Search Result
Results for "
unfolded
" in MedChemExpress (MCE) Product Catalog:
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-132247
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Others
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Cancer
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ErSO is a selective anticipatory unfolded protein response (a-UPR) activator. ErSO acts through ERα to elicit strong and sustained cytotoxic activation of the a-UPR. ErSO can be used for the research of cancer .
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- HY-18705
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Apoptosis
Reactive Oxygen Species
Caspase
Bcl-2 Family
Mitochondrial Metabolism
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Endocrinology
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Azoramide is a potent, orally active small-molecule modulator of the unfolded protein response (UPR). Azoramide improves ER protein folding and elevates ER chaperone capacity, which together protects cells against ER stress. Azoramide alleviates PLA2G6 mutant-induced ER stress through modulating unfolded protein response, and enhances the CERB signaling to rescue mitochondrial function, thereby preventing apoptosis of DA neurons. Azoramide has antidiabetic activity .
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- HY-101991
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PERK
Eukaryotic Initiation Factor (eIF)
Apoptosis
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Cancer
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ML291 is a UPR (unfolded protein response)-inducing sulfonamidebenzamide. ML291 overwhelms the adaptive capacity of the UPR and induces apoptosis in a variety of solid cancer models. ML291 can activate the PERK/eIF2a/CHOP (apoptotic) arm of the UPR and reduce leukemic cell burden .
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- HY-143218
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TPE-MI
2 Publications Verification
Tetraphenylethene maleimide
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Huntingtin
Parasite
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Neurological Disease
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TPE-MI (Tetraphenylethene maleimide) is a thiol probe for measuring unfolded protein load and proteostasis in cells. TPE-MI can report imbalances in proteostasis in induced pluripotent stem cell models of Huntington disease, as well as cells transfected with mutant Huntington exon 1 before the formation of visible aggregates. TPE-MI also detects protein damage following dihydroartemisinin research of the malaria parasitesPlasmodium falciparum .
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- HY-144070
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Others
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Cancer
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ErSO-DFP is an anticipatory unfolded protein response (a-UPR) activator. ErSO-DFP has enhanced selectivity for estrogen receptor alpha-positive (ERα+) cancer cells with a wider selectivity window than ErSO.ErSO-DFP displays antitumor activity and leads to profound regression of MCF-7 tumors in mice model .
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- HY-139214
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IXA4
2 Publications Verification
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IRE1
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Neurological Disease
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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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- HY-N0225
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Epigallocatechin; L-Epigallocatechin
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MMP
Autophagy
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Cancer
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(-)-Epigallocatechin (Epigallocatechin) is the most abundant flavonoid in green tea, can bind to unfolded native polypeptides and prevent conversion to amyloid fibrils.
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- HY-D1781
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Fluorescent Dye
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Others
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NTPAN-MI is a fluorescent probe. NTPAN-MI is selectively activated upon labeling unfolded proteins with exposed thiols, thereby reporting on the extent of proteostasis .
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- HY-153474
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IRE1
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Others
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IRE1α kinase-IN-8, a benzoheterocyclecarboxaldehyde derivative, is a potent IRE-1α inhibitor. IRE1α kinase-IN-8 can be used for research in diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) .
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- HY-132247A
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Others
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Cancer
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(±)-ErSO is the racemate of ErSO. ErSO is a selective anticipatory unfolded protein response (a-UPR) activator .
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- HY-N0225R
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Epigallocatechin(Standard); L-Epigallocatechin (Standard)
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MMP
Autophagy
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Cancer
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(-)-Epigallocatechin (Standard) is the analytical standard of (-)-Epigallocatechin. This product is intended for research and analytical applications. (-)-Epigallocatechin (Epigallocatechin) is the most abundant flavonoid in green tea, can bind to unfolded native polypeptides and prevent conversion to amyloid fibrils.
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- HY-114410
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Mitochondrial Metabolism
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Cancer
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CCI-006 is a selective inhibitor and chemosensitizer of MLL-rearranged leukemia cells, by inhibits mitochondrial respiration resulting in insurmountable mitochondrial depolarization and a pro-apoptotic unfolded protein response (UPR) in a subset of MLL-r leukemia cells .
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- HY-28325
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Reactive Oxygen Species
p38 MAPK
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Cancer
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AMC-04 is an unfolded protein response (UPR) activator, which activates UPR pathway through ROS and p38 MAPK signaling and induces apoptotic cell death. AMC-04 can be used for cancer research .
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- HY-12825
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Estrogen Receptor/ERR
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Cancer
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BHPI is a potent inhibitor of nuclear estrogen–ERα-regulated gene expression; elicits sustained ERα-dependent activation of the endoplasmic reticulum (EnR) stress sensor, the unfolded protein response (UPR), and persistent inhibition of protein synthesis.
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- HY-133859
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Mitochondrial Metabolism
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Metabolic Disease
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M084 is a benzimidazole derivative. M084 inhibits the mitochondrial respiration, activate mitochondrial unfolded protein response and AMPK, recruites SIR-2.1 and SKN-1, and finally through the transcription factor DAF-16, delays the aging process of C. elegans .
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- HY-B0178A
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- HY-153475
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IRE1
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Cancer
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IRE1α kinase-IN-9 (compound 2) is a potent IRE-1α inhibitor,exhibits an average IC50 value of <0.1 μM. IRE1α kinase-IN-9 can be used for research in diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) .
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- HY-13433
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Calcium Channel
SARS-CoV
Apoptosis
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Infection
Cancer
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Thapsigargin, an endoplasmic reticulum (ER) stress inducer, is an inhibitor of microsomal Ca 2+-ATPase. Thapsigargin efficiently inhibits coronavirus (HCoV-229E, MERS-CoV, SARS-CoV-2) replication in different cell types .
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- HY-13547
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Apoptosis
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Cancer
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ADPM06, a lead candidate azadipyrromethene, is a novel nonporphyrin photodynamic therapeutic (PDT) agent. ADPM06 exhibits IC50 values in the micro-molar range in human tumor cells and induces apoptosis .
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- HY-112304A
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- HY-112304
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- HY-N12887
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Mitochondrial Metabolism
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Others
Cancer
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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 .
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- HY-A0098
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Tunicamycin
Maximum Cited Publications
92 Publications Verification
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Bacterial
Fungal
Influenza Virus
Antibiotic
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Infection
Inflammation/Immunology
Cancer
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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 .
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- HY-124293
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AA147
3 Publications Verification
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ATF6
Reactive Oxygen Species
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Neurological Disease
Metabolic Disease
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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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- HY-147039
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NKP-1339 free base; IT-139 free base; KP-1339 free base
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HSP
Autophagy
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Cancer
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BOLD-100 (NKP-1339; IT-139) free base is a ruthenium-based anticancer agent. BOLD-100 free base also is an inhibitor of stress-induced GRP78 upregulation, disrupting endoplasmic reticulum (ER) homeostasis and inducing ER stress and unfolded protein response (UPR). BOLD-100 free base interferes with the complex interplay between ER-stress response, lysosome dynamics, and autophagy execution .
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- HY-121337
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R-40244
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Apoptosis
Bcl-2 Family
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Others
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Flurochloridone (R-40244) is a selective preemergence and persistent herbicide. Flurochloridone induces endoplasmic reticulum (ER) stress and activated unfolded protein response (UPR) signaling pathways. Flurochloridone impairs cell viability and induces cytotoxicity and apoptosis mediated by ER stress via activating eIF2α-ATF4/ATF6-CHOP-Bim/Bax signaling pathways in TM4 cells .
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- HY-136528
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Deubiquitinase
Apoptosis
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Cancer
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RA-9 is a potent and selective proteasome-associated deubiquitinating enzymes (DUBs) inhibitor with favorable toxicity profile and anticancer activity. RA-9 blocks ubiquitin-dependent protein degradation without impacting 20S proteasome proteolytic activity. RA-9 selectively induces onset of apoptosis in ovarian cancer cell lines and primary cultures derived from donors. RA-9 induces endoplasmic reticulum (ER)-stress responses in ovarian cancer cells .
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- HY-121337R
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Apoptosis
Bcl-2 Family
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Others
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Flurochloridone (Standard) is the analytical standard of Flurochloridone. This product is intended for research and analytical applications. Flurochloridone (R-40244) is a selective preemergence and persistent herbicide. Flurochloridone induces endoplasmic reticulum (ER) stress and activated unfolded protein response (UPR) signaling pathways. Flurochloridone impairs cell viability and induces cytotoxicity and apoptosis mediated by ER stress via activating eIF2α-ATF4/ATF6-CHOP-Bim/Bax signaling pathways in TM4 cells .
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- HY-145418
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IRE1
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Others
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IRE1α kinase-IN-3 (compound 2) is a potent IRE1α inhibitor with an Ki of 480 nM. IRE1α kinase-IN-3 is the ATP-competitive ligands of IRE1α .
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- HY-145419
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IRE1
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Others
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IRE1α kinase-IN-4 (compound 6) is a potent IRE1α inhibitor with an Ki of 140 nM. IRE1α kinase-IN-4 is the ATP-competitive ligands of IRE1α .
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- HY-145420
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IRE1
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Others
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IRE1α kinase-IN-5 (compound 7) is a potent IRE1α inhibitor with an Ki of 98 nM. IRE1α kinase-IN-5 is the ATP-competitive ligands of IRE1α .
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- HY-109076
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EBC-46
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PKC
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Cancer
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Tigilanol tiglate (EBC-46) is a protein kinase C (PKC)/C1 domain activator. Tigilanol tiglate is a natural product with antitumor activity used for local administration against a variety of skin malignancies. Tigilanol tiglate is associated with mitochondrial/endoplasmic reticulum (ER) dysfunction, leading to activation of the unfolded protein response (UPRmt/ER) and subsequent induction of ATP depletion, organelles expansion, caspase activation, gasdermin E cleavage, and terminal necrosis. Tigilanol tiglate, as a small anti-tumor molecule with immunomodulatory effects, can be used in the study of head and neck squamous cell carcinoma and soft tissue sarcoma .
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- HY-167701
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Others
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Cancer
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OBHSA is a selective estrogen receptor degrader (SERD) with specific degradation activity against estrogen receptor α (ERα). OBHSA has a significant inhibitory effect on the proliferation of various breast cancer cells, including tamoxifen-sensitive and drug-resistant breast cancer cells. OBHSA blocks the cell cycle by degrading cyclin D1, thereby overcoming tamoxifen resistance. OBHSA also triggers excessive activation of the unfolded protein response (UPR) by inducing an increase in intracellular reactive oxygen species, ultimately leading to cell apoptosis. OBHSA shows great potential in the development of novel inhibitory drugs against endocrine-resistant breast cancer .
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- HY-145422
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IRE1
Apoptosis
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Others
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KIRA9 is a potent IRE1 inhibitor (IC50=4.8 μM in INS-1 cells). KIRA9 is able to fully engage the ATP-binding site of IRE1α. KIRA9 can block ER-localized mRNA decay and apoptosis .
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- HY-108434
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ATF6
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Neurological Disease
Metabolic Disease
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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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- HY-115445
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LCS-1
1 Publications Verification
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Apoptosis
SOD
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Cancer
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LCS-1 is a superoxide dismutase 1 (SOD1) inhibitor. LCS-1 inhibits SOD1 activity with an IC50 value of 1.07 μM. LCS-1 induces the early- and late-stage apoptosis of multiple myeloma (MM.1S) cells .
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- HY-111297
-
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Others
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Cancer
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BMVC4 is a G-quadruplex (G4) stabilizer of the human telomeric sequence d[AG3(T2AG3)3]. Screening by circular dichroism (CD) spectroscopy revealed that BMVC4 is more suitable as the core molecule of G4 stabilizers than BMVC. The results showed that BMVC4-12C and BMVC4-8C3O are better candidates for G4 stabilizers and are worthy of further study. A simple and rapid screening method based on Cu2+-induced G4 unfolding can be used to find better G4 stabilizers for potential anticancer applications. CD results showed that the trivalent cations of 9-substituted BMVC derivatives are more suitable as G4 stabilizers than the divalent cations of BMVC. In addition, by monitoring the disappearance of the 291 nm CD band of human telomeres after Cu2+ addition, it was found that the core molecule of G4 stabilizer BMVC4 has better stability.
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HY-L054
-
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227 compounds
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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 227 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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Cat. No. |
Product Name |
Type |
-
- HY-143218
-
TPE-MI
2 Publications Verification
Tetraphenylethene maleimide
|
Fluorescent Dyes/Probes
|
TPE-MI (Tetraphenylethene maleimide) is a thiol probe for measuring unfolded protein load and proteostasis in cells. TPE-MI can report imbalances in proteostasis in induced pluripotent stem cell models of Huntington disease, as well as cells transfected with mutant Huntington exon 1 before the formation of visible aggregates. TPE-MI also detects protein damage following dihydroartemisinin research of the malaria parasitesPlasmodium falciparum .
|
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- HY-D1781
-
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Fluorescent Dyes/Probes
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NTPAN-MI is a fluorescent probe. NTPAN-MI is selectively activated upon labeling unfolded proteins with exposed thiols, thereby reporting on the extent of proteostasis .
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Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-129960
-
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Peptides
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Others
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L-Selenocystine is a diselenide-bridged amino acid. L-Selenocystine is a redox-active selenium compound that has both anti- and pro-oxidant actions. L-Selenocystine induces an unfolded protein response, ER stress, and large cytoplasmic vacuolization in HeLa cells and has cytostatic effects in a range of cancer cell types .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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