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Mitophagy

Mitophagy is the selective degradation of mitochondria by autophagy. It often occurs to defective mitochondria following damage or stress. Mitophagy is key in keeping the cell healthy. It promotes turnover of mitochondria and prevents accumulation of dysfunctional mitochondria which can lead to cellular degeneration. It is mediated by Atg32 (in yeast) and NIX and its regulator BNIP3 in mammals. Mitophagy is regulated by PINK1 and parkin proteins. In addition to the selective removal of damaged mitochondria, mitophagy is also required to adjust mitochondrial numbers to changing cellular metabolic needs, for steady-state mitochondrial turnover, and during certain cellular developmental stages, such as during cellular differentiation of red blood cells.

  • 3-Methyladenine
    T18795142-23-4
    3-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.
    • $28
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  • Curcumin
    T1516458-37-7
    Curcumin (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
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  • Mdivi-1
    T1907338967-87-6
    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.
    • $39
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  • Dexamethasone
    T107650-02-2
    Dexamethasone (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.
    • $29
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  • Doxorubicin hydrochloride
    T102025316-40-9
    Doxorubicin 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
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  • Ruxolitinib
    T1829941678-49-5
    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.
    • $53
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  • Deferoxamine Mesylate
    T1637138-14-7
    Deferoxamine 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
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  • Olaparib
    T3015763113-22-0
    Olaparib (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
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  • Ruxolitinib phosphate
    T30431092939-17-7
    Ruxolitinib 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
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  • Etoposide
    T013233419-42-0
    Etoposide (VP-16-213) is a topoisomerase II inhibitor that inhibits DNA synthesis by forming a complex with topoisomerase II and DNA (IC50=60.3 μM). Etoposide has antitumor activity and induces apoptosis and autophagy.
    • $33
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  • Valproic acid sodium salt
    T16021069-66-5
    Valproic acid sodium salt (Sodium Valproate) is the sodium salt form of valproic acid with anti-epileptic activity. Valproic acid sodium salt is converted into its active form, valproate ion, in blood. Although the mechanism of action remains to be elucidated, Valproic acid sodium salt increases concentrations of gamma-aminobutyric acid (GABA) in the brain, probably due to inhibition of the enzymes responsible for the catabolism of GABA. This potentiates the synaptic actions of GABA. Valproic acid sodium salt may also affect potassium channels, thereby creating a direct membrane-stabilizing effect.
    • $42
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  • AICAR
    T14772627-69-2
    AICAR (NSC105823) is an AMP-activated protein kinase activator which is used for the treatment of acute lymphoblastic leukemia and may have applications in treating other disorders such as diabetes.
    • $30
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  • Naringin
    T059510236-47-2
    Naringin (Naringoside), a flavanone glycoside, exerts various of pharmacological effects such as blood lipid lowering, antioxidant activity, anticancer activity, and inhibition of cytochrome P450 enzymes.
    • $35
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  • Quercetin
    T2174117-39-5
    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.
    • $42
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  • Liensinine diperchlorate
    T4S11025088-90-4
    Liensinine Diperchlorate is an isoquinoline alkaloid extracted from the embryonic seeds of the sacred lotus. It inhibits late autophagy by blocking autophagosome-lysosome fusion and exhibits biological activities such as anti-arrhythmic, anti-hypertensive, anti-pulmonary fibrosis, and vascular smooth muscle relaxation.
    • $41
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  • Kaempferol
    T2177520-18-3
    Kaempferol (Robigenin) is a natural flavonoid and an inverse agonist of ERRα and ERRγ. Kaempferol has a wide range of antitumor, anti-inflammatory, antioxidant, antibacterial and antiviral activities.
    • $46
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  • Sulfosuccinimidyl oleate
    T13036135661-44-8In house
    Sulfosuccinimidyl oleate (Sulfo-N-succinimidyl oleate) (Sulfo-N-succinimidyl oleate) is a long chain fatty acid that inhibits fatty acid transport into cells. Sulfosuccinimidyl oleate is a potent and irreversible inhibitor of mitochondrial respiratory chain. Sulfosuccinimidyl oleate binds the CD36 receptor on the surface of microglia. Sulfosuccinimidyl oleate is neuroprotective and alleviates stroke-induced neuroinflammation [1] [2].
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  • Resveratrol
    T1558501-36-0
    Resveratrol (SRT 501) is a polyphenolic natural product, a plant antitoxin with antioxidant and chemopreventive activities. Resveratrol has a wide range of targets including COX, SIRT, LOC, etc. Resveratrol induces autophagy and apoptosis.
    • $36
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  • Brefeldin A
    T606220350-15-6
    Brefeldin A (Cyanein) belongs to the class of macrolide antibiotics and is an ATPase inhibitor (IC50=0.2 μM). Brefeldin A can induce tumor cell differentiation and apoptosis, and also possesses autophagy inhibitory activity.
    • $34
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  • Oxidopamine hydrochloride
    T1235228094-15-7
    Oxidopamine hydrochloride (6-Hydroxydopamine hydrochloride) is an neurotransmitter dopamine antagonist.
    • $39
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  • Vorinostat
    T1583149647-78-9
    Vorinostat (SAHA) is a pan-histone deacetylase (HDAC) inhibitor (IC50=10 nM) with inhibitory activity against HDAC1/2/3/6/7/11. Vorinostat has antitumor activity, induces cell differentiation, blocks the cell cycle and induces apoptosis.
    • $44
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  • U0126-EtOH
    T62231173097-76-1
    U0126-EtOH (U0126 Ethanol) is a non-ATP competitive specific inhibitor of MEK1/2 (IC50: 0.07/0.06 μM).
    • $30
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  • U0126
    T21332109511-58-2
    U0126, an effective and selective non-competitive inhibitor of MAP kinase, inhibits MEK-1 and MEK-2 with IC50 values of 0.07 and 0.06 μM respectively. U0126 inhibits autophagy and mitophagy.
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  • ABT-737
    T2099852808-04-9
    ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w (EC50s: 78.7/30.3/197.8 nM).
    • $64
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  • Tripterin
    T302834157-83-0
    Tripterin (Celastrol) is a natural product, a proteasome inhibitor that inhibits the pancreatic rennet-like activity of the 20S proteasome (IC50=2.5 μM). Tripterin has anti-inflammatory, anti-infectious, and immunomodulatory properties.
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  • Metformin hydrochloride
    T07401115-70-4
    Metformin hydrochloride (1,1-Dimethylbiguanide hydrochloride) , a widely used anti-diabetic drug, has a potential function as an anti-Y medicine. It inhibits the proliferation of a variety of Y cells including colon, prostate, and etc.
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  • Betulinic acid
    T2830472-15-1
    Betulinic acid (ALS-357) is a pentacyclic lupane-type triterpene derivative of betulin (isolated from the bark of Betula alba, the common white birch) which has antiretroviral, antimalarial, and anti-inflammatory properties, as well as a more recently discovered potential as an anticancer agent, by inhibition of topoisomerase.
    • $33
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  • Tanespimycin
    T629075747-14-7
    Tanespimycin (KOS 953) (17-AAG) is an inhibitor of Hsp90 that selectively inhibits BT474 tumor cell Hsp90 (IC50: 5 nM).
    • $38
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  • Oxidopamine hydrobromide
    T12352L636-00-0
    Oxidopamine hydrobromide (6-OHDA hydrobromide) is a neurotransmitter dopamine antagonist.
    • $56
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  • URB-597
    T6714546141-08-6
    URB-597 (FAAH Inhibitor II) is an effective, orally bioavailable FAAH inhibitor (IC50: 4.6 nM), and no effect on other cannabinoid-related targets.
    • $34
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  • 5-Aminolevulinic acid hydrochloride
    T16625451-09-2
    5-Aminolevulinic acid hydrochloride (5-ALA) serves as an intermediate in the body's heme biosynthesis and is the universal precursor of tetrapyrroles.
    • $33
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  • Melatonin
    T165973-31-4
    Melatonin (Melatonine) is a biogenic amine that is found in animals and plants. In mammals, melatonin is produced by the PINEAL GLAND. Its secretion increases in darkness and decreases during exposure to light. Melatonin is implicated in the regulation of SLEEP, mood, and REPRODUCTION. Melatonin is also an effective antioxidant.
    • $31
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  • Sunitinib
    T0374L557795-19-4
    Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that inhibits VEGFR2 and PDGFRβ (IC50=80/2 nM). Sunitinib has antitumor activity and can be used for the treatment of kidney cancer and gastrointestinal tumors.
    • $53
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  • Pitavastatin calcium
    T2534147526-32-7
    Pitavastatin calcium (NK-104) is a potent inhibitor of HMG-CoA reductase (Ki: 1.7 nM). It lowers both total cholesterol and low-density lipoprotein cholesterol in animals and humans. Metabolism of pitavastatin by the cytochrome P450 system is minimal, reducing the risk of drug-drug interactions.
    • $34
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  • Aspirin
    T000550-78-2
    Aspirin (Acetylsalicylic Acid) is a potent and selective inhibitor of COX with various pharmacological activities, such as anti-inflammation and pain relief. Aspirin is a histone deacetylase inhibitors to up-regulate cell cycle arrest protein p21, which can suppresses ovarian Y cells harboring COX-1. Aspirin also inhibits the expression of COX-2 in HUVEC and neonatal rat ventricular cardiomyocytes, and then reduce PG production and the down-regulation of ERK and NF-KB, respectively.
    • $31
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  • Adezmapimod
    T1764152121-47-6
    Adezmapimod (SB 203580) is a p38 MAPK inhibitor (IC50=0.3-0.5 μM) that is selective and ATP-competitive. Adezmapimod possesses autophagy and mitochondrial autophagy activating activity. Adezmapimod displays more than 100-fold higher selectivity than PKB, LCK, and GSK-3β.
    • $30
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  • Simvastatin
    T068779902-63-9
    Simvastatin (MK 733) is an HMG-CoA reductase inhibitor (Ki=0.2 nM) with oral activity. Simvastatin has hypolipidemic activity, inhibits hepatic production of cholesterol, and is also used for the prevention of cardiovascular disease.
    • $36
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  • Polydatin
    T342727208-80-6
    Polydatin (Piceid), the glycoside of Resveratrol, is originally isolated from the Chinese herb Polygonum cuspidatum. The compound can inhibit platelet aggregation and elevate the ratios of LDL-C/HDL-C and TC/HDL-C. In the myocardial cell, white blood cell, vascular smooth muscle cell, and endothelial cell, Polydatin can inhibit ICAM-1 expression, elevate Ca2+, weaken white blood cell-endothelial cell adhesion, and activate KATP channels.
    • $41
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  • Carbamazepine
    T0943298-46-4
    Carbamazepine (NSC-169864) is a tricyclic compound chemically related to tricyclic antidepressants (TCA) with anticonvulsant and analgesic properties. Carbamazepine exerts its anticonvulsant activity by reducing polysynaptic responses and blocking post-tetanic potentiation. Its analgesic activity is not understood; however, carbamazepine is commonly used to treat pain associated with trigeminal neuralgia.
    • $37
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  • Metformin
    T8526657-24-9
    Metformin (1,1-Dimethylbiguanide) is an AMPK activator with blood-brain barrier permeability. Metformin may improve glycemic control by increasing insulin sensitivity and decreasing intestinal glucose uptake, and is commonly used in type 2 diabetes research.
    • $39
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  • Valproic Acid
    T706499-66-1
    Valproic Acid (2-Propylpentanoic Acid) is an HDAC inhibitor that inhibits HDAC1 activity, induces HDAC2 degradation, and is orally active. Valproic Acid can be used in epilepsy and bipolar disorder research.
    • $50
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  • Quinacrine dihydrochloride
    T094269-05-6
    Quinacrine dihydrochloride (Mepacrine dihydrochloride) is the dihydrochloride salt of the 9-aminoacridine derivative quinacrine with potential antineoplastic and antiparasitic activities.
    • $41
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  • Esmolol hydrochloride
    T150381161-17-3
    Esmolol is a cardioselective beta-blocker used in parenteral forms in the treatment of arrhythmias and severe hypertension. Esmolol has not been linked to instances of clinically apparent drug induced liver injury.
    • $50
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  • Doxazosin mesylate
    T010177883-43-3
    Doxazosin mesylate (UK 33274 mesylate)(UK 33274) is a quinazoline-derivative. It is a selectively antagonizes postsynaptic α1-adrenergic receptors.
    • $38
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  • Salicylic acid
    T064969-72-7
    Salicylic acid (2-Hydroxybenzoic acid), a natural compound extracted from Willow bark, is an anti-inflammatory inhibitor of activity cyclooxygenase.
    • $33
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  • GSK3-IN-3
    T73331331963-27-0
    GSK3-IN-3 is a mitochondrial autophagy (mitophagy) inducer and GSK-3 inhibitor (IC50: 3.01 μM) that induces parkin-dependent mitochondrial autophagy. GSK3-IN-3 is non-ATP and non-substrate competitive and neuroprotective against 6-OHDA.
    • $34
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  • Liensinine
    T5S10992586-96-1
    1. Liensinine, a kind of isoquinoline alkaloid, can antagonize the ventricular arrhythmias.
    • $47
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  • Sunitinib Malate
    T0374341031-54-7
    Sunitinib Malate (Sunitinib) is an indolinone-based tyrosine kinase inhibitor. It blocks the tyrosine kinase activities of VEGFR2, PDGFRβ (IC50: 80/2 nM), and c-kit.
    • $37
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  • D-glutamine
    T64685959-95-5
    D-Glutamine is the D-type stereoisomer of cell-permeable glutamine, one of the 20 amino acids encoded by the standardized genetic code.
    • $30
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  • Dexamethasone acetate
    T09471177-87-3
    Dexamethasone acetate (NSC 39471) is the acetate salt form of Dexamethasone, a synthetic adrenal corticosteroid with potent anti-inflammatory properties. In addition to binding to specific nuclear steroid receptors, dexamethasone also interferes with NF-kB activation and apoptotic pathways. This agent lacks the salt-retaining properties of other related adrenal hormones.
    • $45
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