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Results for "

Unfolded protein response

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (9) ATF6 (2) Autophagy (1) Bcl-2 Family (3) Calcium Channel (1) Caspase (1) Deubiquitinase (1) Estrogen Receptor/ERR (1) Eukaryotic Initiation Factor (eIF) (1) Histone Demethylase (2) HSP (1) IRE1 (7) Mitochondrial Metabolism (4) p38 MAPK (1) PERK (1) PKC (1) Reactive Oxygen Species (3) SARS-CoV (1) SOD (1)
By Research Areas:	Cancer (16) Endocrinology (1) Infection (1) Metabolic Disease (3) Neurological Disease (3)

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-132247

ErSO	Others	Cancer
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 .

HY-18705

Azoramide 5 Publications Verification	Apoptosis Reactive Oxygen Species Caspase Bcl-2 Family Mitochondrial Metabolism	Endocrinology
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 .

HY-139214

IXA4 2 Publications Verification	IRE1	Neurological Disease
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 .

HY-101991

ML291	PERK Eukaryotic Initiation Factor (eIF) Apoptosis	Cancer
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 .

HY-144070

ErSO-DFP	Others	Cancer
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 .

HY-12825

BHPI	Estrogen Receptor/ERR	Cancer
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.

HY-114410

CCI-006	Mitochondrial Metabolism	Cancer
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 .

HY-153474

IRE1α kinase-IN-8	IRE1	Others
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) .

HY-132247A

(±)-ErSO	Others	Cancer
(±)-ErSO is the racemate of ErSO. ErSO is a selective anticipatory unfolded protein response (a-UPR) activator .

HY-28325

AMC-04	Reactive Oxygen Species p38 MAPK	Cancer
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 .

HY-13433

Thapsigargin Maximum Cited Publications 67 Publications Verification	Calcium Channel SARS-CoV Apoptosis	Infection Cancer
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 .

HY-13547

ADPM06	Apoptosis	Cancer
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 .

HY-112304A

(1R,2S)-NCD38 TFA	Histone Demethylase	Others
(1R,2S)-NCD38 TFA is an enantiomer of NCD38 TFA. NCD38 TFA is a LSD1-selective inhibitor .

HY-112304

NCD38 TFA	Histone Demethylase	Others
NCD38 TFA is a LSD1-selective inhibitor .

HY-133859

M084	Mitochondrial Metabolism	Metabolic Disease
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 .

HY-N12887

Mycothiazole	Mitochondrial Metabolism	Others Cancer
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 .

HY-124293

AA147 3 Publications Verification	ATF6 Reactive Oxygen Species	Neurological Disease Metabolic Disease
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 .

HY-147039

BOLD-100 free base NKP-1339 free base; IT-139 free base; KP-1339 free base	HSP Autophagy	Cancer
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 .

HY-153475

IRE1α kinase-IN-9	IRE1	Cancer
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) .

HY-136528

RA-9	Deubiquitinase Apoptosis	Cancer
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 .

HY-145418

IRE1α kinase-IN-3	IRE1	Others
IRE1α kinase-IN-3 (compound 2) is a potent IRE1α inhibitor with an K_i of 480 nM. IRE1α kinase-IN-3 is the ATP-competitive ligands of IRE1α .

HY-145419

IRE1α kinase-IN-4	IRE1	Others
IRE1α kinase-IN-4 (compound 6) is a potent IRE1α inhibitor with an K_i of 140 nM. IRE1α kinase-IN-4 is the ATP-competitive ligands of IRE1α .

HY-145420

IRE1α kinase-IN-5	IRE1	Others
IRE1α kinase-IN-5 (compound 7) is a potent IRE1α inhibitor with an K_i of 98 nM. IRE1α kinase-IN-5 is the ATP-competitive ligands of IRE1α .

HY-121337

Flurochloridone R-40244	Apoptosis Bcl-2 Family	Others
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 .

HY-109076

Tigilanol tiglate EBC-46	PKC	Cancer
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 .

HY-121337R

Flurochloridone (Standard)	Apoptosis Bcl-2 Family	Others
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 .

HY-145422

KIRA9	IRE1 Apoptosis	Others
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 .

HY-167701

OBHSA	Others	Cancer
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 .

HY-108434

Ceapin-A7 5+ Cited Publications	ATF6	Neurological Disease Metabolic Disease
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 .

HY-115445

LCS-1 1 Publications Verification	Apoptosis SOD	Cancer
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 .

Cat. No.	Product Name

HY-L054

Endoplasmic Reticulum Stress Compound Library	227 compounds
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.

Endoplasmic Reticulum Stress Compound Library

227 compounds

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.

Cat. No.	Product Name	Target	Research Area

HY-129960

L-Selenocystine	Peptides	Others
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 .

Thapsigargin 65+ Cited Publications	Infection Classification of Application Fields Terpenoids Source classification Diterpenoids Umbelliferae Plants Disease Research Fields Thapsia garganica L. Cancer	Calcium Channel SARS-CoV Apoptosis
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 .

Mycothiazole	Structural Classification Natural Products Marine natural products Source classification Sponge	Mitochondrial Metabolism
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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