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Autophagy
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Autophagy
Autophagy is the natural, regulated mechanism of the cell that removes unnecessary or disfunctional components. It allows the orderly degradation and recycling of cellular components. Three forms of autophagy are commonly described: macroautophagy, microautophagy, and chaperone-mediated autophagy (CMA). In macroautophagy, expendable cytoplasmic constituents are targeted and isolated from the rest of the cell within a double-membraned vesicle known as an autophagosome, which, in time, fuses with an available lysosome, bringing its specialty process of waste management and disposal; and eventually the contents of the vesicle (now called an autolysosome) are degraded and recycled.
- ChloroquineT868954-05-7Chloroquine is a Toll-like receptor inhibitor that inhibits autophagy. Chloroquine has anti-malarial and anti-inflammatory activity and is widely used in the treatment of malaria and rheumatoid arthritis. Chloroquine also has anti-SARS-CoV-2 (COVID-19) activity and anti-HIV-1 activity.
- $43.2
- $54
SizeQTY
Cited - PX-478T6961685898-44-6PX-478 is a HIF-1α inhibitor with selectivity, oral activity, and blood-brain barrier permeability. PX-478 has antitumor activity and also protects pancreatic β-cell function in diabetes mellitus and is used in type 2 diabetes mellitus research.
- $48
SizeQTY Cited - CurcuminT1516458-37-7Curcumin (Natural Yellow 3) is a phenolic natural product, an inhibitor of histone acetyltransferase p300/CREB (IC50=25 μM) with specificity. Curcumin has a wide range of pharmacological activities such as antitumor, anti-inflammatory and antioxidant.
- $30
SizeQTY Cited - SorafenibT0093L284461-73-0Sorafenib (Bay 43-9006) is a multikinase inhibitor that inhibits 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. Sorafenib has antitumor activity and can induce autophagy and apoptosis as well as agonistic ferroptosis.
- $34
SizeQTY Cited - RegorafenibT1792755037-03-7Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ and is orally active. Regorafenib has antitumor and anti-angiogenic activity.
- $30
SizeQTY Cited - RapamycinT153753123-88-9Rapamycin (AY 22989) is a natural product of macrolides, an mTOR inhibitor with specificity (HEK293 cells: IC50=0.1 nM). Rapamycin has immunosuppressive activity and induces autophagy.
- $30
SizeQTY Cited - VerteporfinT3112129497-78-5Verteporfin (BPD-MA) is a YAP inhibitor that inhibits YAP-TEAD interactions. Verteporfin is also a photosensitizer used in photodynamic therapy. Verteporfin also induces apoptosis and inhibits autophagy.
- $34
SizeQTY Cited - MPP+ iodideT916936913-39-0MPP+ iodide, the metabolite of a neurotoxin MPTP, causes symptom of Parkinson's disease (PD) in animal models by selectively destroying dopaminergic neurons in substantia nigra. MPP+ induces dopamine transporter (DAT) externalization in dopaminergic (DA)
- $33
SizeQTY - ML-SA5T600362418670-70-7ML-SA5 is an MCOLN1 agonist and arrests autophagic flux by perturbing fusion between autophagosomes and lysosomes.
- $33
SizeQTY - LuminespibT1989747412-49-3Luminespib (VER-52296) is a new-type inhibitor of HSP90 (IC50s: 7.8 21 nM for HSP90α β in cell free assay).
- $52
SizeQTY Cited - BI-D1870T6171501437-28-1BI-D1870 is a cell-permeable, ATP-competitive inhibitor of ribosomal S6 kinases (RSKs; IC50s: 31 24 18 15 nM for RSK1 2 3 4).
- $48
SizeQTY Cited - Mdivi-1T1907338967-87-6Mdivi-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.
- $39
SizeQTY Cited - EnzalutamideT6002915087-33-1Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist (IC50=36 nM in LNCaP). Enzalutamide activates autophagy, has antitumor activity, and is commonly used in the treatment of desmoplasia-resistant prostate cancer.
- $40
SizeQTY Cited - BortezomibT2399179324-69-7Bortezomib (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.
- $48
SizeQTY Cited - VenetoclaxT21191257044-40-8Venetoclax (ABT-199) is a Bcl-2 inhibitor (Ki<0.01 nM) with potent, selective, and orally active properties. Venetoclax has a 3-order-of-magnitude lower affinity for Bcl-xL and Bcl-W (Kis=48/245 nM). Venetoclax induces autophagy and apoptosis.
- $48
SizeQTY Cited - CHIR-99021T2310252917-06-9CHIR-99021 (CT99021) is an activator of the Wnt/β-catenin signaling pathway and a GSK-3α/β inhibitor (IC50=10/6.7 nM) with selective and oral activity.CHIR-99021 induces cellular autophagy, which enhances self-renewal in mouse and human embryonic stem cells.
- $36
SizeQTY Cited - (+)-JQ-1T21101268524-70-4(+)-JQ-1 (JQ1) is a BET bromine domain inhibitor that inhibits BRD4 (1 2) (IC50=77 33 nM) with specificity and reversibility. (+)-JQ-1 induces cell autophagy and inhibits cell proliferation.
- $30
SizeQTY Cited - MK-2206 dihydrochlorideT19521032350-13-2MK-2206 dihydrochloride (MK-2206 2HCl) is a variant Akt inhibitor that inhibits Akt1, Akt2, and Akt3 (IC50=8 12 65 nM) with orally active, highly potent and selective potency. MK-2206 dihydrochloride exhibits antitumor activity.
- $30
SizeQTY Cited - ElexacaftorT149352216712-66-0Elexacaftor (VX-445) is a modulator of cystic fibrosis transmembrane conductance regulator (CFTR) and it also facilitates the processing and trafficking of CFTR to increase the amount of CFTR at the cell surface.
- $89
SizeQTY - Deferoxamine MesylateT1637138-14-7Deferoxamine Mesylate (DFOM) is an iron chelator and ferroptosis inhibitor. Deferoxamine Mesylate binds free iron into a stable complex and reduces iron accumulation. Deferoxamine Mesylate up-regulates HIF-1α levels and induces apoptosis.
- $31
SizeQTY Cited - OxaliplatinT016461825-94-3Oxaliplatin (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.
- $50
SizeQTY Cited - MG-132T2154133407-82-6MG-132 (Z-Leu-Leu-Leu-al) is a 26S proteasome inhibitor (IC50=100 nM) that is cell-permeable and reversible. MG-132 acts as an autophagy activator and also induces apoptosis.
- $40
SizeQTY Cited - ForskolinT293966575-29-9Forskolin (Coleonol) is a natural product, an adenylate cyclase activator (EC50=0.5 μM). Forskolin increases cAMP levels, activates PXR and FXR, and induces autophagy. Forskolin produces positive inotropic effects in the heart, and has platelet anticoagulant and antihypertensive effects.
- $36
SizeQTY Cited - TemozolomideT117885622-93-1Temozolomide (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.
- $42
SizeQTY Cited - Bafilomycin A1T674088899-55-2Bafilomycin A1 belongs to the macrolide class of antibiotics and is a V-ATPase inhibitor (IC50=0.44 nM) that is specific and reversible. Bafilomycin A1 is an inhibitor of the late phase of autophagy, blocking the fusion of autophagosomes with lysosomes. Bafilomycin A1 also induces apoptosis.
- $287
SizeQTY Cited - DexamethasoneT107650-02-2Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist and an IL receptor modulator. Dexamethasone has anti-inflammatory and immunosuppressive activity and induces autophagy. Dexamethasone inhibits LPS-induced inflammatory responses in macrophages.
- $45
SizeQTY Cited - 3-MethyladenineT18795142-23-43-Methyladenine (3-MA) is a PI3K inhibitor that selectively inhibits class IB PI3Kγ (IC50=60 μM) and class III VPS34 (IC50=25 μM). 3-Methyladenine inhibits autophagy.
- $35
SizeQTY Cited - RuxolitinibT1829941678-49-5Ruxolitinib (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.
- $53
SizeQTY Cited - Doxorubicin hydrochlorideT102025316-40-9Doxorubicin hydrochloride (Adriamycin) belongs to the anthracycline class of antibiotics and is an inhibitor of human DNA topoisomerase I II (IC50=0.8 2.67 μM). Doxorubicin hydrochloride exhibits cytotoxicity and antitumor activity. Doxorubicin hydrochloride reduces the phosphorylation of AMPK and its downstream target protein acetyl coenzyme A carboxylase, and induces apoptosis and autophagy.
- $34
SizeQTY Cited - TelaglenastatT67971439399-58-2Telaglenastat (CB 839) (IC50 of 24 nM), an effective, specific, and oral inhibitor, which is bioavailable glutaminase, for recombinant human GAC.
- $32
SizeQTY Cited - Urolithin AT71741143-70-0Urolithin A is a secondary metabolite of ellagic acid, a polyphenolic antioxidant, that has antiproliferative, anti-inflammatory, and anti-oxidant properties.
- $42
SizeQTY Cited - LY294002T2008154447-36-6LY294002 (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.
- $34
SizeQTY Cited - (E)-DaporinadT2644658084-64-1(E)-Daporinad (FK866) is a small molecule inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase), with potential antineoplastic and antiangiogenic activities.
- $36
SizeQTY Cited - Vinorelbine ditartrateT6213125317-39-7Vinorelbine ditartrate (KW-2307), a semi-synthetic vinca alkaloid, interacts with tubulin resulting in mitosis inhibition.
- $30
SizeQTY Cited - StreptozocinT150718883-66-4Streptozocin (NSC-85998) is an antibiotic that induces DNA methylation. Streptozocin is toxic to insulin-producing pancreatic islet B-cells and is commonly used in the construction of animal models of type 1 diabetes. The product is unstable in solution and is recommended to be dispensed now.
- $30
SizeQTY Cited - GemcitabineT025195058-81-4Gemcitabine (LY188011) is a synthetic cytosine nucleoside derivative and an inhibitor of DNA synthesis. Gemcitabine has antitumor and antimetabolic activities. Gemcitabine induces autophagy and apoptosis.
- $34
SizeQTY Cited - QuizartinibT2066950769-58-1Quizartinib (AC220) is an inhibitor of FLT3 (Kd: 1.6 nM) and demonstrates high selectivity for FLT3 when tested against a panel of 227 additional kinases.
- $53
SizeQTY Cited - OlaparibT3015763113-22-0Olaparib (KU0059436) is a small molecule inhibitor of PARP1 PARP2 (IC50=5 1 nM), with weak inhibitory activity against PARP tankyrase-1 (IC50=1.5 μM), and is selective and orally active. Olaparib exhibits autophagy and mitochondrial autophagy activation activity.
- $31
SizeQTY Cited - Obeticholic AcidT1789459789-99-2Obeticholic Acid (6-ECDCA) is a Farnesoid X Receptor Agonist. The mechanism of action of obeticholic acid is as a Farnesoid X Receptor Agonist.
- $41
SizeQTY - GCN2iBT113752183470-12-2GCN2iB is an ATP-competitive inhibitor of a serine/threonine-protein kinase general control nonderepressible 2 (GCN2), with an IC50 of 2.4 nM.
- $77
SizeQTY - DAPTT6202208255-80-5DAPT (LY-374973) is a γ-secretase inhibitor that inhibits total Aβ and Aβ42 (IC50=115/200 nM) and is orally active. DAPT is also a Notch inhibitor. DAPT induces cell differentiation, autophagy and apoptosis.
- $53
SizeQTY Cited - AtezolizumabT99021380723-44-3Atezolizumab (anti-PD-L1) is a fully humanized IgG1 monoclonal antibody that blocks the interaction of PD-L1 with both PD-1 and B7.1 but not the interaction of PD-L2 with PD-1.
- $229
SizeQTY - CisplatinT156415663-27-1Cisplatin (CDDP) is a DNA cross-linking agent. Cisplatin has antitumor activity and inhibits DNA synthesis by forming DNA adducts in cancer cells. Cisplatin also activates ferroptosis and induces autophagy.
- $28
SizeQTY Cited - Necrostatin-1T18474311-88-0Necrostatin-1 (Nec-1) is a necrotic apoptosis inhibitor and RIP1 inhibitor with specificity. Necrostatin-1 inhibits TNF-α-induced necrotic apoptosis. Necrostatin-1 also inhibits IDO.
- $30
SizeQTY Cited - Ruxolitinib phosphateT30431092939-17-7Ruxolitinib phosphate (INCB018424)(INCB018424 phosphate) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus JAK3.
- $44
SizeQTY Cited - ButeinT6427487-52-5Butein (2’,3,4,4’-tetrahydroxy Chalcone), a plant polyphenol, is isolated from Rhus verniciflua. It can inhibit the activation of protein tyrosine kinase, NF-κB and STAT3, and also can inhibit EGFR.
- $36
SizeQTY Cited - CapivasertibT19201143532-39-1Capivasertib (AZD5363) is a broad-spectrum AKT inhibitor with inhibitory activity against Akt1, Akt2, and Akt3 (IC50=3 7 7 nM) with oral activity. Capivasertib has antitumor activity for the treatment of breast cancer.
- $34
SizeQTY Cited - PaclitaxelT096833069-62-4Paclitaxel (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.
- $34
SizeQTY Cited - BilobalideT280833570-04-6Bilobalide ((-)-Bilobalide), a bioactive from Gingko Biloba, is active on hypoxia-induced alterations.
- $50
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