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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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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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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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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. -
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. -
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! -
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. -
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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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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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. -
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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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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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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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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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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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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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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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. -
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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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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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. -
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. -
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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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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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. -
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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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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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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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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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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dBRD9 is a PROTAC (proteolysis targeting chimera) and can be used as a selective valuable probe for degrading BRD9.
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Natural Products
| Cat. No. | Product Name | Information | Application | Publication |
|---|---|---|---|---|
| HY-12041 | SP600125 |
SP600125 is an orally active, reversible, and ATP-competitive JNK inhibitor with IC50s of 40, 40 and 90 nM for JNK1, JNK2 and JNK3, respectively. SP600125 is a potent ferroptosis inhibitor. SP600125 induces the transformation of bladder cancer cells from autophagy to apoptosis.
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Cancer
Digestive System Disease
Depression
Pain
Digestive System Inflammation
Parkinson's Disease
Obesity
Lung Fibrosis
|
627
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| HY-A0098 | Tunicamycin |
Tunicamycin is a mixture of homologous nucleoside antibiotic that inhibits N-linked glycosylation and blocks GlcNAc phosphotransferase (GPT). Tunicamycin causes accumulation of unfolded proteins in cell endoplasmic reticulum (ER) and induces ER stress, and causes blocking of DNA synthesis and cell cycle arrest in G1 phase. Tunicamycin inhibits gram-positive bacteria, yeasts, fungi, and viruses and has anti-cancer activity.Tunicamycin increases exosome release in cervical cancer cells.
Source: Streptomyces lysosuperficus |
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180
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| HY-18982 | Anisomycin |
Anisomycin is a potent protein synthesis inhibitor which interferes with protein and DNA synthesis by inhibiting peptidyl transferase or the 80S ribosome system. Anisomycin is a JNK activator, which increases phospho-JNK. Anisomycin is a bacterial antibiotic.
Source: Streptomyces griseolus |
Cancer
Digestive System Disease
Bacterial Infection
Parasitic Infection
Pain
Digestive System Inflammation
|
162
|
| HY-13433 | Thapsigargin |
|
158
|
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| HY-B0075 | Melatonin |
Melatonin is a hormone made by the pineal gland that can activate melatonin receptor and inhibit PANoptosis. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties. Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation. Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress.
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Melatonin Receptor
Autophagy
Mitophagy
Endogenous Metabolite
Apoptosis
PANoptosis
Ligands for Target Protein for PROTAC
Histone Acetyltransferase
Lung Cancer
Breast Cancer
Prostate Cancer
Liver Cancer
Viral Infection
Neurodegenerative Disease
Digestive System Inflammation
SARS-CoV-2 Infection
|
149
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| HY-18072 | GSK2606414 |
GSK2606414 is a cell-permeable and orally available protein kinase R-like endoplasmic reticulum (ER) kinase (PERK) inhibitor with an IC50 of 0.4 nM.
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135
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| HY-N0830B | Palmitic acid sodium |
Palmitic acid sodium is a long-chain saturated fatty acid commonly found in both animals and plants. Palmitic acid sodium can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells. Palmitic acid sodium is used to establish a cell steatosis model .
Source: Widespread |
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122
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| HY-N0830 | Palmitic acid |
Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. PA can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells. Palmitic acid is used to establish a cell steatosis model.
Source: Widespread |
Cancer
Neurological, Eye or Ear Disease
Blood or Cardio-cerebrovascular Disease
Metabolic or Endocrine Disease
|
122
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| HY-19696A | Tauroursodeoxycholate sodium |
Colorectal Cancer
Prostate Cancer
Liver Cancer
Viral Infection
Neurodegenerative Disease
Pain
Digestive System Inflammation
Obesity
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111
|
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| HY-19696 | Tauroursodeoxycholate |
Colorectal Cancer
Prostate Cancer
Liver Cancer
Viral Infection
Neurodegenerative Disease
Pain
Digestive System Inflammation
Glucose Metabolism
Obesity
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111
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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-19707 | 4μ8C |
4μ8C (IRE1 Inhibitor III) is a small-molecule inhibitor of IRE1α.
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74
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| HY-13820 | GSK2656157 |
GSK2656157 is a selective and ATP-competitive inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) with an IC50 of 0.9 nM.
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67
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| HY-13319 | JNK-IN-8 |
JNK-IN-8 (JNK Inhibitor XVI) is a potent JNK inhibitor with IC50s of 4.7 nM, 18.7 nM, and 1 nM for JNK1, JNK2, and JNK3, respectively.
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59
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| HY-12861 | CB-5083 |
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54
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| HY-15845 | STF-083010 |
STF-083010 is a specific IRE1α inhibitor. STF-083010 inhibits Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress.
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53
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| HY-N0431 | Astragaloside IV |
Lung Cancer
Breast Cancer
Colorectal Cancer
Prostate Cancer
Liver Cancer
Pancreatic Cancer
Depression
Pain
Parkinson's Disease
Obesity
Lung Fibrosis
Rheumatoid Arthritis
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43
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| HY-13814 | PR-619 |
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40
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| HY-108434 | Ceapin-A7 |
Ceapin-A7 is a selective blocker of ATF6α signaling in response to ER stress, with an IC50 of 0.59 μM. Ceapin-A7 can be used to explore both the mechanism of activation of ATF6α and its role in pathological settings.
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28
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| HY-15417 | ML-7 hydrochloride |
ML-7 hydrochloride is a selective and highly specific myosin light chain kinase (MLCK) inhibitor that acts as a trabecular meshwork (TM) relaxant. ML-7 hydrochloride enhances Quinocetone (HY-123581)-induced phosphorylation of ERK, p38 MAPK and JNK, attenuates Akt activation, and promotes apoptosis of hepatocellular carcinoma cells. ML-7 hydrochloride reduces Th2 cytokine secretion by inhibiting MLCK, while alleviating smooth muscle hyperplasia and collagen deposition. As a non-antibiotic adjuvant, ML-7 hydrochloride restores the sensitivity of drug-resistant bacteria to Tigecycline (HY-B0117). ML-7 hydrochloride can be used in research related to glaucoma, hepatocellular carcinoma, asthma, and Klebsiella pneumoniae infection.
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25
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| HY-15713 | NMS-873 |
NMS-873 is a potent, selective allosteric VCP/p97 inhibitor with an IC50 value of 30 nM.
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19
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| HY-B0239 | Chloramphenicol |
Chloramphenicol is an orally active, potent and broad-spectrum antibiotic. Chloramphenicol shows antibacterial activity. Chloramphenicol represses the oxygen-labile transcription factor and hypoxia inducible factor-1 alpha (HIF-1α) in hypoxic A549 and H1299 cells. Chloramphenicol suppresses the mRNA levels of vascular endothelial growth factor (VEGF) and glucose transporter 1, eventually decreasing VEGF release. Chloramphenicol can be used for anaerobic infections and lung cancer research.
Source: Streptomyces venezuelae |
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19
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| HY-B1272 | Desipramine hydrochloride |
Desipramine hydrochloride is a first-generation tricyclic antidepressant. Desipramine hydrochloride selectively binds to norepinephrine transporter and blocks neuronal norepinephrine reuptake. Desipramine hydrochloride activates MAPK signaling via ERK1/2, JNK, and p38, represses NF-κB and AP-1 activity, and induces apoptosis via ROS elevation, mitochondrial membrane potential reduction, and intracellular calcium increase. Desipramine hydrochloride also shows anyi-inflammatory activity, inhibiting TNF-α production. Desipramine hydrochloride can be used for the research of hepatocellular cancer, inflammation, and neurological diseases.
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Adrenergic Receptor
ERK
JNK
p38 MAPK
NF-κB
AP-1
Apoptosis
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
TNF Receptor
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18
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| HY-19332 | Kifunensine |
Kifunensine, a potent and selective inhibitor of class I α-mannosidases isolated from Actinomycete, prevents α-mannosidases I from trimming mannose residues on glycoproteins. Kifunensine inhibits ERAD.
Source: actinomycete |
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17
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| HY-N0120A | Polydatin |
Polydatin (Piceid), extracted from the roots of Reynoutria japonica, a widely used traditional Chinese remedies, possesses anti-inflammatory activity in several experimental models. Polydatin (Piceid) inhibits G6PD and induces oxidative and ER stresses.
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16
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| HY-110078 | Eeyarestatin I |
Eeyarestatin I, a potent endoplasmic reticulum-associated protein degradation (ERAD) inhibitor, is a potent protein translocation inhibitor. Eeyarestatin I inhibits Sec61 translocon. Eeyarestatin I targets the p97-associated deubiquitinating process (PAD) and inhibits atx3-dependent deubiquitination. Eeyarestatin I interferes at a step prior to proteasomal degradation. Eeyarestatin I induces cell death via the proapoptotic protein NOXA and has anticancer effects.
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16
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| HY-139214 | IXA4 |
IXA4 is a highly selective, non-toxic IRE1/XBP1s activator. IXA4 activates IRE1/XBP1s signaling without globally activating the unfolded protein response (UPR) or other stress-responsive signaling pathways (e.g., the heat shock response or oxidative stress response). IXA4 reduces secretion of APP through IRE1 activation.
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12
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| HY-12956 | Dinoprost |
Dinoprost (Prostaglandin F2α) is an orally active, potent prostaglandin F (PGF) receptor (FP receptor) agonist. Dinoprost is a luteolytic hormone produced locally in the endometrial luminal epithelium and corpus luteum (CL). Dinoprost plays a key role in the onset and progression of labour.
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10
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| HY-N7140 | Gamma-Linolenic acid |
Gamma-linolenic acid (γ-Linolenic acid) is an orally active unsaturated fatty acid. Gamma-linolenic acid exerts anti-inflammatory effects by inhibiting the NF-κB pathway and the phosphorylation of ERK1/2 and JNK. At the same time, it exerts anticancer effects by inducing apoptosis (Apoptosis) in cancer cells. Additionally, Gamma-linolenic acid also has antioxidant and memory-improving effects. It holds promise for research in the fields of inflammation, neurology, and cancer diseases.
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8
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| HY-125006 | TRi-1 |
TRi-1 is a potent, specific and irreversible inhibitor of cytosolic thioredoxin reductase 1 (TXNRD1), with an IC50 of 12 nM. TRi-1 has little mitochondrial toxicity for anticancer therapy.
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7
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| HY-N0878 | Bufotalin |
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4
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| HY-138364 | YUM70 |
YUM70 is a potent and selective inhibitor of glucose-regulated protein 78 (GRP78), with an IC50 of 1.5 μM for inhibiting GRP78 ATPase activity of the full-length protein. YUM70 induces endoplasmic reticulum (ER) stress-mediated apoptosis in pancreatic cancer. YUM70 also has in vivo efficacy in a pancreatic cancer xenograft model.
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4
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| HY-124293 | AA147 |
AA147 is a endoplasmic reticulum (ER) proteostasis regulator. AA147 promotes protection against oxidative damage in neuronal cells and prevents endothelial barrier dysfunction by activating ATF6 arm (selectively) of the unfolded protein response (UPR) and the NRF2 oxidative stress response. AA147 can rebalances XBP1s expression in vivo, and also induces survival motor neuron (SMN) expression and spinal motorneuron (MN) protection.
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4
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| HY-113402 | Gamma-glutamylcysteine |
Gamma-glutamylcysteine (γ-Glu-Cys) is an orally active, blood-brain barrier permeable dipeptide. Gamma-glutamylcysteine activates AMPK, SIRT1, IL-4/STAT6, AC/cAMP/PI3K, IGF-1R/IRS1/PI3K, and Nrf2 signaling pathways; it inhibits NF-κB, JAK1/STAT1/3, MAPKs, cadmium-induced p38 MAPK, JNK, and PI3K/Akt signaling pathways. Gamma-glutamylcysteine regulates macrophage polarization, modulates the trafficking of CD36 and GLUT4, induces glutathione synthesis, improves metabolic dysfunction, reduces lipid deposition, ameliorates glucose homeostasis, inhibits apoptosis (Apoptosis), stabilizes mitochondria, suppresses lipid peroxidation, iron accumulation and ferroptosis (Ferroptosis), reduces ds-HMGB1 levels, reverses mechanical hyperalgesia, and alleviates hepatic lipid droplet formation. Gamma-glutamylcysteine is applicable to research related to inflammatory bowel disease, type 2 diabetes, cadmium-induced neurotoxicity, Alzheimer's disease, cerebral ischemia/reperfusion injury, neuropathy, and alcoholic liver disease.
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Endogenous Metabolite
Interleukin Related
TNF Receptor
AMPK
Sirtuin
STAT
PI3K
NF-κB
JAK
p38 MAPK
JNK
Akt
Apoptosis
Ferroptosis
Blood or Cardio-cerebrovascular Disease
Digestive System Disease
Digestive System Inflammation
Alzheimer's Disease
Inflammatory Bowel Disease
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4
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| HY-N0139 | Troxerutin |
Troxerutin, also known as vitamin P4, is a tri-hydroxyethylated derivative of natural bioflavonoid rutins which can inhibit the production of reactive oxygen species (ROS) and depress ER stress-mediated NOD activation.
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3
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| HY-P81190 | Phospho-PERK (Thr980) Antibody |
Phospho-PERK (Thr980) Antibody is a Rabbit-derived and non-conjugated IgG polyclonal antibody, targeting to Phospho-PERK (Thr980).
Host: Rabbit; Reactivity: Human, Mouse, Rat |
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2
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| HY-P80379 | ATF6 Antibody (YA831) |
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2
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| HY-19696S1 | Tauroursodeoxycholate-d4 |
Tauroursodeoxycholate-d4 is deuterium labeled Tauroursodeoxycholate. Tauroursodeoxycholate (Tauroursodeoxycholic acid) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
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1
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| HY-123581 | Quinocetone |
Quinocetone is an orally active animal feed additive used to increase the meat production of livestock and poultry. Quinocetone exhibits antibacterial activity against a variety of pathogenic microorganisms. Quinocetone exhibits tissue-specific (liver, lymphocyte) toxicity. Quinocetone induces autophagy in cells through the ATF6/DAPK1 pathway. Quinocetone activates the NF-κB and iNOS pathways, leading to cell apoptosis, hepatocyte vacuolar degeneration and fibrosis. Quinocetone can inhibit Nrf2/HO-1 and induce the generation of reactive oxygen species (ROS), leading to oxidative stress and DNA damage.
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Antibiotic
Bacterial
ATF6
DAPK
Autophagy
NF-κB
NO Synthase
Apoptosis
Reactive Oxygen Species (ROS)
Keap1-Nrf2
Heme Oxygenase (HO)
Breast Cancer
Colorectal Cancer
Pancreatic Cancer
Ovarian Cancer
Bacterial Infection
Pain
Digestive System Inflammation
Parkinson's Disease
Lung Fibrosis
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1
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| HY-19696AS | Tauroursodeoxycholate-d4 sodium |
Tauroursodeoxycholate-d4 (sodium) is the deuterium labeled Tauroursodeoxycholate sodium. Tauroursodeoxycholate (Tauroursodeoxycholic acid; TUDCA) sodium is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
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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-112056 | DIM-C-pPhCO2Me |
DIM-C-pPhCO2Me is a nuclear receptor 4A1 (NR4A1) antagonist. DIM-C-pPhCO2Me induces Apoptosis. DIM-C-pPhCO2Me decreases PAX3-FOXO1A, N-Myc, Rassf4, MyoD1, Grem1, and DAPK1 proteins. DIM-C-pPhCO2Me decreases expression of TXNDC5 and IDH1, induces markers of ER stress (CHOP, ATF4 and p-PERK). DIM-C-pPhCO2Me inhibits renal cell carcinoma, breast cancer. DIM-C-pPhCO2Me can also be used in rhabdomyosarcoma research.
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1
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| HY-137813 | PERK-IN-4 |
PERK-IN-4 is a PERK inhibitor with a human IC50 of 0.3 nM and selectivity relative to other kinases. PERK-IN-4 displays moderate rat blood clearance and pharmacokinetic properties.
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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-132182 | HPA-12 |
HPA-12 is a blood-brain barrier-permeable small-molecule inhibitor of ceramide transfer protein (CERT) with four stereoisomers (the (1R,3R)-stereoisomer exhibits the highest activity). HPA-12 blocks the transport of ceramide from the endoplasmic reticulum to the Golgi apparatus by binding to the START domain of CERT, leading to intracellular ceramide accumulation and inhibition of sphingomyelin (SM) synthesis. HPA-12 induces endoplasmic reticulum stress via the GRP78/ATF6/CHOP axis and activates mitochondrial autophagy, thereby inhibiting cell growth and inducing apoptosis. In in vivo experiments, HPA-12 significantly reduces the leukemia burden and splenomegaly in mouse models of acute myeloid leukemia (AML) and prolongs survival. HPA-12 is applicable for the research of lipid metabolism in acute myeloid leukemia and Alzheimer's disease.
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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-101484A | NE-100 hydrochloride |
NE-100 hydrochloride is an orally active and selective sigma-1 receptor antagonist with an IC50 of 4.16 nM. NE-100 hydrochloride can improve cognitive impairment and has neuroprotective and antipsychotic activities. NE-100 hydrochloride can be used for research on nervous system diseases.
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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-P81233 | DDIT3 Antibody (YA3507) |
DDIT3 Antibody is a Mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to DDIT3.
Host: Mouse; Reactivity: Human, Mouse, Rat |
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1
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| HY-A0281S3 | 4-Phenylbutyric acid-d4 |
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| HY-149918 | Antiproliferative agent-23 |
Antiproliferative agent-23 is a microtubule-destabilizing agent (MDA) and efficiently disturbes the tubulin-microtubule system. Antiproliferative agent-23 induces apoptosis via a mitochondrion-dependent pathway by downregulating the Bcl-2 protein, upregulating Bax and Cyt c proteins, and activating the caspase cascade. Antiproliferative agent-23 initiates reactive oxygen species (ROS)-mediated endoplasmic reticulum stress in A549/CDDP cells (cisplatin resistant cancer cell line) via the PERK/ATF4/CHOP signaling pathway. Antiproliferative agent-23 has anti-tumor activity.
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| HY-19696S | Tauroursodeoxycholate-d5 |
Tauroursodeoxycholate-d5 is the deuterium labeled Tauroursodeoxycholate. Tauroursodeoxycholate (Tauroursodeoxycholic acid) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
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| HY-158104 | LPPM-8 |
LPPM-8 is a ligand of Med25 and an inhibitor of Med25 protein-protein interactions (PPIs). LPPM-8 engages Med25 through interaction with the H2 face of its Activator Interaction Domain and stabilizes full-length protein in the cellular proteome. LPPM-8 is an orthosteric inhibitor of H2-binding transcriptional activators (such as ATF6a). LPPM-8 can be used for studying Med25 and Mediator complex biology.
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| HY-12292G | IM-12 (GMP) |
IM-12 GMP is IM-12 (HY-12292) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. IM-12 is an orally active anti-inflammatory agent that targets and inhibits the NF-κB and STAT3 signaling pathways. IM-12 activates the Wnt signaling pathway and promotes the nuclear translocation of β-catenin by inhibiting GSK3β, while also blocking the tyrosine kinase activity of p210BCR/ABL. IM-12 reduces the levels of IL-6, IL-17, NO, prostaglandin E2, iNOS and COX-2, and induces ER stress, Ca2+ release, autophagy and apoptosis. IM-12 is heat-sensitive and does not induce autophagy in IM-resistant p210BCR/ABLT315I mutant cells. IM-12 is also a component of the 5iLA medium used for naive pluripotent stem cell research. IM-12 has been applied in studies related to carrageenan (HY-125474)-induced hind paw edema, TNBS-induced colitis, and acute and chronic myeloid leukemia.
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| HY-P11264 | Cyclic peptide P1-1 |
Cyclic peptide P1-1 is a high-potent GPR55 antagonist. Cyclic peptide P1-1 antagonizes GPR55 and suppresses collagen secretion. Cyclic peptide P1-1 reduces ROS production, attenuates ER stress, and inhibits mitochondria-associated Apoptosis. Cyclic peptide P1-1 inhibits the expression of α-SMA and COL1α. Cyclic peptide P1-1 ameliorates CCl4 (HY-Y0298)-induce and MCD-diet-induce acute liver inflammation and fibrosis.
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| HY-P1556 | Vasonatrin Peptide (VNP) |
Vasonatrin Peptide (VNP) is a chimera of atrial natriuretic peptide (ANP) and C-type natriuretic peptide (CNP). Vasonatrin peptide possesses the venodilating actions of CNP, the natriuretic actions of ANP, and unique arterial vasodilating actions not associated with either ANP or CNP. Vasonatrin Peptide protects the diabetic heart against ischemia-reperfusion injury by inhibiting ER stress via the cGMP-PKG signaling pathway.
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| HY-12956S2 | Dinoprost-13C5 |
Dinoprost-13C5 is 13C labeled Dinoprost (HY-12956). Dinoprost (Prostaglandin F2α) is an orally active, potent prostaglandin F (PGF) receptor (FP receptor) agonist. Dinoprost is a luteolytic hormone produced locally in the endometrial luminal epithelium and corpus luteum (CL). Dinoprost plays a key role in the onset and progression of labour.
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| HY-P11298 | d-T101 peptide |
d-T101 peptide, a human hormone-peptide, is a T1/ST2 receptor ligand. d-T101 peptide binds to the T1/ST2 receptor and activates caspases 8, 9 and 3 mediated apoptosis, together with activation of JNKinase and p38 MAPKinase. d-T101 peptide also changes Golgi structural with function loss and downregulation of the endoplasmic reticulum (ER) stress repair mechanism. d-T101 peptide has immunostimulatory and anticancer activity, selectively induces apoptosis in proliferating cancer cells and increases IL-2 and IFN-γ expression as well as the recruitment of NK cells and M1 macrophages to the tumor site.
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| HY-13433R | Thapsigargin (Standard) |
Thapsigargin (Standard) is the analytical standard of Thapsigargin (HY-13433). This product is intended for research and analytical applications. Thapsigargin, an endoplasmic reticulum (ER) stress inducer, is an inhibitor of microsomal Ca2+-ATPase. Thapsigargin efficiently inhibits coronavirus (HCoV-229E, MERS-CoV, SARS-CoV-2) replication in different cell types.
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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-19332R | Kifunensine (Standard) |
Bromperidol decanoate (Standard) is the analytical standard of Bromperidol decanoate. This product is intended for research and analytical applications. Bromperidol decanoate (R46541) is a compound used for the inhibition of schizophrenia and has certain clinical inhibitory activity.
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| HY-P3444A | CD31 TFA |
CD31 (PECAM-1) TFA is platelet endothelial cell adhesion molecule-1, serves as the endothelial cell-specific receptor of clostridium perfringens b-Toxin (CPB). CD31 TFA is also an ER-MP12 antigen, acts as a linker between mechanical stress, metabolism and inflammation. CD31 TFA peptide is able to sustain phosphorylation of the CD31 ITIM686 and of SHP2 and to inhibit TCR-induced T-cell activation-.
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| HY-19696S2 | Tauroursodeoxycholate-d4-1 |
Tauroursodeoxycholate-d4-1 is the deuterium labeled Tauroursodeoxycholate. Tauroursodeoxycholate (Tauroursodeoxycholic acid) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
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| HY-134800 | IBT21 |
IBT21 is an endoplasmic reticulum stress inhibitor that binds to unfolded or misfolded proteins and prevents their aggregation. IBT21 inhibits UPR activation of the ATF6, IRE1 and PERK branches under ER stress, with IC50 values of 0.24 μM, 0.33 μM, and 0.46 μM, respectively. IBT21 protects cells from ER stress-induced death and mutant prion protein (protein toxin)-induced growth inhibition. IBT21 exhibits chemical chaperone activity distinct from UPR modulators, does not affect protein translation, moderately reduces DTT (HY-15917)-induced ER stress, and fails to inhibit the heat shock response. IBT21 is useful for research related to prion diseases.
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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-B0852S2 | Tebuconazole-d6 |
Tebuconazole-d6 is a deuterium labeled Tebuconazole (HY-B0852). Tebuconazole is an orally active agricultural azole fungicide which can also inhibit CYP51 with IC50s of 0.9 and 1.3 μM for Candida albicans CYP51 (CaCYP51) and truncated Homo sapiens CYP51 (Δ60HsCYP51), respectively. Tebuconazole induces lipid accumulation and oxidative stress in HepG2 Cells. Tebuconazole decreases MAC-T cells viability and proliferation, induces ER-stress-mediated apoptosis and increases oxidative stress levels in MAC-T cells.
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| HY-138844 | 3-AP-Me |
3-AP-Me is a dimethyl derivative of the nucleotide reductase inhibitor 3-AP (SML0568). 3-AP-Me can activate the endoplasmic reticulum (ER) stress pathway by promoting the phosphorylation of eIF2α and increasing the gene expression of transcription factors ATF4 and ATF6, leading to cell apoptosis. Additionally, 3-AP-Me can activate the stress kinases c-Jun N-terminal kinase (JNK) and p38 mitogen-activated protein kinases. 3-AP-Me also leads to the upregulation of the spliced mRNA variant XBP1, can be used in cancer research.
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| HY-W104821 | Rosolic acid |
Rosolic acid is a Michael acceptor molecule isolated from the rhizomes of Plantago asiatica L. Rosolic acid inhibits Keap1, promotes Nrf2 nuclear translocation, and upregulates HO-1 and NQO-1. Rosolic acid reduces ER stress markers PERK, ATF-6, GRP78, and CHOP, as well as oxidative stress, ROS production, inflammation, and apoptosis. Rosolic acid upregulates SOD, CAT, and GPx activities, induces angiogenesis and insulin secretion, and restores endothelial function and pancreatic beta cell protection under ER stress. Rosolic acid can be used in research on diabetes and endothelial dysfunction.
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Keap1-Nrf2
Quinone Reductase
PERK
ATF6
Reactive Oxygen Species (ROS)
Apoptosis
SOD
Glutathione Peroxidase
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| HY-123581R | Quinocetone (Standard) |
Quinocetone (Standard) is the analytical standard of Quinocetone (HY-123581). This product is used for research and analytical purposes. Quinocetone is an orally active animal feed additive used to increase the meat production of livestock and poultry. Quinocetone exhibits antibacterial activity against a variety of pathogenic microorganisms. Quinocetone exhibits tissue-specific (liver, lymphocyte) toxicity. Quinocetone induces autophagy in cells through the ATF6/DAPK1 pathway. Quinocetone activates the NF-κB and iNOS pathways, leading to cell apoptosis, hepatocyte vacuolar degeneration and fibrosis. Quinocetone can inhibit Nrf2/HO-1 and induce the generation of reactive oxygen species (ROS), leading to oxidative stress and DNA damage.
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Reference Standards
Antibiotic
Bacterial
ATF6
DAPK
Autophagy
NF-κB
NO Synthase
Apoptosis
Reactive Oxygen Species (ROS)
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| HY-A0281S2 | 4-Phenylbutyric acid-d5 |
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| HY-P1556A | Vasonatrin Peptide (VNP) TFA |
Vasonatrin Peptide (VNP) TFA is a chimera of atrial natriuretic peptide (ANP) and C-type natriuretic peptide (CNP). Vasonatrin peptide TFA possesses the venodilating actions of CNP, the natriuretic actions of ANP, and unique arterial vasodilating actions not associated with either ANP or CNP. Vasonatrin Peptide TFA protects the diabetic heart against ischemia-reperfusion injury by inhibiting ER stress via the cGMP-PKG signaling pathway.
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| HY-P990805 | Anti-Human/Mouse GRP78 Antibody (C38) |
Anti-Human/Mouse GRP78 Antibody (C38) is a kind of mouse IgG2b antibody inhibitor, targeting to GRP78. Anti-Human/Mouse GRP78 Antibody (C38) inhibits RhoA, ROCK and AKT activation. Anti-Human/Mouse GRP78 Antibody (C38) can be used for the researches of cancer and metabolic disease, such as melanoma and diabetes.
Species: Human/Mouse |
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| HY-P3444 | CD31 |
CD31 (PECAM-1) is platelet endothelial cell adhesion molecule-1, serves as the endothelial cell-specific receptor of clostridium perfringens b-Toxin (CPB). CD31 is also an ER-MP12 antigen, acts as a linker between mechanical stress, metabolism and inflammation. CD31 peptide is able to sustain phosphorylation of the CD31 ITIM686 and of SHP2 and to inhibit TCR-induced T-cell activation-.
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| HY-A0281S | 4-Phenylbutyric acid-d11 |
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| HY-15654S | Phenylbutyrate-d11 sodium |
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| HY-152153 | GRP78-IN-3 |
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| HY-N16308 | ER-Laurdan |
ER-Laurdan is a derivative of the membrane-permeable fluorescent probe Laurdan (HY-D0080) that targets the endoplasmic reticulum (ER). As a membrane fluidity reporter, ER-Laurdan specifically localizes to the ER luminal membrane, and exhibits a prominent solvatochromic response to fluidity changes caused by membrane packing and exogenous saturated fatty acid stress. ER-Laurdan shows no overlapping localization with mitochondria, enables quantitative analysis of ER membrane fluidity via generalized polarization ratio measurement, and allows automatic signal masking with the help of ER markers. With high specificity and quantitative capability, ER-Laurdan serves as an important tool for investigating metabolic disorders and associated changes in the physical properties of cell membranes.
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| HY-W020952 | Palladium(Ⅱ) acetylacetonate |
Palladium(II) acetylacetonate is a metal-organic complex. Palladium(II) acetylacetonate upregulates the expression of GRP78, ATF-4, XBP-1, CHOP, and phosphorylated c-Jun. Palladium(II) acetylacetonate induces Apoptosis. Palladium(II) acetylacetonate has anticancer effects against non-small cell lung cancer, gastric cancer, leukemia, and cervical cancer.
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| HY-P73256 | IRE1 Protein, Human (Active, sf9, His-GST) |
IRE1 is a key serine/threonine protein kinase and endoribonuclease essential for sensing the unfolded protein response (UPR) in the endoplasmic reticulum. In cellular homeostasis, it remains monomeric by binding to HSPA5/BiP. IRE1 Protein, Human (sf9, His-GST) is the recombinant human-derived IRE1 protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag.
Species: Human; Source: Sf9 insect cells |
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| HY-P73858 | IRE1 Protein, Human (sf9) |
IRE1 is a key serine/threonine protein kinase and endoribonuclease essential for sensing the unfolded protein response (UPR) in the endoplasmic reticulum. In cellular homeostasis, it remains monomeric by binding to HSPA5/BiP. IRE1 Protein, Human (sf9) is the recombinant human-derived IRE1 protein, expressed by Sf9 insect cells , with tag free.
Species: Human; Source: Sf9 insect cells |
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| HY-P80781 | PERK Antibody (YA233) |
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| HY-P80554 | ATF6 Antibody (YA604) |
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| HY-P82630 | VCP Antibody (YA2375) |
VCP Antibody (YA2375) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to VCP.
Host: Rabbit; Reactivity: Human, Mouse, Rat |
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| HY-P85324 | PERK Antibody (YA5016) |
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| HY-P84401 | VCP Antibody (YA4098) |
VCP Antibody (YA4098) is a Mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to VCP.
Host: Mouse; Reactivity: Human, Mouse |
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| HY-P86626 | ATF6 Antibody (YA6318) |
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