Autophagy

Autophagy is an intracellular catabolic mechanism. In certain stressful situations, lysosomes degrade degenerated, damaged, aged or non-functional cells, organelles and biomolecules such as proteins and nucleic acids to achieve cellular protection and organelles from cell damage. Autophagy is achieved by forming a bilayer membrane structure in the cytoplasm that wraps the material to be removed and transports it to the lysosome for degradation. In multicellular organisms, newly formed autophagic vesicles form autophagic endosomes by fusing with vesicles in different stages of the endocytic lysosomal pathway, such as early endosomes and late endosomes, before fusing with lysosomes, a process known as autophagic vesicle maturation. Abnormalities in autophagosome maturation, which is precisely regulated by cellular trophic state and stress signaling pathways, lead to the accumulation of large amounts of damaged organelles and toxic protein aggregates in cells.

Cat. No.	Product name
BP12538	Cilengitide
BP12538	Cilengitide is a potent integrin inhibitor for the αvβ3/5 receptor (IC50: 4.1/79 nM, in cell-free assays); ~10-fold selectivity against gpIIbIIIa.
BP12539	Salvigenin
BP12539	Salvigenin is a potent hMAO-A inhibitor, has neuroprotective, antitumor and immunomodulatory effects.
BP12540	Cudraflavone B
BP12540	Cudraflavone B has anti-proliferative activity, mouse brain monoamine oxidase (MAO) inhibitory effects, apoptotic actions in human gastric carcinoma cells and mouse melanoma cells, and hepatoprotective activity. It may be a lead for the development of a potential candidate for human oral squamous cell carcinoma cells.
BP12541	Lonafarnib
BP12541	Lonafarnib is an orally bioavailable FPTase inhibitor for H-ras, K-ras-4B, and N-ras (IC50: 1.9/5.2/2.8 nM).
BP12542	SB 239063
BP12542	SB239063 is a potent and selective p38 MAPKα/β inhibitor with IC50 of 44 nM, showing no activity against the γ- and δ-kinase isoforms.
BP12543	SB 242235
BP12543	SB-242235 is a potent and selective p38 MAP kinase inhibitor that may be an effective therapy for cytokine-mediated diseases.
BP12544	Nesolicaftor
BP12544	PTI-428 specifically enhances cystic fibrosis transmembrane conductance regulator protein synthesis.
BP12545	Wortmannin
BP12545	Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM, with little selectivity within the PI3K family. Also blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM.
BP12546	FMK 9a
BP12546	FMK 9a is an irreversible inhibitor of ATG4B with IC50 values of 80 and 73 nM in the TR-FRET and cellular-based LRA assays.
BP12547	3,3'-Diindolylmethane
BP12547	DIM (3, 3'-diindolylmethane), a small molecule compound, is a proposed Y preventive agent.
BP12548	Amiodarone hydrochloride
BP12548	Amiodarone hydrochloride is an antianginal and class III antiarrhythmic drug. It increases the duration of ventricular and atrial muscle action by inhibiting POTASSIUM CHANNELS and VOLTAGE-GATED SODIUM CHANNELS. There is a resulting decrease in heart rate and in vascular resistance.
BP12549	Nicotinamide N-oxide
BP12549	Nicotinamide N-oxide is recognized as an in vivo metabolite of nicotinamide which is a precurser of nicotinamide-adenine dinucleotide (NAD+) in animals. The enzyme that catalyzes the reduction of nicotinamide N-oxide to nicotinamide in the liver is xanthine oxidase.
BP12550	Alisol A
BP12550	Alisol A may be an autophagic inducer, it has anti-cancer activity, it presents inhibitory effects on cancer cell lines tested(HepG2, MDA-MB-231, and MCF-7 cells).
BP12551	Cilengitide TFA
BP12551	Cilengitide is a potent integrin inhibitor for αvβ3 receptor and αvβ5 receptor with IC50 of 4.1 nM and 79 nM in cell-free assays, respectively; ~10-fold selectivity against gpIIbIIIa. Phase 2.
BP12552	Talarozole
BP12552	Talarozole (R115866) is an oral systemic all-trans retinoic acid metabolism blocking agent (RAMBA) which increases intracellular levels of endogenous all-trans retinoic acid (RA). Talarozole inhibits both CYP26A1 and CYP26B1 with IC50s of 5.4 and 0.46 nM, respectively.
BP12553	Brefeldin A
BP12553	Brefeldin A, a Penicillium brefeldianum metabolite, which is a macrocyclic lactone exhibiting a wide range of antibiotic activity. It is also an ATPase inhibitor for protein transport in HCT 116 cells(IC50=0.2 μM), inducing Y cell differentiation and apoptosis.
BP12554	Coniferaldehyde
BP12554	Coniferaldehyde can significantly inhibit the growth of viability of strains of Oenococcus oeni. Coniferaldehyde exerts anti-inflammatory properties by inducing heme oxygenase-1(HO-1).
BP12555	Rutin hydrate
BP12555	Rutin hydrate, a kind of glycoside, widely exists in many plants including citrus fruit.
BP12556	MRT68921 dihydrochloride
BP12556	MRT68921 dihydrochloride is a potent ULK1 and ULK2 inhibitor (IC50 of 2.9 nM and 1.1 nM, respectively).
BP12557	Berberine
BP12557	Berberine is a potent oral hypoglycemic agent with beneficial effects on lipid metabolism. Berberine may as a broad-spectrum anti-microbial medicine, a complementary therapeutic agent for HIV/AIDS. Berberine seems to act as an herbal antidepressant and a neuroprotector against neurodegenerative disorders. Berberine is used in histology for staining heparin in mast cells. As a natural dye, berberine has a colour index of 7516. Berberine reduces hepatic fat content in rats with nonalcoholic fatty liver disease; also prevents proliferation of hepatic stellate cells (HSCs), which are central for the development of fibrosis during liver injury. Berberine can ameliorate proinflammatory cytokines-induced intestinal epithelial tight junction damage in vitro, and berberine may be one of the targeted therapeutic agents that can restore barrier function in intestinal disease states. Berberine has antineoplastic effects, including breast cancer, leukemia, melanoma, epidermoid carcinoma, hepatoma, pancreatic cancer, oral carcinoma, tongue carcinoma, glioblastoma, prostate carcinoma and gastric carcinoma, etc.