endoplasmic reticulum

RH01687 is a potent β-cell protector , exhibits β-cell-protective activities against endoplasmic reticulum (ER) stress.

Tauroursodeoxycholate (UR 906), also known as ursodoxicoltaurine, is a highly hydrophilic tertiary bile acid that is produced in humans at a low concentration. Tauroursodeoxycholate is the more hydrophilic form of ursodeoxycholic acid, which is the more abundant naturally produced bile acid in humans.Tauroursodeoxycholate is being investigated for use in several conditions such as Primary Biliary Cirrhosis (PBC), insulin resistance, amyloidosis, Cystic Fibrosis, Cholestasis, and Amyotrophic Lateral Sclerosis.

Thapsigargin is a natural product, an inhibitor of sarcoplasmic/endoplasmic reticulum Ca2+ ATPase (SERCA) and an endoplasmic reticulum stress inducer. Thapsigargin increases cytoplasmic calcium concentration by blocking the ability of cells to pump calcium into the sarcoplasmic and endoplasmic reticulum.

Cyclic ADP-ribose (cADPR) is an effective calcium mobilization second messenger synthesized from NAD+ by ADP-ribosyl cyclase. It mainly increases cytosolic calcium through Ryanodine receptor-mediated endoplasmic reticulum release and extracellular influx via the opening of TRPM2 channels.

alphaSYN-IN-NAB2, a neuron-protective agent, is a protein encoded by the NAB2 gene. NAB2 effectively and selectively protects a variety of cells from alpha-SYN toxicity. NAB2 promotes endosomal transport dependent on E3 ubiquitin ligase Rsp5/Nedd4. NAB2 identifies a viable molecular node in alpha-SYN biology that corrects multiple aspects of its underlying pathology, including dysfunctional endosomes and endoplasmic reticulum to Golgi vesicles transport. NAB2 is involved in cellular processes such as cell differentiation, apoptosis and stress response, and can be used to study cancer, neurodevelopment and neuronal activity.

ICL-CCIC-0019, an inhibitor of choline kinase alpha (ChoKα), induces G1 arrest, endoplasmic reticulum stress, and apoptosis in cancer cell lines.

GSK-J4 (GSK J4 HCl) is a cell permeable prodrug of GSK-J1, a dual inhibitor of the H3K27me3/me2 demethylases JMJD3/KDM6B and UTX/KDM6A (IC50=8.6/6.6 μM). GSK-J4 induces endoplasmic reticulum stress-related apoptosis.

α-Lipoic Acid (DL-α-Lipoic acid) an octanoic acid bridged with two sulfurs so that it is sometimes also called a pentanoic acid in some naming schemes. It is biosynthesized by cleavage of LINOLEIC ACID and is a coenzyme of oxoglutarate dehydrogenase (KETOGLUTARATE DEHYDROGENASE COMPLEX). It is used in DIETARY SUPPLEMENTS.

Butylhydroxyanisole (BHA) is an antioxidant consisting of a mixture of two isomeric organic compounds, 2-tert-butyl-4-hydroxyanisole and 3-tert-butyl-4-hydroxyanisole.

Triheptanoin (IND 106011) is a fatty acid metabolic modulator. It potentially for the treatment of fatty acid oxidation disorders and GLUT1.

α-Lipoic Acid (Alphalipoic acid) inhibits NF-κB-dependent HIV-1 LTR activation. α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells.α-Lipoic Acid is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes.

4-Phenylbutyric acid (Benzenebutyric acid) is a histone deacetylase (HDAC) inhibitor and an endoplasmic reticulum stress (ERS) inhibitor. 4-Phenylbutyric acid can be used to treat urea cycle disorders.

Lomitapide (AEGR-733) is a small molecule inhibitor of microsomal triglyceride transfer protein (MTP), an enzyme located in the lumen of the endoplasmic reticulum responsible for absorbing dietary lipids and transferring triglycerides onto apolipoprotein B (apo-B) in the assembly of very-low-density lipoprotein.

Tauroursodeoxycholate sodium (TUDC) is an endoplasmic reticulum (ER) stress inhibitor, used for the treatment of gallstones and liver cirrhosis.

2,5-Di-tert-butylhydroquinone (BHQ) is an effective and selective endoplasmic reticulum Ca2+-ATPase inhibitor.

Dibutyl phthalate (1,2-Benzenedicarboxylic acid) is a plasticizer, commonly used in industrial manufacturing, that causes cardiac damage by disrupting Ca(2+) transfer from the endoplasmic reticulum to the mitochondria and triggering subsequent cellular death.Dibutyl phthalate induces oxidative damage in the brain of zebrafish.

20-HC-Me-Pyrrolidine is a potent Aster protein inhibitor with IC50=0.06~0.71 μm for Aster-A, Aster-B, and Aster-C that blocks the ability of Aster proteins to bind and transfer cholesterol, including inhibiting the movement of LDL cholesterol to the endoplasmic reticulum.

Gcase activator 2 is a β-glucocerebrosidase activator that induces dimerization of GCase at the endoplasmic reticulum (ER) and lysosomal pHs, increases lysosomal substrate metabolism, and has therapeutic potential for the treatment of Parkinson's and Gosheimer's diseases.

ERAP1-IN-1 is an endoplasmic reticulum aminopeptidase 1 (ERAP1) inhibitor that allosterically activates ERAP1's hydrolysis of fluorogenic and chromogenic amino acid substrates, while competitively inhibiting its activity toward a nonamer peptide representative of physiological substrates.

Ganoderic acid F exhibits antitumor and antimetastatic activities through inhibition of angiogenesis and alteration of proteins involving cell proliferation and/or cell death, carcinogenesis, oxidative stress, calcium signaling, and endoplasmic reticulum

TTA-Q6, a selective T-type Ca2+ channel antagonist, exhibits potential antitumor and immunomodulatory activities for treating neurological disorders by inhibiting the uptake of extracellular calcium ions by tumor cells, thereby inducing intracellular calcium deficiency and endoplasmic reticulum (ER) stress.

ZX-29 is a potent and selective inhibitor of ALK with IC50 values of 2.1 nM, 1.3 nM, and 3.9 nM for ALK, ALK [L1196M], and ALK [G1202R] mutations, respectively. It also induces protective autophagy and exhibits antitumor effects.

ABTL-0812 induces endoplasmic reticulum (ER) stress-mediated autophagy, and with anti-cancer activity.

AA147 (ATF6-activator-147) is a small molecule endoplasmic reticulum (ER) proteostasis regulator. The selectively activates ATF6 arm of the unfolded protein response (UPR) .It acts as a prodrug that preferentially triggers ATF6 signaling through a mechanism involving localized metabolic activation and selective covalent modification of ER resident proteins that regulate ATF6 activity.