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AutophagyMitophagy
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.
Olaparib
Cited
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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CitedDoxorubicin hydrochloride Cited
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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CitedRuxolitinib Cited
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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CitedMdivi-1 Cited
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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CitedRuxolitinib phosphate Cited
T30431092939-17-7
Ruxolitinib phosphate (INCB18424 phosphate) is a JAK1 2 inhibitor with IC50 of 3.3 nM 2.8 nM. Its selectivity for JAK1 2 is more than 130 times that of JAK3.
- $44
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CitedMetformin Cited
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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CitedABT-737 Cited
T2099852808-04-9
ABT-737 is a BH3 mimetic and an inhibitor of Bcl-2, Bcl-xL, and Bcl-w (EC50=30.3 nM 78.7 nM 197.8 nM). ABT-737 exhibits antitumor activity and anti-aging activity.
- $64
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CitedBrefeldin A Cited
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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CitedDeferoxamine Mesylate Cited
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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CitedDexamethasone Cited
T107650-02-2
Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist and IL receptor modulator with anti-inflammatory and immunosuppressive properties that induces autophagy and inhibits LPS-induced inflammatory responses in macrophages.
- $29
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CitedQuercetin Cited
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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CitedKaempferol Cited
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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CitedMetformin hydrochloride Cited
T07401115-70-4
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.
- $33
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CitedAdezmapimod Cited
T1764152121-47-6
Adezmapimod (SB 203580) is a selective, ATP-competitive p38 MAPK inhibitor (IC50=0.3-0.5 μM) that activates autophagy and mitochondrial autophagy, with more than 100-fold higher selectivity over PKB, LCK, and GSK-3β.
- $30
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CitedTripterin Cited
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.
- $46
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CitedP62-mediated mitophagy inducer
T138091809031-84-2
P62-mediated mitophagy inducer (PMI) is a regulator of mitophagy.
- $39
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Tanespimycin
Cited
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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CitedGinsenoside Rb1
T282241753-43-9
Ginsenoside Rb1 (Gypenoside Ⅲ) is part of a class of steroid glycosides; may have properties that inhibit or prevent the growth of tumors.
- $39
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Vorinostat Cited
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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CitedOxidopamine hydrochloride Cited
T1235228094-15-7
Oxidopamine hydrochloride (6-Hydroxydopamine hydrochloride) is an neurotransmitter dopamine antagonist.
- $39
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CitedAICAR Cited
T14772627-69-2
AICAR (Acadesine) is an AMPK activator that causes ZMP accumulation, thereby mimicking the stimulatory effect of AMP on both AMPK and AMPKK. It is commonly used in research related to diabetes, cardiovascular diseases, and tumors.
- $30
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CitedIohexol
T155466108-95-0
Iohexol is an X-ray contrast agent containing varying concentrations of iohexol, which can be used for a variety of imaging applications.
- $41
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Oxidopamine hydrobromide Cited
T12352L636-00-0
Oxidopamine hydrobromide (6-OHDA hydrobromide) is a neurotransmitter dopamine antagonist.
- $56
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CitedAspirin Cited
T000550-78-2
Aspirin (Acetylsalicylic Acid) is a COX inhibitor that inhibits COX1 and COX2 (IC50=5 210 μg mL) with selective, irreversible, and oral activity. Aspirin is also a histone deacetylase inhibitor that up-regulates the cell cycle blocking protein, p21. Aspirin has a variety of activities. Aspirin has anti-inflammatory, antipyretic and analgesic, and antiplatelet aggregation activities.
- $31
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CitedU0126-EtOH Cited
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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CitedSunitinib Cited
T0374L557795-19-4
Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that inhibits VEGFR2 and PDGFRβ (IC50=80 2 nM). It exhibits antitumor activity and is used for treating kidney cancer and gastrointestinal tumors.
- $53
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CitedPitavastatin
T7072147511-69-1
Pitavastatin (NK-104) is a potent inhibitor of hydroxymethylglutaryl-CoA (HMG-CoA) reductase, effectively inhibiting cholesterol synthesis from acetic acid in HepG2 cells with an IC50 of 5.8 nM. It also induces hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptors and exhibits therapeutic activities such as anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective, and reno-protective effects.
- $970
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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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Quinacrine dihydrochloride Cited
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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CitedValproic acid sodium salt Cited
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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CitedNaringin Cited
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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CitedIsoniazid
T097254-85-3
Isoniazid (Isonicotinic hydrazide) is an antibacterial agent used primarily as a tuberculostatic.
- $36
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Carbamazepine Cited
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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CitedPitavastatin calcium Cited
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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CitedSunitinib 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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Torkinib
T24141092351-67-1
Torkinib (PP 242) (PP 242) is a selective and ATP-competitive mTOR inhibitor (IC50: 8 nM). It also inhibits mTORC1 2 (IC50s: 30 58 nM).
- $52
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AICAR phosphate
T14149681006-28-0
AICAR phosphate (Acadesine phosphate) is an AMPK activator and inhibitor of autophagy, YAP, and mitophagy. It serves as an adenosine analog, regulating glucose and lipid metabolism, and inhibiting the production of pro-inflammatory cytokines and iNOS.
- $49
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BC1618
T89292222094-18-8
BC1618 (2-Propanol, 1-[bis(phenylmethyl)amino]-3-[4-(trifluoromethyl)phenoxy]-) is an orally active Fbxo48 inhibitor that stimulates Ampk-dependent signaling. It promotes mitochondrial fission, promotes autophagy and improves hepatic insulin sensitivity.
- $30
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Clioquinol
T0876130-26-7
Clioquinol (Iodochlorhydroxyquin) is an orally bioavailable, lipophilic, copper-binding, halogenated 8-hydroxyquinoline with antifungal, antiparasitic and potential antitumor activities.
- $31
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URB-597 Cited
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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CitedDoxazosin 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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Resveratrol analog 1
T12708861446-16-4
Resveratrol analog 1, an analog of Resveratrol, is a natural polyphenolic phytoalexin with antioxidant, anti-inflammatory, cardioprotective, and anti-cancer properties.
- $39
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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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GSK2578215A
T22401285515-21-0
GSK2578215A is a potent and selective LRRK2 kinase inhibitor.
- $29
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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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U0126 Cited
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.
- $158
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CitedSulfosuccinimidyl oleate
T13036135661-44-8In house
Sulfosuccinimidyl oleate (Sulfo-N-succinimidyl oleate) is a long-chain fatty acid that inhibits fatty acid transport into cells. It is a potent and irreversible inhibitor of the mitochondrial respiratory chain and binds the CD36 receptor on the surface of microglia. Sulfosuccinimidyl oleate is neuroprotective and alleviates stroke-induced neuroinflammation [1] [2].
- $1,520
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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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