Search Result
Results for "
ER signaling
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-100487
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TAK-243
Maximum Cited Publications
83 Publications Verification
MLN7243
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E1/E2/E3 Enzyme
NF-κB
Apoptosis
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Cancer
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TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis .
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- HY-158101
-
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CC-94676
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PROTACs
Androgen Receptor
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Cancer
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BMS-986365 (CC-94676) is an orally active and selective targeted androgen receptor (AR) PROTAC degrader (DC50 of 10-40 nM). BMS-986365 is capable of inducing cereblon (CRBN) E3 ligase-dependent ubiquitination and degradation of the androgen receptor (AR), as well as various AR mutants. BMS-986365 shows no degradation of the close AR family members estrogen receptor (ER), progesterone receptor (PR), and glucocorticoid receptor (GR). BMS-986365 shows significant in vivo potency, degrading AR, inhibiting AR signaling, and restricting tumor growth in animal models of advanced prostate cancer. BMS-986365 can be used for the study of metastatic castration-resistant prostate cancer (mCRPC) .
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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-18705
-
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Apoptosis
Reactive Oxygen Species (ROS)
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-15483
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DY131
3 Publications Verification
GSK 9089
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Estrogen Receptor/ERR
Smo
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Endocrinology
Cancer
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DY131 (GSK 9089) is a potent and selective ERRγ and ERRβ agonist. DY131displays inactive against ERRα, ERα and ERβ . DY131 also inhibits Smo signaling .
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- HY-N16308
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Fluorescent Dye
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Others
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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-14933
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ERB-041
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Estrogen Receptor/ERR
Wnt
Apoptosis
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Cancer
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Prinaberel (ERB-041) is a potent and selective estrogen receptor (ER) β agonist with IC50s of 5.4, 3.1 and 3.7 nM for human, rat and mouse ERβ, respectively. Prinaberel displays >200-fold selectivity for ERβ over ERα. Prinaberel is a potent skin cancer chemopreventive agent that acts by dampening the WNT/β-catenin signaling pathway. Prinaberel induces ovarian cancer apoptosis .
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- HY-12724
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Adrenergic Receptor
Parasite
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Cardiovascular Disease
Cancer
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Guanabenz is an orally active α-2-adrenoceptor agonist. Guanabenz has antihypertensive effect and antiparasitic activity. Guanabenz interferes ER stress-signalling and has protective effects in cardiac myocytes. Guanabenz also is used for the research of high blood pressure .
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- HY-134809
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CADA
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HIV
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Infection
Inflammation/Immunology
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Cyclotriazadisulfonamide (CADA) is a specific CD4-targeted HIV entry inhibitors. Cyclotriazadisulfonamide (CADA) inhibits the co-translational translocation of human CD4 (huCD4) into the ER lumen in a signal peptide (SP)-dependent way. Cyclotriazadisulfonamide is also a Sec61 translocon inhibitor .
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- HY-116572A
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Reactive Oxygen Species (ROS)
JNK
Apoptosis
Caspase
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Cancer
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TASIN-1 is a selective inhibitor of truncated APC TR (adenomatous polyposis coli gene) that exerts cytotoxic effects by inhibiting cholesterol biosynthesis. TASIN-1 specifically targets colorectal cancer (CRC) cells carrying APC truncated mutations, while having no significant toxicity to wild-type APC cells. TASIN-1 exerts cytotoxic effects by targeting Emopamil binding protein (EBP) to inhibit cholesterol biosynthesis, triggering endoplasmic reticulum (ER) stress, reactive oxygen species (ROS) generation, and JNK-mediated apoptosis, and inhibiting Akt survival signaling. TASIN-1 can be used to prevent and intervene in APC mutant colorectal cancer .
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- HY-121410
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Narasin
2 Publications Verification
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Bacterial
Apoptosis
Parasite
NF-κB
Antibiotic
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Infection
Cancer
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Narasin is a cationic ionophore antibiotic and coccidiostat agent. Narasin inhibits NF-κB signaling and induces tumor cells apoptosis. Narasin has antimicrobial, antiviral anticancer activity. Narasin inhibits tumor metastasis and growth of ERα‑positive breast cancer cells by inactivation of the TGF-β/SMAD3 and IL‑6/STAT3 signaling pathways .
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- HY-W010451
-
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Hydroxyhydroquinone
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PERK
Eukaryotic Initiation Factor (eIF)
Potassium Channel
Apoptosis
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Cardiovascular Disease
Cancer
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1,2,4-Trihydroxybenzene (Hydroxyhydroquinone) is an ER stress inducer that targets proteins such as PKR-like ER kinase PERK to induce cytotoxicity. 1,2,4-Trihydroxybenzene selectively activates eIF2α phosphorylation, activates the PERK-eIF2α signaling pathway and induces stress granule formation. 1,2,4-Trihydroxybenzene subsequently exacerbates oxidative stress and causes DNA double-strand breaks, destroying organelles such as mitochondria and ER, and inducing cell death. 1,2,4-Trihydroxybenzene also has the potential to exhibit anti-tumor effect, increase blood pressure, and relieve spasm .
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- HY-12724A
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Parasite
Adrenergic Receptor
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Cardiovascular Disease
Cancer
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Guanabenz hydrochloride is an orally active α-2-adrenoceptor agonist. Guanabenz hydrochloride has antihypertensive effect and antiparasitic activity. Guanabenz hydrochloride interferes ER stress-signalling and has protective effects in cardiac myocytes. Guanabenz hydrochloride also is used for the research of high blood pressure .
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- HY-126066
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- HY-110193
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SPP-86
2 Publications Verification
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RET
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Cancer
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SPP-86 is a potent and selective cell permeable inhibitor of RET tyrosine kinase, with an IC50 of 8 nM. SPP-86 inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells . SPP-86 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-N0910
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- HY-13636A
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ICI 182780 (S enantiomER); ZD 9238 (S enantiomER); ZM 182780 (S enantiomER)
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Drug Isomer
Estrogen Receptor/ERR
p38 MAPK
Apoptosis
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Cancer
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Fulvestrant (ICI 182780; ZD 9238) S enantiomer is the S-enantiomer of Fulvestrant (HY-13636), a potent estrogen receptor inhibitor. Fulvestrant binds to and blocks the estrogen receptor, promotes its degradation, and thereby inhibits receptor dimerization, nucleocytoplasmic shuttling and transcriptional activity. Fulvestrant effectively blocks estrogen signaling, MAPK pathway activation and ER-regulated protein expression. Fulvestrant induces apoptosis, inhibits the proliferation of breast cancer and prolactinoma cells, and reduces the mineralization level, alkaline phosphatase activity and osteocalcin expression of preosteoblasts. Prenatal exposure to Fulvestrant impairs ovarian follicular development and causes ovarian structural damage. Fulvestrant has been widely used in studies related to breast cancer, prolactinoma and other conditions .
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- HY-121337
-
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R-40244
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Environmental Pollutants
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-112903A
-
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Protein Arginine Deiminase
MDM-2/p53
PERK
mTOR
Autophagy
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Cancer
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YW3-56 (hydrochloride) is a PAD inhibitor. YW3-56 (hydrochloride) activates p53 target genes. YW3-56 (hydrochloride) activates ATF and blocks autophagy flux. YW3-56 induces ER stress through the PERK-eIF2α-ATF4 signaling cascade and inhibits the mTOR signaling. YW3-56 (hydrochloride) inhibits triple-negative breast cancer .
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- HY-13559
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Azaspirane ; SKF 106615-12; SKF 106615A12
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STAT
Apoptosis
Autophagy
Reactive Oxygen Species (ROS)
Caspase
Bcl-2 Family
p62
Atg8/LC3
PARP
NF-κB
PERK
JAK
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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Atiprimod (Azaspirane) is a STAT3 inhibitor with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of IL-6 and VEGF by inhibiting the phosphorylation of signal transducer and activator of STAT3. Atiprimod blocks the JAK-STAT signaling pathway by inhibiting the phosphorylation of JAK2 and JAK3. Atiprimod also inhibits cell proliferation, induces cell cycle arrest, and induces autophagy and apoptosis. Atiprimod triggers persistent ER stress-mediated apoptosis in breast cancer cells by activating the PERK/eIF2α/ATF4/CHOP axis and inhibiting the nuclear translocation of STAT3/NF-κB. Atiprimod shows great anti-tumor activities in tumor xenograft mouse models. Atiprimod can be used for the study of pituitary adenoma, breast cancer, multiple myeloma and acute myeloid leukemia (AML) .
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- HY-179433
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PROTACs
Androgen Receptor
Estrogen Receptor/ERR
Src
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Cancer
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PROTAC AR Degrader-12 is a highly efficient PROTAC targeting AR coactivator binding site (AR-CBS). PROTAC AR Degrader-12 induces AR degradation in a ubiquitin proteasome system (UPS) pathway-dependent manner. PROTAC AR Degrader-12 inhibits tumor cell growth by affecting DNA replication and cell division PROTAC AR Degrader-12 could not only effectively degrade AR, but also potently inhibit the proliferation of MCF-7 and multiple mutant or resistant BC cells. PROTAC AR Degrader-12 effectively blocked estrogen receptor α (ERα) signaling through a dual mechanism involving ERα protein downregulation and suppression of its transcriptional activity. PROTAC AR Degrader-12 significantly inhibits the mRNA expression of FOXA1, GREB1, SRC, and PELP1. PROTAC AR Degrader-12 can be used for the study of breast cancer .
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- HY-P1556
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PKG
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Cardiovascular Disease
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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-130133
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PI3K
mTOR
Akt
Apoptosis
Paraptosis
p38 MAPK
Mitochondrial Metabolism
P-glycoprotein
CDK
MMP
HIF/HIF Prolyl-Hydroxylase
VEGFR
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Cancer
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DHW-221 is a potent orally active dual PI3K/mTOR inhibitor, exhibiting low nanomolar potency against all four Class I PI3K isoforms and mTOR (PI3Kα, IC50 = 0.50 nM; PI3Kβ, IC50 = 1.9 nM; PI3Kγ, IC50 = 1.8 nM; PI3Kδ, IC50 = 0.74 nM; mTOR, IC50 = 3.9 nM). DHW-221 exerts antitumor effects by blocking the PI3K/Akt/mTOR pathway and inducing mitochondrial apoptosis and paraptosis (via Endoplasmic Reticulum (ER) stress and MAPK signaling) and arrests cell cycle, thereby inhibiting cell migration, invasion and angiogenesis. DHW-221 inhibits tumor growth in both the A549/Taxol (HY-B0015) and the HCC827 xenograft mouse models. DHW-221 can be used for non-small cell lung cancer (NSCLC), colon and breast cancer research .
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- HY-153761
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- HY-175348
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- HY-176225
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PROTACs
Src
Estrogen Receptor/ERR
Apoptosis
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Cancer
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BY13 is a SRC-3 PROTAC degrader with a DC50 of 0.031 μM. BY13 selectively blocks the ER signaling pathway over that of androgen receptor (AR)) through down-regulating ERα level. BY13 potently overcomes endocrine resistance in breast cancer by inducing cell cycle arrest in G1 phase and apoptosis, with superior effect over Fulvestrant (HY-13636). BY13 significantly inhibits the growth of drug-resistant breast tumors without obvious toxicity in LCC2 xenograft mice model . Pink: SRC-3 ligand (SI-2) (HY-101447); Blue: CRBN ligase ligand (HY-41547); Black: linker (HY-176226)
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- HY-13559A
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Azaspirane dimaleate; SKF 106615-12 dimaleate; SKF 106615A12 dimaleate
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STAT
Apoptosis
Caspase
Interleukin Related
Autophagy
Reactive Oxygen Species (ROS)
Atg8/LC3
p62
JAK
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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Atiprimod (Azaspirane) (dimaleate) is a STAT3 inhibitor with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of IL-6 and VEGF by inhibiting the phosphorylation of signal transducer and activator of STAT3. Atiprimod blocks the JAK-STAT signaling pathway by inhibiting the phosphorylation of JAK2 and JAK3. Atiprimod also inhibits cell proliferation, induces cell cycle arrest, and induces autophagy and apoptosis. Atiprimod triggers persistent ER stress-mediated apoptosis in breast cancer cells by activating the PERK/eIF2α/ATF4/CHOP axis and inhibiting the nuclear translocation of STAT3/NF-κB. Atiprimod shows great anti-tumor activities in tumor xenograft mouse models. Atiprimod can be used for the study of pituitary adenoma, breast cancer, multiple myeloma and acute myeloid leukemia (AML) .
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- HY-110102
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Azaspirane hydrochloride; SKF 106615-12 hydrochloride; SKF 106615
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JAK
STAT
Apoptosis
Autophagy
Reactive Oxygen Species (ROS)
Caspase
Atg8/LC3
p62
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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Atiprimod (Azaspirane) hydrochloride is a STAT3 inhibitor with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of IL-6 and VEGF by inhibiting the phosphorylation of signal transducer and activator of STAT3. Atiprimod blocks the JAK-STAT signaling pathway by inhibiting the phosphorylation of JAK2 and JAK3. Atiprimod also inhibits cell proliferation, induces cell cycle arrest, and induces autophagy and apoptosis. Atiprimod triggers persistent ER stress-mediated apoptosis in breast cancer cells by activating the PERK/eIF2α/ATF4/CHOP axis and inhibiting the nuclear translocation of STAT3/NF-κB. Atiprimod shows great anti-tumor activities in tumor xenograft mouse models. Atiprimod can be used for the study of pituitary adenoma, breast cancer, multiple myeloma and acute myeloid leukemia (AML) .
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- HY-121033
-
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Sigma Receptor
p38 MAPK
Apoptosis
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Cancer
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BS148 is a selective sigma-2 receptor (S2R) agonist with a Ki 20 nM. BS148 shows >80-fold selective for S2R than S1R. BS148 activates the endoplasmic reticulum stress response through the upregulation of protein kinase R-like ER kinase (PERK), activating transcription factor 4 (ATF4) genes, and C/EBP homologous protein (CHOP). BS148 induces apoptosis in melanoma cell. BS148 downregulates genes related to the cholesterol pathway and activates the MAPK signaling pathway. BS148 can be used for the study of melanoma .
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- HY-116572
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Reactive Oxygen Species (ROS)
JNK
Apoptosis
Caspase
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Cancer
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TASIN-1 hydrochloride is a selective inhibitor of truncated APC TR (adenomatous polyposis coli gene) that exerts cytotoxic effects by inhibiting cholesterol biosynthesis. TASIN-1 hydrochloride specifically targets colorectal cancer (CRC) cells carrying APC truncated mutations, while having no significant toxicity to wild-type APC cells. TASIN-1 hydrochloride exerts cytotoxic effects by targeting Emopamil binding protein (EBP) to inhibit cholesterol biosynthesis, triggering endoplasmic reticulum (ER) stress, reactive oxygen species (ROS) generation, and JNK-mediated apoptosis, and inhibiting Akt survival signaling. TASIN-1 hydrochloride can be used to prevent and intervene in APC mutant colorectal cancer .
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- HY-173474
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Estrogen Receptor/ERR
Androgen Receptor
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Cancer
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ERβ agonist-1 (Compound 8) is a dual-active selective ERβ agonist (EC50: 46.8 nM) and AR antagonist (IC50: 1555 nM). ERβ agonist-1 activates ERβ signaling by binding to ERβ and inhibits AR activity. ERβ agonist-1 retains selective ERβ agonist activity in mouse models and can be used to study prostate cancer .
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- HY-142926
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Estrogen Receptor/ERR
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Cancer
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ER degrader 2 is a potent degrader of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. ER degrader 2 has the potential for the research of cancer diseases (extracted from patent CN112830919A, compound 1) .
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- HY-142925
-
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Estrogen Receptor/ERR
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Cancer
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ER degrader 1 is a potent degrader of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. ER degrader 1 has the potential for the research of cancer diseases (extracted from patent WO2021139756A1, compound 11) .
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- HY-142927
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Estrogen Receptor/ERR
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Cancer
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ER degrader 3 is a potent degrader of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. ER degrader 3 has the potential for the research of cancer diseases (extracted from patent WO2018233591A1, compound 1) .
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- HY-P10393
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ERα (295-311)
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Apoptosis
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Cancer
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ERα17p (ERα 295-311) is the epitope of the CaM binding site on the estrogen receptor α (ER), which interacts with calmodulin (CaM) in a calcium-dependent manner. ERα17p regulates the migration of cancer cells MCF-7, SK-BR-3, T47D, and MDA-MB-231 through Rho/ROCK and PI3K/Akt signaling pathways. ERα17p inhibits proliferations of breast cancer cells, induces apoptosis, and inhibits tumor growth in mouse models .
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- HY-167838
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ERK
Akt
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Others
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Coelogin is an orally active osteoprotective agent which activates the ER-Erk and Akt-dependent signaling pathways that stimulate the osteoblastogenesis in osteoblast cells. Coelogin can be utilized in osteoporosis research .
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- HY-121337R
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R-40244 (Standard)
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Reference Standards
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-167868
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TRP Channel
Apoptosis
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Neurological Disease
Cancer
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DWP-05195 is a TRPV1 antagonist that can inhibit the pain signal transduction. DWP-05195 induces ER stress-dependent apoptosis through the ROS-p38-CHOP pathway in human ovarian cancer cells .
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- HY-144139
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Estrogen Receptor/ERR
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Cancer
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Estrogen receptor antagonist 3 is a potent antagonist of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. Estrogen receptor antagonist 3 has the potential for the research of cancer diseases (extracted from patent WO2021213358A1, compound 7) .
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- HY-144202
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Estrogen Receptor/ERR
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Cancer
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Estrogen receptor antagonist 4 is a potent antagonist of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. Estrogen receptor antagonist 4 has the potential for the research of cancer diseases (extracted from patent WO2021213358A1, compound 1) .
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- HY-W010451R
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Hydroxyhydroquinone (Standard)
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Reference Standards
PERK
Potassium Channel
Apoptosis
Eukaryotic Initiation Factor (eIF)
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Cardiovascular Disease
Cancer
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1,2,4-Trihydroxybenzene (Hydroxyhydroquinone) (Standard) is the analytical standard of 1,2,4-Trihydroxybenzene (HY-W010451). This product is intended for research and analytical applications. 1,2,4-Trihydroxybenzene (Hydroxyhydroquinone) is an ER stress inducer that targets proteins such as PKR-like ER kinase PERK to induce cytotoxicity. 1,2,4-Trihydroxybenzene selectively activates eIF2α phosphorylation, activates the PERK-eIF2α signaling pathway and induces stress granule formation. 1,2,4-Trihydroxybenzene subsequently exacerbates oxidative stress and causes DNA double-strand breaks, destroying organelles such as mitochondria and ER, and inducing cell death. 1,2,4-Trihydroxybenzene also has the potential to exhibit anti-tumor effect, increase blood pressure, and relieve spasm .
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- HY-12724AR
-
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Parasite
Adrenergic Receptor
Reference Standards
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Cardiovascular Disease
Cancer
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Guanabenz (hydrochloride) (Standard) is the analytical standard of Guanabenz (hydrochloride). This product is intended for research and analytical applications. Guanabenz hydrochloride is an orally active α-2-adrenoceptor agonist. Guanabenz hydrochloride has antihypertensive effect and antiparasitic activity. Guanabenz hydrochloride interferes ER stress-signalling and has protective effects in cardiac myocytes. Guanabenz hydrochloride also is used for the research of high blood pressure .
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- HY-P1556A
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PKG
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Metabolic Disease
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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-170849
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Nuclear Hormone Receptor 4A/NR4A
Apoptosis
PERK
IRE1
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Cancer
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Nur77 modulator 4 (Compound 15h) is a Nur77 inducer with a KD of 0.477 μM. Nur77 modulator 4 significantly induces Nur77 expression and apoptosis, showing excellent growth inhibition in HepG2 and MCF-7 cells, with an IC50 of less than 5 μM. Nur77 modulator 4 activates Nur77-mediated ER stress through the PERK-ATF4 and IRE1 signaling pathways, thereby inducing cell apoptosis. Nur77 modulator 4 can be used in cancer research applications .
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- HY-108514
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Sigma Receptor
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Neurological Disease
Cancer
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(±)-PPCC hemioxalate is a compound that has the ability to regulate the activity of the sigma-1 receptor. (±)-PPCC hemioxalate can selectively bind sigma-1 protein (s1), and then activate s1 receptor leading to dissociation of s1-BIP complex to regulate ER-mitochondrial calcium signaling, which plays an important role in cell bioenergy and cell survival. (±)-PPCC hemioxalate can be used to study sigma-1 receptors in cocaine addiction, forgetting, pain, depression, Alzheimer's disease, stroke, and cancer .
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- HY-161874
-
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Apoptosis
MDM-2/p53
Bcl-2 Family
Caspase
PARP
Autophagy
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Cancer
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RPS6-IN-1 (Compound 22o) inhibits cell metastasis, induces cell apoptosis (increases the expression of Bax, p53, cleaved-caspase 3, and cleaved-PARP). RPS6-IN-1 decreases mitochondrial membrane potential. RPS6-IN-1 activates autophagy through the PI3K-Akt-mTOR signaling pathway, damages intracellular mitochondria and lysosomes, and cause ER stress. RPS6-IN-1 inhibits RPS6 phosphorylation. RPS6-IN-1 is an anticancer agent with low systemic toxicity .
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- HY-181172
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Estrogen Receptor/ERR
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Cancer
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FRAGHIT-4 is an estrogen receptor alpha (ERα) inhibitor. FRAGHIT-4 exhibits antineoplastic activity against breast cancer via targeting ER signaling. FRAGHIT-4 can be used for the research of breast cancer .
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- HY-179510
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Estrogen Receptor/ERR
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Cancer
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CDD-1274 is an ERα (Estrogen receptor α) variant inhibitor. CDD-1274 induces proteasomal degradation of ERα variants in breast cancer cell lines and causes Y537S ERα degradation. CDD-1274 potently blocks ligand-dependent and ligand-independent ER signaling in endocrine-resistant breast cancer cells. CDD-1274 can be used for the study of breast cancer .
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- HY-P2674
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MHC
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Inflammation/Immunology
Cancer
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KDEL is a tetrapeptide serving as an endoplasmic reticulum (ER) retrieval/retention signal. KDEL can target and deliver exogenous antigen peptides to the ER, significantly enhance and prolong MHC class I molecule presentation, and effectively boost anti-tumor immune responses .
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- HY-181171
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Estrogen Receptor/ERR
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Cancer
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HIT-2 is an estrogen receptor alpha (ERα) inhibitor that can bind to the ERα ligand binding domain. HIT-2 forms stable interactions including hydrogen bonds, π-π stacking, and hydrophobic contacts to disrupt ERα-driven signaling. HIT-2 exhibits antineoplastic activity against breast cancer. HIT-2 can be used for the research of breast cancer .
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- HY-182674
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Sec61
HIV
Flavivirus
Neurotensin Receptor
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Infection
Cancer
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VGD020 is a highly potent and selective Sec61 translocon inhibitor . VGD020 suppresses the expression of cell surface CD4 by inhibiting signal peptide-dependent co-translational ER translocation, interferes with the initiation of ER translocation of dengue virus polyprotein, and reduces the expression of Sortilin in breast cancer cells. VGD020 exhibits broad anti-flavivirus and anti-HIV activities. VGD020 can be used in research related to dengue virus infection, Zika virus infection, yellow fever virus infection, human immunodeficiency virus infection, and breast cancer .
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- HY-108434R
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Reference Standards
ATF6
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Neurological Disease
Metabolic Disease
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Ceapin-A7 (Standard) is the analytical standard of Ceapin-A7 (HY-108434). This product is intended for research and analytical applications. 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-D2925
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dTCO-SNAP
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Biochemical Assay Reagents
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Others
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dTCOBG (dTCO-SNAP) is a SNAP-tag reactive benzylguanine (BG) analogue specifically designed for the specific labeling of immune cells. dTCOBG forms a stable thioether bond through the cysteine at the active site of SNAP-tag and O6-benzylguanine, resulting in a covalent linkage. dTCOBG demonstrates unique advantages in the labeling of macrophages derived from ER-HoxB8: it only labels SNAP-tag + macrophages, with no background signal in the control group. dTCOBG can be used for click chemistry labeling .
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- HY-100487R
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MLN7243 (Standard)
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E1/E2/E3 Enzyme
Reference Standards
NF-κB
Apoptosis
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Cancer
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TAK-243 (Standard) is the analytical standard of TAK-243 (HY-100487). This product is intended for research and analytical applications. TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis .
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- HY-12292G
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NF-κB
STAT
GSK-3
β-catenin
Bcr-Abl
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Cancer
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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, Ca 2+ release, autophagy and apoptosis. IM-12 is heat-sensitive and does not induce autophagy in IM-resistant p210BCR/ABL T315I 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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-
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HY-L054
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356 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 356 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 |
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- HY-D2925
-
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dTCO-SNAP
|
Fluorescent Dyes
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dTCOBG (dTCO-SNAP) is a SNAP-tag reactive benzylguanine (BG) analogue specifically designed for the specific labeling of immune cells. dTCOBG forms a stable thioether bond through the cysteine at the active site of SNAP-tag and O6-benzylguanine, resulting in a covalent linkage. dTCOBG demonstrates unique advantages in the labeling of macrophages derived from ER-HoxB8: it only labels SNAP-tag + macrophages, with no background signal in the control group. dTCOBG can be used for click chemistry labeling .
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- HY-12292G
-
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Fluorescent Dyes
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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, Ca 2+ release, autophagy and apoptosis. IM-12 is heat-sensitive and does not induce autophagy in IM-resistant p210BCR/ABL T315I 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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| Cat. No. |
Product Name |
Type |
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- HY-12292G
-
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Biochemical Assay Reagents
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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, Ca 2+ release, autophagy and apoptosis. IM-12 is heat-sensitive and does not induce autophagy in IM-resistant p210BCR/ABL T315I 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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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P1556
-
|
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PKG
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Cardiovascular Disease
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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-P10393
-
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ERα (295-311)
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Apoptosis
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Cancer
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ERα17p (ERα 295-311) is the epitope of the CaM binding site on the estrogen receptor α (ER), which interacts with calmodulin (CaM) in a calcium-dependent manner. ERα17p regulates the migration of cancer cells MCF-7, SK-BR-3, T47D, and MDA-MB-231 through Rho/ROCK and PI3K/Akt signaling pathways. ERα17p inhibits proliferations of breast cancer cells, induces apoptosis, and inhibits tumor growth in mouse models .
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- HY-P10477
-
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Peptides
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Cancer
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CT-08 (CT8, Compound 3) is a macrocyclic Sec61 modulator, blocks protein secretion in a signal sequence-dependent manner. CT-08 blocks Sec61-mediated translocation of VCAMss-GLuc into the ER, resulting in a loss of luciferase activity. CT-08 inhibits VCAM expression in transfected cells .
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- HY-P1556A
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PKG
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Metabolic Disease
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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-P2674
-
|
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MHC
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Inflammation/Immunology
Cancer
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|
KDEL is a tetrapeptide serving as an endoplasmic reticulum (ER) retrieval/retention signal. KDEL can target and deliver exogenous antigen peptides to the ER, significantly enhance and prolong MHC class I molecule presentation, and effectively boost anti-tumor immune responses .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-N16308
-
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Structural Classification
Lipid
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Fluorescent Dye
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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-W010451
-
|
Hydroxyhydroquinone
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Cardiovascular Disease
Microorganisms
Classification of Application Fields
Phenols
Polyphenols
Disease Research Fields
Source Classification
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PERK
Eukaryotic Initiation Factor (eIF)
Potassium Channel
Apoptosis
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|
1,2,4-Trihydroxybenzene (Hydroxyhydroquinone) is an ER stress inducer that targets proteins such as PKR-like ER kinase PERK to induce cytotoxicity. 1,2,4-Trihydroxybenzene selectively activates eIF2α phosphorylation, activates the PERK-eIF2α signaling pathway and induces stress granule formation. 1,2,4-Trihydroxybenzene subsequently exacerbates oxidative stress and causes DNA double-strand breaks, destroying organelles such as mitochondria and ER, and inducing cell death. 1,2,4-Trihydroxybenzene also has the potential to exhibit anti-tumor effect, increase blood pressure, and relieve spasm .
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-
- HY-126066
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-
-
- HY-N0910
-
-
-
- HY-W010451R
-
|
Hydroxyhydroquinone (Standard)
|
Structural Classification
Microorganisms
Phenols
Polyphenols
Source Classification
|
Reference Standards
PERK
Potassium Channel
Apoptosis
Eukaryotic Initiation Factor (eIF)
|
|
1,2,4-Trihydroxybenzene (Hydroxyhydroquinone) (Standard) is the analytical standard of 1,2,4-Trihydroxybenzene (HY-W010451). This product is intended for research and analytical applications. 1,2,4-Trihydroxybenzene (Hydroxyhydroquinone) is an ER stress inducer that targets proteins such as PKR-like ER kinase PERK to induce cytotoxicity. 1,2,4-Trihydroxybenzene selectively activates eIF2α phosphorylation, activates the PERK-eIF2α signaling pathway and induces stress granule formation. 1,2,4-Trihydroxybenzene subsequently exacerbates oxidative stress and causes DNA double-strand breaks, destroying organelles such as mitochondria and ER, and inducing cell death. 1,2,4-Trihydroxybenzene also has the potential to exhibit anti-tumor effect, increase blood pressure, and relieve spasm .
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-
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-12292G
-
|
|
NF-κB
STAT
GSK-3
β-catenin
Bcr-Abl
|
Cancer
|
|
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, Ca 2+ release, autophagy and apoptosis. IM-12 is heat-sensitive and does not induce autophagy in IM-resistant p210BCR/ABL T315I 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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