a derivative of cortisol that is produced by aldosterone synthase (CYP11B2). 18-Oxocortisol is a naturally occurring mineralocorticoid agonist. 18-Oxocortisol is a biomarker in adrenal vein sampling.
|
|
/
|
| HY-W015061R | Phenylacetylglycine (Standard) |
Phenylacetylglycine (Standard) is the analytical standard of Phenylacetylglycine. This product is intended for research and analytical applications. Phenylacetylglycine is a gut microbial metabolite that can activate β2AR. Phenylacetylglycine protects against cardiac injury caused by ischemia/reperfusion.
|
|
/
|
| HY-B0932S | Levocarnitine propionate-d3 hydrochloride |
Levocarnitine propionate-d3 (hydrochloride) is the deuterium labeled Levocarnitine propionate hydrochloride. Levocarnitine propionate hydrochloride (L-Propionylcarnitine chloride; ST-261) is a ligand of carnitine acetyltransferase (CAT) with high enzyme affinity. Levocarnitine propionate hydrochloride possesses antioxidant activity. Levocarnitine propionate hydrochloride increases intracellular L-carnitine reserves. Levocarnitine propionate hydrochloride exerts a protective effect against myocardial ischemia-reperfusion injury. Levocarnitine propionate hydrochloride can be used in research related to myocardial ischemia-reperfusion injury and chronic ischemic heart disease.
|
|
/
|
| HY-P991363 | AX-202 |
AX-202 is a humanized IgG4 monoclonal antibody targeting S100A4. AX-202 neutralizes the activity of S100A4. AX-202 effectively reverses established fibrosis and reduces inflammation and fibrosis-related biomarkers in a mouse model of skin fibrosis. AX-202 is applicable for the research of fibrotic and inflammatory diseases.
Species: Human |
|
/
|
| HY-W018324 | 5-Hydroxymethylcytosine |
5-Hydroxymethylcytosine (5hmC) is an oxidized forms of 5-methylcytosine (5mC) in mammalian DNA. 5-Hydroxymethylcytosine is produced from 5mC in an enzymatic pathway involving three 5mC oxidases, Ten-eleven translocation (TET)1, TET2, and TET3. The conversion of 5mC into 5hmC can be the first step in a pathway leading towards DNA demethylation. 5-Hydroxymethylcytosine is associated with gene transcription and frequently used as a mark to investigate dynamic DNA methylation conversion during mammalian development. 5-Hydroxymethylcytosine can be used for the study of non-small cell lung cancer (NSCLC), neurodegenerative diseases (Alzheimer’s, Parkinson’s) and hematological malignancies (acute myeloid leukemia, myelodysplastic syndromes).
|
Metabolic or Endocrine Disease
Lung Cancer
Leukemia/Lymphoma/Myeloma
Alzheimer's Disease
Parkinson's Disease
|
/
|
| HY-I0626S2 | Cytosine-d2 |
|
/
|
|
| HY-W923198 | Fluorescein O-methacrylate |
Fluorescein O-methacrylate (Methacryloyloxy fluorescein) is a pH-responsive fluorescent monomeric dye. Fluorescein O-methacrylate exhibits pH-responsive fluorescence properties: its fluorescence is activated under alkaline conditions and quenched under neutral or acidic conditions; reversible switching of fluorescence is achievable by adjusting the pH of the solution. Fluorescein O-methacrylate can be used as a monomer for the synthesis of amphiphilic fluorescein polymers. These polymers can self-assemble into stable polymer nanoparticles with enhanced aqueous-phase fluorescence, and also enable the conjugation of nanoparticles with amine-containing biomolecules to support sensitive optical detection of biomarkers (Ex/Em = 490/520 nm).
|
|
/
|
| HY-109037S3 | Mavacamten-d5 |
Mavacamten-d5 (MYK461-d5; SAR439152-d5) is deuterium labeled Mavacamten (HY-109037). Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
|
|
/
|
| HY-B0710R | Betaine (Standard) |
Betaine (Standard) is the analytical standard of Betaine. This product is intended for research and analytical applications. Betaine (Trimethylglycine) is a natural compound found in many foods and also an active methyl-donor which can maintain normal DNA methylation patterns. Betaine is found ubiquitously in plants, animals, microorganisms, and rich dietary sources including seafood, spinach, and wheat bran. Betaine also acts as an osmolyte, to maintain the avian’s cellular water and ion balance to improve the avian’s capacity against heat stress via preventing dehydration and osmotic inactivation. It helps in maintaining the protective osmolytic activity, especially in heat-stressed birds. Betaine may promote various intestinal microbes against osmotic variations and thus improve microbial fermentation activity.
|
|
/
|
| HY-113248 | 3-Nitro-L-tyrosine |
3-Nitro-L-tyrosine serves as a biomarker of oxidative stress. 3-Nitro-L-tyrosine attenuates the pressor and vasoconstrictive effects of angiotensin II by inhibiting the α1-adrenergic receptor-mediated signaling pathway, and participates in hemodynamic regulation under pathological conditions such as inflammation and ischemia. 3-Nitro-L-tyrosine can be used in studies related to atherosclerosis, ischemia-reperfusion and sepsis.
|
|
/
|
| HY-P990294 | Anti-Mouse CD106/VCAM-1 Antibody (M/K-2.7) |
Anti-Mouse CD106/VCAM-1 Antibody (M/K-2.7) is an anti-mouse CD106/VCAM-1 IgG1 monoclonal antibody. Anti-Mouse CD106/VCAM-1 Antibody (M/K-2.7) reduces inflammatory response and oxidative stress by lowering p-STAT3 and reactive oxygen species (ROS) levels. Anti-Mouse CD106/VCAM-1 Antibody (M/K-2.7) can alleviate cardiac inflammation and fibrosis by reducing the expression of collagen I and collagen III. Anti-Mouse CD106/VCAM-1 Antibody (M/K-2.7) can be used for research on cardiovascular conditions such as hypertensive heart condition and subretinal fibrosis.
Species: Mouse |
|
/
|
| HY-NP002E | PSA Protein (Porcine) |
PSA Protein (Porcine) (Porcine Serum Albumin) is a serum albumin protein that contains a flexible C-terminal region. PSA Protein (Porcine) can serve both as a pork allergen and as a biomarker for detecting pork.
|
|
/
|
| HY-125773 | β-cyano-L-Alanine |
β-cyano-L-Alanine (Beta-cyano-l-alanine), a nitrile of widespread occurrence in higher plants, is enzymatically produced by cyanoalanine synthase from cyanide and cysteine as substrates. β-cyano-L-Alanine abolishes the protective effect of ethanol on cerebral ischemia/reperfusion (I/R) injury.
|
|
/
|
| HY-13257G | Thiazovivin (GMP) |
Thiazovivin (GMP) is Thiazovivin (HY-13257) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Thiazovivin is a potent ROCK inhibitor.
|
|
/
|
| HY-129763 | Di-4-ANEPPS |
Di-4-ANEPPS is a voltage-sensitive dye that acts on voltage-gated ion channels (such as sodium channels) and inhibits sodium current, significantly reducing sodium current density, although specific values like IC50 remain unclear. It mainly binds to the voltage-sensitive regions on the cell membrane, changing its fluorescence properties to reflect membrane potential changes and thus affecting the function of ion channels to exert its activity. This substance can be used in cardiovascular research, such as the electrophysiology of cardiomyocytes, myocardial ischemia, and the effects of drugs on cardiomyocytes. It is of great value in evaluating drug cardiotoxicity and exploring the mechanisms of arrhythmias.
|
|
/
|
| HY-W073080 | Coproporphyrin I dihydrochloride |
Coproporphyrin I dihydrochlorideIt is an organic compound belonging to the class of porphyrins. It is a derivative of heme, an iron-containing molecule found in hemoglobin and other proteins. Coproporphyrin I dihydrochlorideOften used as a biomarker in the assessment of certain liver and metabolic diseases, especially those related to bile synthesis and transport. It can also be used as a reference standard for analytical chemistry and pharmacological research.
|
|
/
|
| HY-N4283 | Coniferyl alcohol |
Coniferyl alcohol is an orally active lignin biosynthesis intermediate and antifungal agent. Coniferyl alcohol specifically inhibits the growth of fungi (Verticillium longisporum). Coniferyl alcohol inhibits the growth of Nicotiana benthamiana seedlings. Coniferyl alcohol improves cardiac dysfunction in renovascular hypertension and cardiac inflammation.
|
|
/
|
| HY-W014075 | 1-Hydroxypyrene |
1-Hydroxypyrene, a biomarker of exposure to polycyclic aromatic hydrocarbons (PAHs), is analyzed in urine samples. 1-Hydroxypyrene is the major biomarker of exposure to pyrenes. 1-Hydroxypyrene is the orally active agonist for aryl hydrocarbon receptor (AhR) and can lead to renal fibrosis.
|
|
/
|
| HY-110228 | Metformin-d6 hydrochloride |
Metformin-d6 hydrochloride is a deuterium labeled Metformin hydrochloride. Metformin hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin hydrochloride also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, metformin hydrochloride regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo.
|
|
/
|
| HY-113092 | Propionylcarnitine |
Propionylcarnitine is metabolized by carnitine acetyltransferase from propionyl-CoA. Increased propionylcarnitine is regarded as a biomarker of vitamin B12 deficiency.
|
|
/
|
| HY-P99555 | Tomaralimab |
Tomaralimab (OPN-305) is a humanized anti-TLR2 IgG4 monoclonal antibody. Tomaralimab inhibits TLR2, MyD88, NLRP3, and reduces pro-inflammatory cytokine (IL-1β, IL-6, IL-8) production. Tomaralimab reduces tau pathology. Tomaralimab improves cognition, atopic dermatitis. Tomaralimab has anticancer effects on pancreatic ductal adenocarcinoma. Tomaralimab is being studied in myelodysplastic syndrome (MDS), atopic dermatitis, pancreatic ductal adenocarcinoma, Alzheimer's disease, and myocardial ischemia/reperfusion injury.
Species: Human |
Cancer
Neurological, Eye or Ear Disease
Inflammation or Immune System Disease
Blood or Cardio-cerebrovascular Disease
|
/
|
| HY-P991219 | Anti-IL11RA Antibody (X209) |
Anti-IL11RA Antibody (X209) (EnX209) is a human-derived IgG4, κ-type antibody inhibitor targeting IL11RA, with a KD of 6 nM. Anti-IL11RA Antibody (X209) blocks the IL11RA signaling pathway, inhibits ERK-dependent activation, and reduces the activation level of ERK1/2. Anti-IL11RA Antibody (X209) exerts a protective effect against fibrosis. Anti-IL11RA Antibody (X209) is applicable to studies related to liver fibrosis, cardiac fibrosis and other related conditions. Recommended isotype control: Human IgG4 kappa, Isotype Control (HY-P99003).
Species: Human |
|
/
|
| HY-P99505 | Ziltivekimab |
Ziltivekimab (COR-001) is a fully human monoclonal antibody and also an IL-6 inhibitor. Ziltivekimab significantly reduces inflammatory biomarkers and Lipoprotein (a) in chronic kidney disease patients with systemic inflammation. Ziltivekimab does not increase pro-atherosclerotic lipid levels. Ziltivekimab is used in studies related to atherosclerotic thrombotic diseases and chronic kidney disease.
Species: Human |
|
/
|
| HY-P99047 | Simtuzumab |
Simtuzumab (AB 0024; GS 6624) is a monoclonal antibody directed against Lysyl oxidase like-2 (LOXL2). Simtuzumab non-competitively blocks collagen cross-linking, reduces LOXL2 protein expression and attenuates extracellular matrix changes. Simtuzumab reduces myocardial fibrosis and prevents cardiac dysfunction. Simtuzumab lowers Myh7 and Nppa gene expression, reduces contraction heterogeneity, and cuts COL1A1 deposition. Simtuzumab can be used for the research of LMNA mutation-induced dilated cardiomyopathy, idiopathic pulmonary fibrosis, and primary sclerosing cholangitis.
Species: Human |
|
/
|
| HY-NP007 | Myoglobin |
Myoglobin is an oxygen-binding heme protein. Myoglobin scavenges ROS via its peroxidase activity, and binds to and inactivates NO in the heart and oxidative skeletal muscle. Myoglobin stores, buffers and facilitates intracellular oxygen diffusion, maintains aerobic metabolism under hypoxic/anoxic conditions, and provides oxygen supply support for mitochondria. Myoglobin alleviates oxidative stress, protects cardiac function and affects cardiac redox pathways. Myoglobin can be used in studies related to ischemia-reperfusion injury, oxidative stress-induced cardiac dysfunction and acute myocardial infarction.
|
|
/
|
| HY-101952G | Prostaglandin E2 (GMP) |
Prostaglandin E2 (GMP) is Prostaglandin E2 (HY-101952) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Prostaglandin E2, an inflammatory mediator, is a endogenous hormone-like substance that participate in a wide range of body functions.
|
|
/
|
| HY-P99116 | Faricimab |
Faricimab, an overall good safety and tolerability profile, is a bispecific antibody targeting Angiopoietin-2 (Ang-2) and vascular endothelial growth factor-A (VEGF-A). Faricimab prevents retinal vascular leakage, cell death and inflammation in retinal ischemia/reperfusion (I/R) injury and sCNV mouse models. Faricimab demonstrates statistically superior visual acuity gains versus Ranibizumab (HY-P9951). Faricimab can be used for retinal diseases, such as age-related macular degeneration (w-AMD), diabetic macular edema (DME) and macular edema following retinal vein occlusion (RVO).
Species: Human |
Blood or Cardio-cerebrovascular Disease
Metabolic or Endocrine Disease
Visual System Disease
Ischemia-Reperfusion Injury
|
/
|
| HY-P10272 | Rusfertide |
Rusfertide is a peptide mimetic of natural hepcidin, which targets and degrades ferroportin, reduces serum iron and transferrin-saturation, and thus regulates the production of red blood cells. Rusfertide ameliorates the polycythemia vera, β-thalassemia and hereditary hemochromatosis.
|
|
/
|
| HY-W015114 | L-2-Hydroxyglutaric acid disodium |
L-2-Hydroxyglutaric acid disodium is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid disodium can inhibit histone demethylases and hence promote histone methylation. L-2-Hydroxyglutaric acid inhibits mitochondrial creatine kinase (Mi-CK) activity with Km and Ki of 2.52 mM and 11.13 mM, respectively.
|
|
/
|
| HY-P99396 | Spesolimab |
Spesolimab (BI 655130) is a mouse-derived humanized IgG1k antibody against IL-36R. IL-36 plays an important role in the immune system and Spesolimab is being investigated in palmoplantar pustulosis (PPP). Spesolimab was associated with a reduction in biomarkers associated with the innate, Th1/Th17 and neutrophil pathways.
Species: Human |
|
/
|
| HY-B1770 | Sodium Iodide,99% |
Sodium Iodide is a compound composed of sodium ions and iodine ions. Sodium Iodide scavenges hydrogen peroxide. Sodium Iodide maintains the level of thyroid hormone T3 through its iodine component. Sodium Iodide protects tissues from oxidative damage and regulates thyroid homeostasis. Sodium Iodide relieves acute myocardial infarction.
|
|
/
|
| HY-N9410 | Lysophosphatidylcholine 18:2 |
Lysophosphatidylcholine 18:2 (1-Linoleoyl-2-Hydroxy-sn-glycero-3-PC), a lysophospholipid, is a potential biomarker identified from insulin resistance (IR) polycystic ovary syndrome (PCOS). Low plasma Lysophosphatidylcholine 18:2 also has been shown to predict impaired glucose tolerance, insulin resistance, type 2 diabetes, coronary artery disease, and memory impairment.
|
|
/
|
| HY-107754 | Cesium chloride |
Cesium chloride is a blocker of potassium channel. Cesium chloride prevents the decrease of Na+ transport produced by Alloxan. Cesium chloride has induced cardiac arrhythmias, including torsade de pointes in animal models.
|
|
/
|
| HY-113491 | 3-Phosphoglyceric acid |
3-Phosphoglyceric acid is a metabolic intermediate in both glycolysis and the Calvin cycle. 3-Phosphoglyceric acid is involved in alveolar macrophage epigenetic regulation.
|
|
/
|
| HY-P72094 | ATP2A2 Protein, Human (His) |
The ATP2A2 protein is a magnesium-dependent enzyme that hydrolyzes ATP and transfers calcium from the cytoplasm to the sarcoplasmic reticulum. It participates in autophagy during starvation and interacts with VMP1 to achieve ER isolating membrane contact. ATP2A2 Protein, Human (His) is the recombinant human-derived ATP2A2 protein, expressed by E. coli , with N-6*His labeled tag.
Species: Human; Source: E. coli |
|
/
|
| HY-P71469 | Cardiac troponin I/Tnni3 Protein, Mouse (His-SUMO) |
Cardiac troponin I, also known as Tnni3, plays a key role as an inhibitory subunit in the troponin complex, a key regulator of calcium sensitivity in actomyosin ATPase activity in striated muscle.Tnni3 interacts with TRIM63, emphasizing its involvement in complex cellular processes.Cardiac troponin I/Tnni3 Protein, Mouse (His-SUMO) is the recombinant mouse-derived Cardiac troponin I/Tnni3 protein, expressed by E.coli , with N-SUMO, N-6*His labeled tag.
Species: Mouse; Source: E. coli |
|
/
|
| HY-P701199 | CSRP3 Protein, Human (HEK293, His) |
CSRP3 Protein, Human (HEK293, His) is the recombinant human-derived CSRP3 protein, expressed by HEK293, with C-6*His tag.
Species: Human; Source: HEK293 |
|
/
|
| HY-P71372 | Troponin C/TNNC1 Protein, Human (His, solution) |
Troponin C, represented by the TNNC1 gene, centrally regulates striated muscle contraction. In the troponin complex consisting of Tn-I, Tn-T, and Tn-C, Tn-I inhibits the actomyosin ATPase, while Tn-T binds to tropomyosin. Troponin C/TNNC1 Protein, Human (His) is the recombinant human-derived Troponin C/TNNC1 protein, expressed by E. coli , with N-6*His labeled tag.
Species: Human; Source: E. coli |
|
/
|
| HY-P71532 | MYBPC3 Protein, Human (His-SUMO) |
MYBPC3 Protein, positioned in the crossbridge region of vertebrate striated muscle A bands, binds to myosin heavy chain (MHC), F-actin, and native thin filaments, influencing actin-activated myosin ATPase. Its presence suggests potential modulation of muscle contraction, indicating a functional impact on the contractile apparatus, or a structural role in muscle fibers. MYBPC3 Protein, Human (His-SUMO) is the recombinant human-derived MYBPC3 protein, expressed by E. coli , with N-SUMO, N-6*His labeled tag.
Species: Human; Source: E. coli |
|
/
|
| HY-P72275 | Cardiac phospholamban/PLN, Human (P.pastoris, GST) |
Cardiac phospholamban (PLN) strictly regulates ATP2A2 in the cardiac sarcoplasmic reticulum, reversibly inhibits ATPase activity and affects myocardial contractility. Modulation of PLN reduces the affinity of ATPase for Ca(2+), thereby affecting calcium reuptake during muscle relaxation and maintaining cardiac calcium homeostasis. Cardiac phospholamban/PLN, Human (P.pastoris, GST) is the recombinant human-derived Cardiac phospholamban/PLN, expressed by P. pastoris , with N-GST labeled tag.
Species: Human; Source: P. pastoris |
|
/
|
| HY-P71532A | MYBPC3 Protein, Human (HEK293, His) |
MYBPC3 Protein, positioned in the crossbridge region of vertebrate striated muscle A bands, binds to myosin heavy chain (MHC), F-actin, and native thin filaments, influencing actin-activated myosin ATPase. Its presence suggests potential modulation of muscle contraction, indicating a functional impact on the contractile apparatus, or a structural role in muscle fibers. MYBPC3 Protein, Human (HEK293, His) is the recombinant human-derived MYBPC3 protein, expressed by HEK293 , with C-6*His labeled tag.
Species: Human; Source: E. coli |
|
/
|
| HY-P703646 | Tnnt2 Protein, Mouse (His, Flag) |
Tnnt2 Protein, Mouse (His, Flag) is the recombinant mouse-derived Tnnt2, expressed by E. coli , with C-6*His, C-Flag labeled tag. ,
Species: Mouse; Source: E. coli |
|
/
|
| HY-P705691 | Cardiac troponin I/Tnni3 Protein, Human (His) |
Species: Human; Source: E. coli |
|
/
|
| HY-P71372A | Troponin C/TNNC1 Protein, Human (N-His) |
Troponin C, represented by the TNNC1 gene, centrally regulates striated muscle contraction. In the troponin complex consisting of Tn-I, Tn-T, and Tn-C, Tn-I inhibits the actomyosin ATPase, while Tn-T binds to tropomyosin. Troponin C/TNNC1 Protein, Human (N-His) is the recombinant human-derived Troponin C/TNNC1 protein, expressed by E. coli , with N-6*His labeled tag.
Species: Human; Source: E. coli |
|
/
|
| HY-P86432 | Cardiac Troponin T Antibody (YA6124) |
Cardiac Troponin T Antibody (YA6124) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to Cardiac Troponin T.
Host: Rabbit; Reactivity: Human, Mouse, Rat |
|
/
|
| HY-P81877 | Phospholamban Antibody (YA1622) |
Phospholamban Antibody (YA1622) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to Phospholamban.
Host: Rabbit; Reactivity: Human, Mouse, Rat |
|
/
|
| HY-P82974 | Cardiac Troponin T Antibody (YA2719) |
Cardiac Troponin T Antibody (YA2719) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to Cardiac Troponin T.
Host: Rabbit; Reactivity: Human, Mouse, Rat |
|
/
|
| HY-P81144 | Cardiac Troponin I Antibody (YA3484) |
Cardiac Troponin I Antibody (YA3484) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to Cardiac Troponin I.
Host: Rabbit; Reactivity: Human |
|
/
|
| HY-P811586 | Alpha-cardiac actin Antibody (YA10111) |
Alpha-cardiac actin Antibody (YA10111) is a Mouse-derived and non-conjugated IgG1 recombinant monoclonal antibody, targeting to Alpha-cardiac actin.
Host: Mouse; Reactivity: Human, Mouse, Rat |
|
/
|
| HY-P81877A | Phospholamban Antibody (YA1622)(PBS only) |
Phospholamban Antibody (YA1622) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to Phospholamban.
Host: Rabbit; Reactivity: Human, Mouse, Rat |
|
/
|
| HY-P85398 | Cardiac Troponin I Antibody (YA5090) |
Cardiac Troponin I Antibody (YA5090) is a Mouse-derived and non-conjugated monoclonal antibody, targeting to Cardiac Troponin I.
Host: Mouse; Reactivity: Human, Rat, Mouse |
|
/
|
| HY-P85398A | Cardiac Troponin I Antibody (YA5090)(PBS only) |
Cardiac Troponin I Antibody (YA5090) is a Mouse-derived and non-conjugated monoclonal antibody, targeting to Cardiac Troponin I.
Host: Mouse; Reactivity: Human, Rat, Mouse |
|
/
|
| HY-P86427 | Cardiac Troponin I Antibody (YA6119) |
Cardiac Troponin I Antibody (YA6119) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to Cardiac Troponin I.
Host: Rabbit; Reactivity: Human, Mouse, Rat |
|
/
|
| HY-P86834 | Calsequestrin 2 Antibody (YA6527) |
Calsequestrin 2 Antibody (YA6527) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to Calsequestrin 2.
Host: Rabbit; Reactivity: Human, Mouse, Rat |
|
/
|
| HY-K6303 | Human iPSC/ESC Cardiomyocyte Induction Differentiation Kit |
MCE Human iPSC/ESC Cardiomyocyte Induction Differentiation Kit is based on the classical GiWi system. By precisely modulating the Wnt/β-catenin signaling pathway in a temporally controlled manner (sequential activation and inhibition), the kit enables highly efficient directed differentiation of human pluripotent stem cells into cardiomyocytes. It is suitable for cardiac disease modeling, drug cardiotoxicity assessment, and mechanistic studies. |
|
/
|
Targets/Pathways































































































































































































































































































































































































































































































































































































































































































































































































































































































































