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
BP12438	GNE0877
BP12438	GNE-0877 is a highly effective and specific leucine-rich repeat kinase 2 (LRRK2) inhibitor (Ki: 0.7 nM).
BP12439	SR9011
BP12439	SR9011 is a REV-ERB agonist (IC50: 790 nM, REV-ERBα; IC50: 560 nM, REV-ERBβ).
BP12440	SR9009
BP12440	SR9009, a REV-ERB agonist, increases the constitutive repression of genes regulated by REV-ERBα/ERBβ (IC50: 670/800 nM). Through activation of REV-ERB, SR9009 can decrease circadian locomotor activity during the dark phase and alter the expression pattern of core clock genes in the hypothalami of mice. The circadian pattern of expression of an array of metabolic genes in the liver, skeletal muscle, and adipose tissue was also altered in mice exposed to SR9009, resulting in increased energy expenditure. In Diet-induced obese mice, SR9009 (100 mg/kg, i.p., b.i.d., for 30 days) could decrease fat mass and markedly improve dyslipidemia and hyperglycemia.
BP12441	JMS-17-2
BP12441	JMS-17-2 is a potent and selective antagonist of CX3CR1( IC50 : 0.32 nM).
BP12442	Vps34-IN-1
BP12442	Vps34-IN1 is a potent and highly selective Vps34 inhibitor with IC50 of 25 nM invitro, which does not significantly inhibit the isoforms of class I as well as class II PI3Ks.
BP12443	Vps34-PIK-III
BP12443	PIK-III, a selective inhibitor of VPS34 enzymatic activity, inhibits autophagy and results in the stabilization of autophagy substrates.
BP12444	Tropifexor
BP12444	Tropifexor is a novel and highly potent agonist of FXR with an EC50 of 0.2 nM.
BP12445	Samotolisib
BP12445	LY3023414 is an oral ATP competitive inhibitor of the class I PI3K isoforms, DNA-PK, and mTOR. LY3023414 has been used in trials studying the treatment of Neoplasm, Solid Tumor, COLON CANCER, BREAST CANCER, and Advanced Cancer, among others.
BP12446	LYS01
BP12446	LYS01 free base is a new lysosomal autophagy inhibitor.
BP12447	Lys05
BP12447	Lys05, or Lys01 trihydrochloride, is a potent, water soluble lysosomal autophagy inhibitor. Lys05 is a previously undescribed dimeric chloroquine which more potently accumulates in the lysosome and blocks autophagy compared with HCQ. Lys05 produced more potent antitumor activity as a single agent both in vitro and in vivo in multiple human cancer cell lines and xenograft models compared with HCQ. Lys05 is therefore a new lysosomal autophagy inhibitor that has potential to be developed further into a drug for cancer and other medical applications.
BP12448	BIX-01294 trihydrochloride
BP12448	BIX01294 is an inhibitor of G9a histone methyltransferase.In a cell-free assay, the IC50=2.7 μM for G9a histone methyltransferase.
BP12449	KN-93
BP12449	KN-93 is a selective inhibitor of Ca2+/calmodulin-dependent kinase II (CaMKII), competitively blocking CaM binding to the kinase.
BP12450	RSVA405
BP12450	RSVA 405 is an AMPK activator (EC50 = 1 μM), and is STAT3 inhibitor
BP12451	Vancomycin
BP12451	Vancomycin is an antibiotic used to treat serious bacterial infections by stopping the growth of bacteria.
BP12452	Vancomycin hydrochloride
BP12452	Vancomycin Hydrochloride is the hydrochloride salt of vancomycin, a branched tricyclic glycosylated peptide with bactericidal activity against most organisms and bacteriostatic effect on enterococci.
BP12453	ABT-751
BP12453	ABT-751 has been investigated for the treatment of Lung Cancer, Non-Small Cell Lung Cancer, and Non-Small-Cell Lung Cancer.
BP12454	Levosimendan
BP12454	Levosimendan is a calcium sensitizer used in the management of acutely decompensated congestive heart failure. It increases the sensitivity of the heart to calcium, thus increasing cardiac contractility without a rise in intracellular calcium. Levosimendan exerts its effect by increasing calcium sensitivity of myocytes by binding to cardiac troponin C in a calcium-dependent manner.
BP12455	Crizotinib hydrochloride
BP12455	Crizotinib hydrochloride is a novel inhibitor of anaplastic lymphoma kinase and c-Met(IC50s of 20 and 8 nM)
BP12456	Dronedarone hydrochloride
BP12456	Dronedarone hydrochloride is an amiodarone analog which has an effective and promising treatment for Atrial fibrillation.
BP12457	Dronedarone
BP12457	Dronedarone is an amiodarone analogue which has an effective and promising treatment for Atrial fibrillation.