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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.

  • 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.
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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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  • 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.
    • $35
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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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  • 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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  • 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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  • 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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  • 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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  • 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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  • Dexamethasone
    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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  • 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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  • 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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  • 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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  • ABT-737
    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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  • Metformin hydrochloride
    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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  • 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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  • P62-mediated mitophagy inducer
    T138091809031-84-2
    P62-mediated mitophagy inducer (PMI) is a regulator of mitophagy.
    • $39
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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.
    • $46
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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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  • AICAR
    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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  • Adezmapimod
    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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  • 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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  • 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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  • Oxidopamine hydrochloride
    T1235228094-15-7
    Oxidopamine hydrochloride (6-Hydroxydopamine hydrochloride) is an neurotransmitter dopamine antagonist.
    • $39
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  • Ginsenoside 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.
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  • Aspirin
    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.
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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). It exhibits antitumor activity and is used for treating kidney cancer and gastrointestinal tumors.
    • $53
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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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  • Iohexol
    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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  • Parthenolide
    T214020554-84-1
    Parthenolide ((-)-Parthenolide) is a natural sesquiterpene lactone that is an NF-κB inhibitor and also specifically inhibits HDAC1 protein, but is inactive against other class I II HDACs. Parthenolide has anti-inflammatory, anti-tumor, and anti-viral activities.
    • $50
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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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  • 5-Aminolevulinic acid hydrochloride
    T16625451-09-2
    5-Aminolevulinic acid hydrochloride (5-ALA) is an intermediate in heme biosynthesis and a universal precursor of tetrapyrroles.
    • $33
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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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  • Pitavastatin
    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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  • Oxidopamine hydrobromide
    T12352L636-00-0
    Oxidopamine hydrobromide (6-OHDA hydrobromide) is a neurotransmitter dopamine antagonist.
    • $56
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  • Liensinine
    T5S10992586-96-1
    1. Liensinine, a kind of isoquinoline alkaloid, can antagonize the ventricular arrhythmias.
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  • Ivermectin
    T113170288-86-7
    Ivermectin (MK-933) is an activator of glutamate-gated chloride channels (GluCls) with antiparasitic activity.
    • $32
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  • Melatonin
    T165973-31-4
    Melatonin (Melatonine) is a natural hormone secreted by the pineal gland that activates melatonin receptors. Melatonin is a hormone that regulates the biological clock and also has antioxidant and anti-inflammatory activities.
    • $31
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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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  • Matrine
    T2870519-02-8
    Matrine (Vegard), an alkaloid isolated from the Sophora genus, acts as a kappa opioid receptor agonist.
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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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  • 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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  • 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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  • 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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  • Isoniazid
    T097254-85-3
    Isoniazid (Isonicotinic hydrazide) is an antibacterial agent used primarily as a tuberculostatic.
    • $36
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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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  • 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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  • 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.
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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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  • 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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