autophagy

Sorafenib (Bay 43-9006) is a multikinase inhibitor that targets Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6/22/90/15/20/20/57/58 nM) with oral activity. It exhibits antitumor properties and can induce autophagy, apoptosis, and agonistic iron death.

Oxaliplatin (L-OHP) is a DNA alkylating agent, an inhibitor of DNA synthesis. Oxaliplatin causes DNA cross-linking damage, preventing DNA replication and transcription and leading to cell death. Oxaliplatin induces autophagy.

Gemcitabine (LY188011) is a synthetic cytosine nucleoside derivative and an inhibitor of DNA synthesis. Gemcitabine has antitumor and antimetabolic activities. Gemcitabine induces autophagy and apoptosis.

Gefitinib (ZD1839) is an EGFR first-generation inhibitor with oral activity that inhibits the EGFR 19 Del and L858R mutations. Gefitinib has antitumor activity and is used for the treatment of EGFR-mutated non-small-cell lung cancers. Gefitinib administration RESULTS in the development of the EGFR C797S resistance mutation.

Ruxolitinib (INCB018424) is a JAK1/2 inhibitor (IC50=3.3/2.8 nM) that is potent and selective. Rixolitinib exhibits antitumor activity and induces autophagy and apoptosis.

Necrostatin-1 (Nec-1) is a specific RIP1 inhibitor and necrotic apoptosis inhibitor, which inhibits TNF-α-induced necrotic apoptosis and also inhibits IDO.

Mdivi-1 (Mitochondrial division inhibitor 1) is a mitochondrial division inhibitor that inhibits DRP1 and Dynamin I (IC50=1-10 μM). Mdivi-1 inhibits mitochondrial autophagy.

LY294002 (SF 1101) is a broad-spectrum inhibitor of PI3K, inhibiting PI3Kα, PI3Kδ, and PI3Kβ (IC50=0.5/0.57/0.97 μM). LY294002 is also an inhibitor of DNA-PK (IC50=1.4 μM) and an inhibitor of CK2 (IC50=98 nM). LY294002 activates apoptosis and autophagy.

Trametinib (GSK1120212) is a MEK inhibitor that inhibits MEK1 and MEK2 (IC50=0.7/0.9 nM) with ATP non-competitive and oral activity. Trametinib activates autophagy and induces apoptosis.

Quercetin, a flavonoid natural product, is a SIRT1 activator. It is also a PI3K inhibitor, inhibiting PI3Kγ, PI3Kδ, and PI3Kβ with IC50 values of 2.4, 3.0, and 5.4 μM, respectively. Recognized as a heat shock protein inhibitor, Quercetin can significantly reduce exosome release in TII models by downregulating Hsp70 or Hsp90.

Bortezomib (LDP 341) is a 20S proteasome inhibitor (Ki=0.6 nM) that is reversible and selective. Bortezomib has antitumor activity and inhibits NF-κB, which can disrupt the cell cycle and induce apoptosis.

Rotenone is a natural plant-derived insecticide that acts as an inhibitor of mitochondrial electron transport chain complex I. It promotes the generation of mitochondrial reactive oxygen species, induces apoptosis, and is commonly used to establish Parkinson's disease models.

(-)-Epigallocatechin Gallate (EGCG) is a phenolic antioxidant polyphenol flavonoid found in plants such as green and black tea, which inhibits telomerase and DNA methyltransferase, blocks the activation of EGF receptors and HER-2 receptors, inhibits cellular oxidation, and prevents free radical damage to cells.

Rosiglitazone (BRL49653) is a PPARγ agonist, TRPC5 activator, and TRPM3 inhibitor with oral activity. Rosiglitazone is also a hypoglycemic agent and a thiazolidinedione insulin sensitizer.

Metformin hydrochloride (1,1-Dimethylbiguanide hydrochloride), a widely used anti-diabetic drug, exhibits potential anti-Y properties by inhibiting the proliferation of various Y cells, including colon and prostate.

Rutin (Quercetin 3-O-rutinoside), a flavonoid, has a variety of biological activities including antiallergic, anti-inflammatory, antiproliferative, and anticarcinogenic properties.

Paclitaxel (Taxol) is a natural product and a microtubule polymer stabilizer. Paclitaxel has anti-tumor activity and causes cell death by inducing mitotic arrest, apoptosis, and cell autophagy.

Doxorubicin hydrochloride is an anthracycline antibiotic with cytotoxic and antitumor activity. It is an effective inhibitor of human DNA topoisomerase I and II, with IC50 values of 0.8 μM and 2.67 μM, respectively. In addition to inhibiting DNA topoisomerases, it can reduce the phosphorylation of AMPK and its downstream target, acetyl-CoA carboxylase. Doxorubicin hydrochloride also induces apoptosis and autophagy. In animal studies, it is commonly used to induce models of acute renal failure, chronic kidney injury, and heart failure.

Dexamethasone is a glucocorticoid receptor agonist and IL receptor modulator with anti-inflammatory, immunosuppressive, and apoptosis-inducing activities. It inhibits the production of inflammatory miRNA-155 exosomes in macrophages, significantly reduces inflammatory cytokine expression in neutrophils and monocytes, suppresses LPS-induced macrophage inflammation, and induces autophagy. It is commonly used to induce animal models of depression, muscle atrophy, and hypertension, and holds potential in COVID-19 research.

Temozolomide (TMZ) is a DNA alkylating agent with blood-brain barrier permeability and oral activity. Temozolomide has antitumor activity and antiangiogenic activity, and also induces apoptosis and autophagy. Temozolomide is stable under acidic conditions and hydrolyzes under neutral or slightly alkaline conditions.

Cycloheximide (Naramycin A) is a natural product . Cycloheximide‘s IC50 values for protein synthesis and RNA synthesis in vivo are 532.5 nM and 2880 nM, respectively. Cycloheximide inhibits ferroptosis and autophagy and is an antifungal antibiotic.

Deferoxamine (Desferrioxamine B) is an iron chelator. Deferoxamine can be used to reduce the accumulation and deposition of iron in tissues. Deferoxamine can improve neurological dysfunction by inhibiting ferroptosis and neuroinflammation after traumatic brain injury. It has antioxidant, anti-proliferation and anti-tumor activities, and can induce the production of HIF-1α, apoptosis and autophagy in cancer cells. It can be used to treat acute iron toxicity and COVID-19 related diseases.

Elexacaftor (VX-445) is a cystic fibrosis transmembrane conductance regulator (CFTR) corrector. It promotes the processing and trafficking of CFTR, increases the amount of CFTR on the cell surface, and improves the processing and trafficking of Phe508del CFTR protein.

Streptozotocin (Streptozocin, NSC-85998) is an antibiotic that enters pancreatic β-cells via the glucose transporter (GLUT2) and induces DNA methylation, leading to β-cell apoptosis. It is toxic to insulin-producing cells and commonly used to establish diabetic animal models. This product is unstable in solution and is recommended to be prepared freshly before use.