Autophagy Inhibitor

Ezurpimtrostat hydrochloride (GNS561 hydrochloride) is an orally active PPT1 inhibitor, autophagy inhibitor, immunomodulator, anti-inflammatory agent, and anticancer agent. Ezurpimtrostat hydrochloride inhibits PPT1, dysregulates lysosomal function, redistributes mTOR, and induces apoptosis. Ezurpimtrostat hydrochloride reduces IFN‑α, CRP, immune complex deposition, and SARS‑CoV‑2 viral load. Ezurpimtrostat hydrochloride can be used for the study of systemic lupus erythematosus, SARS‑CoV‑2, hepatocellular carcinoma, fibrosis, and related disorders.

ATG7-IN-2 (compound 1) is a potent ATG7 inhibitor, with an IC₅₀ of 0.089 μM. ATG7-IN-2 inhibits autophagy marker LC3B.

Nordeoxycholic acid (3α,12α-Dihydroxynorcholanic acid) is an orally active hydrophobic bile acid metabolite. Nordeoxycholic acid inhibits autophagic flux, induces endoplasmic reticulum stress and causes hepatocyte injury. Nordeoxycholic acid impairs intestinal barrier integrity in mice. Nordeoxycholic acid can be used in the research of alcohol-associated liver disease.

Tenovin-6, an analog of Tenovin-1 (HY-13423), is an activator of p53 transcriptional activity. Tenovin-6 inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 with IC₅₀s of 21 μM, 10 μM, and 67 μM, respectively. Tenovin-6 also inhibits dihydroorotate dehydrogenase (DHODH).

Mefloquine (Mefloquin), an orally active and potent quinoline antimalarial agent, is an anti-SARS-CoV-2 entry inhibitor. Mefloquine is also a K⁺ channel (KvQT1/minK) antagonist with an IC₅₀ of ~1 μM. Mefloquine can be used for malaria, systemic lupus erythematosus and cancer research.

AZ PFKFB3 26 is a potent and selective PFKFB3 inhibitor with an IC₅₀ of 23 nM. AZ PFKFB3 26 inhibits PFKFB1 and PFKFB2 with IC₅₀s of 2.06 and 0.384 μM, respectively. AZ PFKFB3 26 can be used in the study of non-small cell lung cancer.

Cinchonine is a natural compound present in Cinchona bark with antimalarial, antitumor, anti-inflammatory, anti platelet-aggregation and anti-obesity properties. Cinchonine inhibits cells proliferation and autophagy and induces apoptosis through activation of Caspase-3. Cinchonine activates endoplasmic reticulum stress-induced apoptosis in human liver cancer cells.

NSC 185058 is an inhibitor of ATG4B, a major cysteine protease. Inhibition of ATG4B using NSC 185058 markedly attenuates autophagic activity.

Rotenone (Standard) is the analytical standard of Rotenone. This product is intended for research and analytical applications. Rotenone is a mitochondrial electron transport chain complex I inhibitor. Rotenone induces apoptosis through enhancing mitochondrial reactive oxygen species production.

Pepstatin (Pepstatin A) Trifluoroacetate is a specific, orally active aspartic protease inhibitor produced by actinomycetes, with IC₅₀s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin Trifluoroacetate also inhibits HIV protease.

Dexpramipexole ((R)-Pramipexole) dihydrochloride is an orally active, blood-brain barrier permeable mitochondrial protective agent. Dexpramipexole dihydrochloride upregulates the expression of Parkin, PINK1, GPX4 and FSP1; binds to mitochondrial F1/Fo-ATP synthase; blocks the Na_v1.8 sodium channel; and inhibits the activation of the NLRP3 inflammasome. Dexpramipexole dihydrochloride induces mitophagy, inhibits ferroptosis, pyroptosis, apoptosis, neuroinflammation and eosinophilopoiesis; maintains mitochondrial function and redox homeostasis; reduces reactive oxygen species production; and decreases myocardial infarct size. Dexpramipexole dihydrochloride is applicable to studies on eosinophilic asthma, myocardial ischemia/reperfusion injury, sepsis-associated encephalopathy, analgesia, and more.

Recombinant Humanized Type III Collagen 28.6kDa is a 28.6 kDa recombinant humanized type III collagen. Recombinant Humanized Type III Collagen possesses a variety of biological functions, such as promoting the regeneration of the skin extracellular matrix and improving the cellular microenvironment. Recombinant Humanized Type III Collagen can also inhibit the proliferation, migration and invasion of breast cancer cells. Recombinant Humanized Type III Collagen plays a role in cell adhesion, migration, proliferation and differentiation by interacting with Integrin.

Chloroquine (phosphate) (Standard) is the analytical standard of Chloroquine (phosphate). This product is intended for research and analytical applications. 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).

KAN0438757 is a potent and selective inhibitor of the metabolic kinase PFKFB3 with an IC₅₀ of 0.19 μM.

Dehydrodiisoeugenol is an orally active anti-inflammatory and anti-tumor agent. Dehydrodiisoeugenol inhibits the proliferation of colorectal cancer cells, and induces apoptosis, autophagy, endoplasmic reticulum stress and cell cycle arrest. Dehydrodiisoeugenol also exerts anti-inflammatory effects by inhibiting the activation of NF-κB and the expression of COX-2. Dehydrodiisoeugenol can be used in the research related to colorectal cancer, inflammatory diseases and ulcerative colitis.

Ginkgo biloba extract is a natural product that can be isolated from Ginkgo biloba leaves. Ginkgo biloba extract alleviates oxidative stress-induced neuronal apoptosis (Apoptosis) by stabilizing mitochondrial function, regulating Bcl-2 family proteins and inhibiting caspase activation. Ginkgo biloba extract alleviates testicular injury by upregulating SKP2 and inhibiting Beclin1-independent autophagy (Autophagy). Ginkgo biloba extract alleviates various types of neuronal damage in animal models. Ginkgo biloba extract reduces behavioral sensitization in rats. Ginkgo biloba extract counteracts Aβ-induced neurotoxicity by blocking a series of Aβ-triggered events, including glucose uptake, ROS accumulation, AKT activation, mitochondrial dysfunction, JNK and ERK 1/2 pathways, and apoptosis, and also interferes with the formation of Aβ oligomers. Ginkgo biloba extract is applicable to research related to cerebral hypoperfusion, testicular injury, Alzheimer's disease, Parkinson's disease, multi-infarct dementia, stroke, traumatic brain injury and amyotrophic lateral sclerosis.

Astragaloside II is an orally active Cycloartane-type triterpene glycoside. Astragaloside II can be extracted from Astragalus membranaceus. Astragaloside II inhibits Autophagy, decreases pro-inflammatory cytokines (IL-6, IL-1β), HIF-α, p-p65, p-IκB and increases SOD. Astragaloside II regulates immunity and reduces inflammatory responses. Astragaloside II can be used in the research of diseases such as liver cancer, osteoporosis, immunosuppressive diseases, and ulcerative colitis.

Kumatakenin is an orally active apoptosis inducer and autophagy inhibitor, with a K_d value of 2.94 μM for mouse ATG5. Kumatakenin increases the activities of caspase-3, caspase-8 and caspase-9, thereby inducing caspase-dependent apoptosis in ovarian cancer cells. Kumatakenin reduces the expression of chemokines and pro-oncogenic factors in ovarian cancer cells, and inhibits M2 macrophage polarization. Kumatakenin inactivates TRIM65 function, reduces the expression and stability of FASN, and thus inhibits the proliferation, migration, invasion and tumor progression of esophageal cancer cells. Kumatakenin interacts with ATG5 to reduce its protein level, decrease LC3 level, and reduce the number of autophagosomes in the hippocampus. Kumatakenin binds to Eno3 to upregulate its expression, reduce the stability and expression level of IRP1 mRNA, inhibit ferroptosis, alleviate intestinal inflammation, and restore epithelial barrier function. Kumatakenin enhances the efficacy of antibiotics against pathogenic bacteria, inhibits SARS-CoV-2 replication, and reduces cytokine production. Kumatakenin is applicable to research related to ovarian cancer, esophageal cancer, depression and colitis.

DC-LC3in-D5 acts as an autophagy inhibitor by attenuating LC3B lipidation. DC-LC3in-D5 binds with LC3B. DC-LC3in-D5 disrupts the LC3B-LBP2 interaction with an IC₅₀ of 200 nM. DC-LC3in-D5 may contribute to anti-HCV or combination researchs in cancer through inhibiting autophagy.

Melatonin-d₄ is deuterium labeled Melatonin. Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Antioxidative and anti-inflammatory properties. Melatonin is a selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation.