Search Result
Results for "
lysosomal degradation
" in MedChemExpress (MCE) Product Catalog:
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-148673
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AZD0780; PCSK9-IN-12
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PCSK9
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Cardiovascular Disease
Metabolic Disease
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Laroprovstat (AZD0780) is an orall active PCSK9 inhibitor. PCSK9-IN-12 has bind affinity for PCSK9 with a Kd value of <200 nM. Laroprovstat binds to a pocket in the PCSK9 C-terminal domain and does not affect the PCSK9-LDL receptor (LDLR) interaction. Laroprovstat inhibits lysosomal trafficking of PSCK9-LDLR complexes and prevents PCSK9-induced LDLR degradation. Laroprovstat can be used for the research of hypercholesterolemia .
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- HY-D2449
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Fluorescent Dye
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Others
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DQ-BSA-Red is a bovine serum albumin labeled with a red fluorescent dye that can be used to detect lysosomal activity. The excitation wavelength and emission wavelength of DQ-BSA-Red are 590 nm and 620 nm, respectively. The BSA molecule in DQ-BSA-Red is labeled with high concentration of red fluorescent dye in multiple sites, which shows high fluorescence self-inhibition. Once DQ-BSA-RED enters the lysosome, DQ-BSA is cleaved by lysosomal proteases, resulting in unquenched and released fluorescent fragments, emitting bright fluorescence. Inactivated lysosomes are unable to degrade the BSA protein and thus have a lower or even no fluorescent signal .
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- HY-13817
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IU1
Maximum Cited Publications
25 Publications Verification
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Deubiquitinase
Autophagy
Apoptosis
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Cardiovascular Disease
Neurological Disease
Endocrinology
Cancer
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IU1 is a selective, reversible USP14 inhibitor with an IC50 of 4-5 μM. IU1 binds USP14’s catalytic cleft to block deubiquitinase activity. IU1 induces calpain-dependent Tau cleavage, causes ATP deficits, reduces E1~Ub thioester levels and 26S proteasome assembly. IU1 enhances 26S proteasome chymotrypsin-like activity, modulates LC3B-dependent autophagy flux, reduces cancer cell proliferation and migration, and blocks G0/G1 to S phase cell cycle transition in follicular thyroid cancer cells. IU1 activates autophagy-lysosomal and ubiquitin-proteasome pathways, triggers apoptosis, and reduces cervical cancer cell growth. IU1 enhances degradation of proteasome substrates linked to neurodegenerative disease, accelerates oxidized protein degradation, and increases oxidative stress resistance. IU1 can be used for the research of Alzheimer’s disease, follicular thyroid cancer, ischemic stroke, cervical cancer, and neurodegenerative disease .
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- HY-128144
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Lipase
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Metabolic Disease
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Lalistat 2 is an inhibitor of many lipases especially Lysosomal acid lipase (LAL, IC50 = 152 nM), which is a key enzyme that degrades neutral lipids at an acidic pH in lysosomes. Lalistat 2 is commonly used to investigate the cell-specific functions of LAL and LAL deficiency in vitro, as well as specifically measure LAL activity in human blood samples or cells .
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- HY-13822
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SphK
Wnt
Apoptosis
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Cancer
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SKI-II is an oral active and synthetic inhibitor of sphingosine kinase (SK) activity, with IC50 values of 78 μM and 45 μM for SK1 and for SK2, respectively. SKI II causes an irreversible inhibition of SK1 by inducing its lysosomal and/or proteasomal degradation .
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- HY-155747
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FDW028
1 Publications Verification
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Autophagy
Akt
mTOR
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Cancer
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FDW028 a potent and highly selective FUT8 inhibitor. FUT8 exhibits potent anti-tumor activity by defucosylation and impelling lysosomal degradation of B7-H3 through the chaperone-mediated autophagy (CMA) pathway. FDW028 can be used for metastatic colorectal cancer (mCRC) research .
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- HY-107811
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Harmol
1 Publications Verification
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Autophagy
α-synuclein
Apoptosis
Monoamine Oxidase
Mitosis
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Neurological Disease
Cancer
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Harmol is an orally active β-carboline alkaloid. Harmol is a TFEB activator and monoamine oxidase inhibitor. Harmol can induce cell mitosis, Autophagy and Apoptosis. Harmol promotes the degradation of α-synuclein by regulating the autophagy-lysosomal pathway. Harmol has anti-tumor, anti-depressant and anti-aging activities. Harmol improves motor impairment in a mouse Parkinson's disease model .
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- HY-148118A
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LYTACs
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Cancer
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Tri-GalNAc(OAc)3 TFA is a trivalent N-acetylgalactosamine (GalNAc) derivative that can be used to synthesize GalNAc-LYTAC. Tri-GalNAc is a specific ligand targeting the asialoglycoprotein receptor (ASGPR), mediating the endocytosis and transport of cell surface proteins (such as EGFR, HER2) to lysosomes for degradation by lysosomal targeting chimeras (LYTACs). Tri-GalNAc significantly reduces the level of target proteins and inhibits downstream signaling pathways (such as EGFR-mediated Akt and MAPK signals). Tri-GalNAc(OAc)3 TFA can be used for hepatocyte targeting studies, and can degrade carcinogenic membrane proteins and inhibit tumor cell proliferation in liver cancer cell models .
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- HY-133736
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PROTAC-Linker Conjugates for PAC
ADC Payload
Epigenetic Reader Domain
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Cancer
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PROTAC BRD4 Degrader-5-CO-PEG3-N3 is a PROTAC-linker Conjugate for PAC, comprises the BRD4 degrader (MZ 1 (HY-107425) analog) and PEG-based linker. PROTAC BRD4 Degrader-5-CO-PEG3-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups. PROTAC BRD4 Degrader-5-CO-PEG3-N3 can be used for the research of HER2-positive breast cancer .
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- HY-P6438
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Integrin
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Others
Cancer
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Alkyne-cRGD is an integrin ligand. Alkyne-cRGD can be used in the study of degraders. Alkyne-cRGD undergoes copper-catalyzed azide-alkyne cycloaddition reaction .
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- HY-148409
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Ferroptosis
Apoptosis
Autophagy
MDM-2/p53
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Cancer
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MMRi62, a ferroptosis inducer targeting MDM2-MDM4 (negative regulators of tumor suppressor p53). MMRi62 shows a P53-independent pro-apoptotic activity against pancreatic ductal adenocarcinoma (PDAC) cells and induce autophagy. MMRi62 inducesferroptosis, resulting in a increase of reactive oxygen and lysosomal degradation of ferritin heavy chain (FTH1). MMRi62 also leads to proteasomal degradation of mutant p53, also inhibits orthotopic xenograft PDAC mouse model in vivo with high frequency mutation characteristics of KRAS and TP53.12 .
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- HY-123058
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PI3K
Autophagy
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Cancer
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Vps34-IN-4 (compound 19) is a potent, selective, and orally active inhibitor of VPS34. Vps34-IN-4 inhibits the autophagy in vivo. Autophagy is a dynamic process that regulates lysosomal-dependent degradation of cellular components .
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- HY-125168
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EGA
2 Publications Verification
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EGFR
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Infection
Inflammation/Immunology
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EGA is an inhibitor that selectively targets the endosomal trafficking pathways. EGA targets the proteins involved in the endosomal trafficking pathways through which multiple toxins and viruses enter cells. EGA exerts its activity by inhibiting the trafficking from early endosomes to late endosomes, blocking the entry of multiple acid-dependent bacterial toxins and viruses into mammalian cells and delaying the lysosomal targeting and degradation of EGFR .
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- HY-161746
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AUTOTACs
Autophagy
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Neurological Disease
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Anle138b-F105 is an autophagy-targeting chimera (AUTOTAC) that targets p62/Sequestosome-1/SQSTM1. Anle138b-F105 binds to the ZZ domain of p62, induces conformational activation, self-oligomerization, interaction with LC3, and formation of autophagosomes. Anle138b-F105 induces autophagic flux of ubiquitin-conjugated aggregated proteins, leading to their lysosomal degradation. Anle138b-F105 is applicable for the research of neurodegenerative proteinopathies .
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- HY-W489121
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p62
Autophagy
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Cancer
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YTK-105 is a p62/ZZ binding domain ligand and Autophagy enhancer. YTK-105 activates p62-dependent selective macroautophagy. YTK-105 serves as an autophagy-targeting ligand (ATL) for synthesizing AUTOTAC degraders .
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- HY-175209
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Keap1-Nrf2
Ferroptosis
Reactive Oxygen Species (ROS)
Atg8/LC3
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Cancer
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Nrf2-IN-4 is a Nrf2 inhibitor. Nrf2-IN-4 induces ferroptosis via NRF2 inhibition. Nrf2-IN-4 disrupts cellular iron homeostasis, facilitates ferritin degradation, and ultimately triggers ferroptosis. Nrf2-IN-4 induces lysosome activation by promoting iron-dependent ROS production and lysosomal acidification. Nrf2-IN-4 demonstrates significant antitumor efficacy. Nrf2-IN-4 can be used for the study of breast cancer .
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- HY-153880
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LYTACs
Ras
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Cancer
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KRAS degrader-1 is a potent KRAS degrader. KRAS degrader-1 targets specific proteins for degradation via the autophagy-lysosomal degradation pathway. KRAS degrader-1 is suitable for use in cancer research. (Blue: KRAS G12C-IN-72 (HY-128414); Black: Linker (HY-175587); Pink: 5-Iodoindolin-2-one (HY-76986); Blue + Black: KRAS ligand-Linker Conjugate 7 (HY-175586)) .
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- HY-125900
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NCA
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Others
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Cancer
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Neocarzilin A (NCA) reduces BST-2 levels via lysosomal degradation. Neocarzilin A has antimigratory and antiproliferative effects on cancer cells. Neocarzilin A inhibits cancer cell migration via irreversible binding to the synaptic vesicle membrane protein VAT-1 .
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- HY-150286
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Prion Protein
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Neurological Disease
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SM875 is a cellular prion protein (PrP) degrader (IC50: 7.87 μM). SM875 targets PrP folding intermediates and promotes its degradation through the autophagy-lysosomal pathway. SM875 only acts on nascent, immature PrP molecules and has no effect on mature PrP before synthesis. SM875 can inhibit prion replication and has potential in the study of neurodegenerative diseases (i.e., prion diseases) .
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- HY-174468
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LYTACs
PD-1/PD-L1
HSP
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Cancer
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dPDL1-4 is a potent and selective eHSPTAC eHSP90 PD-L1 degrader with DC50s of 7.77 μM and 6.52 μM in HeLa and B16F10 cells. dPDL1-4 bridges eHSP90 with the target protein, inducing lysosomal degradation. dPDL1-4 can degrade PD-L1 significantly and inhibits tumor growth. dPDL1-4 can be used for the study of cervical cancer and melanoma. ((Pink: eHSP90 ligand (HY-174476); Blue: PD-L1 ligand (HY-116274); Black: Linker (HY-W021787); HSP ligand + linker: HY-174799)) .
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- HY-125859E
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Glutathione Peroxidase
Bacterial
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Infection
Inflammation/Immunology
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Myeloperoxidase, Human Neutrophil is a peroxidase. Myeloperoxidase, Human Neutrophil is a potent antibacterial agent by catalyzing the H2O2-dependent oxidation of chloride anion to generate hypochlorous acid. Myeloperoxidase, Human Neutrophil catalyzes the degradation of N-retinyl-idene-N-retinylethanolamine, a toxic form of retinal lipofuscin. Myeloperoxidase, Human Neutrophil also triggers lysosomal stress and cell death. Myeloperoxidase, Human Neutrophil can be used for the researches of inflammation and infection .
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- HY-175209A
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Keap1-Nrf2
Ferroptosis
Reactive Oxygen Species (ROS)
Atg8/LC3
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Cancer
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Nrf2-IN-4 (Compound PhcY) hydrobromide is a Nrf2 inhibitor. Nrf2-IN-4 hydrobromide induces ferroptosis via NRF2 inhibition. Nrf2-IN-4 hydrobromide disrupts cellular iron homeostasis, facilitates ferritin degradation, and ultimately triggers ferroptosis. Nrf2-IN-4 hydrobromide induces lysosome activation by promoting iron-dependent ROS production and lysosomal acidification. Nrf2-IN-4 hydrobromide demonstrates significant antitumor efficacy. Nrf2-IN-4 hydrobromide can be used for the study of breast cancer .
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- HY-162972
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PROTACs
PD-1/PD-L1
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Inflammation/Immunology
Cancer
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PROTAC PD-L1 degrader-2 is a PD-L1 PROTAC degrader with an IC50 of 197.4 nM and a Kd of 301 nM. PROTAC PD-L1 degrader-2 induces PD-L1 endocytosis, drives degradation via the proteasomal and lysosomal pathways, and inhibits the PD-1/PD-L1 interaction. As an immune activator, PROTAC PD-L1 degrader-2 increases the levels of CD4 +, CD8 +, granzyme B and perforin. PROTAC PD-L1 degrader-2 can be used in studies related to colon cancer immunology .
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- HY-147656
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ATTECs
NAMPT
Autophagy
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Cancer
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NAMPT degrader-1 (Compound A3), an autophagosome-tethering compound (ATTEC), is an nicotinamide phosphoribosyltransferase (NAMPT) degrader with an IC50 of 0.023 μM. NAMPT degrader-1 significantly induces the degradation of NAMPT through the autophagy-lysosomal pathway and shows excellent cellular antitumor potency .
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- HY-107811A
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Autophagy
α-synuclein
Apoptosis
Monoamine Oxidase
Mitosis
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Neurological Disease
Cancer
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Harmol hydrochloride is an orally active β-carboline alkaloid. Harmol hydrochloride is a TFEB activator and monoamine oxidase inhibitor. Harmol hydrochloride can induce cell mitosis, Autophagy and Apoptosis. Harmol hydrochloride promotes the degradation of α-synuclein by regulating the autophagy-lysosomal pathway. Harmol hydrochloride has anti-tumor, anti-depressant and anti-aging activities. Harmol hydrochloride improves motor impairment in a mouse Parkinson's disease model .
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- HY-P5377
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Cathepsin K substrate
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Ser/Thr Protease
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Others
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Abz-HPGGPQ-EDDnp (Cathepsin K substrate) is a biological active peptide. (Cathepsins are a class of globular lysosomal proteases, playing a vital role in mammalian cellular turnover. They degrade polypeptides and are distinguished by their substrate specificities. Cathepsin K is the lysosomal cysteine protease involved in bone remodeling and resorption. It has potential as a drug target in autoimmune diseases and osteoporosis.This FRET peptide can be used to monitor selectively cathepsin K activity in physiological fluids and cell lysates. Abz-HPGGPQ-EDDnp [where Abz represents o-aminobenzoic acid and EDDnp represents N -(2, 4-dinitrophenyl)-ethylenediamine], a substrate initially developed for trypanosomal enzymes, is efficiently cleaved at the Gly-Gly bond by cathepsin K. This peptide is resistant to hydrolysis by cathepsins B, F, H, L, S and V, Ex/Em=340 nm/420 nm.)
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- HY-169385
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AUTOTACs
Androgen Receptor
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Cancer
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ATC-324 is an bivalent AR (Androgen Receptor) degrader based on the protein degradation technology platform AUTOphagy-TArgeting Chimera (AUTOTAC). ATC-324 induces the formation of AR/p62 complex, leading to autophagy-lysosomal degradation of AR. ATC-324 can reduce nuclear AR levels and downregulate target gene expression of AR and AR-v7, and also has a degradation effect on common AR mutants in PCa . ATC-324 is composed of target-binding ligand (TBL) Enzalutamide (HY-70002) and p62/SQSTM1 autophagy-targeting ligand (ATL) YT 6-2 analog-1 (HY-169386), connected by Boc-NH-PEG4-CH2CH2NH2 (HY-W008352). Among them, the active control of the target protein ligand is Enzalutamide carboxylic acid (HY-70002B), and the conjugate composed of the autophagy-targeting ligand and the linker is YT 6-2-PEG3-C2-NH2 (HY-169387).
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- HY-175392
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PROTACs
Epoxide Hydrolase
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Metabolic Disease
Inflammation/Immunology
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PROTAC sEH-degrader-3 (Compound 1a) is a targeted sEH PROTAC degrader that can selectively degrade sEH in the cytosol without affecting sEH in peroxisomes. PROTAC sEH-degrader-3 degrades sEH through a CRBN-dependent lysosomal pathway rather than the proteasome, with an IC50 of 0.8 nM against hsEH. PROTAC sEH-degrader-3 can inhibit endoplasmic reticulum stress and can be used in the research of inflammation, metabolic diseases, and other diseases related to endoplasmic reticulum stress. (Pink: sEH inhibitor (HY-114266); Black: Linker (HY-W008352); Blue: E3 Ligase Ligand (HY-14658)) .
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- HY-203817
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Autophagy
Apoptosis
Mitochondrial Metabolism
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Cancer
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IITZ-02 is a lysosomotropic Autophagy inhibitor. IITZ-02 enhances autophagosome accumulation but inhibits autophagosomal degradation by impairing lysosomal function, finally inducing the inhibition of autophagy. IITZ-02 abolishes mitochondrial membrane potential and induces apoptosis through the mitochondria-mediated pathway. IITZ-02 has a potent antitumor activity in MDA-MB-231 xenograft mouse models. IITZ-02 can be used for cancers research .
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- HY-173150
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YAP
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Cancer
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Hapalindole Q (Compound (+)-1) is an autophagy (Autophagy) inhibitor targeting YAP1. Hapalindole Q binds to the Hippo pathway transcription factor YAP1 with a Kd of 9.13 μM and induces its degradation via the chaperone-mediated autophagy (CMA) pathway. This process inhibits Rab7-mediated fusion of autophagosomes and lysosomes, thereby reducing overall autophagy levels without affecting lysosomal function. Hapalindole Q holds promise for research in cancer (e.g., liver cancer, breast cancer, etc.) .
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- HY-107811R
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Apoptosis
Monoamine Oxidase
Autophagy
α-synuclein
Mitosis
Reference Standards
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Neurological Disease
Cancer
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Harmol (Standard) is the analytical standard of Harmol (HY-107811). This product is intended for research and analytical applications. Harmol hydrochloride is an orally active β-carboline alkaloid. Harmol hydrochloride is a TFEB activator and monoamine oxidase inhibitor. Harmol can induce cell mitosis, Autophagy and Apoptosis. Harmol promotes the degradation of α-synuclein by regulating the autophagy-lysosomal pathway. Harmol has anti-tumor, anti-depressant and anti-aging activities. Harmol improves motor impairment in a mouse Parkinson's disease model .
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- HY-183061
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LYTACs
Epigenetic Reader Domain
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Neurological Disease
Cancer
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MrTAC-8, methylarginine-targeting chimera (MrTAC), is a BRD4 degrader with DC50 values of 46 nM in HeLa cells. MrTAC-8 recruits PRMT1, PRMT3, PRMT4, PRMT5, and PRMT7 to target proteins, inducing arginine methylation that triggers lysosomal degradation. MrTAC-8 degrades proteins across diverse subcellular localizations and independent of native proteolytic routes. MrTAC-8 can be used for the research of cervical cancer, glioblastoma .
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- HY-181829
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EGFR
PSMA
LYTACs
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Cancer
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Ctx-L3 is a selective EGFR PTAC (PSMA-targeted chimera) degrader (DC50: 4.3 pM in LNCaP cells) and LYTAC. Ctx-L3 recruits prostate-specific membrane antigen (PSMA) and mediates lysosomal degradation of EGFR in PSMA-positive prostate cancer cells. Ctx-L3 exhibits degrading activity against EGFR in prostate cancer cells. Ctx-L3 is applicable to related research on prostate cancer .
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- HY-181830
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PD-1/PD-L1
PSMA
LYTACs
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Cancer
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Atz-L5 is a PD-L1 PTAC (PSMA-targeted chimera) degrader (DC50: 18 pM in PC3-PIP cells; 2 pM in LNCaP cells) and LYTAC. Atz-L5 promotes lysosomal degradation of PD-L1 in PSMA-positive prostate cancer cells. Atz-L5 is applicable to the research of prostate cancer .
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- HY-P992066
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Discoidin Domain Receptor
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Inflammation/Immunology
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Anti-Mouse DDR2 Antibody (DAB0065) is a mAb that specifically targets mouse discoidin domain receptor DDR2 without cross-reacting with DDR1. Anti-Mouse DDR2 Antibody (DAB0065) binds to the extracellular domain of native mouse DDR2, induces endocytosis and lysosomal degradation of DDR2, and this process is independent of collagen binding. Anti-Mouse DDR2 Antibody (DAB0065) exhibits significant therapeutic effects in both the unilateral ureteral obstruction (UUO) mouse model of renal fibrosis and the bleomycin (HY-108345)-induced mouse model of pulmonary fibrosis, effectively downregulating the mRNA expression of type I collagen Col1a1 and fibronectin Fn1. Anti-Mouse DDR2 Antibody (DAB0065) can be humanized and has the potential to be developed as a targeted agent for diseases such as idiopathic pulmonary fibrosis and renal fibrosis .
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- HY-180571
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PROTACs
CCR
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Cancer
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LUF7996 is a CCR2 PROTAC Degrader degrading CCR2 with DC50 = 2.6 μM. LUF7996 demonstrates engagement of both and the E3 ligase cereblon and displays sustain and concentration-dependent degradation of CCR2. LUF7996 reliance on the lysosomal pathway to induce CCR2 degradation. LUF7996 efficiently inhibits monocyte migration in virto .
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- HY-183660
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Autophagy
Amyloid-β
Tau Protein
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Neurological Disease
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F-SLOH is a brain-penerant and orally active TFEB activator and amyloid-β inhibitor with an IC50 of 3.4 μM against amyloid-β. F-SLOH promotes nuclear translocation of TFEB, driving autophagy and lysosomal biogenesis. F-SLOH reduces amyloid-β oligomers and Tau aggregates via autophagy lysosomal degradation pathway. F-SLOH can be used for the research of Alzheimer’s disease .
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- HY-179558
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PD-1/PD-L1
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Cancer
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MS1-96 is an orally active PD-L1 (programmed death-ligand 1) degrader. MS1-96 effectively reduced PD-L1 protein levels across multiple colorectal cancer (CRC) cell lines. MS1-96 directly binds to PD-L1 (KD = 2.58 μM) and enhances the interaction between HIP1R and PD-L1, thereby altering the intracellular trafficking of PD-L1 within clathrin-coated vesicles. MS1-96 induces abnormal N-glycosylation of PD-L1, destabilizing the protein and hastening its lysosome-mediated degradation. MS1-96 can be used for the study of colorectal cancer .
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- HY-183717
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Cancer
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M4K3233 is a selective ALK2 PROTAC degrader with a pDC50 of 7.3 and a pIC50 of 6.6. M4K3233 recruits CRBN to form a ternary complex with ALK2, mediating ALK2 degradation via the proteasomal and lysosomal pathways. M4K3233 induces moderate downregulation of RIPK2 and significant downregulation of SIK3 in mammalian cells. M4K3233 is applicable to research related to glioblastoma .
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- HY-180222
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CDK
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Cancer
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KGA-4066 is a novel non-ATP-competitive CDK2 inhibitor. KGA-4066 inhibits CDK2/Cyclin A2 with an IC50 value of 236.7 nM, disrupts their interaction, promots CDK2 degradation via the lysosomal pathway. KGA-4066 has anticancer activity against hepatocellular carcinoma .
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- HY-186196
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Ferroptosis
Reactive Oxygen Species (ROS)
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Cancer
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Fentomycin-1 is a ferroptosis inducer. Fentomycin-1 activates lysosomal iron 2+ under acidic conditions with hydrogen peroxide to form a reactive iron-oxo species, which induces oxidative degradation, oxidation, and lipolysis of membrane phospholipids, triggering ferroptosis. Fentomycin-1 can be used for the research of pancreatic ductal adenocarcinoma, breast cancer metastasis, and melanoma .
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- HY-182959
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Hsp-targeting Chimeras
LYTACs
PD-1/PD-L1
HSP
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Cancer
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Hsp70TAC PD-1 Degrader-2 is a PD-L1 Hsp70TAC (Hsp70-targeting Chimeras) degrader with Kd values of 0.36 μM. Hsp70TAC PD-1 Degrader-2 forms a ternary complex with Hsp70 and PD-L1 to drive PD-L1 degradation. Hsp70TAC PD-1 Degrader-2 induces degradation of mature membrane-bound PD-L1 in an Hsp70-dependent manner and via caveolin-mediated endocytosis and lysosomal trafficking. Hsp70TAC PD-1 Degrader-2 accumulates preferentially in tumor cells with elevated Hsp70 expression for tumor-selective PD-L1 degradation. Hsp70TAC PD-1 Degrader-2 can be used for the research of cancer, such as breast invasive carcinoma, glioblastoma multiforme, diffuse large b-cell lymphoma . (Pink: PD-1/PD-L1 ligand (HY-19745A); Blue: Hsp70 ligand (HY-182979); Black: linker (HY-182982)).
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- HY-183257
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Autophagy
Beclin1
Reactive Oxygen Species (ROS)
p97
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Cancer
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ATI-1 is an autophagy initiation inhibitor. ATI-1 targets valosin-containing protein (VCP/p97, disrupts its interaction with UFL1, impairs UFMylation homeostasis associated with VCP, promotes polyubiquitination and degradation of Beclin1, and blocks the formation of early autophagosomes. ATI-1 induces synergistic death of autophagy-dependent malignant tumor cells under nutrient deprivation conditions, accompanied by decreased mitochondrial membrane potential, reduced ROS levels and lysosomal stress. ATI-1 exhibits anti-tumor efficacy in a pancreatic adenocarcinoma xenograft mouse model. ATI-1 can be used for the research of pancreatic adenocarcinoma and lung cancer .
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- HY-P991888
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STAT
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Cardiovascular Disease
Cancer
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INCA033989 is a fully human IgG1 monoclonal antibody targeting mutCALR (KD = 1.75 nM for mutCALR del52; KD = 6.78 nM for mutCALR ins5). INCA033989 antagonizes mutCALR-driven signaling and proliferation. INCA033989 selectively inhibits pSTAT3/pSTAT5. INCA033989 prevents thrombocytosis and reduces the expansion of mutCALR-positive cells. INCA033989 is useful for research on myeloproliferative neoplasms .
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HY-L029
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1,956 compounds
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Autophagy is a lysosomal degradation pathway that is essential for cell survival, differentiation, development, and homeostasis. The process of autophagy in mammalian cells is as follows: a portion of cytoplasm, including organelles, is enclosed by a phagophore or isolation membrane to form an autophagosome. The outer membrane of the autophagosome subsequently fuses with the endosome and then the lysosome, and the internal material is degraded. Autophagy plays a wide variety of physiological and pathophysiological roles. Defective autophagy contributes to various pathologies, including infections, cancer, neurodegeneration, aging, and heart disease.
MCE provides a unique collection of 1,956 autophagy pathway-related compounds that is a useful tool for the research of autophagy-related regulation and diseases.
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| Cat. No. |
Product Name |
Type |
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- HY-D2449
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Fluorescent Dyes
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DQ-BSA-Red is a bovine serum albumin labeled with a red fluorescent dye that can be used to detect lysosomal activity. The excitation wavelength and emission wavelength of DQ-BSA-Red are 590 nm and 620 nm, respectively. The BSA molecule in DQ-BSA-Red is labeled with high concentration of red fluorescent dye in multiple sites, which shows high fluorescence self-inhibition. Once DQ-BSA-RED enters the lysosome, DQ-BSA is cleaved by lysosomal proteases, resulting in unquenched and released fluorescent fragments, emitting bright fluorescence. Inactivated lysosomes are unable to degrade the BSA protein and thus have a lower or even no fluorescent signal .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P6438
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Integrin
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Others
Cancer
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Alkyne-cRGD is an integrin ligand. Alkyne-cRGD can be used in the study of degraders. Alkyne-cRGD undergoes copper-catalyzed azide-alkyne cycloaddition reaction .
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- HY-P5377
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Cathepsin K substrate
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Ser/Thr Protease
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Others
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Abz-HPGGPQ-EDDnp (Cathepsin K substrate) is a biological active peptide. (Cathepsins are a class of globular lysosomal proteases, playing a vital role in mammalian cellular turnover. They degrade polypeptides and are distinguished by their substrate specificities. Cathepsin K is the lysosomal cysteine protease involved in bone remodeling and resorption. It has potential as a drug target in autoimmune diseases and osteoporosis.This FRET peptide can be used to monitor selectively cathepsin K activity in physiological fluids and cell lysates. Abz-HPGGPQ-EDDnp [where Abz represents o-aminobenzoic acid and EDDnp represents N -(2, 4-dinitrophenyl)-ethylenediamine], a substrate initially developed for trypanosomal enzymes, is efficiently cleaved at the Gly-Gly bond by cathepsin K. This peptide is resistant to hydrolysis by cathepsins B, F, H, L, S and V, Ex/Em=340 nm/420 nm.)
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| Cat. No. |
Product Name |
Target |
Research Area |
Image |
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- HY-P992066
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Discoidin Domain Receptor
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Inflammation/Immunology
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Anti-Mouse DDR2 Antibody (DAB0065) is a mAb that specifically targets mouse discoidin domain receptor DDR2 without cross-reacting with DDR1. Anti-Mouse DDR2 Antibody (DAB0065) binds to the extracellular domain of native mouse DDR2, induces endocytosis and lysosomal degradation of DDR2, and this process is independent of collagen binding. Anti-Mouse DDR2 Antibody (DAB0065) exhibits significant therapeutic effects in both the unilateral ureteral obstruction (UUO) mouse model of renal fibrosis and the bleomycin (HY-108345)-induced mouse model of pulmonary fibrosis, effectively downregulating the mRNA expression of type I collagen Col1a1 and fibronectin Fn1. Anti-Mouse DDR2 Antibody (DAB0065) can be humanized and has the potential to be developed as a targeted agent for diseases such as idiopathic pulmonary fibrosis and renal fibrosis .
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(5)
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- HY-P991888
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STAT
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Cardiovascular Disease
Cancer
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INCA033989 is a fully human IgG1 monoclonal antibody targeting mutCALR (KD = 1.75 nM for mutCALR del52; KD = 6.78 nM for mutCALR ins5). INCA033989 antagonizes mutCALR-driven signaling and proliferation. INCA033989 selectively inhibits pSTAT3/pSTAT5. INCA033989 prevents thrombocytosis and reduces the expansion of mutCALR-positive cells. INCA033989 is useful for research on myeloproliferative neoplasms .
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(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-107811
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- HY-125900
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NCA
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Natural Products
Microorganisms
Source Classification
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Others
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Neocarzilin A (NCA) reduces BST-2 levels via lysosomal degradation. Neocarzilin A has antimigratory and antiproliferative effects on cancer cells. Neocarzilin A inhibits cancer cell migration via irreversible binding to the synaptic vesicle membrane protein VAT-1 .
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- HY-173150
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Structural Classification
Alkaloids
Microorganisms
Other Alkaloids
Source Classification
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YAP
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Hapalindole Q (Compound (+)-1) is an autophagy (Autophagy) inhibitor targeting YAP1. Hapalindole Q binds to the Hippo pathway transcription factor YAP1 with a Kd of 9.13 μM and induces its degradation via the chaperone-mediated autophagy (CMA) pathway. This process inhibits Rab7-mediated fusion of autophagosomes and lysosomes, thereby reducing overall autophagy levels without affecting lysosomal function. Hapalindole Q holds promise for research in cancer (e.g., liver cancer, breast cancer, etc.) .
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- HY-107811R
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| Cat. No. |
Product Name |
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Classification |
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- HY-133736
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PROTAC Synthesis
Azide
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PROTAC BRD4 Degrader-5-CO-PEG3-N3 is a PROTAC-linker Conjugate for PAC, comprises the BRD4 degrader (MZ 1 (HY-107425) analog) and PEG-based linker. PROTAC BRD4 Degrader-5-CO-PEG3-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups. PROTAC BRD4 Degrader-5-CO-PEG3-N3 can be used for the research of HER2-positive breast cancer .
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- HY-P6438
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Alkynes
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Alkyne-cRGD is an integrin ligand. Alkyne-cRGD can be used in the study of degraders. Alkyne-cRGD undergoes copper-catalyzed azide-alkyne cycloaddition reaction .
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