Autophagy Inducer

Selenomethionine is a naturally occurring amino acid containing selenium that has oral activity and is a common natural food source. Selenomethionine has antitumor activity.

Enzastaurin (LY317615) is a potent, selective, and CNS-penetrant PKCβ inhibitor with an IC₅₀ of 6 nM, showing 6- to 20-fold selectivity over PKCα, PKCγ and PKCε.

Sildenafil citrate is a potent phosphodiesterase type 5 (PDE5) inhibitor with IC₅₀ of 5.22 nM.

Phenformin (Phenethylbiguanide) hydrochloride is an orally active biguanide hypoglycemic agent. Phenformin hydrochloride inhibits mitochondrial respiratory chain complex I, leading to an increased AMP/ATP ratio, activation of AMPK, and subsequent inhibition of the mTOR pathway, thereby suppressing cell proliferation, inducing apoptosis and autophagy. Phenformin hydrochloride inhibits cancer stem cells (CSCs) and possesses potent antitumor potential.

XCT-790 is a potent and selective inverse agonist for ERRα with an IC₅₀ value of 0.37 μM. XCT-790 induces cell death in chemotherapeutic resistant cancer cells. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ.

Tubastatin A Hydrochloride (Tubastatin A HCl) is a potent and selective HDAC6 inhibitor with IC₅₀ of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more). Tubastatin A Hydrochloride also inhibits HDAC10 and metallo-β-lactamase domain-containing protein 2 (MBLAC2).

AMG PERK 44 is an orally active and highly selective PERK inhibitor with an IC₅₀ of 6 nM. AMG PERK 44 has 1000-fold and 160-fold selectivity over GCN2 (IC₅₀=7300 nM) and B-Raf (IC₅₀ >1000 nM), respectively. AMG PERK 44 induces autophagy.

Shogaol ([6]-Shogaol), an active compound isolated from Ginger (Zingiber officinale Rosc), exhibits a variety of biological activities including anticancer, anti-inflammation, and anti-oxidation.

Lanatoside C is a cardiac glycoside, can be used in the treatment of congestive heart failure and cardiac arrhythmia.Lanatoside C has an IC50 of 0.19 μM for dengue virus infection in HuH-7 cells. Lanatoside C can effectively inhibit all four serotypes of dengue virus, flavivirus Kunjin, alphavirus Chikungunya, Sindbis virus and the human enterovirus 71.

Lomustine (CCNU; NSC 79037) is a DNA alkylating agent, with antitumor activity.

Corilagin, a gallotannin, has anti-tumor, anti-inflammatory and hepatoprotective activities. Corilagin inhibits activity of reverse transcriptase of RNA tumor viruses. Corilagin also inhibits the growth of Staphylococcus aureus with a MIC of 25 μg/mL. Corilagin shows anti-tumor activity on hepatocellular carcinoma and ovarian cancer model. Corilagin shows low toxicity to normal cells and tissues.

Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC₅₀ of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.

PAC-1 is a procaspase-3 activator that induces apoptosis in cancer cells with an EC₅₀ of 2.08 μM.

Cucurbitacin B belongs to a class of highly oxidized tetracyclic triterpenoids and is oral active. Cucurbitacin B inhibits tumor cell growth, migration and invasion and cycle arrest, but induces cell apoptosis. Cucurbitacin B has potent anti-inflammatory, antioxidant, antiviral, hypoglycemic, hepatoprotective, neuroprotective activity.

Bergapten is a natural anti-inflammatory and anti-tumor agent. Bergapten is inhibitory towards mouse and human CYP isoforms.

Thioridazine hydrochloride, an orally active antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine hydrochloride is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine hydrochloride shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs).

Paeonol is an active extraction from the root of Paeonia suffruticosa, Paeonol inhibits MAO-A and MAO-B with IC₅₀ of 54.6 μM and 42.5 μM, respectively.

(-)-Epicatechin gallate (Epicatechin gallate) inhibits cyclooxygenase-1 (COX-1) with an IC₅₀ of 7.5 μM. (-)-Epicatechin gallate is a GLUT1 and GLUT5 inhibitor. (-)-Epicatechin gallate decreases cell growth of GLUT5-expressing hxt⁰ yeast cells.

Daunorubicin (Daunomycin) is a topoisomerase II inhibitor with potent anti-tumor activity. Daunorubicin inhibits DNA and RNA synthesis. Daunorubicin is a cytotoxin that inhibits cancer cell viability and induces apoptosis and necrosis. Daunorubicin is also an anthracycline antibiotic. Daunorubicin can be used in the research of infection and variety of cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, Wilms' tumor.

Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC₅₀ of 11 nM. Rosuvastatin potently blocks hERG current with an IC₅₀ of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.