Mitophagy

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  1. AMPK activator

    Acadesine is a selective activator of AMPK in both hepatocytes and adipocytes.

  2. PARP inhibitor

    Olaparib (AZD2281) is an inhibitor of poly ADP ribose polymerase (PARP), an enzyme involved in DNA repair.
  3. Celastrol is a triterpenoid antioxidant compound isolated from the Chinese Thunder of God vine (T. wilfordii). In an isolated rat liver assay of lipid peroxidation, celastrol had an IC50 value of 7 µM, equivalent to about 15 times the antioxidant potency of α-tocopherol.

  4. Bcl-2 Inhibitor

    ABT-737 is a pan-Bcl-2 inhibitor. IC50 values ranged from 192 nM (the pre-B cell line Hal-01) to <10 μM (Nalm-6, K562 and HL-60).
  5. glucocorticoid receptor agonist

    Dexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs. It acts as an anti-inflammatory and immunosuppressant. Its potency is about 20-30 times that of the naturally occurring hormone hydrocortisone and 4-5 times of prednisone.
  6. Topoisomerase II inhibitor

    Etoposide forms a ternary complex with DNA and the topoisomerase II enzyme (which aids in DNA unwinding), prevents re-ligation of the DNA strands, and by doing so causes DNA strands to break. Therefore, this causes errors in DNA synthesis and promotes apoptosis of the cancer cell.
  7. Ivermectin is a broad-spectrum antiparasitic avermectin medicine.
  8. ERRα and ERRγ inverse agonist

    Kaempferol is found to inhibit bovine aorta myosin light chain kinase with a Ki of 0.3-0.5 microM and also is found to inhibit VEGF expression and in vitro angiogenesis through a novel ERK-NFκB-cMyc-p21 pathway.
  9. MT1/MT2 agonist

    Melatonin is a endogenous hormone that acts as an agonist at melatonin receptors MT1 and MT2.
  10. Metformin hydrochloride is a biguanide hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification.
  11. Parthenolide ((-)-Parthenolide) is a sesquiterpene lactone which occurs naturally in the plant feverfew (Tanacetum parthenium).
  12. HMG-CoA reductase inhibitor

    Pitavastatin Calcium is a competitive inhibitor of the enzyme HMGCR (HMG-CoA reductase) results in a reduction in LDL cholesterol synthesis.
  13. PLA inhibitor

    Polydatin protects cerebral cells from ischemic damages via improvement of microcirculation and inhibition of platelet aggregation. In addition, polydatin inhibits ICAM-1 expression in endothelial cells stimulated by lipopolysaccharide; it also attenuates adhesion between white blood cells and endothelial cells.
  14. mTOR Inhibitor

    PP242 is a potent and selective mTOR inhibitor in both mTORC1 and mTORC2.
  15. MAO-B inhibitor

    Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C.
  16. MAO-B inhibitor

    Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C.
  17. Resveratrol has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases???LOX, IC50=2.7 μM???, kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects.
  18. Salidroside (Rhodioloside) is a glucoside of tyrosol found in the plant Rhodiola rosea. It is thought to be one of the compounds responsible for the antidepressant and anxiolytic actions of this plant, along with rosavin.
  19. HMG-CoA reductase inhibitor

    Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM.
  20. HDAC inhibitor

    Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2.
  21. RTK inhibitor

    Sunitinib is an oral, small-molecule, multi-targeted receptor tyrosine kinase (RTK) inhibitor for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST).
  22. MEK inhibitor

    U0126-EtOH is an inhibitor of both MEK1 and MEK2 with an IC50 of 72 nM and 58 nM respectively.
  23. HDAC inhibitor

    Vorinostat is an inhibitor of HDACs, inhibiting deacetylation and leading to an accumulation of both hyperacetylated histones and transcription factors.
  24. JAK1/2 Inhibitor

    INCB018424 is a potent and selective inhibitor of Janus-associated kinase (JAK) 1 and 2, with IC50 to be 2.7, 4.5 and 332 nM for JAK1, JAK2 and JAK3 respectively;
  25. PDGFR/FLT3 Inhibitor

    Crenolanib (CP-868596) is an orally bioavailable, selective small molecule inhibitor of the PDGFR tyrosine kinase, inhibiting both PDGFRA and PDGFRB at picomolar concentrations.
  26. Autophagy/PI3K Inhibitor

    3-Methyladenine is an inhibitor of class III phosphatidylinositol 3-kinase (PI 3-kinase).
  27. Protein translocation Inhibitor

    Brefeldin A blocks binding of ADP-ribosylation factor to the Golgi apparatus and inhibits GDP-GTP exchange.
  28. JAK1/2 inhibitor

    Ruxolitinib sulfate (INCB018424 sulfate) is the first potent, selective JAK1/2 inhibitor to enter the clinic with IC50s of 3.3 nM/2.8 nM, and has > 130-fold selectivity for JAK1/2 versus JAK3.
  29. JAK inhibitor

    Ruxolitinib Phosphate is the phosphate salt form of ruxolitinib, an orally bioavailable Janus-associated kinase (JAK) inhibitor with potential antineoplastic and immunomodulating activities.
  30. AMP-activated protein kinase (AMPK) activator

    Metformin is an AMP-activated protein kinase (AMPK) activator that improves glycemic control by improving insulin sensitivity and decreasing intestinal absorption of glucose.
  31. COX-1/COX-2 inhibitor

    Aspirin is a non-selective and irreversible inhibitor of COX-1 and COX-2 with IC50s of 5 and 210 μg/mL.
  32. Betulinic acid is a naturally occurring pentacyclic triterpenoid which has antiretroviral, antimalarial, and anti-inflammatory properties.
  33. Mitochondrial respiratory chain inhibitor

    Sulfosuccinimidyl 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.
  34. HMG-CoA reductase inhibitor

    Pitavastatin Lactone is an HMG-CoA reductase inhibitor.
  35. DRP1 inhibitor

    Mdivi-1 is a selective cell-permeable inhibitor of mitochondrial division DRP1 (dynamin-related GTPase) and mitochondrial division Dynamin I (Dnm1) with IC50 of 1-10 uM.
  36. Topoisomerase II inhibitor

    Doxorubicin is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage and apoptosis.
  37. Polydatin, a natural precursor of resveratrol, induces β-defensin production and reduces inflammatory response.
  38. JAK inhibitor

    S-Ruxolitinib is the chirality of INCB018424, is a potent and selective small-molecule Janus kinase 1 (JAK1) and JAK2 inhibitor.
  39. glucocorticoid receptor agonist

    Dexamethasone acetate (Dexamethasone 21-acetate) is a glucocorticoid receptor agonist.
  40. Mitochonic Acid 5 is a derivative of the plant hormone indole-3-acetic acid.
  41. glucocorticoid receptor agonist

    Dexamethasone Phosphate disodium is a is a water-soluble form of the synthetic glucocorticoid dexamethasone.
  42. HDAC inhibitor

    Valproic acid is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2; Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.
  43. multi-targeted receptor tyrosine kinase inhibitor

    Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively.
  44. glucocorticoid receptor agonist

    Dexamethasone palmitate (DXP) is a prodrug of Dexamethasone, which is a glucocorticoid receptor agonist. Dexamethasone palmitate (DXP) has a 47-fold lower affinity for the glucocorticoid receptor than Dexamethasone. Anti-inflammatory agent.
  45. mitophagy regulator

    P62-mediated mitophagy inducer is a mitophagy regulator which activates mitophagy without recruiting Parkin or collapsing δ??m and retains activity in cells devoid of a fully functional PINK1/Parkin pathway.
  46. Urolithin A, a gut-microbial metabolite of ellagic acid, exerts anti-inflammatory, antiproliferative, and antioxidant properties. Urolithin A induces autophagy and apoptosis, suppresses cell cycle progression, and inhibits DNA synthesis.
  47. AMP-activated protein kinase activator

    AICAR phosphate is an activator of AMP-activated protein kinase (AMPK).
  48. autophagy/mitophagy inhibitor

    Liensinine is an autophagy/mitophagy inhibitor. Liensinine, a major isoquinoline alkaloid, extracted from the seed embryo of Nelumbo nucifera Gaertn, has a wide range of biological activities, including anti-arrhythmias, anti-hypertension, anti-pulmonary fibrosis, relaxation on vascular smooth muscle, etc.
  49. antiviral agent

    cis-Resveratrol exhibits signifcant antiviral activity. cis-Resveratrol inhibits enteroviruses with IC50s of 12.2 ?M and 37.6 ?M for coxsackievirus B3 (CVB3) and enterovirus 71 (EV71), respectively.

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