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PROTAC, which exploit the ubiquitin-proteasome pathway to specifically degrade target proteins. PROTACs not only solve the problem of undruggability but they also have other advantages compared to traditional drug targeting strategies.
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PROTAC — Target Selection and Design
2022-07-08
A PROTAC molecule consists of three components: a target protein binding ligand, an E3 ligase ligand, and a linker connecting these two moieties. Here, we will discuss the conventional approaches for the rational design of PROTAC molecules. -
Organoids represent an important bridge between 2D cultures and in vivo mouse/human models. The organoid technology exerts enormous potential in evaluation of efficacy and toxicity of drugs, regenerative medicine, and precision medicine.In this article, we will briefly introduce organoid technology.
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Development of Intestinal Organoid
2022-07-28
3D organoid is one of the revolutionary developments in biomedical field during the past 10 years. The establishment of intestinal organoids is an important milestone in the development of organoid technology. -
BacPROTACs is composed of a POI ligand, a chemical linker and a ClpCNTD anchor. BacPROTACs can induce in vitro and in vivo degradation of non-eukaryotic proteins in bacteria without the ubiquitin proteasome system.
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RNA therapeutics have changed the landscape of drug development, which possess broader spectrum of drug targets, simplicity and efficiency in development and manufacturing.In this article, we will discuss the underlying mechanisms of RNA-based drugs on the market or in clinical stages.
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Organoids have great potential in research of organ development, disease modeling, drug screening and, precision and regenerative medicin. In this article, we will expalin the origin of the organoids. Adult stem cells (ASCs) or pluripotent stem cells (PSCs) , which is the better choice.
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Autophagy, derived from the Greek meaning "eating of self", plays an indispensable role in maintaining homeostasis. p27 is an inhibitor of cyclin CDKs, but how p27 regulates autophagy remains unknown. This article will cover the mechanism of autophagy and p27-related cell cycle regulation.
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AlphaFold2 can predict disease-related protein structures at low cost, and then find potential drugs for these diseases through drug repositioning, virtual screening, and other methods. ZINC is a public database summarizing information about billions of compounds. AlphaFold2 + ZINC20 speeds up the virtual screening process and improves the computing speed.
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CMA (chaperone-mediated autophagy) plays an essential role in maintaining neuronal protein stability and preventing neurodegeneration. In this article, we will comprehensively clarify the role of CMA in the occurrence and development of neurodegenerative diseases.
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As powerful pain relievers, the opioids morphine and fentanyl have been "checked" by their side effects (listed as controlled substances). How to reduce its side effects? What is its mechanism? This research will explore its mechanism.
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Understanding the mechanism of aging not only has guiding significance for prolonging human life but also has important clinical significance for the prevention and treatment of diseases in the elderly population , thus, improving their life quality and well-being.
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The latest study of Cell magazine "Neural mechanism underlying depressive-like state associated with social status loss" considers social factors as a breakthrough point. It has been found that the downward transition of social status induces depression-like behavior in mice whereas improves the depressive state by restoring their social environment.
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PROTAC - Design Strategy for Targeting
2023-04-23
Protein degradation targeting chimera (PROTAC) is a technology that uses the ubiquitin proteasome pathway to silent target protein. However, PROTAC still has problems such as solubility, membrane permeability, and selectivity. In this article, we have summarized three strategies for optimization: light-controlled linker, PAC molecule, and specific E3 ligase. -
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. -
How to Perform Western Blot?
2023-07-13
Western blot is one of the most frequently performed experiments in molecular biology, biochemistry and immunology. This article describes in detail how to do WB. -
Organoid Culture: Questions & Answers
2023-07-26
In the last issue, we conducted a live lecture on the theme of organoid culture. Today, we have a special topic to solve your doubts in the last live class! -
WHO's Q2 drug list has been updated. Let's take you through the list of the most noteworthy small molecule drugs that we should pay attention to.
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FDA Approved Drug List!
2023-09-14
In the first half of 2023 (as of June 27), the FDA approved 26 new drugs, let's take you learn about it through the article. -
SPR, which stands for Surface Plasmon Resonance, essentially works by detecting the interaction between ligands and analytes on a biosensor chip. This in turn allows us to probe the properties and structure of substances. With this technology, we can analyze molecules, proteins, DNA, and various organic and inorganic substances in samples in real-time with precision.
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Science | A "new" mechanism for non-ubiquitinated Midnolin-proteasomal degradation pathway
2024-04-26
“ubiquitin-mediated protein degradation” won the Nobel Prize in Chemistry in 2004! In fact, proteasomes degrade not only ubiquitinated proteins but also non-ubiquitinated ones. The mechanism remains shrouded in mystery. After reading this piece today, you might have a lightbulb moment! -
Common Questions and Solutions for WB
2024-05-09
Come to understand the common problems and solutions of WB, and better complete the experiment! -
Exosomes, which won the Nobel Prize in 2013, are still a research hotspot in the national natural sciences, and their popularity has only increased over the past decade (in 2022, they still rank 5th in the national natural sciences hotspots!). Why have exosomes become the darling of scientific research? Let's take a look together~
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Degrade target proteins through the autophagy-lysosome pathway including LYTAC, AUTAC, and ATTEC have gained increasing attention in recent years due to their significant research potential!
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Streptavidin-Biotin System
2024-08-03
Streptavidin strongly binding small molecule biotin is one of the most popular non-covalent coupling methods. Streptavidin can be coupled to various carriers such as magnetic beads and agarose matrix, and become a highly specific affinity medium to capture various biotin-labeled ligands. -
2024 Nobel Prize Announcements! Curious about the details? Click to dive into the exciting developments!
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Delve into the intricate networks that govern mitochondrial quality control. By examining key mechanisms such as biogenesis, mitochondrial dynamics (fission and fusion), proteolysis, and mitophagy.
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In early January 2025, MIT Tech Review unveiled its annual list of top 10 breakthrough technologies poised to redefine the future. Among these, stem cell therapy stood out for its potential to treat diverse diseases—including neurodegenerative disorders, diabetes, cancer, and heart failure. This groundbreaking approach uses stem cells to replace damaged cells, offering hope for millions worldwide.
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When you hear "inflammation" and "DNA damage," you might immediately think of disease or injury. However, in brains, these two processes are key steps in forming long-term memories, particularly related to specialized cells in our brain called hippocampal neurons.
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Autophagy is a fundamental process that degrades various components within the cell.
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nside cells, the homeostasis and degradation of proteins is a precisely regulated process. If proteins cannot be degraded in time, it may lead to the occurrence of various diseases such as neurodegenerative diseases and cancer. This article will tell you the process of how proteins are recognized, labeled and then degraded!
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As a pivotal branch in the post - genomic era, proteomics is committed to comprehensively elucidating the types, abundances, structures, functions, and interactions of all proteins within living organisms. This article will tell you the key steps of proteomics sample preparation based on mass spectrometry. This article will tell you the key steps of proteomics sample preparation based on mass spectrometry.
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Western blotting is a crucial and fundamental technique in life science research. It plays a significant role in exploring protein expression and function. The following article will comprehensively and thoroughly elaborate on the specific procedures and detailed key points of this experiment.
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In protein biology, Co-IP is a powerful tool to uncover protein "social networks." But poorly performed, it easily becomes an awkward lab "meet-and-greet." Today, we discuss making Co-IP experiments elegant and efficient—so you pull down target proteins with confidence and precision.
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Have you ever noticed that after staying up late, your appetite—especially for high-calorie foods—gets out of control? If this sounds familiar, today’s article might offer some good news.
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For all the protein research folks out there, techniques like IP and Co-IP are no stranger, right? And of course, there's a faster and more convenient go-to tool—Protein A/G magnetic beads! In this article, let's chat about how these beads work their magic in classic experiments like IP and Co-IP.
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Microglia– the only immune cells within the brain parenchyma. With advancements in imaging technologies, people’s understanding of microglia has shifted from being viewed as 'resting' cells to 'highly active' cells, particularly due to their dynamic processes that seem to be probing surrounding tissues and monitoring neuronal activity. This has made microglia a focal point of research in the field of neuroscience.
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Exosomes—natural nanoscale carriers—are revolutionizing targeted therapy. This article uncovers the science behind their precision in drug delivery.
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Cracking the PROTAC Permeability Barrier: CD36-Mediated Endocytosis as a Potential Breakthrough
2025-12-03
This article provides an in-depth analysis of cutting-edge literature revealing CD36 as a key mediator of cellular uptake for PROTACs and bRO5 compounds. By structurally optimizing PROTAC molecules to enhance their affinity for CD36, membrane permeability can be markedly improved, leading to significantly enhanced antitumor efficacy. -
Efficient Generation of Mouse Small Intestinal Organoids: A Complete Experimental Protocol Guide
2025-12-10
How to successfully create mouse small intestine organoids? A detailed, hands-on guide to the entire process, all in one article! -
Molecular glue degraders have evolved from a serendipitous observation to one of the most dynamic and transformative fields in biomedical research.
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Targeting the ‘Undruggable’ with PROTACs
2025-06-18
This review introduces the fundamental principles and mechanisms of PROTACs, highlights recent advances in molecular design and clinical development, and discusses emerging opportunities and remaining challenges in targeted protein degradation. -
Advances in Alzheimer's Disease Research
2025-07-16
This review summarizes current understanding of AD pathophysiology, including amyloid and tau pathology, neuroinflammation, synaptic dysfunction, and vascular abnormalities, and evaluates therapeutic strategies and experimental models. -
This review critically examines the role of the JAK-STAT pathway in immunity and autoimmune diseases, reviews current clinical applications of targeted therapies, and highlights emerging trends in autoimmune drug development.
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This review discusses recent progress in molecular glue technologies, illustrating how targeted protein degradation strategies enable the modulation of previously undruggable proteins.
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This review highlights the roles of microglia in AD pathology, focusing on metabolic reprogramming and microglia-targeted therapeutic strategies.
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This review summarizes the hallmarks of aging and aging-related diseases, discusses mechanistic insights into aging processes, and highlights emerging anti-aging interventions.
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This review outlines macrophage functions and classification, and provides practical experimental guidelines for macrophage differentiation, polarization, and identification.
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Review advances in target discovery, disease modeling, and biomarkers for Parkinson’s disease, highlighting their interplay and future directions for translational research.
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The Dual Role of Cellular Senescence in Cancer: Mechanisms, Microenvironment, and Therapeutics
2026-05-21
Explore the dual role of cellular senescence in cancer, including tumor suppression, SASP-driven tumor promotion, senescence heterogeneity and plasticity, and advances in senescence-targeted therapies. -
Explore the mechanisms driving immune tolerance breakdown in autoimmune diseases and emerging tolerance-restoring strategies, with a focus on IL-2-based immune modulation.
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Review the evolution of molecular glues from serendipitous discovery to rational design, highlighting how emerging targets and advances in screening, proteomics, structural biology, and AI are expanding the druggable proteome.
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Explore how anti-Aβ therapy is reshaping the AD treatment landscape, the rationale for multi-pathology combination strategies, and advances in biomarker-guided precision treatment.
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Explore how mitochondrial quality control, inflammatory signaling, and metabolic–epigenetic reprogramming regulate cellular senescence and the SASP, along with strategies to restore mitochondrial homeostasis.
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AZD5991, a macrocyclic molecule with high selectivity for Mcl-1, reduces Mcl-1 protein in AZD5991-sensitive but not in AZD5991-resistant MM cell lines.
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CF53 is a highly potent, selective and orally active inhibitor of BET protein, with anti-tumor activity in acute leukemia and breast cancer cell lines.
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HJB97 is a BET PROTAC inhibitor with good anti-tumor activity, and effectively blocks the degradation of BRD2, BRD3, and BRD4 proteins induced by BETd-260.
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BR351 is a Brain Penetrant MMP Inhibitor
2019-04-05
BR351 is a brain penetrant MMP inhibitor, and a potential tool for the molecular imaging of activated MMPs with PET, with an IC50 in the nanomolar range. -
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. -
COH000 is an allosteric, covalent and irreversible inhibitor of SUMO-activating enzyme, with an IC50 of 0.2 μM for SUMOylation in vitro.
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PhiKan 083 is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a Kd of 167 μM.
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IITZ-01 is a potent lysosomotropic autophagy inhibitor with single-agent antitumor activity, with an IC50 of 2.62 μM for PI3Kγ.
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Y06036 is a potent and selective BET inhibitor for potential treatment of castration-resistant prostate cancer. With nanomolar inhibition.
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Y06137 is a potent and selective BET inhibitor, which binds to the BRD4(1) bromodomain with a Kd of 81 nM. Antitumor activity.
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NRX-252262 is a β-catenin:β-TrCP interaction enhancer, and its cognate E3 ligase, SCFβ-TrCP, induces mutant β-catenin degradation, with an EC50 of 3.8 nM
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TAK-981 is a selective inhibitor of the SUMOylation enzymatic cascade, with potential immune-activating and antineoplastic activities
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TD-428 is a Highly Specific BRD4 Degrader
2019-04-29
TD-428, a immunomodulatory drug analog, is a highly specific BRD4 degrader with a DC50 of 0.32 nM. TD-428 reduces c-Myc levels more efficiently than JQ1. -
SLLN-15 is an oral activ enhancer of autophagy that activates cytostatic macroautophagy/autophagy in triple-negative breast cancer (TNBC).
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A1874 is a nutlin-based and BRD4-degrading PROTAC with a DC50 of 32 nM. Effective in inhibiting many cancer cell lines proliferation
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BSJ-03-123, a Degrader with Proteome-wide Selectivity for CDK6 (PROTAC). Induces a G1 cell-cycle arrest without a measurable increase in apoptosis.
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FT671 is a potent, non-covalent and selective USP7 inhibitor with an IC50 of 52 nM and binds to the USP7 catalytic domain with a Kd of 65 nM.
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ZM223 is a non-sulfamide NEDD8 activating enzyme (NAE) inhibitor, with IC50 value of 100 nM in cells. ZM223 has potential to treat colon cancer.
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ACY-1083, a Highly Selective HDAC6 Inhibitor, Reverses Chemotherapy-induced Peripheral Neuropathy
2019-05-12
ACY-1083 is a selective and brain-penetrating HDAC6 inhibitor with an IC50 of 3 nM. ACY-1083 effectively reverses chemotherapy-induced peripheral neuropathy -
MS4077 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) with a Kd of 37 nM for binding affinity to ALK. Efficacy for breast cancer and lung cancer.
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VL285, is a Potent VHL Ligand
2019-05-24
VL285 is a Potent VHL Ligand. -
SNIPER(TACC3)-1 targets the TACC3 protein for degradation via the ubiquitin-proteasome pathway. SNIPER(TACC3)-1 induces cancer cell death.
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IWP-O1, a Highly Potent Porcupine Inhibitor, Functions by Preventing the Secretion of Wnt Proteins
2019-06-03
IWP-O1 is a Porcupine (Porcn) inhibitor, with an EC50 of 80 pM in L-Wnt-STF cells. IWP-O1 functions by preventing the secretion of Wnt proteins[ -
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%. -
JMS-17-2 is a CX3CR1 Antagonist
2019-06-12
JMS-17-2 is a potent and selective CX3CR1 antagonist with an IC50 of 0.32 nM. Has potential to treat cancers such as breast cancer. -
TAS4464 is a highly potent and selective inhibitor of NEDD8 activating enzyme (NAE), with an IC50 of 0.955 nM. TAS4464 shows antitumor activity.
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ERD-308 is a highly potent PROTAC degrader of ER for ER+ breast cancer treatment. ERD-308 induces >95% of ER degradation at concentrations as low as 5 nM.
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JG-98, an Hsp70 inhibitor, binds tightly to a conserved site on Hsp70 and disrupts the Hsp70-Bag3 interaction. JG-98 shows anti-cancer activities.
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MZP-55 is a selective PROTAC degrader of BRD3/4, shows no obvious effect on BRD2. MZP-55 exhibits excellent activity in cancer research.
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dBET6 is a potent PROTAC degrader of BET, shows high affinity to BRD4(1), and possess good efficacy in T cell acute lymphoblastic leukemia activity.
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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. -
MT-802 is a potent BTK degrader based on PROTAC technology, with a DC50 of 1 nM. MT-802 has potential to treat C481S mutant chronic lymphocytic leukemia.
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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. -
dMCL1-2 is a potent and selective degrader of myeloid cell leukemia 1 (MCL1) based on PROTAC, which binds to MCL1 with a KD of 30 nM.
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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. -
ARV-825 is a PROTAC, and acts as a potent BRD4 degrader, with Kds of 90 and 28 nM for BRD4 BD1 and BRD4 BD2, respectively.
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GMB-475 is a PROTAC BCR-ABL1 degrader, overcomes BCR-ABL1-dependent drug resistance, targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel Lindau.
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dBET57 is a potent and selective degrader of BRD4BD1 based on the PROTAC technology and mediates recruitment to the CRL4CRBN E3 ubiquitin ligase.
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MD-224 is a human MDM2 degrader based on the PROTAC concept. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells.
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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. -
PK11007 is a Mild Alkylating Agent with Anticancer Activity and induces mutant p53 cancer cell death by increasing reactive oxygen species (ROS) levels.
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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. -
MG-277 works as a PROTAC molecular glue, inducing degradation of a translation termination factor, GSPT1 to achieve its potent anticancer activity.
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MS432 is a first-in-class and highly selective PD0325901-based VHL-recruiting PROTAC degrader for MEK1 and MEK2 with good anti-cancer activity.
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KB02-JQ1 is a highly potent and selective PROTAC BRD4 degrader that degrades nuclear proteins by engaging CUL4-DDB1 E3 ubiquitin ligases DCAF16.
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M8891 is an orally active, reversible and brain penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor with antiangiogenic and antitumoral activity.
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TCH-165 is a modulator of proteasome assembly, which increases 20S levels and facilitates 20S-mediated protein degradation, such as IDPs, α-syn, and tau.
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6RK73 is a covalent irreversible and specific UCHL1 inhibitor,which specifically inhibits UCHL1 activity in breast cancer.
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Ro 90-7501, an Aβ42 fibril assembly inhibitor, inhibits PP5 in a TPR-dependent manner and has radiosensitizing effects on cervical cancer cells.
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CCT367766, a PROTAC-based Pirin-targeting PDP, exhibits a moderate affinity for the CRBN-DDB1 complex and reveals a good affinity for Pirin and CRBN.
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E64FC26 is a highly potent pan-style inhibitor of the protein disulfide isomerase (PDI) family with anti-myeloma activities.
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NU1025 is a potent PARP inhibitor and potentiates the cytotoxicity of ionizing radiation drug. NU1025 has anti-cancer and neuroprotective activity.
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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 . -
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. -
ARCC-4 is a low-nanomolar AR degrader, and effectively degrades clinically relevant AR mutants associated with antiandrogen therapy.
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UT-34 is a potent, selective and orally active second-generation pan-androgen receptor (AR) antagonist and degrader with anti-prostate cancer efficacy.
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HM03 is a potent and selective HSPA5 inhibitor with anticancer activity. HSPA5 plays a key role in monitoring protein transport through the cell.
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XZ739 is a PROTAC BCL-XL Degrader
2020-06-18
XZ739 is a PROTAC BCL-XL Degrader. XZ739 is potent against various cancer cell lines. PROTAC is an emerging therapeutic modality. -
JCN037 is a potent, non-covalent, and brain-penetrant EGFR tyrosine kinase inhibitor. JCN037 has potent anti-cancer activity.
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RA-9 is a potent and selective proteasome-associated DUBs inhibitor with favorable toxicity profile and anticancer activity.
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HLI373 represents a potential drug-able lead for the development of therapeutically efficacious inhibitors of Hdm2. Hdm2 is an ubiquitin protein ligase.
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RA375, a RPN13 inhibitor, inhibits proteasome function in muscle. RA375 is highly active against cell lines of multiple myeloma and diverse solid cancers.
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KCC-07 prevents binding of MBD2 to methylated DNA and activates BAI1 inducing anti-proliferative BAI1/p53/p21 signaling. Anticancer activity.
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MPT0G211, an orally active and selective HDAC6 inhibitor, ameliorates tau phosphorylation, and cognitive deficits in an Alzheimer’s disease model.
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RapaLink-1, a third-generation bivalent mTOR inhibitor, potently blocking cancer-derived, activating mutants of mTOR. It can cross the blood-brain barrier.
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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. -
BSJ-04-132 is a potent and selective Ribociclib-based CDK4 degrader (PROTAC) and does not induce CDK6 and IKZF1/3 degradation with anti-cancer activity.
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BSJ-03-204 is a potent and selective Palbociclib-based CDK4/6 dual degrader (PROTAC) and does not induce IKZF1/3 degradation with anti-cancer activity.
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KB02-SLF is a PROTAC-based nuclear FKBP12 degrader. KB02-SLF promotes nuclear FKBP12 degradation by covalently modifying DCAF16 (E3 ligase).
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DT2216 is a potent and selective BCL-XL degrader based on PROTAC technology. DT2216 inhibits leukemia and has potent anti-cancer activity.
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dTRIM24 will be a useful tool to further probe the function of TRIM24 by rapid chemical depletion in hematopoietic cancers and other biological contexts.
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ZXH-3-26 is a Selective PROTAC BRD4 Degrader
2020-11-17
ZXH-3-26 is a Selective PROTAC BRD4 Degrader and allows pharmacologic targeting of BRD4 without significant inhibition or degradation of BRD2/3. -
BETd-260 is a Potent PROTAC BET Degrader
2020-11-18
BETd-260 is a highly potent, efficacious, and promising BET degrader. -
SIAIS178 is a potent and selective BCR-ABL degrader based on PROTAC technology by recruiting VHL E3 ubiquitin ligase. SIAIS178 has anticancer activity.
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GNE-987, a potent chimeric BET degrader, exhibits picomolar cell BRD4 degradation activity. GNE-987 can be used in PROTAC-Antibody Conjugate (PAC).
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BI-3663 is a highly selective PTK2/FAK PROTAC (DC50=30 nM), with cereblon ligands to hijack E3 ligases for PTK2 degradation.
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dFKBP-1 induces potent and dose-dependent degradation of FKBP12 in 293FT-WT cells. A facile and general new strategy to control target protein stability.
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UNC6852 is a chemical degrader that targets polycomb repressive complex 2 (PRC2). Anti-proliferative in diffuse large B cell lymphoma cell lines.
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VZ185 is a highly selective, potent, and rapid dual degrader with a slight preference for BRD9 over BRD7.
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PQR530 is a potent, ATP-competitive, orally bioavailable and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor. Antitumor activity.
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MZP-54 is a Selective BRD3/4 PROTAC Degrader
2020-12-02
MZP-54 is a PROTAC that would link together specific VHL ligand and BET bromodomain ligand. MZP-54 induces degradation of BRD3/4. -
CHDI-390576, a potent and CNS penetrant class IIa HDAC inhibitor, show selectivity over class I HDACs, HDAC8 and the class IIb HDAC6 isoform.
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BI-3802, a BCL6 degrader, inhibits the BCL6 BTB domain. BI-3802 induces the polymerization of BCL6 and promotes BCL6 degration depended on E3 ligase SIAH1.
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JH-XI-10-02, a highly Potent CDK8 Degrader, modulates the CDK8 protein levels. A viable therapeutic strategy in cancer.
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dCBP-1 is a potent and selective degrader of p300/CBP based on PROTAC. dCBP-1 is exceptionally potent at killing multiple myeloma cells.
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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. -
NAZ2329 is an allosteric, noncompetitive and reversible inhibitor of R5 RPTP subfamily and PTPRZ/PTPRG with anti-cancer activity.
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BrBzGCp2 is a Glyoxalase 1 (GLO1) inhibitor for a variety of disorders. Possesses antitumor and neuroprotective activity.
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Conglobatin inhibits proliferation and induces apoptosis by binding to N-terminus of Hsp90 and disrupting Hsp90-Cdc37 complex formation.
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YUM70 inhibits GRP78. Induces endoplasmic reticulum stress-mediated apoptosis. Pancreatic cancer. Acts as a novel anticancer agent.
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LC-2 is a potent and first-in-class PROTAC capable of degrading endogenous KRAS G12C, with DC50s between 0.25 and 0.76 μM.
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ML-00253764 is a brain penetrant nonpeptidic melanocortin receptor 4 (MC4R) antagonist with a Ki/IC50 of 0.16 µM/0.103 µM, respectively.
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PROTAC MDM2 degrader MD-222 is highly potent and effective in inducing degradation of MDM2 and in activating wild-type p53 in cells.
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Butaprost is a selective prostaglandin E receptor (EP2) agonist. Butaprost can effectively mitigate kidney fibrogenesis in various fibrosis models.
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Lenalidomide, a CRBN ligand, is an orally active immunomodulator that effective treatment for myelodysplastic syndrome and multiple myeloma.
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AUTAC4 is a mitochondria-targeting autophagy-targeting chimera, which can be used for the study of mitochondrial dysfunction.
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ARV-110 is an orally active, specific androgen receptor (AR) PROTAC degrader. ARV-110 can be used for the research of prostate cancer.
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Vorasidenib is an orally available, brain penetrant second-generation dual mutant isocitrate dehydrogenases 1 and 2 (mIDH1/2) inhibitor.
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BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC). BSJ-4-116 exhibits potent antiproliferative effects.
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EMD527040 is a highly selective αvβ6 antagonist with antifibrotic activities.
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SJ6986 is a selective and orally active GSPT1/GSPT2 degrader, displaying selectivity over classical IMiD neosubstrates, such as IKZF1/3
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DP-C-4 is a CRBN-Based dual PROTAC for EGFR and PARP could provide an effective study for cancer diseases.
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XY028-140 is a potent and selective PROTAC-based CDK4/6 degrader, which can inhibit RB-E2F signaling and reduce CDK4 and CDK6 protein levels.
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NRX-2663 is a potent enhancer of the interaction between β-catenin SCFβ-TrCP, potentiates the ubiquitylation of mutant β-Catenin by β-TrCP.
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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. -
Iberdomide (CC-220) is an orally active cereblon (CRBN) E3 ligase modulator (CELMoD) with antitumor and immunostimulatory activities。
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GSK2606414 is an orally available PERK inhibitor and is a potent compound of cancer and neurological diseases.
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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. -
SB 258719 is a selective 5-HT7 receptor antagonist and can be used for the research of cancer and neurological disease.
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MB710 is a stabilizer of oncogenic p53 mutation Y220C. MB710 binds to the Y220C pocket and stabilizes p53-Y220C, with a Kd of 4.1 μM.
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Trolox is an analogue of vitamin E with a powerful antioxidant effect. Trolox is also a powerful inhibitor of membrane damage.
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AZD1390 is a potent, highly selective, orally bioavailable, brain-penetrant ATM inhibitor with an IC50 of 0.78 nM.
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MS4322 is a first-in-class PRMT5 degrader and a valuable chemical tool for exploring the PRMT5 functions in vitro and in vivo.
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MS170 is a PROTAC AKT Degrader
2022-02-27
MS170 is a CRBN-recruiting degrader, the AKT proteolysis targeting chimera (PROTAC) degrader. -
AUTAC2 is a FKBP12-targeting autophagy-mediated degrader (AUTAC). AUTAC2 contains an FBnG and an SLF moiety.
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Oprozomib (PR-047) is an orally active peptide epoxyketone proteasome inhibitor.
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Epoxomicin is an epoxyketone-containing natural product and a selective and irreversible proteasome inhibitor. Cross the blood-brain barrier.
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DD1, a proteasome inhibitor, targets Bax activation and P70S6K degradation during acute myeloid leukemia (AML) apoptosis.
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PU-H54 is a potent purine-based (PU) Grp94-selective inhibitor. PU-H54 has the potential for the research of breast cancer.
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MS159 is a frist-In-class nuclear receptor binding SET NSD2 PROTAC degrader for multiple myeloma research.
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ARV-471 is an oral estrogen receptor PROTAC degrader for breast cancer. ARV-471 robustly degrades ER in ER-positive breast cancer cell lines.
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AZD-9574 is a potent and brain penetrant PARP1 inhibitor and shows >8000-fold selectivity for PARP1 compared to PARP2/3/5a/6.
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ARD-69 is a potent PROTAC androgen receptor degrader and induces degradation of AR protein in AR-positive prostate cancer cell lines.
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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. -
Golcadomide is a potent and orally active CRBN E3 ligase modulator with immunomodulating and antineoplastic activities.
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U7D-1 is a selective USP7 PROTAC degrader. U7D-1 induces apoptosis in Jeko-1 cells and shows anticancer activity.
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Olutasidenib (FT-2102) is an orally active, brain penetrant inhibitor of mutant IDH1. Olutasidenib is used for AML or MDS Research.
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A947 is a selective SMARCA2 (PROTAC). A947 also is a moderately selective SMARCA2 degrader. A947 can be used for the research of cancer.
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SJ988497 is a cell permeable PROTAC JAK2 degrader that degrades JAK2 in vitro and in vivo, and shows anticancer activity against leukemia.
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MMRi62, a Ferroptosis inducer targeting MDM2-MDM4. MMRi62 shows a P53-independent pro-apoptotic activity against PDAC cells.
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TD1092 is a pan-IAP degrader, degrades cIAP1, cIAP2, and XIAP. TD1092 inhibits NF-κB pathway and epithelial-mesenchymal transition (EMT).
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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). -
YX-2-107 is a PROTAC that selectively degrades CDK6.
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SZUH280, a potent and selective PROTAC HDAC8 degrader, ,shows antitumor activity in an A549 nude mouse model.
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MS8815 is a selective EZH2 PROTAC degrader. MS8815 can be used for the research of triple-negative breast cancer (TNBC),
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J-113397 is a potent and selective nonpeptidyl ORL1 receptor antagonist without any agonistic effects on other opioid receptors.
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dBRD9 is a PROTAC (proteolysis targeting chimera) and can be used as a selective valuable probe for degrading BRD9.
Products
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All
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Inhibitors & Agonists
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Isotope-Labeled Compounds
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Fluorescent Dye
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Peptides
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Screening Libraries
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Kits
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Reference Standards
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GMP Small Molecules
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Biochemical Assay Reagents
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Natural Products
| Cat. No. | Product Name | Information | Application | Publication |
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| HY-L028 | CNS-Penetrant Compound Library |
The blood-brain barrier (BBB) is the complex network of brain microvessels. It protects the brain from the external bloodstream environment and supplies the brain with the required nutrients for normal function. However, blood-brain barrier is also the obstacle to deliver beneficial drugs to treat CNS (central nervous system) diseases or brain tumors, as it has the least permeable capillaries in the entire body due to physical barriers (tight junctions). Therefore, it is crucial to discover drugs which can cross this barrier for the treatment of brain-based diseases, such as Alzheimer’s disease (AD), Parkinson’s disease (PD) and epilepsy.
MCE offers a unique collection of 1,170 compounds with confirmed CNS-Penetrant property. It’s a useful tool for the discovery of drugs used for brain diseases, such as brain tumors, mental disorders, and neurodegenerative diseases.
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91
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| HY-L089 | Mitochondria-Targeted Compound Library |
Mitochondria plays an important role in many vital processes in cells, including energy production, fatty-acid oxidation and the Tricarboxylic Acid (TCA) cycle, calcium signaling, permeability transition, apoptosis and heat production. At present, it is recognized that many diseases are associated with impaired mitochondrial function, such as increased accumulation of ROS and decreased OXPHOS and ATP production. Mitochondria are recognized as one of the most important targets for new drug design in cancer, cardiovascular, and neurological diseases, etc. Some small molecule drugs or biologics can act on mitochondria through various pathways, including ETC inhibition, OXPHOS uncoupling, mitochondrial Ca2+ modulation, and control of oxidative stress via decrease or increase of mitochondrial ROS accumulation.
MCE supplies a unique collection of 1,182 mitochondria-targeted compound that mainly targeting Mitochondrial Metabolism, ATP Synthase, Mitophagy, Reactive Oxygen Species, etc. MCE Mitochondria-Targeted Compound Library is a useful tool for mitochondria-targeted drug discovery and related research.
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89
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| HY-L063 | Chemical Probe Library |
Chemical probes are simply reagents with high potency, selectivity and cell-permeability which play important roles in both fundamental and applied biological research. In their most common application, chemical probes can establish the tractability of a specific target. They are used to interrogate the relationship between a target and its phenotype (biological tractability) as well as an ability to modulate that phenotype using a small molecule. Otherwise, chemical probes also have had a major impact in enabling and accelerating discoveries along the path to pioneer medicines. They have helped to improve the understanding of targets and pathways and have created opportunities for proprietary drug discovery efforts to an extent that would not have been possible otherwise.
MCE provides a unique collection of 282 chemical probes with high potency (at least 100 nM potency), selectivity (at least 10-fold selectivity against any other target) and cell-permeability (at least 10 μM potency). MCE Chemical probe library is a useful tool for target identification and mechanism research.
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84
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| HY-L0116V | Asinex Macrocycles for RNA Library |
Macrocycles are promising scaffolds for the design of novel RNA targeting molecules. This collection of macrocycles for RNA consists of very diverse, drug-like molecules which incorporate certain known RNA-recognition elements (e.g. nucleobase ring systems and analogs) distributed within macrocyclic rings or peripheral fragments. As macrocyclic molecules tend to be larger than traditional screening molecules, it is vital to carefully assess and control their physicochemical properties. All macrocycles have been tested for aqueous and DMSO solubility with cutoffs applied at 10 mM in DMSO and 50 µM in PBS (pH 7.4); PAMPA permeability has also been tested for representative set of macrocycles.
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83
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| HY-L0123V | Life Chemicals CNS Focused Screening Library |
The incidence and significance of central nervous system diseases are increasing at an alarming rate all over the world. Although substantial research efforts have been applied to develop new CNS-active drugs, only a few CNS disorders are addressed satisfactorily, while the remaining ones pose significant clinical challenges. Blood-brain barrier (BBB) permeability is one of the most important limiting factors in the design and development of novel CNS-targeted pharmaceuticals for the treatment of neurological disorders.
Carefully selected from the HTS Compound Collection to meet the parameters optimized for high BBB-permeability, our CNS Focused Screening Library comprising over 30,300 structurally-diverse and potentially CNS-active screening compounds. This original Screening Compound Library is aimed at supporting CNS drug design projects and HTS efforts in search for novel neurotherapeutics.
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83
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| HY-L137 | Molecular Glue Compound Library |
Targeted protein degradation(TPD) is a novel and promising approach to new drug discovery and development. It shows great potential for treating diseases with “undruggable” pathogenic protein targets and for overcoming drug resistance. Molecular glues and PROTACs are both targeted protein degraders that have attracted the most attention.
Molecular glues are small molecular degraders that mainly induce novel interaction between an E3 ligase and a target protein to form a ternary complex, leading to protein ubiquitination and subsequent proteasome degradation. Compared with PROTACs, molecular glues generally possess more favorable drug-like properties, such as lower MW, higher cell permeability, and better oral absorption. Molecular glues are emerging as a promising new therapeutic strategy.
MCE supplies a unique collection of 124 molecular glues which target various proteins. MCE Molecular Glue Compound Library is a useful tool to conduct scientific research and disease mechanism study.
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83
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| HY-L144 | Mitochondrial Protection Compound Library |
Normal mitochondrial function is critical for maintaining cellular homeostasis because mitochondria produce ATP and are the major intracellular source of free radicals. Cellular dysfunctions induced by intracellular or extracellular insults converge on mitochondria and induce a sudden increase in permeability on the inner mitochondrial membrane, the so-called mitochondrial membrane permeability transition (MMPT). MMPT is caused by the opening of pores in the inner mitochondrial membrane, matrix swelling, and outer membrane rupture. The MMPT is an endpoint to initiate cell death because the pore opening together with the release of mitochondrial cytochrome c activates the apoptotic pathway of caspases.
The normal operation of mitochondrial function is important for maintaining normal cell death and treatment of mitochondrial diseases. MCE offers a unique collection of 1,112 compounds with identified and potential mitochondrial protective activity. MCE Mitochondrial Protection Compound Library is critical for drug discovery and development.
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83
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| HY-L919 | MCE CNS BBB Lead-like Library |
With the aging population and increasing competitive pressures, neurodegenerative diseases of the central nervous system (CNS) have become a serious medical challenge in modern society, including Parkinson's disease, Alzheimer's disease, brain tumors, and multiple sclerosis. However, the success rate of CNS drug development remains remarkably low, primarily due to the blood-brain barrier (BBB).
The blood-brain barrier (BBB) is a semipermeable barrier structure that surrounds the microvasculature of the CNS. In capillaries, the wedged endothelial cells are tightly packed and wedge-shaped, lining the interior of the vessels to form extensive tight junctions. Along with a range of receptors, transporters, efflux pumps, and other cellular components, this barrier regulates the entry and exit of molecules between the bloodstream and the brain. The intact BBB blocks the passage of most blood-borne substances into the brain, preventing nearly 100% of large-molecule drugs and over 98% of small-molecule drugs from entering.
Compared to non-CNS drugs, physicochemical properties such as hydrogen bonds, lipophilicity, and molecular weight significantly influence a compound's ability to cross the BBB. Using artificial intelligence (AI) algorithms to predict BBB permeability, a predicted value greater than 0.75 indicates that the compound has strong potential to cross the BBB, providing a promising starting point for CNS drug discovery.
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83
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| HY-L920 | CNS MPO Lead-like Library |
With the aging population and increasing competitive pressures, neurodegenerative diseases of the central nervous system (CNS) have become a serious medical challenge in modern society, including Parkinson's disease, Alzheimer's disease, brain tumors, and multiple sclerosis.
The CNS MPO (Multi-Parameter Optimization) score is a widely recognized algorithm in medicinal chemistry. Developed by Pfizer, this method is based on an analysis of approved CNS drugs and their interior CNS drug candidates, establishing the CNS MPO rules. It incorporates six key physicochemical properties (ClogP, ClogD, MW, TPSA, HBD, and pKa) to prospectively optimize CNS drug attributes—such as high blood-brain barrier (BBB) permeability, low P-gp efflux liability, low metabolic clearance, and high safety—thereby improving the clinical success rate of CNS drug candidates.
The CNS MPO compound library is a collection of compounds with CNS MPO scores greater than 5, specifically designed for CNS drug discovery.
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83
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| HY-L949 | Spirocyclic Privileged Scaffold Lead-like Library |
Spirocyclic compounds, with rigid 3D structures, high Fsp³ and strong conformational restriction, are highly privileged scaffolds in small-molecule drug screening. They overcome drawbacks of planar aromatic compounds such as poor solubility, high off-target risks and weak druggability. Their orthogonal bicyclic geometry fits well into protein pockets, improving target affinity, subtype selectivity, metabolic stability and membrane permeability, making them ideal for hit identification against kinases, GPCRs, PPIs and other targets.
Spirocyclic scaffolds have been widely applied in oncology, antivirals, hypertension and CNS diseases, leading to many approved drugs and clinical candidates. SAR studies show that spiro-atom chirality, ring size and heteroatom substitution dominate bioactivity and selectivity, with the scaffold mainly serving as a conformational anchor. Azaspirocycles, spirooxindoles and spirosteranes target GPCRs, kinases, MDM2-p53 and PPIs. Approved drugs including irbesartan, spironolactone and rolapitant confirm their druggability, while revumenib and SAR405838 show promise against undruggable targets.
The MCE Spirocyclic Druglike Library contains over 1,000 diverse, stereospecific molecules selected by Lipinski’s rules. It covers privileged cores such as azaspirocycles, oxaspirocycles and spirooxindoles. These molecules bear rich chiral centers and distinct 3D orientations, reducing non-specific binding and enhancing screening efficiency. Featuring novel scaffolds, the library offers a highly innovative starting point for drug discovery.
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83
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| HY-D0040 | Calcein |
Calcein is a fluorescent dye and self-quenching probe, used as an indicator of lipid vesicle leakage, and also as a complexometric indicator for titration of calcium ions with EDTA, and for fluorometric determination of calcium. Calcein cannot directly cross the intact cell membrane of a living cell, unlike Calcein-AM (HY-D0041) which is cell-permeable. Calcein can also be used as a model drug for evaluating efficiency and bioavailability of drug delivery systems.
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15
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| HY-P1291A | PKI 14-22 amide,myristoylated TFA |
PKI 14-22 amide, myristoylated TFA is a selective, cAMP-dependent, competitive PKA inhibitor with Ki=~36 nM. The myristoylation modification of PKI 14-22 amide, myristoylated TFA makes it more permeable to cell membranes and blood-brain barriers than the precursor molecule. PKI 14-22 amide, myristoylated TFA can block the phosphorylation of cAMP-dependent downstream targets (such as CREB). PKI 14-22 amide, myristoylated TFA can prevent the development of analgesic tolerance in mice, and also inhibits protein translation and negative-strand RNA synthesis of Zika virus. PKI 14-22 amide, myristoylated TFA can be used in research fields such as opioid tolerance mechanisms and antiviral drugs.
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3
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| HY-P1291 | PKI 14-22 amide,myristoylated |
PKI 14-22 amide, myristoylated is a selective, cAMP-dependent, competitive PKA inhibitor with Ki=~36 nM. The myristoylation modification of PKI 14-22 amide, myristoylated makes it more permeable to cell membranes and blood-brain barriers than the precursor molecule. PKI 14-22 amide, myristoylated can block the phosphorylation of cAMP-dependent downstream targets (such as CREB). PKI 14-22 amide, myristoylated can prevent the development of morphine analgesic tolerance in mice, and also inhibits protein translation and negative-strand RNA synthesis of Zika virus. PKI 14-22 amide, myristoylated can be used in research fields such as opioid tolerance mechanisms and antiviral drugs.
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3
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| HY-P2259 | TAT-GluA2 3Y |
TAT-GluA2 3Y is a blood-brain barrier-permeable AMPA receptor inhibitory peptide that crosses cell membranes via the HIV-1 TAT protein domain. TAT-GluA2 3Y blocks the endocytosis of AMPA receptors, including the internalization of GluA1/GluA2 subunits, by disrupting interactions with the AP2, Brag2 and Syt3-GluA2 complexes, while also inhibiting long-term depression. TAT-GluA2 3Y blocks hypoxia-mediated AMPAR internalization, alleviates A1R-induced persistent synaptic inhibition, and reduces cerebral ischemic volume, neurological deficits and spatial memory deficits. TAT-GluA2 3Y blocks the effect of NLRP3 deficiency on fear generalization, inhibits amphetamine-induced behavioral/neurochemical sensitization, weakens the unconditioned stimulus-conditioned stimulus association of morphine, and promotes the extinction of morphine CPP. TAT-GluA2 3Y can be used in studies related to fear generalization, ischemic stroke, hypoxia, drug addiction and opioid addiction.
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2
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| HY-112624I | Dextran T3 (MW 3,000) |
Dextran T3 (Dextran 3; Dextran T3(MW 2400-3600)) is a neural tracer and intestinal permeability probe that can move anterogradely and retrogradely in neuronal axons by passive diffusion. Dextran T3 (MW 3,000) is able to permeate across the intestinal epithelial cell membrane in the presence of cholera toxin-induced cytoskeletal disturbance. Dextran T3 (MW 3,000) is used as a fluorescent marker to rapidly label developing neurons (such as Xenopus retinal ganglion cells) and to assess intestinal barrier function. It can be used to study axonal transport in neuroanatomy and permeability changes in intestinal pathophysiology. The Dextran series of compounds are also natural polysaccharide drug carriers that can be connected to drugs through covalent bonding methods such as ester bonds, amide bonds or click chemistry, or self-assembled to form carriers such as nanoparticles and hydrogels. Dextran is biodegradable and biocompatible, and can achieve targeted delivery and controlled release of drugs. Dextran derivatives can prolong the half-life of drugs, increase local concentrations, and reduce the activity of immune clearance.
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1
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| HY-P5623 | RVG |
RVG (RVG29) is a blood-brain barrier-permeable peptide derived from rabies virus glycoprotein, which binds to the α-7 subunit of neuronal nicotinic acetylcholine receptor (AchR). RVG efficiently delivers drugs to nerve cells and antigen-presenting cells in a targeted manner, and enhances the efficiency of antigen presentation and drug delivery.
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1
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| HY-P2529 | Penetratin |
Penetratin is a cell-penetrating peptides derived from a nonviral protein. Penetratin can powerfully enhance drug absorption. Penetratin can be used for drug delivery research in the treatment of various diseases.
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1
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| HY-148033 | Trimethyl chitosan |
Trimethyl chitosan (N,N,N-Trimethylchitosan) is a multifunctional polymer and a derivative of Chitosan (HY-B2144A). Trimethyl chitosan targets the absorption enhancing proteins of tight junctions of intestinal and mucosal epithelial cells, induces tight junction protein rearrangement, and increases intercellular permeability. Trimethyl chitosan can stimulate the activity of promoting transmembrane transport of hydrophilic drugs (such as peptides and proteins) and can be used for drug delivery and synthesis of nanoparticles.
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1
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| HY-W700452 | Y-27632-d4 hydrochloride hydrate |
Y-27632-d4 hydrochloride hydrate is the deuterium labeled Y-27632 hydrochloride hydrate (HY-10071A). Y-27632 hydrochloride hydrate is an orally active, ATP-competitive inhibitor of ROCK-I and ROCK-II, with Kis of 220 and 300 nM, respectively. Y-27632 hydrochloride hydrate attenuates Doxorubicin-induced apoptosis of human cardiac stem cells. Y-27632 hydrochloride hydrate also suppresses dissociation-induced apoptosis of murine prostate stem/progenitor cells. Y-27632 hydrochloride hydrate primes human induced pluripotent stem cells (hIPSCs) to selectively differentiate towards mesendodermal lineage via epithelial-mesenchymal transition-like modulation.
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| HY-B0364AS | Dyclonine-d9 hydrochloride |
Dyclonine-d9 hydrochloride (Dyclocaine-d9 hydrochloride) is the deuterated-labeled Dyclonine hydrochloride (HY-B0364A). Dyclonine hydrochloride (Dyclocaine hydrochloride) is an orally active, blood-brain barrier-permeable piperidine phenylacetone small molecule commonly used as a local anesthetic. Dyclonine hydrochloride acts as a highly selective allosteric antagonist of TRPV3; it also reversibly inhibits G9a, ALDH2 and ALDH3A1, non-competitively blocks AChE. Dyclonine hydrochloride activates the Nrf2/ARE pathway, relieves the epigenetic silencing of FXN, blocks Aβ42 aggregation, and promotes remyelination and reparative polarization of microglia. Dyclonine hydrochloride alleviates pruritus via TRPV3 inhibition; it is used in studies of neurodegenerative disease models based on its AChE inhibitory, antioxidant and remyelinating effects; it sensitizes drug-resistant tumors through ALDH inhibition, and combined use with protease inhibitors induces more tumor cell apoptosis; it inhibits Candida albicans in vitro. Dyclonine hydrochloride can be used for research on multiple diseases including neurodegenerative diseases, cancer and pruritic dermatitis.
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Isotope-Labeled Compounds
TRP Channel
Aldehyde Dehydrogenase (ALDH)
Cholinesterase (ChE)
Keap1-Nrf2
Amyloid-β
Fungal
Apoptosis
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| HY-N7848R | Linoleamide (Standard) |
1-Phenyl-2-propanol (Standard) is the analytical standard of 1-Phenyl-2-propanol. This product is intended for research and analytical applications. 1-Phenyl-2-propanol (Benzylmethylcarbinol) is a natural product.
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| HY-P3305 | NBD-LLLLpY |
NBD-LLLLpY is an enzymatically forming intranuclear peptide for selectively killing human induced pluripotent stem cells.
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| HY-P11322 | NHIP peptide |
NHIP peptide is a peptide segment containing 20 amino acids located in the nucleus of the cell. NHIP is highly expressed in neuronal derived cells such as LUHMES cells. NHIP peptide can promote the proliferation of 293T cells. NHIP peptide regulates gene networks related to neural development and autism spectrum disorder (ASD).
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| HY-D2341 | 6FC-GABA-Taxol |
6FC-GABA-Taxol is a fluorescent probe with cell permeability, which is formed by connecting 6FC to the anticancer drug Taxol (HY-B0015) via γ-aminobutyric acid (GABA). 6FC-GABA-Taxol can bind to microtubules in living cells and image them through confocal microscopy. Additionally, 6FC-GABA-Taxol enables the quantification of microtubule binding using flow cytometry without the addition of efflux inhibitors.
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| HY-116705G | 2-Deoxy-2-fluoro-L-fucose (GMP) |
2-Deoxy-2-fluoro-L-fucose (2-Fluorofucose) GMP is a fucosyltransferase inhibitor that inhibits core fucosylation modification in cells. 2-Deoxy-2-fluoro-L-fucose GMP promotes the production of defucosylated IgG1 antibodies in IgG1-expressing cell culture systems; it regulates the levels of inflammatory cytokines such as IL-1β, IL-6 and TGF-β in human induced pluripotent stem cell-derived microglia. 2-Deoxy-2-fluoro-L-fucose GMP can be used in the research of related diseases including dengue fever and Alzheimer's disease.
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| HY-12299G | WH-4-023 (GMP) |
WH-4-023 GMP is WH-4-023 (HY-12299) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. WH-4-023 (Dual LCK/SRC inhibitor) is a Lck/Src dual target inhibitor with functions in stem cell maintenance and differentiation regulation. WH-4-023 blocks epithelial-mesenchymal transition, supports the self-renewal of porcine embryonic stem cells, and inhibits their differentiation into mesoderm and endoderm. WH-4-023 is a key component of 3i/LAF medium, and enables the stable establishment and long-term maintenance of porcine pre-gastrulation epiblast stem cell lines. Removal of WH-4-023 reduces the expression of pluripotency factors in porcine and human extended pluripotent stem cells. WH-4-023 can be applied to relevant studies such as non-small cell lung cancer resistant to EGFR-TKIs.
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| HY-Y0850U5 | PVA (Mw 27000, 98-99% hydrolyzed, ~600 polymerization) |
PVA (Polyvinyl alcohol) (Mw 27000, 98-99% hydrolyzed, ~600 polymerization) is a nonionic ethanol homopolymer with hydrophilicity, water solubility and biodegradability. PVA (Mw 27000, 98-99% hydrolyzed, ~600 polymerization) exhibits biocompatibility, non-toxicity and non-carcinogenicity, as well as antibacterial activity against Gram-positive bacteria, Gram-negative bacteria and fungal strains. PVA (Mw 27000, 98-99% hydrolyzed, ~600 polymerization) can serve as a solubilizer, stabilizer, mucoadhesive agent and sustained-release agent, and has a synergistic solubilizing effect on voriconazole/sulfobutyl ether β-cyclodextrin complexes. By stabilizing such complexes, PVA (Mw 27000, 98-99% hydrolyzed, ~600 polymerization) forms freeze-thaw hydrogels with high mucoadhesion, sustained drug release and ex vivo corneal permeability. When compounded with hyaluronic acid hydrogels, PVA (Mw 27000, 98-99% hydrolyzed, ~600 polymerization) supports chondrocyte growth in vitro, and also forms complexes with Cu2+, Co2+, Ni2+ and Zn2+ ions. PVA (Mw 27000, 98-99% hydrolyzed, ~600 polymerization) can be used in studies related to fungal keratitis, bacterial infections and fungal infections.
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| HY-N0565AG | Doxycycline (hydrochloride) (GMP) |
Doxycycline hydrochloride GMP is Doxycycline (hydrochloride) (HY-N0565A) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Doxycycline hydrochloride is an orally active highly lipophilic, tissue-permeable MMP inhibitor with broad-spectrum antibacterial activity. Doxycycline hydrochloride is also a semi-synthetic antibiotic with chelating properties, which blocks bacterial protein synthesis and inhibits extracellular matrix degradation through interactions with zinc and calcium atoms. Doxycycline hydrochloride also inhibits mitochondrial biogenesis, translation, and the expression of respiratory chain proteins. Doxycycline hydrochloride induces apoptosis, inhibits autophagy and EMT, downregulates stem cell markers, and activates the PI3K-AKT pathway, thereby effectively inhibiting the viability and proliferation of cancer cells such as breast cancer cells. Doxycycline hydrochloride also promotes the survival and self-renewal of embryonic stem cells and neural stem cells, and reduces the frequency of medium changes in culture. Doxycycline hydrochloride has been applied in studies related to breast cancer, prostate cancer, bladder cancer, and other cancers.
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Infection
Neurological, Eye or Ear Disease
Inflammation or Immune System Disease
Breast Cancer
Prostate Cancer
Bladder Cancer
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| HY-16129 | CBP-501 |
CBP-501, a cell-permeable calmodulin-binding peptide and a G2-abrogating drug candidate, inhibits the activity of multiple Ser216-specific kinases, such as MAPKAP-K2, C-Tak1, CHK1 and CHK2, with IC50 values of 0.9 μM, 1.4 μM 3.4 μM and 6.5 μM, respectively. CBP-501 is used for various types of cancer.
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| HY-P10502 | L57 |
L57 is a low-density lipoprotein receptor-related protein 1 (LRP1)-binding peptide. L57 exhibits high affinity for LRP1, with an EC50 of 45 nM. L57 possesses blood-brain barrier (BBB) permeability and plasma stability. L57 can serve as a carrier for central nervous system drug delivery.
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| HY-P4866 | Q-Peptide |
Q-Peptide is an angiopoietin-1 derived peptide (QHREDGS). Q-Peptide interacts with β1-integrin, binds to integrins on the surface of osteoblasts, and serves as an acyl donor substrate for Streptomyces mobaraensis transglutaminase. Q-Peptide activates Akt, MAPKp42/44, ILK, ERK1/2, and downregulates caspase-3/7. Q-Peptide inhibits cell apoptosis, enhances cell adhesion and migration, and promotes osteoblast differentiation, bone matrix deposition and mineralization. Q-Peptide can be used in studies related to myocardial infarction, bone regeneration, diabetic wound repair and human induced pluripotent stem cells.
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| HY-W131101 | Sorbitan tristearate |
Sorbitan tristearate is a non-ionic surfactant, with a synergistic effect on skin permeability. Sorbitan tristearate can be used as an excipient, such as emulsifier. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs.
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| HY-DY1091 | Calcein (solution) |
Calcein (solution) (Fluorexon (solution)) is a fluorescent dye and self-quenching probe, used as an indicator of lipid vesicle leakage, and also as a complexometric indicator for titration of calcium ions with EDTA, and for fluorometric determination of calcium. Calcein cannot directly cross the intact cell membrane of a living cell, unlike Calcein-AM (HY-D0041) which is cell-permeable. Calcein can also be used as a model drug for evaluating efficiency and bioavailability of drug delivery systems.
Solvent and concentration: DMSO: 2 mM The 1 mL volume is defined as the base specification. All larger sizes correspond to incremental volumes of this base. |
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| HY-P4047 | Cyclo(RGDfK(Mal)) |
Cyclo(RGDfK(Mal)) is a pentapeptide. Cyclo(RGDfK(Mal)) improves the attachment and infiltration of human pluripotent stem cells. Cyclo(RGDfK(Mal)) can be used for 3D stem cell culture and expansion.
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| HY-15147G | XAV-939 (GMP) |
XAV-939 (GMP) is XAV-939 (HY-15347) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. XAV-939 is a tankyrase inhibitor.
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| HY-P10502A | L57 acetate |
L57 acetate is a Low-density lipoprotein receptor-related protein 1 (LRP1)-binding peptide. L57 acetate exhibits high affinity to LRP1 with Ki of 45 nM. L57 acetate exhibits blood-brain barrier (BBB) permeability and plasma stability. L57 acetate can be utilized as the carrier for CNS drug delivery.
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| HY-N6784 | Oligomycin B |
Oligomycin B is an antibiotic that acts as a non-selective inhibitor of ATP Synthase. Oligomycin B increases mitochondrial membrane potential. Oligomycin B induces apoptosis and necrosis. Oligomycin B impairs the motility of Plasmopara viticola zoospores and induces their lysis. Oligomycin B inhibits Magnaporthe oryzae (wheat blast fungus) and suppresses the development of wheat blast. Oligomycin B reduces hyphal growth and spore germination of Botrytis cinerea, and protects Arabidopsis thaliana against Botrytis cinerea infection. Oligomycin B exacerbates cytotoxic brain edema in rats with cerebral cortical contusion, increases intracranial pressure and brain water content, and aggravates mitochondrial damage in these rats. Oligomycin B is used in studies related to grape downy mildew, traumatic brain injury, wheat blast, and gray mold.
Source: the marine Streptomyces strains B8496 and B8739 |
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| HY-P5755 | SWELYYPLRANL-NH2 |
SWELYYPLRANL-NH2 is an E-cadherin and N-cadherin antagonist. SWELYYPLRANL-NH2 inhibits phage clone binding to E- or N-cad/Fc chimeric protein (IC50: 0.7 and 0.09 μM respectively). SWELYYPLRANL-NH2 inhibits cell aggregation. SWELYYPLRANL-NH2 can be used to promote drug delivery through epithelial and endothelial permeability barriers.
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| HY-P10233A | SAAP 148 TFA |
SAAP 148 TFA is a synthetic antimicrobial peptide (bacteria) that interacts with and disrupts the lipid bilayer of bacterial cytoplasmic membranes, thereby inducing changes in membrane permeability and bacterial death. SAAP 148 TFA kills drug-resistant, multidrug-resistant and persister bacterial strains, inhibits biofilm formation, eliminates established biofilms, and blocks bacterial colonization on implant surfaces. SAAP 148 TFA retains its activity after modification or immobilization, exhibits variable cytotoxicity in different human cell models, and shows reduced efficacy in protein-rich environments. SAAP 148 TFA can be used in infection-related research.
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| HY-N7848 | Linoleamide |
Linoleamide is a linoleic acid amide. Linoleamide regulates Ca (II) ux and inhibits the erg current.
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| HY-P2426 | (D-Trp12,Tyr34)-pTH (7-34) amide (bovine) |
(D-Trp12,Tyr34)-pTH (7-34) amide (bovine) is a potent and competitive antagonist of parathyroid hormone (PTH), with a Ki of 69 nM in bovine renal cortical membrane. (D-Trp12,Tyr34)-pTH (7-34) amide (bovine) can be used for growth and development regulation.
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| HY-10431G | SB-431542 (GMP) |
SB-431542 (GMP) is SB-431542 (HY-10431) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. SB-431542 is a TGF-β receptor kinase inhibitor (TRKI) in SMAD signaling.
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| HY-112624B | Dextran T70 (MW 70,000) |
Dextran 70,000 is a high molecular weight polysaccharide formed by glucose linked by α-(1→6) glycosidic bonds. Dextran 70,000 can expand blood volume through colloidal osmotic pressure effect and inhibit cell adhesion and platelet aggregation through steric hindrance. At the same time, Dextran 70,000 can be used as a drug carrier to achieve targeted delivery through endocytosis. Dextran 70,000 is biologically inert and has low immunogenicity. It can be used for clinical blood volume expansion, anti-thrombotic research, and evaluation of vascular permeability in in vitro experiments. It can also be combined with fluorescent dyes for cell tracking and drug delivery research. The Dextran series of compounds are also natural polysaccharide drug carriers that can be connected to drugs through covalent bonding methods such as ester bonds, amide bonds or click chemistry, or self-assembled to form carriers such as nanoparticles and hydrogels. Dextran is biodegradable and biocompatible, and can achieve targeted delivery and controlled release of drugs. Dextran derivatives can prolong the half-life of drugs, increase local concentrations, and reduce the activity of immune clearance.
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| HY-K3022 | Recombinant Human Serum Albumin Solution (rHSA, 20%) |
MCE Recombinant Human Serum Albumin Solution (rHSA, 20%) can be widely used in various cell culture systems and is particularly suitable for maintaining the undifferentiated growth and expansion of human embryonic stem cells (hESC) and induced pluripotent stem cells (hiPSC) under both feeder-dependent and feeder-free conditions. |
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| HY-K6019 | Stem Cell Cryopreservation Medium |
MCE Stem Cell Cryopreservation Medium is a ready-to-use, serum-free Cryopreservation Medium optimized for human pluripotent stem cells (PSCs). PSCs preserved with this medium exhibit high post-thaw viability (> 90%) and stable expression of pluripotency markers such as OCT4 and NANOG, providing consistent and reliable cell sources for subsequent expansion and differentiation. This product is suitable for long-term, stable storage of PSCs and downstream applications. |
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| HY-K6022 | ECM Gentle Dissociation Solution |
MCE ECM Gentle Dissociation Solution is a gentle ECM-degrading enzyme mixture derived from marine bacteria and Bacillus species, specifically formulated for efficient and low-damage digestion of in-vitro cell systems. It selectively degrades extracellular matrix components while minimizing disruption to the cell membrane and intercellular junctions, thereby significantly reducing mechanical stress during dissociation. This product is compatible with a wide range of cell types, including stem cell colonies, primary cells, neural cells, and organoids, and is particularly well suited for gentle yet effective dissociation of brain organoids and other complex 3D structures. |
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| HY-K6137 | Brain Glioma Organoid Kit |
MCE Brain Glioma Organoid Kit contains brain glioma organoid basal medium and culture supplement. This product can be used to efficiently construct brain glioma organoid. |
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| HY-K6141 | Human Brain Organoid (Expansion) Kit |
MCE Human Brain Organoid (Expansion) Kit contains Human Brain Organoid Expansion Basal Medium and Human Brain Organoid Expansion Culture Supplements. This kit enables the efficient in vitro generation of human forebrain organoids (hFBs). Within this culture system, human brain tissue can spontaneously form organoid structures that faithfully recapitulate key features of in vivo cellular heterogeneity and complex tissue organization. |
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| HY-K6142 | Human Brain (Differentiation) Organoid Kit |
MCE Human Brain (Differentiation) Organoid Kit includes a basic culture medium and differentiation supplements, designed for the induction and culture of human brain organoids (hFBs). |
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| HY-K6143 | Mouse Fetal Brain Organoid (Expansion) Kit |
MCE Mouse Fetal Brain Organoid (Expansion) Kit contains Mouse Fetal Brain Organoid Expansion Basal Medium and Mouse Fetal Brain Organoid Expansion Culture Supplement . This kit enables the efficient in vitro generation of mouse fetal brain organoids (mFBs). Within this culture system, mouse fetal brain tissue can spontaneously form organoid structures that faithfully recapitulate key features of in vivo cellular heterogeneity and complex tissue organization. |
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| HY-K6144 | Mouse Fetal Brain (Differentiation) Organoid Kit |
MCE Mouse Fetal Brain (Differentiation) Organoid Kit includes a basic culture medium and differentiation supplements, designed for the induction and culture of mouse fetal brain organoids (mFBs). |
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| HY-K6301 | Human iPSC/ESC Cortical Brain Organoid Induction Differentiation Kit |
MCE Human iPSC/ESC Cortical Brain Organoid Induction Differentiation Kit is a standardized culture system specifically designed to recapitulate the developmental processes and functional features of the human cerebral cortex through forebrain ventralization-based signaling regulation. By sequentially activating the Wnt/β-catenin pathway and gradually inhibiting BMP/Smad signaling, this system efficiently drives human pluripotent stem cells (PSC) to differentiate into high-purity glutamatergic neurons (VGLUT1/2+ > 85%), while simultaneously promoting the formation of Pax6+/BLBP+ radial glial cells that establish a biomimetic ventricular-zone–like structure. |
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| HY-K6302 | Human iPSC/ESC Whole-Brain Organoid Induction Differentiation Kit |
MCE Human iPSC/ESC Whole-Brain Organoid Induction Differentiation Kit is a non-region-specific brain organoid induction kit designed based on the neuroectoderm self-differentiation system. After 38 d of culture using this kit, the resulting whole-brain organoids stably express core neuronal markers such as TUJ1, SOX2, Nestin, and NeuN, as well as forebrain/cortical markers including FOXG1 and CTIP2. |
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| 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. |
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| HY-K6305 | Human PSC Islet Organoid Differentiation Kit |
MCE Human PSC Islet Organoid Differentiation Kit enables the efficient directed differentiation of human pluripotent stem cells (PSCs) into structurally intact and functionally mature islet organoids within 26 d. |
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| HY-K6501 | Human PSC Maintenance Medium |
MCE Human PSC Maintenance Medium is a ready-to-use, chemically defined formulation designed to support the robust growth and self-renewal of human embryonic stem cells (hESCs) and induced pluripotent stem cells (iPSCs) under feeder-free culture conditions. |
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| HY-K6502 | Human iPSC-Derived Brain Organoid Long-term Culture Medium |
MCE Human iPSC-Derived Brain Organoid Long-term Culture Medium is a specialized culture system developed through systematic reformulation and concentration optimization based on neuronal cell culture platforms. It significantly enhances the adaptability and stability of long-term culture for brain organoids derived from human induced pluripotent stem cells (iPSCs). |
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| HY-K6503 | Human PSC Embryoid Body (EB) Induction Medium |
MCE Human PSC Embryoid Body (EB) Induction Medium is specifically designed to support the efficient and reproducible formation of uniform embryoid bodies from pluripotent stem cells under suspension culture conditions. This optimized culture system integrates microenvironmental regulation with metabolic adaptation strategies, significantly improving the stability and reproducibility of EB formation. |
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| HY-K6504 | Human iPSC/ESC Cortical Brain Organoid Maturation Medium |
MCE Human iPSC/ESC Cortical Brain Organoid Maturation Medium is a ready-to-use culture system specifically formulated for the long-term maintenance and maturation of cortical brain organoids. It serves as a seamless transition from the induction phase and supports the continued growth and functional development of the organoids. Upon switching PSC-derived cortical brain organoids to this medium, organoid viability and structural stability are markedly enhanced, enabling a robust and extended culture period of up to 180 d. |
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