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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. -
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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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. -
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. -
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. -
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 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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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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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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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%. -
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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Inhibitory Antibodies
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Reference Standards
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Induced Disease Models Products
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Biochemical Assay Reagents
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Natural Products
| Cat. No. | Product Name | Information | Application | Publication |
|---|---|---|---|---|
| HY-100218A | RSL3 |
RSL3 ((1S,3R)-RSL3) is an inhibitor of glutathione peroxidase 4 (GPX4) (ferroptosis activator), reduces the expression of GPX4 protein, and induces ferroptotic death of head and neck cancer cell. RSL3 increases the expression of p62 and Nrf2 and inactivates Keap1 in HN3-rslR cells.
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573
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| HY-13027 | DAPT |
DAPT (GSI-IX) is a potent and orally active γ-secretase inhibitor with IC50s of 115 nM and 200 nM for total amyloid-β (Aβ) and Aβ42, respectively. DAPT inhibits the activation of Notch 1 signaling and induces cell differentiation. DAPT also induces autophagy and apoptosis. DAPT has neuroprotection activity and has the potential for autoimmune and lymphoproliferative diseases, degenerative disease and cancers treatment.
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Breast Cancer
Colorectal Cancer
Liver Cancer
Pancreatic Cancer
Digestive System Inflammation
Alzheimer's Disease
Rheumatoid Arthritis
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172
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| HY-P1061 | Colivelin |
Colivelin is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro. Colivelin exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin has the potential for the treatment of alzheimer's disease and ischemic brain injury
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102
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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-L003 | Apoptosis Compound Library |
Apoptosis is an ordered and orchestrated cellular process that occurs in physiological and pathological conditions, which is also called programmed cell death (PCD). Apoptosis plays a crucial role in developing and maintaining the health of the body by eliminating old cells, unhealthy cells and unnecessary cells. Too little or too much apoptosis contribute to many diseases. When apoptosis does not work correctly, cells that should be eliminated may persist and become immortal, for example, in cancer and leukemia. When apoptosis works overly well, it kills too many cells and inflicts grave tissue damage. This is the case in strokes and neurodegenerative disorders such as Alzheimer's, Huntington's, and Parkinson's disease.
MCE designs a unique collection of 3,650 apoptosis-related compounds mainly focusing on the key targets in the apoptosis signaling pathway and can be used in the research of apoptosis signal pathway and related diseases.
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90
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| HY-L054 | Endoplasmic Reticulum Stress Compound Library |
Endoplasmic reticulum (ER) contributes to the production and folding of approximately one third of cellular proteins, and is thus inextricably linked to the maintenance of cellular homeostasis and the fine balance between health and disease. However, some adverse factors negatively impact ER functions and protein synthesis, resulting in the activation of Endoplasmic reticulum stress (ER stress, ERS) and unfolded protein response (UPR) signaling pathways. The UPR is triggered when ER protein folding capacity is overwhelmed by cellular demand and the UPR initially aims to restore ER homeostasis and normal cellular functions. However, if this fails, then the UPR triggers cell death. Chronic ER stress and defects in UPR signaling are emerging as key contributors to a growing list of human diseases, including diabetes, neurodegeneration and cancer.
MCE Endoplasmic Reticulum Stress Compound Library contains 379 ER stress-related compounds that mainly target PERK, IRE1, ATF6, etc. MCE ER stress library is a useful tool for researching ER stress and related diseases.
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85
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| HY-L086 | Neurodegenerative Disease-related Compound Library |
Neurodegenerative diseases are incurable and life-threatening conditions that result in progressive degeneration and/or death of nerve cells. Some common neurodegenerative diseases include Alzheimer’s Disease (AD), Parkinson’s Disease (PD), Motor Neuron Disease (MND), Huntington’s Disease (HD), Spino-Cerebellar Ataxia (SCA), Spinal Muscular Atrophy (SMA), and Amyotrophic Lateral Sclerosis (ALS). Because the pathophysiology of neurodegenerative disorders is generally poorly understood, it is difficult to identify promising molecular targets and validate them. At the same time, about 85% of the drugs fail in clinical trials. Therefore, validating new targets and discovering new drugs to mitigate neurodegenerative disorders is need of the hour.
MCE offers a unique collection of 3,759 compounds with anti-Neurodegenerative Diseases activities or targeting the unique targets of neurodegenerative diseases. MCE Neurodegenerative Disease-related Compound Library is a useful tool for exploring the mechanism of neurodegenerative diseases and discovering new drugs for neurodegenerative diseases.
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85
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| HY-L092 | Glucose Metabolism Compound Library |
Glucose homeostasis is tightly regulated to meet the energy requirements of the vital organs and maintain an individual’s health. Glucose metabolism includes glycolysis, tricarboxylic acid cycle, pentose phosphate pathway, oxidative phosphorylation and other metabolic pathways. Glucose is the major carbon source that provides the main energy for life. Glucose metabolism dysregulation is also implicated in many diseases such as diabetes, heart disease, neurodegenerative diseases and even cancer.
MCE offers a unique collection of 1,777 compounds related to glucose metabolism, which target glucose metabolism related targets, such as GLUT, Hexokinase, Pyruvate Kinase, IDH, etc. MCE glucose metabolism library is a powerful tool for studying glucose metabolism and drug discovery of diseases related to glucose metabolism.
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85
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| HY-L034 | Anti-Aging Compound Library |
Aging is a complex biological process characterized by functional decline of tissues and organs, structural degeneration, and reduced adaptability and resistance, all of which contribute to an increase in morbidity and mortality caused by multiple chronic diseases, such as Alzheimer's disease, cancer, and diabetes. Many theories, which fall into two main categories: programmed and error theories, have been proposed to explain the process of aging, but neither of them appears to be fully satisfactory. The programmed theories imply that aging relies on specific gene regulation, and the error theories emphasize the internal and environmental damages accumulated to living organisms. The damage theories proposed the nine hallmarks that were generally considered to contribute to the aging process: genomic instability, telomere attrition, epigenetic alterations, loss of proteostasis, deregulated nutrient-sensing, mitochondrial dysfunction, cellular senescence, stem cell exhaustion, and altered intercellular communication.
MCE Anti-Aging Compound Library contains 7,771 compounds, mainly targeting Sirtuin, mTOR, IGF-1R, AMPK, p53, Telomerase, Mitophagy, Mitochondrial Metabolism, COX, Cytochrome P450, Oxidase, etc. This library is a useful tool for anti-aging research.
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84
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| HY-L051 | Ferroptosis Compound Library |
Ferroptosis is a novel type of cell death program that is distinct from apoptosis, necroptosis and autophagy. It is dependent on iron and reactive oxygen species (ROS) and is characterized by lipid peroxidation. As a novel type of cell death, ferroptosis has distinct properties and recognizing functions involved in physical conditions or various diseases including cancers, neurodegenerative diseases, acute renal failure, etc.
MCE carefully collected a unique collection of 1,255 ferroptosis signaling pathway related compounds with ferroptosis-inducing or -inhibitory activity. MCE Ferroptosis Compound Library is a useful tool to study ferroptosis mechanism as well as related diseases.
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84
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| HY-L070 | Neuroprotective Compound Library |
Neurodegenerative diseases are characterised by progressive dysfunction and death of neurons, such as Alzheimer’s disease, Parkinson’s disease, and multiple sclerosis (MS). Neuroprotection is an approach to preserve neurons so that neurons cannot be hurt by different pathological factors in neurodegenerative diseases. Neuroprotectors are some agonists and antagonists targeting some key targets in neuroprotactive signal pathways, such as calcium and sodium channel blockers, GABA receptor agonists, NMDA receptor Antagonists, etc. Current neuroprotectors cannot reverse existing damage, but they may protect against further nerve damage and slow down any degeneration of the central nervous system (CNS) and still play important roles in the treatment of neurodegenerative diseases.
MCE offers a unique collection of 1,851 compounds with potential neuroprotective activities. These compounds mainly act on some key targets in neuroprotetive signal pathways, such as calcium channel, sodium channel, adenosine A1 receptor, etc. MCE Neuroprotective Compopund Library is a useful tool in neuroprotective drug discovery.
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84
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| HY-L180 | Mitophagy Compound Library |
Mitochondrial autophagy refers to the selective encapsulation and degradation of damaged mitochondria by cells through the autophagy mechanism, thereby maintaining mitochondrial and cellular homeostasis. The concept of mitochondrial autophagy has received extensive attention since it was proposed. Current studies have shown that the mechanisms of mitochondrial autophagy can generally be divided into two categories: Ubiquitin-dependent pathways and Ub-independent pathways. In addition, mitochondrial autophagy is a research hotspot related to the pathogenesis of neurodegenerative diseases, cardiovascular diseases, cancer, metabolic diseases and other clinical diseases. Therefore, high-throughput screening based on mitochondrial autophagy can effectively screen out compounds that are closely related to the occurrence of diseases and analyze their mechanisms.
MCE can provide a library of 655 mitophagy compounds, which can be used for drug development and mechanism research in cancer, immunity, infection and other hot research fields.
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84
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| HY-L155 | Mitochondrial Toxicity Compound Library |
Mitochondria, as the main place of energy supply in life, is essential to maintain normal life activities. Mitochondrial dysfunction is associated with common diseases, such as cardiovascular diseases, neurodegenerative diseases, diabetes and cancer. The heart, brain and liver rely heavily on mitochondrial function as the main organs for drug metabolism. In addition, mitochondria is also a target of many drugs, some of which induce organotoxicity by inducing mitochondrial toxicity.
MCE contains 545 mitochondrial toxic compounds, which can be used as tool compounds for drug development and disease mechanism research.
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83
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| HY-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-19370 | FPS-ZM1 |
FPS-ZM1 is a high-affinity and BBB-permeable RAGE inhibitor with a Ki of 25 nM.
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73
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| HY-18234A | Leupeptin hemisulfate |
Leupeptin hemisulfate is a broad-spectrum protease inhibitor. By inhibiting the activation of the PTEN/PI3K/Akt/NF-κB/ERK1/2/p38 signaling pathway, Leupeptin hemisulfate significantly reduces LPS-induced NO and ROS production, mitochondrial membrane potential hyperpolarization, phagocytic activity, pro-inflammatory cytokine release, and M1 polarization in mouse peritoneal macrophages, and reverses autophagic flux impairment. It also decreases Concanavalin A (HY-P2149)-induced proliferation index of mouse splenic lymphocytes and the Th1/IL-10 and Th2/IL-10 cytokine ratios, thereby modulating innate and adaptive immune responses. Leupeptin hemisulfate inhibits blood coagulation and tumorigenesis in mouse skin. Leupeptin hemisulfate can be used in research on chronic inflammatory diseases and skin tumorigenesis.
Source: Streptomyces roseus MB-26-AI |
Ser/Thr Protease
Cathepsin
Autophagy
SARS-CoV
Atg8/LC3
NO Synthase
COX
p62
Arginase
PTEN
NF-κB
PI3K
Akt
p38 MAPK
ERK
Reactive Oxygen Species (ROS)
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68
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| HY-Y1269D | Ammonium chloride, for molecular biology |
Ammonium chloride (Salmiac), for molecular biology is an inhibitor of Slc26a4 and SMAD2. Ammonium chloride, for molecular biology reduces the protein expression level of Slc26a4 in lung tissue, and attenuates ozone-induced increases in proinflammatory cytokines, inflammatory cells, pulmonary resistance, goblet cell hyperplasia, peribronchial inflammation and thiocyanate levels in mouse tissues and bronchoalveolar lavage fluid. Ammonium chloride, for molecular biology decreases the level of phosphorylated SMAD2, inhibits autophagy by reducing autophagy-related proteins, and enhances Cisplatin (HY-17394)-induced cancer cell apoptosis and DNA double-strand breaks. Ammonium chloride, for molecular biology also inhibits the TCA cycle, reduces ATP production, increases glucose utilization, regulates the levels of lactic acid, glutamic acid and ATP, and induces morphological degeneration of neuroblastoma cells. Ammonium chloride, for molecular biology can be used in studies related to ozone-induced airway injury, hepatocellular carcinoma, human cervical cancer, hepatic encephalopathy, Reye syndrome, epilepsy and neurodegenerative diseases.
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62
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| HY-P0128 | β-Amyloid (25-35) |
β-Amyloid (25-35) (Amyloid beta-peptide (25-35)) is the fragment Aβ(25-35) of the Alzheimer's amyloid β-peptide, has shown neurotoxic activities in cultured cells.
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51
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| HY-114118B | Semaglutide acetate |
Semaglutide acetate is a long-acting, selective, competitive GLP-1R agonist that can penetrate the blood-brain barrier. After activating GLP-1R, Semaglutide acetate promotes insulin secretion, inhibits gastric emptying and appetite, and at the same time enhances autophagy, inhibits oxidative stress and apoptosis. Semaglutide acetate also regulates mitochondrial function and lipid metabolism (such as reducing de novo lipogenesis in the liver). Semaglutide acetate has activities such as lowering blood sugar, reducing weight, neuroprotection (such as improving motor function in Parkinson's disease models, reducing α-synuclein aggregation) and improving hepatic steatosis. Semaglutide acetate can be used for the study of neurodegenerative diseases and liver diseases such as type 2 diabetes, obesity, Parkinson's disease, metabolic associated fatty liver disease (MASLD), and cancer.
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50
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| HY-114118A | Semaglutide TFA |
Semaglutide TFA is a long-acting, selective, competitive GLP-1R agonist that can penetrate the blood-brain barrier. After activating GLP-1R, Semaglutide TFA promotes insulin secretion, inhibits gastric emptying and appetite, and at the same time enhances autophagy, inhibits oxidative stress and apoptosis. Semaglutide TFA also regulates mitochondrial function and lipid metabolism (such as reducing de novo lipogenesis in the liver). Semaglutide TFA has activities such as lowering blood sugar, reducing weight, neuroprotection (such as improving motor function in Parkinson's disease models, reducing α-synuclein aggregation) and improving hepatic steatosis. Semaglutide TFA can be used for the study of neurodegenerative diseases and liver diseases such as type 2 diabetes, obesity, Parkinson's disease, metabolic associated fatty liver disease (MASLD), and cancer.
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50
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| HY-114118 | Semaglutide |
Semaglutide is a long-acting, selective, competitive GLP-1R agonist that can penetrate the blood-brain barrier. After activating GLP-1R, Semaglutide promotes insulin secretion, inhibits gastric emptying and appetite, and at the same time enhances autophagy, inhibits oxidative stress and apoptosis. Semaglutide also regulates mitochondrial function and lipid metabolism (such as reducing de novo lipogenesis in the liver). Semaglutide has activities such as lowering blood sugar, reducing weight, neuroprotection (such as improving motor function in Parkinson's disease models, reducing α-synuclein aggregation) and improving hepatic steatosis. Semaglutide can be used for the study of neurodegenerative diseases and liver diseases such as type 2 diabetes, obesity, Parkinson's disease, metabolic associated fatty liver disease (MASLD), and cancer.
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50
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| HY-N0148 | Rutin |
Rutin (Rutoside) is a flavonoid found in many plants and shows a wide range of biological activities including anti-inflammatory, antidiabetic, antioxidant, neuroprotective, nephroprotective, hepatoprotective and reducing Aβ oligomer activities. Rutin is also a CBR1 inhibitor, which can cross the blood brain barrier. Rutin attenuates vancomycin-induced renal tubular cell apoptosis via suppression of apoptosis, mitochondrial dysfunction, and oxidative stress.
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Cancer
Digestive System Disease
Digestive System Inflammation
Glucose Metabolism
SARS-CoV-2 Infection
Alzheimer's Disease
Parkinson's Disease
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35
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| HY-D0218 | Thioflavin T |
Thioflavin T is a cationic Benzothiazole dye that shows enhanced fluorescence upon binding to amyloid in tissue sections. Excitation max.: ~385 nm (free); ~450 nm (bound); Emission max.: ~445 nm (free); ~485 nm (bound).
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32
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| HY-P1363B | β-Amyloid (1-42), human, HFIP-treated |
β-Amyloid (1-42), human, HFIP-treated, a 42-amino acid peptide that has been treated with HFIP from β-Amyloid (1-42), human (HY-P1363A), is a brain-penetrant amyloid protein fragment, which can be used in research on Alzheimer's disease and Down’s syndrome. β-Amyloid (1-42), human, HFIP-treated remaining as a monomer exhibits antioxidant and neuroprotective effects. β-Amyloid (1-42), human, HFIP-treated, after being dissolved in DMSO to form the stock solution, on the one hand, can form soluble oligomers (AβOs) when incubated at 4°C, which have synaptic toxicity and neurotoxicity; on the other hand, it can be incubated at 37°C to form insoluble fibrils, with lower neurotoxicity, and participating in the oxidative damage process. Aβ42 oligomers bind to various neuronal surface receptors (such as PrPc, mGluR5, NMDA receptors, etc.), triggering oxidative stress, calcium homeostasis imbalance, and synaptic toxicity via activating downstream signaling pathways, leading to neuronal dysfunction and death.
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27
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| HY-P1363A | β-Amyloid (1-42), human |
β-Amyloid (1-42) (Amyloid β-peptide (1-42)), human, a 42-amino acid peptide that has not been treated with HFIP, is a brain-penetrant amyloid protein fragment, which can be used in research on Alzheimer's disease and Down’s syndrome. β-Amyloid (1-42), human remaining as a monomer exhibits antioxidant and neuroprotective effects. β-Amyloid (1-42), human, after being monomericized by HFIP and dissolved in DMSO to form the stock solution, on the one hand, can form soluble oligomers (AβOs) when incubated at 4 °C, which have synaptic toxicity and neurotoxicity; on the other hand, it can be incubated at 37 °C to form insoluble fibrils, with lower neurotoxicity, and participating in the oxidative damage process. Aβ42 oligomers bind to various neuronal surface receptors (such as PrPc, mGluR5, NMDA receptors, etc.), triggering oxidative stress, calcium homeostasis imbalance, and synaptic toxicity via activating downstream signaling pathways, leading to neuronal dysfunction and death.
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27
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| HY-16900 | Rolipram |
Rolipram is a PDE4 inhibitor, with blood-brain barrier permeability, that reverses β-amyloid-induced learning and memory impairment in rats. Rolipram elevates intracellular cAMP and clevels and regulates the cAMP/CREB signaling pathway, thereby alleviating neuroinflammation and apoptotic responses. Rolipram promotes neuronal differentiation of human bone marrow mesenchymal stem cells and inhibits Methamphetamine- and morphine-induced hyperlocomotion in mice. Rolipram also reduces the viability of glioblastoma stem-like cells and enhances Bevacizumab (HY-P9906)-induced cell death. Rolipram inhibits the expression of proinflammatory cytokines and enhances central noradrenergic transmission. Rolipram is mainly used in studies related to various central nervous system diseases including Alzheimer's disease, major depressive disorder, glioblastoma multiforme, and multiple sclerosis.
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Colorectal Cancer
Bacterial Infection
Depression
SARS-CoV-2 Infection
Alzheimer's Disease
Huntington's Disease
HIV-1 Infection
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19
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| HY-143218 | TPE-MI |
TPE-MI (Tetraphenylethene maleimide) is a thiol probe for measuring unfolded protein load and proteostasis in cells (the excitation wavelength is 350 nm and the emission wavelength is 470 nm). TPE-MI can report imbalances in proteostasis in induced pluripotent stem cell models of Huntington disease, as well as cells transfected with mutant Huntington exon 1 before the formation of visible aggregates. TPE-MI also detects protein damage following dihydroartemisinin research of the malaria parasites Plasmodium falciparum .
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18
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| HY-B0298A | Clemastine fumarate |
Clemastine (HS-592; Meclastine) fumarate is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine fumarate also antagonizes muscarinic acetylcholine receptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine fumarate exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .
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14
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| HY-15136 | Lonafarnib |
Lonafarnib (Sch66336) is an orally active, blood-brain barrier penetrant farnesyltransferase (FPTase) inhibitor. Lonafarnib increases the phosphorylation levels of Akt, CaMKII and CREB, upregulates BDNF expression in the hippocampus, elevates the content of α7nAChR on cell membranes, and blocks the isoprenylation of H-Ras. Lonafarnib repairs synapses and reverses spatial memory deficits in Aβ1-42 model mice. Lonafarnib inhibits RSV fusion and replication, and alleviates virus-induced lung injury. Lonafarnib activates the lysosomal and autophagic pathways, and reduces the phosphorylation and aggregation of tau. Lonafarnib acts synergistically with Sorafenib (HY-10201) to promote apoptosis, and inhibits the proliferation and invasion of melanoma cells. Lonafarnib inhibits the farnesylation of progerin, repairs nuclear membrane defects, and activates the cGAS-STING-STAT1 signaling pathway. Lonafarnib can be used in research related to diseases including Alzheimer's disease, viral infections, melanoma, and progeria.
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14
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| HY-N0373 | Licochalcone B |
Licochalcone B is an extract from the root of Glycyrrhiza uralensis. Licochalcone B inhibits amyloid β (42) self-aggregation (IC50=2.16 μM) and disaggregate pre-formed Aβ42 fibrils, reduce metal-induced Aβ42 aggregation through chelating metal ionsLicochalcone B inhibits phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone B inhibits growth and induces apoptosis of NSCLC cells. Licochalcone B specifically inhibits the NLRP3 inflammasome by disrupting NEK7‐NLRP3 interaction.
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Digestive System Disease
Lung Cancer
Depression
Autoimmune Disease
Digestive System Inflammation
Alzheimer's Disease
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12
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| HY-15594A | Phen-DC3 Trifluoromethanesulfonate |
Phen-DC3 Trifluoromethanesulfonate is a bisquinolinium G-quadruplex (G4) ligand. Phen-DC3 Trifluoromethanesulfonate selectively binds to and stabilizes the hybrid quadruplex-duplex hybrid (QDH) derived from the PIM1 promoter. Phen-DC3 Trifluoromethanesulfonate also binds to the c-myc promoter Pu24T G4 via extensive π-stacking, and induces polymerase stalling at α-synuclein DNA and RNA G4 sequences. Phen-DC3 Trifluoromethanesulfonate downregulates LPS (HY-D1056)-induced TNFRSF21, RIPK3 and p-MLKL in VECs, and ameliorates CLP-induced pulmonary vascular leakage in septic rats. Phen-DC3 Trifluoromethanesulfonate can be used in studies related to neurodegenerative diseases and sepsis-associated vascular injury.
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12
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| HY-153169 | 6PPD-Q |
6PPD-Q (6PPD-Quinone) is an environmental pollutant that can be detected in human urine and is widely present in the environment. 6PPD-Q targets and binds to CNR2, CNR1, AA2AR, LCAT, and TRPA1, with CNR2 exhibiting the highest binding affinity, potentially acting as a CNR2 receptor agonist to activate cannabinoid receptors. 6PPD-Q induces intestinal inflammation and barrier damage by disrupting mitochondrial function, reducing neuronal glycolysis metabolites and TCA cycle intermediates, and exacerbating α-synuclein (α-syn) aggregation.
6PPD-Q is applicable in research on environmental toxicology, neurodegenerative diseases, and inflammation-related disorders.
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11
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| HY-106443B | Arimoclomol citrate |
Arimoclomol citrate (BRX-220 citrate) is an orally active co-inducer of heat shock proteins (HSP). Arimoclomol citrate protects motor neurons by enhancing Hsp expression, thus directly affecting protein aggregation and clearance of misfolded assemblies via the proteasome-ubiquitin system. Arimoclomol citrate can be used for the study of Niemann–Pick disease type C.
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Neurological, Eye or Ear Disease
Inflammation or Immune System Disease
Metabolic or Endocrine Disease
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7
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| HY-106443 | Arimoclomol |
Arimoclomol (BRX-220 free base) is an orally active co-inducer of heat shock proteins (HSP). Arimoclomol protects motor neurons by enhancing Hsp expression, thus directly affecting protein aggregation and clearance of misfolded assemblies via the proteasome-ubiquitin system.Arimoclomol can be used for the study of Niemann–Pick disease type C. Arimoclomol can cross the blood-brain barrier and can be used in research on Niemann-Pick disease type C.
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Neurological, Eye or Ear Disease
Inflammation or Immune System Disease
Metabolic or Endocrine Disease
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7
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| HY-112904 | XRK3F2 |
XRK3F2 is a p62 (sequestosome-1) ZZ domain inhibitor that has specificity for the p62-ZZ domain over other p62 signaling domains. XRK3F2 blocks TNFα effects and upregulation in bone marrow stromal cells, and induces multiple myeloma cell apoptosis. XRK3F2 can be used for the research of multiple myeloma bone disease, acute myeloid leukemia, and multiple myeloma.
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7
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| HY-106443A | Arimoclomol maleate |
Arimoclomol maleate (BRX-220) is an orally active co-inducer of heat shock proteins (HSP). Arimoclomol protects motor neurons by enhancing Hsp expression, thus directly affecting protein aggregation and clearance of misfolded assemblies via the proteasome-ubiquitin system.Arimoclomol maleate can be used for the study of Niemann–Pick disease type C.
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Neurological, Eye or Ear Disease
Inflammation or Immune System Disease
Metabolic or Endocrine Disease
SARS-CoV-2 Infection
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7
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| HY-19948 | Leucomethylene blue mesylate |
Leucomethylene blue (TRx0237) mesylate, an orally active second-generation tau protein aggregation inhibitor (Ki of 0.12 μM), could be used for the study of Alzheimer's Disease. Leucomethylene blue mesylate is a common reduced form of Methylene Blue, Methylene Blue is a member of the thiazine class of dyes.
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6
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| HY-115576 | P62-mediated mitophagy inducer |
P62-mediated mitophagy inducer (PMI) is a P62-mediated mitophagy activator. P62-mediated mitophagy inducer activates mitochondrial autophagy without recruitment of Parkin or collapse of the mitochondrial membrane potential and remains active in cells lacking a fully functional PINK1/Parkin pathway. P62-mediated mitophagy inducer serves as a pharmacological tool to study the molecular mechanisms of mitosis, avoiding toxicity and some of the non-specific effects associated with the sudden dissipation of mitochondria lacking membrane potential.
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6
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| HY-125623 | MitoPerOx |
MitoPerOx is a mitochondrial-targeted, lipid peroxidation-indicating fluorescent probe with BODIPY581/591 fluorophores. The triphenylphosphine cation (TPP+) of MitoPerOx can be selectively enriched in mitochondria (depending on membrane potential) and can be used to detect lipid peroxidation in the inner mitochondrial membrane. Under the action of lipid peroxides, the BODIPY581/591 fluorophores of MitoPerOx shift their emission wavelength from 590 nm (reduced state) to 520 nm (oxidized state), and ratiometric detection can be performed at an excitation wavelength of 488 nm. MitoPerOx can specifically monitor the peroxidation of mitochondrial phospholipids (especially cardiolipin) and is used in the study of oxidative stress-related diseases (such as aging, neurodegenerative diseases, and mitochondrial dysfunction)[1][2].
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5
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| HY-N1501 | Beta-asarone |
Beta-asarone is an orally active and BBB-penetrable anti-inflammatory agent and neuroprotective agent, which is the major ingredient of Acorus tatarinowii Schott. Beta-asarone can protect nerve cells from apoptosis and autophagy, inhibit expression of α-synuclein, as well as myocardial protection. Beta-asarone can be used in the study of neurological and cardiovascular diseases.
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Inflammation or Immune System Disease
Cardiovascular Disease
Alzheimer's Disease
Parkinson's Disease
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4
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| HY-N0743 | Senkyunolide A |
Senkyunolide A is a phthalide, anti-tumor cell proliferation agent with anticancer activity. Senkyunolide A protects neurons from corticosterone (HY-B1618)-induced apoptosis by decreasing protein phosphatase PP2A and α-synuclein phosphorylation and protein level. Senkyunolide A also inhibits osteoarthritis through the NLRP3 signaling pathway and suppresses the expression of CD137, a diagnostic biomarker for atherosclerosis.
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4
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| HY-W020033 | Lanosterol |
Lanosterol is an intermediate of cholesterol synthesis and use of lanosterol induces ubiquitination and degradation of a rate-controlling enzyme of cholesterol synthesis, i.e., HMG CoA reductase. Lanosterol suppresses the aggregation and cytotoxicity of misfolded proteins linked with neurodegenerative diseases.
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4
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| HY-123960A | Raphin1 acetate |
Raphin1 acetate is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 acetate binds strongly to the R15B-PP1c holophosphatase (Kd=33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 acetate crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease.
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3
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| HY-123960 | Raphin1 |
Raphin1 is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 binds strongly to the R15B-PP1c holophosphatase (Kd=33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease.
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3
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| HY-P99407 | Pepinemab |
Pepinemab (VX 15/2503) is a human monoclonal antibody against SEMA4D, a signalling protein 4D (SEMA4D), also known as CD100, which is a regulator of neuronal development and plays a role in a variety of cellular processes. Pepinemab can be used in the study of various neurodegenerative diseases such as Alzheimer's disease by blocking the activity of SEMA4D.
Species: Human |
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3
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| HY-136733 | Ac-DNLD-CHO |
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2
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| HY-113303 | FAPy-adenine |
FAPy-adenine is an oxidized DNA base. Fapy-adenine shows an increased trend levels in the Alzheimer's disease brain. Oxidized nucleosides are biochemical markers for tumors, aging, and neurodegenerative diseases.
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2
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| HY-B0248 | Desonide |
Desonide is a non-fluorinated corticosteroid anti-inflammatory agent that acts on the glucocorticoid receptor. Desonide can also specifically bind to the mutant huntingtin protein (mHTT), reducing the level and toxicity of mHTT. Desonide can be used in the research of Huntington's disease and inflammatory diseases such as atopic dermatitis.
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2
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| HY-101184 | T807 |
T807 a novel tau positron emission tomography (PET) tracer.
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2
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| HY-W010201 | Citronellol |
Citronellol ((±)-Citronellol) is an orally active inducer of apoptosis. Citronellol can prevent oxidative stress, mitochondrial dysfunction, and apoptosis in the SH-SY5Y cell Parkinson's disease model induced by 6-OHDA by regulating the ROS-NO, MAPK/ERK, and PI3K/Akt signaling pathways. Citronellol can induce necroptosis in human lung cancer cells through the TNF-α pathway and accumulation of ROS. Citronellol can reduce the levels of LC-3 and p62 to regulate the autophagy pathway, inhibit oxidative stress and neuroinflammation, and thus have neuroprotective effects on Parkinson's rats. Citronellol exhibits anti-fungal activity against Trichophyton rubrum by inhibiting ergosterol synthesis.
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p62
Environmental Pollutants
Fungal
Atg8/LC3
PI3K
Autophagy
ERK
Apoptosis
Necroptosis
Reactive Oxygen Species (ROS)
TNF Receptor
Respiratory Disease
Breast Cancer
Pancreatic Cancer
Fungal Infection
Pain
Autoimmune Disease
Digestive System Inflammation
Cardiovascular Disease
Non-Small Cell Lung Cancer
Parkinson's Disease
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2
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| HY-129960 | L-Selenocystine |
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2
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| HY-W018791 | Bifendate |
Bifendate (DDB), extracted from Schisandrae chinensis, is an orally active anti-HBV agent against chronic hepatitis B. Bifendate inhibits ATG5-dependent autophagy and attenuates oleic acid-induced lipid accumulation with anti-oxidant properties in vitro. Bifendate can decrease alanine transaminase (ALT) level in mice. Bifendate attenuates hepatic steatosis in cholesterol/bile salt- and high-fat diet-induced hypercholesterolemia in mice. Bifendate potently increases the activity of cytochrome proteins (CYPs) and reverse P-gp-mediated multi-drug resistance (MDR).
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2
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| HY-122704A | Surfen dihydrochloride |
Surfen dihydrochloride is a potent heparan sulfate antagonist. Surfen inhibits FGF2 binding and signal transduction. Surfen binds to glycosaminoglycans and reduces tau hyperphosphorylation. Surfen dihydrochloride inhibits the activity of recombinant uronyl 2-O-sulfotransferase with an IC50 of approximately 2 μM. Surfen dihydrochloride inhibits HSV-1 viral infection. Surfen dihydrochloride inhibits neural differentiation, delays remyelination, and alleviates EAE.
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Inflammation or Immune System Disease
Lung Cancer
Prostate Cancer
Liver Cancer
Viral Infection
Neurodegenerative Disease
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2
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| HY-W004563 | Neocuproine |
Neocuproine is an organic compound commonly used as a complexing reagent and copper ion detector. It can form stable complexes with copper ions, and can play a catalytic role in certain chemical reactions and analytical methods. In addition, this compound is also widely used in some biomedical fields, such as in the study of copper metabolism disorders and neurodegenerative diseases
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2
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| HY-10863 | Anandamide |
Anandamide is an endocannabinoid. Anandamide modulates both neuronal and immune functions through two protein-coupled cannabinoid receptors (CB1 and CB2). Anandamide can activate numerous other receptors like PPARS, TRPV1, and GPR18/GPR55. Anandamide also has potential anti-fungal and anti-inflammatory activities. Anandamide can be used for the research of Alzheimer’s disease (AD) and ulcerative colitis.
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Neurological, Eye or Ear Disease
Inflammation or Immune System Disease
Metabolic or Endocrine Disease
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2
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| HY-W040074 | Glycylglycine hydrochloride hydrate |
Glycylglycine hydrochloride hydrate is a non-selective Glycylglycine hydrochloride hydrate dipeptidase substrate and iNOS inhibitor. Glycylglycine hydrochloride hydrate can cross the cell membrane by passive diffusion and is hydrolyzed to glycine in the cell, participating in energy metabolism and antioxidant processes. Glycylglycine hydrochloride hydrate promotes spermatogonial stem cells (SSCs) proliferation, inhibits astrocyte overactivation and reduces nitric oxide (NO) release, while upregulating the expression of neurotrophic factors (such as PDGFA, FGF2, CNTF) to support nerve myelin repair. Glycylglycine hydrochloride hydrate can be used to study male reproductive biology (such as SSCs proliferation regulation) and neurodegenerative diseases (such as neuroprotective mechanisms in multiple sclerosis).
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1
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| HY-D0214E | Acid Red 94 sodium (80%) |
Acid Red 94 sodium (80%), a synthetic fluorescein derivative, is a deep red dye primarily composed of 4,5,6,7-tetrachloro-2,4,5,7-tetraiodo fluorescein. Acid Red 94 sodium (80%) is widely used as an ophthalmic diagnostic agent to detect dry or damaged cells on the ocular surface. Acid Red 94 sodium (80%) exhibits antitumor activity and can inhibit Friend Leukemia Virus (FLV) infection through photodynamic action. Additionally, Acid Red 94 sodium (80%) can inhibit Aβ aggregation through light irradiation. Acid Red 94 sodium (80%) holds potential for use in cancer, viral infections, and neurodegenerative disease research.
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1
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| HY-139606 | VCP/p97 inhibitor-1 |
VCP/p97 inhibitor-1 is a potent inhibitor of VCP/p97 (also called Cdc48, CDC-. 48, or Ter94) with an IC50 of 54.7 nM. VCP/p97 inhibitor-1 causes the dysregulation of protein homeostasis and disturbs the degradation of misfolded polypeptides by the ubiquitin-proteasome system (UPS).
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1
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| HY-W040269 | Dehydrothio-p-toluidine |
Dehydrothio-p-toluidine (DHPT) is a chemical intermediate used in dyestuff production. Dehydrothio-p-toluidine shows inhalation toxicity in acute and subchronic conditions.
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1
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| HY-W338584 | Hydroxycitric acid tripotassium |
Tripotassium hydroxycitrate is an orally active, multi-target, multi-bioactive organic acid. Tripotassium hydroxycitrate activates Nrf2 and its downstream molecule GPX4, increases glutathione levels, and thereby inhibits ferroptosis. Tripotassium hydroxycitrate activates the Nrf2/Keap1 and ACLY/NF-κB signaling pathways, upregulates the activities of antioxidant enzymes such as superoxide dismutase, reduces MDA content, thereby alleviating oxidative stress and renal tubular epithelial cell apoptosis, and improves pulmonary vascular and right ventricular remodeling. Tripotassium hydroxycitrate activates both the AMPK and mTORC1/S6K pathways, triggers the unfolded protein response, arrests the cancer cell cycle, and induces DNA fragmentation.
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Keap1-Nrf2
Ferroptosis
Apoptosis
mTOR
NF-κB
ATP Citrate Lyase
AMPK
Ribosomal S6 Kinase (RSK)
DNA/RNA Synthesis
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1
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| HY-148089 | Eplontersen |
Eplontersen is a triantennary N-acetyl galactosamine (GalNAc3-7a)-conjugated antisense oligonucleotide targeting transthyretin (TTR) mRNA to inhibit production of both variant and wild-type TTR protein. Misfolded TTR induces amyloid fibrils formation in the heart and peripheral nerves, leads to amyloid TTR (ATTR) amyloidosis diseases.
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1
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| HY-N0805A | Alisol B |
Alisol B is a triterpene with diverse biological activities. Alisol B binds human soluble epoxide hydrolase (sEH) with a Ki of 5.97 μM and reduces sEH activity. Alisol B inhibits RANKL-induced JNK phosphorylation, NFATc1 and c-Fos expression, osteoclast formation, mature osteoclast pit-forming and actin ring activity, and SERCA pump activity. Alisol B induces calcium mobilization, CaMKK-AMPK-mTOR pathway activation, autophagic flux, autophagosome formation, G1 phase cell cycle arrest, endoplasmic reticulum stress, unfolded protein responses, and cancer cell apoptosis. Alisol B can be used for the research of hypercalcemia, osteoporosis, rheumatoid arthritis, periodontitis, acute kidney injury, and breast cancer.
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1
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| HY-136780 | SEN177 |
SEN177 is an orally effect glutamine cyclase (QC) inhibitor. The Ki of SEN177 for human glutamine cyclase (hQC) is 20 nM, and the IC50 is 13 nM. SEN177 interferes with the interaction between CD47 and SIRRPα, and has anti-tumor activity. SEN177 reduces aggregation and apoptosis caused by HTT mutation in Huntington model, and can be used in the study of neurodegenerative diseases.
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1
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| HY-148089A | Eplontersen sodium |
Eplontersen sodium the sodium salt form of Eplontersen (HY-148089). Eplontersen sodium is a triantennary N-acetyl galactosamine (GalNAc3-7a)-conjugated antisense oligonucleotide targeting transthyretin (TTR) mRNA to inhibit production of both variant and wild-type TTR protein. Misfolded TTR induces amyloid fibrils formation in the heart and peripheral nerves, leads to amyloid TTR (ATTR) amyloidosis diseases.
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1
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| HY-N1458 | Isoschaftoside |
Isoschaftoside, a C-glycosylflavonoid from Desmodium uncinatum root exudate, can inhibit the growth of germinated S. hermonthica radicles. Isoschaftoside reduces reactive oxygen species (ROS) and induces proliferation in senescent cells. Isoschaftoside activates autophagy. Isoschaftoside can be used for anti-tumor, anti-inflammatory, antioxidant, antihypertensive, hepatoprotective and nematicidal study.
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Cancer
Inflammation or Immune System Disease
Metabolic or Endocrine Disease
Parasitic Infection
Hypertension
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1
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| HY-111126 | K67 |
K67 is a selective the interaction between Keap1 and S349 phosphorylated p62 inhibitor, with an IC50 of 1.5 μM. K67 has a weaker inhibitory effect on the interaction between Keap1 and Nrf2 (IC50 is 6.2 μM). K67 competitively binds to the binding site of Keap1 with p-p62, blocking the abnormal activation of the p62-dependent Nrf2 pathway. K67 inhibits tumor cell proliferation and enhances the sensitivity of hepatocellular carcinoma (HCC) to chemotherapeutic drugs by restoring Keap1-mediated ubiquitination and degradation of Nrf2.
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1
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| HY-N1437 | Hydroxycitric acid |
Hydroxycitric acid is an orally active, multi-target, multi-bioactive organic acid. activates Nrf2 and its downstream molecule GPX4, increases glutathione levels, and thereby inhibits ferroptosis. Hydroxycitric acid activates the Nrf2/Keap1 and ACLY/NF-κB signaling pathways, upregulates the activities of antioxidant enzymes such as superoxide dismutase, reduces MDA content, thereby alleviating oxidative stress and renal tubular epithelial cell apoptosis, and improves pulmonary vascular and right ventricular remodeling. Hydroxycitric acid activates both the AMPK and mTORC1/S6K pathways, triggers the unfolded protein response, arrests the cancer cell cycle, and induces DNA fragmentation.
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Apoptosis
DNA/RNA Synthesis
NF-κB
mTOR
Ribosomal S6 Kinase (RSK)
AMPK
Ferroptosis
Keap1-Nrf2
ATP Citrate Lyase
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1
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| HY-D0914 | Fast Green FCF |
Fast Green FCF is a sea green triarylmethane food dye, with absorption maximum ranging from 622 to 626 nm. Fast Green FCF inhibits α-synuclein aggregation, as well as Aβ and P2X4 receptor, and TLR4/Myd88/NF-κB. Fast Green FCF is widely used as a staining agent like quantitative stain for histones at alkaline pH after acid extraction of DNA, and as a protein stain in electrophoresis. Fast Green FCF improves cognitive impairment, depression, relieves pain allergies, and promotes reproductive function.
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1
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| HY-W050044 | L-Azetidine-2-carboxylic acid |
L-Azetidine-2-carboxylic acid is a proline analog. L-Azetidine-2-carboxylic acid upregulates the lipid autophagy marker LC3-II via activation of the PERK pathway. L-Azetidine-2-carboxylic acid increases pro-apoptotic BAX protein. L-Azetidine-2-carboxylic acid induces ATF6 cleavage and upregulates phosphorylated eIF2α levels. L-Azetidine-2-carboxylic acid induces ER stress, inducing protein misfolding and aggregation. L-Azetidine-2-carboxylic acid shows teratogenic, pro-inflammatory and pro-apoptotic effects.
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Endogenous Metabolite
PERK
Atg8/LC3
Autophagy
Bcl-2 Family
Apoptosis
Eukaryotic Initiation Factor (eIF)
ATF6
Cancer
Neurological, Eye or Ear Disease
Metabolic or Endocrine Disease
Digestive System Disease
Digestive System Inflammation
Cardiovascular Disease
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1
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| HY-109521A | Manganese chloride tetrahydrate, molecular biology grade,≥99.0% (KT) |
Manganese chloride (tetrahydrate), molecular biology grade,≥99.0% (KT) is an orally active and a blood-brain barrier penetrant compound. It affects the activities of multiple enzymes in cells, such as regulating the activities of histone acetyltransferase (HAT) and histone deacetylase (HDAC), thereby affecting gene expression. It has multiple activities such as neurotoxicity, embryotoxicity, and reproductive toxicity. It is currently mainly used in neurodegenerative diseases and toxicology research.
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1
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| HY-D0214 | Acid Red 94 sodium |
Acid Red 94 sodium, a synthetic fluorescein derivative, is a deep red dye primarily composed of 4,5,6,7-tetrachloro-2,4,5,7-tetraiodo fluorescein. It is widely used as an ophthalmic diagnostic agent to detect dry or damaged cells on the ocular surface. Acid Red 94 sodium exhibits antitumor activity and can inhibit Friend Leukemia Virus (FLV) infection through photodynamic action. Additionally, Acid Red 94 sodium can inhibit Aβ aggregation through light irradiation. Acid Red 94 sodium holds potential for use in cancer, viral infections, and neurodegenerative disease research.
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1
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| HY-P990110 | Lecanemab (Mouse IgG2a) |
Lecanemab (Mouse IgG2a) (Mab158) is a monoclonal antibody that targets soluble β-amyloid and has the potential to reduce cognitive decline. The variable region of Lecanemab (Mouse IGG2a) is consistent with that of Lecanemab, while the constant region is of Mouse IgG2a sequence. Lecanemab (Mouse IgG2a) almost abolishes Aβ accumulation in astrocytes and rescues neurons from Aβ-induced cell death. Lecanemab (Mouse IgG2a) holds promise for research in the field of Alzheimer's disease.
Species: Human |
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1
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| HY-100857 | PrPSc-IN-1 |
PrPSc-IN-1 is a fluorescent probe, binds to the misfolded protein PrPSc, inhibits its accumulation, with an IC50 of 1.6 μM. Anti-prion activity.
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| HY-161895 | CFTR corrector 14 |
CFTR corrector 14 (Compound SVQ26) is a class 3 corrector for cystic fibrosis transmembrane conductance regulator (CFTR), that promotes the CFTR activity (EC50 of 3.08 μM with presence of C1 class corrector VX-809). CFTR corrector 14 regulates the mutant-caused misfolding and impaired function of the CFTR protein. CFTR corrector 14 can be used in research about cystic fibrosis.
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| HY-184247 | SR-32685 |
SR-32685 is a NAMPT activator and neuroprotective agent. SR-32685 enhances the enzymatic activity of hNAMPT, prevents intracellular NAD depletion, and protects neurons from death induced by toxic misfolded prion proteins. SR-32685 can be used in the research of protein misfolding neurodegenerative diseases and metabolic diseases.
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| HY-W004287R | Methyl tridecanoate (Standard) |
Methyl tridecanoate (Standard) is the analytical standard of Methyl tridecanoate. This product is intended for research and analytical applications. Methyl tridecanoate moderately inhibits β-amyloid aggregation. Methyl tridecanoate weakly inhibits acetylcholinesterase (AChE).
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| HY-181764 | LZL50 |
LZL50 is an orally effective human caseinolytic protease P (hClpP) activator with an EC50 of 0.29 μM. LZL50 activates hClpP, a serine protease that mediates mitochondrial quality control by degrading damaged or misfolded mitochondrial proteins. LZL50 exhibits antitumor activity in a breast cancer xenograft mouse model. LZL50 can be used in research related to breast cancer.
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| HY-18956B | (E/Z)-Icerguastat acetate |
(E/Z)-Icerguastat ((E/Z)-Sephin1) acetate is a selective inhibitor of the phosphatase regulatory subunit PPP1R15A (R15A). (E/Z)-Icerguastat acetate can be used for protein misfolding diseases research.
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| HY-P11080 | Oncocin |
Oncocin is an antibacterial peptide. It belongs to proline-rich antimicrobial peptides (PrAMPs). Oncocin works against Gram-negative bacteria. It has MIC values of 0.125-8 μg/mL for 34 strains and clinical isolates of Enterobacteriaceae and nonfermenters. Oncocin binds to the substrate-binding domain of the chaperone DnaK. The binding has dissociation constants in the micromolar range. This binding causes protein misfolding and aggregation and the bacteria death.
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| HY-114613 | D-Trp-Aib |
D-Trp-Aib is a dipeptide and amyloid-β inhibitor with a Kd of 29.6 nM. D-Trp-Aib triggers formation of non-toxic, non-β-sheet, amorphous amyloid β clusters from misfolded amyloid β monomers and toxic amyloid β oligomers, and reduces toxic amyloid β1-42 deposits. D-Trp-Aib inhibits amyloid fibril formation of α‑synuclein, IAPP and calcitonin. D-Trp-Aib can be used for the research of Alzheimer's disease.
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| HY-P10613 | RERMS |
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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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/
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| HY-W707693 | Scyllo-Inositol-d6 |
Scyllo-Inositol-d6 is the deuterium labeled Scyllo-Inositol (HY-W010041). Scyllo-Inositol is an inhibitor that targets the aggregation of misfolded proteins (such as α-synuclein and Amyloid-β), is orally effective, and can cross the blood-brain barrier. Scyllo-Inositol can selectively bind to and stabilize non-toxic oligomers, preventing them from converting into toxic fibers, exerting protein homeostasis regulation and neuroprotective activity. Scyllo-Inositol binds to the hydrophobic region of pathogenic proteins, inhibits protein aggregation, and promotes lysosome- and proteasome-mediated degradation pathways, thereby reducing neurotoxicity. Scyllo-Inositol can be used in the study of neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, and Huntington's disease.
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| HY-DY1024 | TPE-MI (solution) |
TPE-MI (Tetraphenylethene maleimide) (solution) is a thiol probe for measuring unfolded protein load and proteostasis in cells (the excitation wavelength is 350 nm and the emission wavelength is 470 nm). TPE-MI can report imbalances in proteostasis in induced pluripotent stem cell models of Huntington disease, as well as cells transfected with mutant Huntington exon 1 before the formation of visible aggregates. TPE-MI also detects protein damage following dihydroartemisinin research of the malaria parasitesPlasmodium falciparum .
Solvent and concentration: DMSO: 10 mM |
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| HY-N15556 | Thaigranatumin C |
Thaigranatumin C is a protolimonoid compound found in the seeds of the Thai mangrove (Xylocarpus granatum). Thaigranatumin C is promising for research of neurodegenerative diseases such as Parkinson's diseases.
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| HY-P4308 | Z-Pro-Pro-aldehyde-dimethyl acetal |
Z-Pro-Pro-aldehyde-dimethyl acetal is a potent inhibitor of prolyl endopeptidase (PREP), a cytoplasmic serine endoprotease (IC50= 12 nM). Z-Pro-Pro-aldehyde-dimethyl acetal plays an important role in cognitive dysfunction in aging and neurodegenerative diseases including Alzheimer's disease.
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| HY-N15559 | Thaigranatumin F |
Thaigranatumin F is a protolimonoid compound found in the seeds of the Thai mangrove (Xylocarpus granatum). Thaigranatumin F is promising for research of neurodegenerative diseases such as Parkinson's diseases.
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| HY-B1588S | Carbenoxolone-d4 |
Carbenoxolone-d4 is the d4 labeled Carbenoxolone (HY-B1588). Carbenoxolone is a blood-brain barrier-permeable Pannexin1 inhibitor, gap junction (Gap junction) blocker, and β-amyloid 42 inhibitor. Carbenoxolone modulates voltage-gated currents of wild-type and mutant Panx1, and inhibits stimulus-activated Panx1 channel function. Carbenoxolone interacts with stable residues of β-amyloid 42 peptides, fibrils and oligomers, thereby inhibiting their aggregation. Carbenoxolone alleviates liver fibrosis. Carbenoxolone exerts neuroprotective and nootropic effects. Carbenoxolone can be used in studies related to Alzheimer's disease and liver fibrosis.
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| HY-153830S | LacCer (d18:1/16:0)-d3 |
LacCer (d18:1/16:0) (C16 Lactosylceramide (d18:1/16:0))-d3 is the deuterium labeled LacCer (d18:1/16:0) (HY-153830). LacCer (d18:1/16:0) is an endogenous bioactive sphingolipid that can form membrane microdomains with Lyn kinase and the αi subunits of inhibitory G protein-coupled receptors (GPCRs). LacCer (d18:1/16:0) are elevated in the plasma of insulin-resistant cattle. LacCer (d18:1/16:0) is also upregulated in a mouse model of Niemann-Pick type C1 disease (a neurodegenerative cholesterol-sphingolipid lysosomal storage disorder). LacCer (d18:1/16:0) can be used in research on metabolic diseases and neurodegenerative diseases.
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| HY-P991380 | TXB4 |
TXB4 is a brain-permeable human monoclonal antibody (mAb) targeting CD71. TXB4 prevents 6-OHDA-induced death of TH-positive neurons in the SNc in a 6-OHDA mouse model of Parkinson's disease (PD). TXB4 can be used in neurodegenerative diseases, acute brain and spinal cord injury, and depression research.
Species: Human |
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| HY-P992411 | MEDI-8490 |
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| HY-124375 | IND81 |
IND81 is an orally active antiprion with IC50 value of 1.95 μM. IND81 reduces abnormal, misfolded, disease-causing forms of benign prion proteins that are normally present on or within cells.
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| HY-185357 | TAU-IN-6 |
TAU-IN-6 (Compound 13) is a Tau protein misfolding and aggregation inhibitor. TAU-IN-6 inhibits stress granules composed of tau and TIA1. TAU-IN-6 is applicable for Alzheimer's disease research.
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| HY-P10077 | GL189 |
GL189 is a β-secretase inhibitor. GL189 has neuroprotective effect, and can be used for research of neurodegenerative diseases.
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| HY-N15545 | Thaigranatumin I |
Thaigranatumin I is a limonoid compound found in the seeds of the Thai mangrove (Xylocarpus granatum). Thaigranatumin I is promising for research of neurodegenerative diseases such as Parkinson's diseases.
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| HY-184246 | SR-34831 |
SR-34831 is a NAMPT activator, NAD level stabilizer and neuroprotective agent. SR-34831 enhances the enzymatic activity of human NAMPT, prevents intracellular NAD depletion, and counteracts neuronal death induced by toxic misfolded prion proteins. SR-34831 exhibits metabolic stability in human liver microsomes and can be used for the research of protein misfolding neurodegenerative diseases.
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| HY-N15557 | Thaigranatumin D |
Thaigranatumin D is a protolimonoid compound found in the seeds of the Thai mangrove (Xylocarpus granatum). Thaigranatumin D is promising for research of neurodegenerative diseases such as Parkinson's diseases.
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| HY-N2898 | Artanin |
Artanin is a coumarin, has biological activities related to Alzheimer’s disease. Artanin exerts function including AChE inhibitory and AChE- and self-induced amyloid beta (Aβ) aggregation inhibitory activities, with IC50s of 51 μM, 98 μM, and 124 μM, respectively.
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| HY-N15572 | 1,2,4,6-Tetra-O-galloyl-β-D-glucose |
1,2,4,6-Tetra-O-galloyl-β-D-glucose is an acetylcholinesterase inhibitor with an IC50 of 1.5 μM against human targets. 1,2,4,6-Tetra-O-galloyl-β-D-glucose inhibits the aggregation of amyloid-β. 1,2,4,6-Tetra-O-galloyl-β-D-glucose exhibits anti-herpesvirus activity against both HSV-1 and HSV-2 in vitro. 1,2,4,6-Tetra-O-galloyl-β-D-glucose possesses superoxide dismutase-like antioxidant activity, and also inhibits tyrosinase and hyaluronidase. 1,2,4,6-Tetra-O-galloyl-β-D-glucose can be used in studies related to Alzheimer's disease, herpesvirus infection and antioxidation.
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| HY-B1378S2 | Ethosuximide-13C, d3 |
Ethosuximide-13C, d3 is the 13C- and deuterium labeled Ethosuximide (HY-B1378). Ethosuximide, a widely prescribed anti-epileptic agent, improves the phenotypes of multiple neurodegenerative disease models and blocks the low voltage activated T-type calcium channel.
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| HY-187320S | [U-15N]-Aβ(1-40)/[U-15N]-Aβ(1-42) |
[U-15N]-Aβ(1-40)/[U-15N]-Aβ(1-42) is the 15N-labeled Aβ(1-40) and Aβ(1-42). Abnormal levels and aggregation of beta-amyloid (Aβ) in the brain are considered key factors in the pathogenesis of Alzheimer's disease (AD). This isotope can be used in NMR studies of disease mechanisms and in mass spectrometry analysis.
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| HY-N15554 | Thaigranatumin A |
Thaigranatumin A is a protolimonoid compound found in the seeds of the Thai mangrove (Xylocarpus granatum). Thaigranatumin A is promising for research of neurodegenerative diseases such as Parkinson's diseases.
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| HY-N12887 | Mycothiazole |
Mycothiazole is an inhibitor for mitochondrial electron transport chain (ETC) complex I. Mycothiazole exhibits cytotoxicity in cancer cells Huh7 (IC50 is 55.8 μM), U87 and MCF7. Mycothiazole induces apoptosis in Huh7. Mycothiazole utilizes the unfolded protein response (UPR) and heat shock response (HSR) pathway involved transcription factors ATFS-1 and HSF1, to extend the lifespan of C. elegans.
Source: marine sponge |
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| HY-15728S | Radotinib-d6 |
Radotinib-d6 is deuterium labeled Radotinib (HY-15728). Radotinib (IY-5511) is an orally active and BBB-permeable selective tyrosine kinase Bcr-Abl1 inhibitor with an IC50 of 34 nM. Radotinib has anti-prion and anti-tumor activities. Radotinib can inhibit the proliferation, induce cell cycle arrest and apoptosis of tumor cells . Radotinib can be used in the research of cancer such as chronic myeloid leukemia and multiple myeloma, as well as neurodegenerative diseases such as prion diseases.
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| HY-P1378 | β-Amyloid (1-43)(human) |
β-Amyloid (1-43)(human) is more prone to aggregation and has higher toxic properties than the long-known Aβ1-42. β-Amyloid (1-43)(human) shows a correlation with both sAPPα and sAPPβ. β-Amyloid (1-43)(human) could be considered an added Alzheimer's disease (AD) biomarker together with the others already in use.
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| HY-181907 | NBE5 |
NBE5 is an orally active hydrophobic tag-targeting (Hyt) degrader (HyTTD) that targets Keap1. NBE5 mimics protein misfolding and recruits the molecular chaperone Hsp90, while achieving targeted degradation of Keap1 through both the ubiquitin-proteasome system and the autophagy-lysosome system. Consequently, NBE5 relieves the inhibition of the transcription factor Nrf2 by Keap1, potently activates the Nrf2-mediated endogenous antioxidant pathway, and upregulates the expression of downstream antioxidant proteins such as HO-1 and GCLM. NBE5 effectively alleviates oxidative stress and inflammatory damage, and exhibits excellent in vivo activity in a mouse model of acute colitis induced by DSS (HY-116282C).
NBE5 consists of a hydrophobic tag (HY-W022007), a Keap1-Nrf2 ligand (HY-14909), and a linker (HY-W014831). |
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| HY-P1051 | β-Amyloid (12-28) |
β-Amyloid (12-28) (Amyloid β-Protein (12-28)) is a peptide fragment of β-amyloid protein (β1-42). β1-42, a 42 amino acid protein , is the major component of senile plaque cores. β-Amyloid (12-28) shows aggregation properties. β-Amyloid (12-28) has the potential for Alzheimer’s disease research.
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| HY-160791 | Claramine |
Claramine is a steroid polyamine with blood-brain barrier permeability. Claramine can regulate the properties of lipid membranes and protect cells from various biological toxins, including misfolded protein oligomers and biological protein-based toxins.
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| HY-17387S1 | (-)-Huperzine A-d4 hydrochloride |
(-)-Huperzine A-d4 hydrochloride is deuterated labeled (-)-Huperzine A (HY-17387). (-)-Huperzine A (Huperzine A) is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease.
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| HY-B1378S1 | Ethosuximide-d5 |
Ethosuximide-d5 is deuterium labeled Ethosuximide. Ethosuximide, a widely prescribed anti-epileptic agent, improves the phenotypes of multiple neurodegenerative disease models and blocks the low voltage activated T-type calcium channel.
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| HY-175481 | CB2R agonist 4 |
CB2R agonist 4 is a cannabinoid receptor 2 (CB2R) agonist with an EC50 value of 6.9 μM. CB2R agonist 4 can induce cell apoptosis, ROS production and protein misfolding. CB2R agonist 4 shows cytotoxicity to a panel of tumor cell lines. CB2R agonist 4 can be used for the research of cancer.
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| HY-W004287S | Methyl tridecanoate-d25 |
Methyl tridecanoate-d25 is the deuterium labeled Methyl tridecanoate. Methyl tridecanoate moderately inhibits β-amyloid aggregation. Methyl tridecanoate weakly inhibits acetylcholinesterase (AChE).
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| HY-P4040 | Ac-D-DGla-LI-Cha-C |
Ac-D-DGla-LI-Cha-C is a potent HCV protease inhibitor peptide. Ac-D-DGla-LI-Cha-C can be used for the research of cancer, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurodegenerative diseases, infectious diseases, lung diseases, heart and vascular diseases and metabolic diseases.
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Cancer
Infection
Neurological, Eye or Ear Disease
Inflammation or Immune System Disease
Metabolic or Endocrine Disease
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| HY-B1126S | Orphenadrine-d3 hydrochloride |
Orphenadrine-d3 (hydrochloride) is the deuterium labeled Orphenadrine hydrochloride. Orphenadrine hydrochloride is an orally active and non-competitive NMDA receptor antagonist (crosses the blood-brain barrier) with a Ki of 6.0 μM. Orphenadrine hydrochloride relieves stiffness, pain and discomfort due to muscle strains, sprains or other injuries. Orphenadrine hydrochloride is also used to relieve tremors associated with parkinson's disease. Orphenadrine citrate has good neuroprotective properties, can be used in studies of neurodegenerative diseases.
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| HY-180425 | Cloridarol |
Cloridarol is a human islet amyloid peptide (hIAPP) inhibitor that prevents its abnormal misfolding and aggregation. Cloridarol can increase cell viability, inhibit apoptosis, and protect islet β-cells from hIAPP-induced cell toxicity. Cloridarol can be used for the research of type 2 diabetes (T2D).
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| HY-P3846 | (Glu20)-Amyloid β-Protein (1-42) |
(Glu20)-Amyloid β-Protein (1-42) is a slower fibrillizing variant of amyloid β-protein (Aβ). The Glu20 mutation reduces the aggregation propensity of Aβ42 and prevents accumulation of the slowly fibrillizing peptide. Amyloid β-protein is the primary component of both vascular and parenchymal amyloid deposits in Alzheimer's disease.
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| HY-N12321 | 2',3'-Dihydroxy-4',6'-dimethoxychalcone |
2',3'-Dihydroxy-4',6'-dimethoxychalcone (compound 1) can inhibit Amyloid β-protein (Aβ42) fibrillization and aggregation. 2',3'-Dihydroxy-4',6'-dimethoxychalcone has oral activity and can be detected in the brain.
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| HY-N15558 | Thaigranatumin E |
Thaigranatumin E is a protolimonoid compound found in the seeds of the Thai mangrove (Xylocarpus granatum). Thaigranatumin E is promising for research of neurodegenerative diseases such as Parkinson's diseases.
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| HY-W050044R | L-Azetidine-2-carboxylic acid (Standard) |
L-Azetidine-2-carboxylic acid is a proline analog. L-Azetidine-2-carboxylic acid upregulates the lipid autophagy marker LC3-II via activation of the PERK pathway. L-Azetidine-2-carboxylic acid increases pro-apoptotic BAX protein. L-Azetidine-2-carboxylic acid induces ATF6 cleavage and upregulates phosphorylated eIF2α levels. L-Azetidine-2-carboxylic acid induces ER stress, inducing protein misfolding and aggregation. L-Azetidine-2-carboxylic acid shows teratogenic, pro-inflammatory and pro-apoptotic effects.
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Reference Standards
Endogenous Metabolite
PERK
Atg8/LC3
Autophagy
Bcl-2 Family
Apoptosis
Eukaryotic Initiation Factor (eIF)
ATF6
Cancer
Neurological, Eye or Ear Disease
Blood or Cardio-cerebrovascular Disease
Metabolic or Endocrine Disease
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| HY-117259S | Valiltramiprosate-d6 |
Valiltramiprosate-d6 (ALZ-801-d6) is deuterium labeled Valiltramiprosate. ALZ-801 is a potent and orally available small-molecule β-amyloid (Aβ) anti-oligomer and aggregation inhibitor, valine-conjugated proagent of Tramiprosate with substantially improved PK properties and gastrointestinal tolerability compared with the parent compound. ALZ-801 is an advanced and markedly improved candidate for the treatment of alzheimer’s disease.
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| HY-N0805AR | Alisol B (Standard) |
Alisol B (Standard) is the analytical standard of Alisol B (HY-N0805A). This product is intended for research and analytical applications. Alisol B is a triterpene with diverse biological activities. Alisol B binds human soluble epoxide hydrolase (sEH) with a Ki of 5.97 μM and reduces sEH activity. Alisol B inhibits RANKL-induced JNK phosphorylation, NFATc1 and c-Fos expression, osteoclast formation, mature osteoclast pit-forming and actin ring activity, and SERCA pump activity. Alisol B induces calcium mobilization, CaMKK-AMPK-mTOR pathway activation, autophagic flux, autophagosome formation, G1 phase cell cycle arrest, endoplasmic reticulum stress, unfolded protein responses, and cancer cell apoptosis. Alisol B can be used for the research of hypercalcemia, osteoporosis, rheumatoid arthritis, periodontitis, acute kidney injury, and breast cancer.
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| HY-W746544 | Nervonic acid-d18 |
Nervonic acid-d18 (Selacholeic acid-d18) is the deuterium labeled Nervonic acid (HY-N2526). Nervonic acid is a monounsaturated fatty acid with oral activity. Nervonic acid exerts anti-inflammatory activity by inhibiting NF-κB signaling. Nervonic acid can be used in the study of neurodegenerative diseases.
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| HY-164539 | TMU 35435 |
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| HY-106443AR | Arimoclomol maleate (Standard) |
Arimoclomol maleate (Standard) is the analytical standard of Arimoclomol maleate (HY-106443A). This product is intended for research and analytical applications. Arimoclomol maleate (BRX-220) is an orally active co-inducer of heat shock proteins (HSP). Arimoclomol protects motor neurons by enhancing Hsp expression, thus directly affecting protein aggregation and clearance of misfolded assemblies via the proteasome-ubiquitin system.Arimoclomol maleate can be used for the study of Niemann–Pick disease type C.
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| HY-NP144 | Nerve Growth Factor 7S,murine submaxillary gland |
Nerve Growth Factor 7S,murine submaxillary gland is a high-molecular-weight α2β2γ2 neurotrophic factor complex isolated from murine submaxillary glands. Nerve Growth Factor 7S,murine submaxillary gland prevents the binding of active β-NGF dimers to neuronal receptors by sequestering the receptor-interacting region of β-NGF within the complex. Nerve Growth Factor 7S,murine submaxillary gland lacks neurotrophic activity due to the sequestration of β-NGF dimers and the occlusion of receptor-binding sites. Nerve Growth Factor 7S,murine submaxillary gland can be used in research related to neurodegenerative diseases.
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| HY-W002438R | 6-Hydroxyindole (Standard) |
6-Hydroxyindole (Standard) is the analytical standard of 6-Hydroxyindole (HY-W002438). This product is intended for research and analytical applications. 6-Hydroxyindole is an orally active, endogenous long-acting OATP1B1 inhibitor. 6-Hydroxyindole does not alter the cell surface expression or subcellular localization of OATP1B1. 6-Hydroxyindole protects cells against Ferroptosis. 6-Hydroxyindole possesses intrinsic radical-trapping antioxidant activity. 6-Hydroxyindole serves as a component of oxidative hair dyes. 6-Hydroxyindole can be used in research related to renal failure and neurodegenerative diseases.
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| HY-N9379 | Fissistigine A |
Fissistigine A is an alkaloid separated of the basic fractions from Formosan Fissistigma glaucescens, F. oldhamii and Goniothalamus amuyon. Fissistigine A has a weak inhibitory effect on amyloid beta 42 aggregation (IC50 50 µM).
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| HY-N7046S | Silybin B-d3 |
Silybin B-d3 (Silibinin B-d3) is a deuterated Silybin B (HY-N7046). Silybin B (Silibinin B) is an orally active amyloid-β aggregation inhibitor and ATR pathway activator, that can cross the blood-brain barrier. Silybin B inhibits Aβ fibril formation and promotes amorphous aggregate formation, while activating the ATR-mediated DNA damage repair pathway and inhibiting JNK/p38 MAPK signaling. Silybin B can reduce Cisplatin (HY-17394)-induced neuronal DNA damage and apoptosis. Silybin B has anti-oxidative stress, cell cycle regulation and neuroprotective activities. Silybin B is mainly used in the study of Alzheimer's disease and Cisplatin chemotherapy-related neurotoxicity.
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| HY-P10494 | FEFEFKFK |
FEFEFKFK is an octapeptide that self-assembles into fibrillar structures. FEFEFKFK is able to form gels at concentrations greater than about 7 mg/mL. The self-assembly and gelation properties of FEFEFKFK help to understand the mechanism of amyloid fibril formation in protein misfolding diseases such as Alzheimer's disease and Parkinson's disease.
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| HY-P4886 | Amyloid β-Protein (3-42) |
Amyloid β-Protein (3-42) is the precursor of Pyr peptide. Pyroglutamate-modified Aβ (pEAβ) (3-42) is the core of the amyloid template block in Alzheimer's disease. pEAβ(3-42) accelerated the aggregation of Aβ(1-42), while Aβ(1-42) significantly slowed the primary and secondary nucleation of pEAβ(3-42).
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| HY-121845 | 4-Br-Bnlm |
4-Br-Bnlm is a selective inhibitor of glucose-regulated protein 94 (Grp94) with an EC50 value of 0.96 µM. 4-Br-Bnlm reduces the levels of mutant myocilin proteins as well as wild-type myocilin misfold in cells. 4-Br-Bnlm promotes the clearance of toxic formsof myocilin and reduces myocilin toxicity.
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| HY-D0404 | Direct red 254 |
Direct Red 254 is a bisazo dye for textile applications. Direct Red 254 can be used for amyloid tissue staining in basic research on neurodegenerative diseases (e.g., Alzheimer's disease).
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| HY-P1388F | FITC-Ahx-β-Amyloid (1-42), (rat/mouse) tris |
FITC-Ahx-β-Amyloid (1-42), (rat/mouse) (tris) (FITC-Ahx-Amyloid β-peptide (1-42) (rat/mouse) (tris)) is a fluorescently labeled (FITC) form of β-Amyloid (1-42), (rat/mouse) (HY-P1388), which can be used in Alzheimer's disease-related research, such as aggregation, fiber formation, cellular uptake or imaging experiments. This product is provided in the form of Tris salt.
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| HY-111447 | VAS 3947 |
VAS 3947, a specific NADPH oxidase (NOX) inhibitor, exerts a potent antiplatelet effect. VAS3947 induces apoptosis independently of anti-NOX activity, via UPR activation, mainly due to aggregation and misfolding of proteins.
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| HY-P4704 | α-Synuclein (61-95) (human) |
α-Synuclein (61-95) (human) is the hydrophobic core region of α-synuclein, and induces neuronal cell death. α-Synuclein (61-95) (human) can be used for research of neurodegenerative diseases, including Alzheimer’s disease (AD) and Parkinson’s disease (PD).
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| HY-W020033R | Lanosterol (Standard) |
Lanosterol (Standard) is the analytical standard of Lanosterol. This product is intended for research and analytical applications. Lanosterol is an intermediate of cholesterol synthesis and use of lanosterol induces ubiquitination and degradation of a rate-controlling enzyme of cholesterol synthesis, i.e., HMG CoA reductase. Lanosterol suppresses the aggregation and cytotoxicity of misfolded proteins linked with neurodegenerative diseases[1][2].
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| HY-W004287 | Methyl tridecanoate |
Methyl tridecanoate is a fatty acid methyl ester. Methyl tridecanoate exhibits an IC50 of 3.26 μM and a Ki of 2.30 μM against AsOBP21f in Anopheles sinensis. Methyl tridecanoate induces electroantennographic responses in female Anopheles sinensis. Methyl tridecanoate shows a dose-dependent attractive effect on Anopheles sinensis. Methyl tridecanoate weakly inhibits β-amyloid aggregation and AChE activity. Methyl tridecanoate can be used in the research of malaria and Alzheimer's disease.
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| HY-B1378S | Ethosuximide-d3 |
Ethosuximide-d3 is the deuterium labeled Ethosuximide. Ethosuximide, a widely prescribed anti-epileptic agent, improves the phenotypes of multiple neurodegenerative disease models and blocks the low voltage activated T-type calcium channel.
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| HY-W020033S | Lanosterol-d6 |
Lanosterol-d6 is deuterium labeled Lanosterol. Lanosterol is an intermediate of cholesterol synthesis and use of lanosterol induces ubiquitination and degradation of a rate-controlling enzyme of cholesterol synthesis, i.e., HMG CoA reductase. Lanosterol s
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| HY-P992142 | Vonaprument |
Vonaprument (ANX-007) is an intravitreally injected C1q antibody fragment (with a molecular weight of approximately 48 kDa) and a human monoclonal antibody. Vonaprument inhibits the activation of the classical complement cascade by specifically recognizing the globular head of C1q and blocking substrate binding. After intravitreal injection, Vonaprument distributes to the retina, choroid and optic nerve, and achieves complete C1q target binding in the aqueous humor and retinal tissues. Vonaprument can be used in research related to neurodegenerative eye diseases such as age-related macular degeneration and glaucoma.
Species: Human |
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| HY-161743A | PBA-1105 TFA |
PBA-1105 TFA is an autophagy-targeting chimera (AUTOTAC) that induces p62 self-oligomerization. PBA-1105 TFA selectively binds to exposed hydrophobic regions of misfolded proteins, facilitating their degradation via the autophagic pathway. PBA-1105 TFA increases the autophagic flux of Ub-conjugated aggregates.
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| HY-P1378A | β-Amyloid (1-43)(human) TFA |
β-Amyloid (1-43)(human) TFA is more prone to aggregation and has higher toxic properties than the long-known Aβ1-42. β-Amyloid (1-43)(human) TFA shows a correlation with both sAPPα and sAPPβ. β-Amyloid (1-43)(human) TFA could be considered an added Alzheimer's disease (AD) biomarker together with the others already in use.
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| HY-132593 | Rovanersen |
Rovanersen (WVE-120101) is an antisense oligonucleotide that specifically targets mutated mRNA copies of the huntington (HTT) gene without affecting healthy mRNA of HTT gene, thereby preventing the production of faulty Huntingtin protein. Rovanersen can be used for huntington’s disease research.
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| HY-132593A | Rovanersen sodium |
Rovanersen sodium is an antisense oligonucleotide that specifically targets mutated mRNA copies of the huntington (HTT) gene without affecting healthy mRNA of HTT gene, thereby preventing the production of faulty Huntingtin protein. Rovanersen sodium can be used for huntington’s disease research.
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| HY-W015787 | 2-Hydroxyphenylethanol |
2-Hydroxyphenylethanol is a molecular chaperone that rescues misfolded P123S mutant pendrin, promoting translocation from the cytoplasm to the plasma membrane. 2-Hydroxyphenylethanol can be used for the research of pendred syndrome.
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| HY-P5968A | [Ala28]-β Amyloid(25-35) TFA |
[Ala28]-β Amyloid(25-35) (β(25-35)KA) TFA is an electrically neutral mutant peptide of Aβ(25-35) that accelerates the aggregation of Firefly Luciferase.
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| HY-117856 | IND24 |
IND24 is a potent antiprion agent with an EC50 value of 1.27 µM. IND24 decreases abnormal, misfolded, pathogenic forms of benign normally occurring prion protein on the cell surface or inside the cell.
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| HY-N11286 | Tridocosahexaenoylglycerol |
Tridocosahexaenoylglycerol (TG-DHA) is an orally active dietary supplement that improves autoimmune encephalomyelitis in mice. Tridocosahexaenoylglycerol shows beneficial effects on neurodegenerative diseases and also improves macular function in diabetic retinopathy. Tridocosahexaenoylglycerol can be used for research on neurological diseases, inflammatory immune diseases, and metabolic diseases.
Source: Fish Oil |
Neurological, Eye or Ear Disease
Inflammation or Immune System Disease
Metabolic or Endocrine Disease
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| HY-P4886A | Amyloid β-Protein (3-42) TFA |
Amyloid β-Protein (3-42) TFA is a precursor of Pyr peptide. Pyroglutamic acid-modified Aβ (pEAβ) (3-42) is the core of the amyloid plaque in Alzheimer's disease. pEAβ (3-42) accelerates the aggregation of Aβ(1-42), while Aβ(1-42) significantly slows down the primary and secondary nucleation of pEAβ(3-42).
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| HY-18956 | (E/Z)-Icerguastat |
(E/Z)-Icerguastat ((E/Z)-Sephin1) is a selective inhibitor of the phosphatase regulatory subunit PPP1R15A (R15A). (E/Z)-Icerguastat can be used for protein misfolding diseases research.
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| HY-N13742 | Dihydrohonokiol B |
Dihydrohonokiol B (Dihydrohonokiol) is an anxiolytic agent. Dihydrohonokiol B can reduce the neurotoxicity induced by amyloid β protein by stimulating the GABAC receptor. Dihydrohonokiol B can be used in the research of neurodegenerative diseases such as Alzheimer's disease.
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| HY-160791B | Claramine hydrochloride |
Claramine hydrochloride is a steroid polyamine with blood-brain barrier permeability. Claramine hydrochloride can regulate the properties of lipid membranes and protect cells from various biological toxins, including misfolded protein oligomers and biological protein-based toxins.
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| HY-P10530 | Nrf2 (69-84) |
Nrf2 (69-84) is a peptide fragment of Nrf2 protein that contains the key ETGE motif, which is an important region for binding to the Kelch domain of Keap1 protein. Nrf2 (69-84) can be used to study the role of Nrf2 in the development and progression of diseases, especially in cancer, neurodegenerative diseases and inflammatory diseases.
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| HY-111772A | (R)-Elexacaftor |
(R)-Elexacaftor ((R)-VX-445) is the enantiomer of Elexacaftor (HY-111772). Elexacaftor is an orally active CFTR modulator that targets nucleotide-binding domain 1. Elexacaftor stabilizes misfolded F508del-CFTR protein, enhances its trafficking to the plasma membrane, and significantly improves metabolic stability, thermal stability and ion conductivity. Elexacaftor not only restores chloride transport function in nasal epithelial cells and rescues multiple CFTR mutation subtypes, but also exerts multiplicative synergistic effects with Ivacaftor (HY-13017), and is often used in a triple combination therapy with Tezacaftor (HY-15448). Elexacaftor is widely used in basic and clinical translational research on cystic fibrosis.
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| HY-N1100 | Vasicinone |
Vasicinone is a quinazoline alkaloid isolated from the Adhatoda vasica. Vasicinone is a potential agent for Parkinson's disease and possibly other oxidative stress-related neurodegenerative disorders.
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| HY-160426 | Gcase activator 3 |
Gcase activator 3 is a β-glucocerebrosidase (GCase) activator with an EC50 of 1.49 μM. By binding to the allosteric site of GCase, Gcase activator 3 partially stabilizes GCase and enhances its activity. Gcase activator 3 can be conjugated with fluorophores to form fluorescent probes, which are used for high-throughput screening of GCase. Gcase activator 3 is applicable to research related to Gaucher's disease, Parkinson's disease, dementia with Lewy bodies, and multiple system atrophy.
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| HY-125287 | (Rac)-Minzasolmin |
(Rac)-Minzasolmin ((Rac)-UCB0599; NPT200-11) is a blood-brain barrier penetrated alpha-synuclein (ASYN) misfolding inhibitor. (Rac)-Minzasolmin acts on the early stage of ASYN aggregation process, by replacing the membrane-bound oligomers ASYN, allowing them to revert to the monomeric form, while preventing pathological aggregation. (Rac)-Minzasolmin effectively improves the ASYN deposition in the retina and the neuro-pathological indicators in two α-synuclein transgenic mouse models. (Rac)-Minzasolmin can be used for the studies of Parkinson's disease (PD) and dementia with Lewy bodies (DLB).
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| HY-132579 | Tominersen |
Tominersen (RG6042) is a second-generation 2′-O-(2-methoxyethyl) antisense oligonucleotide that targets huntingtin protein (HTT) mRNA and potently suppresses HTT production. Tominersen improves survival and reduces brain atrophy in mice. Tominersen can be used for the research of Huntington’s disease (HD).
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| HY-160791A | Claramine TFA |
Claramine TFA is a steroidal polyamine. Claramine TFA can regulate the properties of lipid membranes and protect cells from various biological toxins, including misfolded protein oligomers and toxins derived from biological proteins.
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| HY-W007551 | 1-Aminoindan |
1-Aminoindan (1-Indanamine; 2,3-Dihydro-1H-inden-1-amine) is an α-synuclein (α-synuclein) binder. By binding to α-synuclein, 1-Aminoindan promotes the formation of its neuroprotective "cyclic" conformation, thereby reducing the misfolding and aggregation of α-synuclein. 1-Aminoindan is a metabolite of Rasagiline (HY-14605A). 1-Aminoindan can be used in research related to Parkinson's disease.
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| HY-W002438 | 6-Hydroxyindole |
6-Hydroxyindole is an orally active, endogenous long-acting OATP1B1 inhibitor. 6-Hydroxyindole does not alter the cell surface expression or subcellular localization of OATP1B1. 6-Hydroxyindole protects cells against Ferroptosis. 6-Hydroxyindole possesses intrinsic radical-trapping antioxidant activity. 6-Hydroxyindole serves as a component of oxidative hair dyes. 6-Hydroxyindole can be used in research related to renal failure and neurodegenerative diseases.
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| HY-P991734 | VHB937 |
VHB937 is a potent and selective TREM2 agonist, a human monoclonal antibody, with sub-nanomolar affinity. VHB937 enhances TREM2 surface expression and downstream signaling, such as Syk phosphorylation and calcium mobilization. VHB937 exhibits robust neuroprotective effects in vivo, significantly reducing pathology and pro-inflammatory markers across a broad range of animal models of neuroinflammation and neurodegeneration. VHB937 can be used for neurodegenerative diseases research.
Species: Human |
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| HY-156103 | mHTT-IN-2 |
mHTT-IN-2 (compound 27) is a potent inhibitor (EC50=0.066 μM) of mutant huntingtin (mHTT). mHTT-IN-2 reduces canonical splicing of HTT RNA exons [49-50] and is a splicing regulator of the huntingtin (HTT) gene. mHTT-IN-2 exhibits inhibitory activity in vitro and in vivo in human HD stem cells and mouse BACHD models. mHTT-IN-2 may be used in the study of branaplam-related peripheral neuropathy.
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| HY-DY1073 | MitoPerOx (solution) |
MitoPerOx (solution) is a mitochondrial-targeted, lipid peroxidation-indicating fluorescent probe with BODIPY581/591 fluorophores. The triphenylphosphine cation (TPP+) of MitoPerOx can be selectively enriched in mitochondria (depending on membrane potential) and can be used to detect lipid peroxidation in the inner mitochondrial membrane. Under the action of lipid peroxides, the BODIPY581/591 fluorophores of MitoPerOx shift their emission wavelength from 590 nm (reduced state) to 520 nm (oxidized state) , and ratiometric detection can be performed at an excitation wavelength of 488 nm. MitoPerOx can specifically monitor the peroxidation of mitochondrial phospholipids (especially cardiolipin) and is used in the study of oxidative stress-related diseases (such as aging, neurodegenerative diseases, and mitochondrial dysfunction) .
Solvent and concentration: DMSO: 2 mM |
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| HY-161743 | PBA-1105 |
PBA-1105 is an autophagy-targeting chimera (AUTOTAC) that induces p62 self-oligomerization. PBA-1105 selectively binds to exposed hydrophobic regions of misfolded proteins, facilitating their degradation via the autophagic pathway. PBA-1105 increases the autophagic flux of Ub-conjugated aggregates.
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| HY-125616 | Biotinoyl tripeptide-1 |
Biotinoyl tripeptide-1 (Biotinyl-GHK) is a biotinylating reagent linked to a GHK (glycyl-L-histidyl-L-lysine) tripeptide. Biotin tripeptide-1 is a bioactive peptide with hair care (improves the appearance and feel of hair) and hair growth effects. Biotinoyl tripeptide-1 has a certain affinity for streptavidin. Biotinoyl tripeptide-1 inhibits the production of ROS and has antioxidant effects. Biotinoyl tripeptide-1 reduces the production of carbonylated amyloid-β (Aβ) and inhibits Aβ aggregation. Biotinoyl tripeptide-1 can be used in the study of neurodegenerative diseases.
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| HY-P99213 | Ozanezumab |
Ozanezumab (GSK1223249) is a humanized, Fc-inactivated monoclonal antibody that targets the nervous system protein Nogo-A. Ozanezumab promotes neurite outgrowth and axonal regeneration by neutralizing Nogo-A signaling. Ozanezumab is used for research on neurodegenerative diseases such as amyotrophic lateral sclerosis and multiple sclerosis[1].
Species: Human |
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| HY-N7046 | Silybin B |
Silybin B (Silibinin B) is an orally active amyloid-β aggregation inhibitor and ATR pathway activator that can cross the blood-brain barrier. Silybin B inhibits Aβ fibril formation and promotes amorphous aggregate formation, while activating the ATR-mediated DNA damage repair pathway and inhibiting JNK/p38 MAPK signaling. Silybin B can reduce Cisplatin (HY-17394)-induced neuronal DNA damage and apoptosis. Silybin B has anti-oxidative stress, cell cycle regulation and neuroprotective activities. Silybin B is mainly used in the study of Alzheimer's disease and Cisplatin chemotherapy-related neurotoxicity.
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| HY-NP009 | α-Lactalbumin |
α-Lactalbumin is a globular whey protein that exists in milk. α-Lactalbumin binds Ca2+, Mg2+, Mn2+, Na+, K+ and Zn2+ ions; among these, Ca2+ binding enhances protein stability, while Zn2+ binding reduces stability and induces aggregation. α-Lactalbumin forms amyloid fibrils, amorphous aggregates, nanoparticles and nanotubes depending on external conditions. α-Lactalbumin exhibits bactericidal and antiviral activities. α-Lactalbumin has anxiolytic and antidepressant activities, and its effects are enhanced under stress conditions.
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| HY-132579A | Tominersen sodium |
Tominersen sodium is a second-generation 2′-O-(2-methoxyethyl) antisense oligonucleotide that targets huntingtin protein (HTT) mRNA and potently suppresses HTT production. Tominersen improves survival and reduces brain atrophy in mice. Tominersen sodium can be used for the research of Huntington’s disease (HD).
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| HY-P4704A | α-Synuclein (61-95) (human) TFA |
α-Synuclein (61-95) (human) TFA is the hydrophobic core region of α-synuclein, and induces neuronal cell death. α-Synuclein (61-95) (human) TFA can be used for research of neurodegenerative diseases, including Alzheimer’s disease (AD) and Parkinson’s disease (PD).
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| HY-113524S | N-Acetyl-L-aspartic acid-d3 |
N-Acetyl-L-aspartic acid-d3 is the deuterium labeled N-Acetyl-L-aspartic acid (HY-113524). N-Acetyl-L-aspartic acid is a derivative of Aspartic acid (HY-N0666) and endogenous compound. N-Acetyl-L-aspartic acid acts as an acetyl donor. N-Acetyl-L-aspartic acid is involved in brain metabolism. N-Acetyl-L-aspartic acid is used in the research of neurodegenerative diseases (such as Canavan disease).
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| HY-107130 | Alirinetide |
Alirinetide (GM604) is an oligopeptide containing 6 amino acids. Alirinetide can cross the blood-brain barrier and can be used for the research of multiple neurodegenerative diseases.
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| HY-W010041 | Scyllo-Inositol |
Scyllo-Inositol is an inhibitor that targets the aggregation of misfolded proteins (such as α-synuclein and Amyloid-β), is orally effective, and can cross the blood-brain barrier. Scyllo-Inositol can selectively bind to and stabilize non-toxic oligomers, preventing them from converting into toxic fibers, exerting protein homeostasis regulation and neuroprotective activity. Scyllo-Inositol binds to the hydrophobic region of pathogenic proteins, inhibits protein aggregation, and promotes lysosome- and proteasome-mediated degradation pathways, thereby reducing neurotoxicity. Scyllo-Inositol can be used in the study of neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, and Huntington's disease.
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| HY-P2358 | PSMα3 |
PSMα3 is an inhibitor of NF-κB p65 and p38 MAPK. PSMα3 forms membrane pores and binds to residues of human insulin B chain to inhibit insulin aggregation. PSMα3 forms α-type amyloid-like fibrils to exert cytotoxic effects, and acts as a functional amyloid virulence determinant of Staphylococcus aureus. PSMα3 is applicable to research related to spondyloarthritis, rheumatoid arthritis, insulin-derived amyloidosis, and Staphylococcus aureus infection.
Source: S. aureus |
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| HY-145580 | Minzasolmin |
Minzasolmin (UCB0599; (R)-NPT200-11) is an orally active, blood-brain-permeable α-synuclein (α-Syn) inhibitor that selectively binds to α-Syn misfolded intermediates (such as oligomers) and inhibits aggregation and fibril formation by regulating their conformational stability. Minzasolmin can reduce the generation of pathological oligomers and block neurotoxic signaling, thereby reducing the abnormal accumulation of α-Syn in the brain. Minzasolmin significantly improved motor deficits, reduced neuroinflammatory markers, and α-Syn-related pathological deposition in transgenic mouse models.
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| HY-W015236 | H-Gly-Gly-Gly-OH |
H-Gly-Gly-Gly-OH, also known as Triglycine, is a tripeptide composed of glycine, glycine and glycine, which are linked by peptide bonds. Often used as a model compound in the study of protein structure and function. Glycylglycylglycine also acts as a neurotransmitter in the central nervous system and has been shown to have antioxidant properties. Furthermore, it may have potential research roles in various diseases such as cancer, diabetes and neurodegenerative diseases.
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| HY-156650 | Votoplam |
Votoplam (PTC518) is a blood-brain barrier-permeable HTT pre-mRNA inhibitor with an IC50 ≤ 0.1 μM. Votoplam modulates the splicing process of HTT pre-mRNA to include a pseudo-exon carrying a premature translation termination codon, thereby triggering HTT mRNA degradation. Votoplam is applicable to research related to Huntington's disease.
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| HY-157839 | PROTAC α-Synuclein/Tau degrader 1 |
PROTAC α-Synuclein/Tau degrader 1 is a blood-brain barrier-penetrant dual PROTAC degrader of α-synuclein (α-Syn) and tau, with DC50 of 1.57 μM and 4.09 μM, respectively. PROTAC α-Synuclein/Tau degrader 1 binds to α-Syn and tau PFF, with KDs of 0.47 and 2.78 μM, respectively. PROTAC α-Synuclein/Tau degrader 1 exhibits degradation effect mediated by the ubiquitin-proteasome system (UPS). PROTAC α-Synuclein/Tau degrader 6 can be used for the study of Parkinson’s disease (PD) (Pink: α-Synuclein/Tau ligand (HY-151035); Blue: CRBN ligase ligand (HY-14658); Black: Linker (HY-128803)).
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| HY-NP0204 | MSA Protein |
MSA Protein (Mouse Serum Albumin) is most abundant protein in plasma, which leaks into the brain parenchyma when the blood-brain barrier (BBB) is impaired. Mouse Serum Albumin induces astrocytes to A1 phenotype to remarkably increase levels of Elovl1. Mouse Serum Albumin promotes VLSFAs secretion and causes neuronal lippoapoptosis through endoplasmic reticulum stress response pathway. MSA-activated microglia triggeres remarkable tau phosphorylation at multiple sites (Ser202/Thr205) through NLRP3 inflammasome pathway. Mouse Serum Albumin decreases the spatial learning and memory abilities in mice. Mouse Serum Albumin can be used for the study of neurodegenerative diseases like Alzheimer’s disease (AD) and frontotemporal dementia (FTD).
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| HY-P99405 | Prasinezumab |
Prasinezumab (PRX 002) is a humanized IgG1 monoclonal antibody directed against aggregated α-synuclein. Prasinezumab has the potential for Parkinson's disease research.
Species: Human |
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| HY-P99471 | Bepranemab |
Bepranemab is a humanized IgG4 monoclonal antibody that binds to the central region of tau protein. Bepranemab inhibits the seeding, aggregation of pathological tau protein and the spread of tau pathology to distal brain regions. Bepranemab is applicable to research related to Alzheimer's disease.
Species: Human |
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| HY-138669 | C004019 |
C004019 is a BBB-penetrable and small-molecule PROTAC that targets tau. C004019 can simultaneously recruit tau and E3 ligase, and effectively clear tau proteins by promoting the ubiquitination and proteasome-dependent degradation of tau, thereby improving synaptic and cognitive functions in Alzheimer's disease (AD) mice. C004019 can be used in the research of AD and tau protein-related diseases.
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| HY-P991049 | Atrosimab |
Atrosimab is an Fv-Fc1K fusion protein with an EC50 value of 0.37 nM against humans. Atrosimab inhibits TNF-induced TNFR1 activation, release of IL-6 and IL-8, and cell death, and alleviates neuroinflammation. Atrosimab is applicable to research related to inflammatory diseases, neurodegenerative diseases, acute and chronic inflammation, experimental arthritis, non-alcoholic steatohepatitis, and experimental autoimmune encephalomyelitis.
Species: Human |
Experimental Autoimmune Encephalomyelitis
Experimental Autoimmune Encephalomyelitis
Fatty Liver Disease
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| HY-134850 | QC-01–175 |
QC-01-175 is a Tau PROTAC degrader, with Kd values of 1.2 μM, 1.7 μM and 2.5 μM for wild-type, A152T mutant and P301L mutant tau-441 proteins, respectively. QC-01-175 binds to both Tau and CRBN, triggering ubiquitination and proteasomal degradation of Tau. QC-01-175 preferentially targets disease-associated Tau proteins in frontotemporal dementia. QC-01-175 inhibits MAO activity, with an IC50 of 8.56 μM. QC-01-175 suppresses the elevation of ROS levels. QC-01-175 can be used in studies related to frontotemporal dementia and amyotrophic lateral sclerosis.
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| HY-P9999 | Trontinemab |
Trontinemab (RG6102) is a brain-penetrant, anti-amyloid, bispecific and humanizedized IgG1-κ antibody, targeting to Aβ plaques and transferrin receptor 1 (TFR1). Trontinemab binds to fibrillar Aβ as well as Aβ plaques triggering plaque clearance by engaging immune cells on Alzheimer disease (AD) brain sections. Trontinemab also shows specific affinity to cynomolgus and human TFR1.
Species: Human |
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