Autophagy Inhibitor

Vancomycin hydrochloride is an antibiotic for the treatment of bacterial infections. It acts by inhibiting the second stage of cell wall synthesis of susceptible bacteria. Vancomycin also alters the permeability of the cell membrane and selectively inhibits ribonucleic acid synthesis.

Dimethyl 2-oxoglutarate (Dimethyl α-ketoglutarate) is a cell-permeable derivative of 2-oxoglutarate and tricarboxylic acid cycle metabolite with antioxidant properties. Dimethyl 2-oxoglutarate inhibits Autophagy. Dimethyl 2-oxoglutarate prevents mitochondrial damage and reduces ROS production. Dimethyl 2-oxoglutarate alleviates Carbon tetrachloride (HY-Y0298)-induced liver fibrosis. Dimethyl-2-oxoglutaric acid can be used in the research of diseases such as Alzheimer's disease, diabetes, and cardiomyopathy.

GSK2606414 is a cell-permeable and orally available protein kinase R-like endoplasmic reticulum (ER) kinase (PERK) inhibitor with an IC₅₀ of 0.4 nM.

Hydroxychloroquine (HCQ) is a synthetic oral antimalarial drug that can be used in the study of malaria and autoimmune diseases such as systemic lupus erythematosus and rheumatoid arthritis. Hydroxychloroquine is a potent autophagic flux inhibitor with antiviral activity (such as SARS-CoV-2 virus) that inhibits Toll-like receptor 7/9 (TLR7/9) signaling.

Vancomycin is an antibiotic for the treatment of bacterial infections.

Chloroquine phosphate is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine phosphate is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine phosphate is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC₅₀=1.13 μM).

Tanespimycin (17-AAG) is a potent HSP90 inhibitor with an IC₅₀ of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90. Tanespimycin depletes cellular STK38/NDR1 and reduces STK38 kinase activity. Tanespimycin also downregulates the stk38 gene expression.

AS1842856, a specific Foxo1 inhibitor (IC₅₀=30 nM), potently suppresses autophagy. AS1842856 reduces Foxo1 activity and, to a lesser extent, inhibits Foxo1 protein expression by simply binding to Foxo1.

KU-55933 is a potent ATM inhibitor with an IC₅₀ and K_i of 12.9 and 2.2 nM, respectively, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR.

VER-155008 is an inhibitor of Hsp70, with IC₅₀s of 0.5 μM, 2.6 μM, and 2.6 μM for Hsp70, Hsc70 and Grp7, respectively, and with a K_d of 0.3 μM for Hsp70.

Purmorphamine is a smoothened/Smo receptor agonist with an EC₅₀ of 1 μM.

TPEN (TPEDA) is a specific cell-permeable heavy metal chelator. TPEN has a higher affinity for Zn²⁺, but a lower affinity for Mg²⁺ and Ca²⁺. TPEN induces DNA damage and increases intracellular ROS production. TPEN also inhibits cell proliferation and induces apoptosis.

E-64 (Proteinase inhibitor E 64) is a potent irreversible inhibitor against general cysteine proteases with IC₅₀ of 9 nM for papain.

Acetyl-coenzyme A (Acetyl-CoA) trisodium is a membrane-impermeant central metabolic intermediate, participates in the TCA cycle and oxidative phosphorylation metabolism. Acetyl-coenzyme A trisodium, regulates various cellular mechanisms by providing (sole donor) acetyl groups to target amino acid residues for post-translational acetylation reactions of proteins. Acetyl Coenzyme A trisodium is also a key precursor of lipid synthesis.

SBI-0206965 is a potent, selective and cell permeable autophagy kinase ULK1 inhibitor with IC₅₀s of 108 nM for ULK1 kinase and 711 nM for the highly related kinase ULK2. SBI-0206965 is also an AMPK inhibitor that can paradoxically increase Thr172 phosphorylation.

Methylprednisolone (U 7532) is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone improve severe or critical COVID-19 by activating ACE2 and reducing IL-6 levels.

Ammonium chloride, as a heteropolar compound with pH value regulation, can cause intracellular alkalization and metabolic acidosis thus effecting enzymatic activity and influencing the process of biological system. Ammonium chloride is an autophagy inhibitor. Ammonium chloride is also a lysosome inhibitor.

Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects. Emodin is a potent selective 11β-HSD1 inhibitor with the IC₅₀ of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice.

Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC₅₀ of 12 nM.

Heparin is a highly sulfated glycosaminoglycan,that is widely used as an injectable anticoagulant, and has the highest negative charge density of any known biological molecule. Heparin significantly inhibits exosome-cell interactions.