Autophagy Signaling

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  1. Autophagy inhibitor

    Lys05 is a potent lysosomal autophagy inhibitor. Lys05 is a previously undescribed dimeric chloroquine which more potently accumulates in the lysosome and blocks autophagy compared with HCQ.
  2. Azithromycin Dihydrate is an acid stable orally administered macrolide antimicrobial drug, structurally related to erythromycin.
  3. Chloroquine phosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator.
  4. glucocorticoid receptor agonist

    Dexamethasone acetate (Dexamethasone 21-acetate) is a glucocorticoid receptor agonist.
  5. GPR35/CXCR8 agonist

    Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8.
  6. Sevelamer hydrochloride is a phosphate binding drug used to treat hyperphosphatemia in patients with chronic kidney disease; consists of polyallylamine that is crosslinked with epichlorohydrin.
  7. ULK1 activator

    LYN-1604 is a potential ULK1 agonist with IC50 of 1.66 μM against MDA-MB-231 cells and it binds to wild-type ULK1 with a binding affinity in the nanomole range (Kd=291.4 nM). The ULK1 (Y89A) mutant protein caused a sharp decrease in binding affinity with lower response and Kd than wild-type ULK1, ULK1 (K50A) and ULK1 (L53A) mutants.
  8. Mitochonic Acid 5 is a derivative of the plant hormone indole-3-acetic acid.
  9. Autophagy inhibitor

    ROC-325 is an autophagy inhibitor. ROC-325 exhibited superior in vitro anticancer effects compared with the existing autophagy inhibitor hydroxychloroquine (HCQ) in 12 different cancer cell lines with diverse genetic backgrounds.
  10. glucocorticoid receptor agonist

    Dexamethasone Phosphate disodium is a is a water-soluble form of the synthetic glucocorticoid dexamethasone.
  11. ATG4B antagonist

    NSC 185058 is an inhibitor of ATG4B, a cysteine protease that activates LC3B during the initiation of autophagy.
  12. LRRK2 inhibitor

    CZC-25146 is a potent LRRK2 inhibitor.
  13. CXCR4 Antagonist

    MSX-130 is CXCR4 antagonist.
  14. CXCR4 receptor modulator

    NSC-23026 is a CXCR4 receptor modulator.
  15. LRRK2 inhibitor

    PF-06371900 is a potent and highly selective leucine rich repeat kinase 2 (LRRK2) inhibitor.
  16. PPT1 inhibitor

    DC661 is a potent palmitoyl-protein thioesterase 1 (PPT1) inhibitor. DC661 inhibits autophagy. DC661 is capable of deacidifying the lysosome and inhibiting autophagy significantly better than hydroxychloroquine (HCQ).
  17. Autophagy inhibitor

    Autophinib is a novel potent autophagy inhibitor, inhibiting autophagy induced by starvation or Rapamycin by targeting the lipid kinase VPS34.
  18. tricyclic antidepressant

    Nortriptyline hydrochloride (Desmethylamitriptyline hydrochloride) is a tricyclic antidepressant and the main active metabolite of Amitriptyline, and used to relieve the symptoms of depression.
  19. Lumefantrine, also known as HSDB 7210, is an antimalarial agent used to treat acute uncomplicated malaria. It is administered in combination with artemether for improved efficacy. This combination therapy exerts its effects against the erythrocytic stages of Plasmodium spp. and may be used to treat infections caused by P. falciparum and unidentified Plasmodium species, including infections acquired in chloroquine-resistant areas.
  20. 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.
  21. nucleoside analog

    Cytarabine hydrochloride, a nucleoside analog, causes S phase cell cycle arrest and inhibits DNA polymerase. Cytarabine inhibits DNA synthesis with an IC50 of 16 nM.
  22. Ambroxol is a secretolytic agent used in the treatment of respiratory diseases associated with viscid or excessive mucus.
  23. CoA reductase inhibitor

    Atorvastatin, (+/-)- is a Hydroxymethylglutaryl-CoA reductase inhibitor.
  24. iron chelator

    Deferoxamine mesylate is an iron chelator that binds free iron in a stable complex, preventing it from engaging in chemical reactions.
  25. 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.
  26. hepatoprotective agent

    Bicyclol, also known as SY 801, is a hepatoprotective agent. Bicyclol upregulates transcription factor Nrf2, HO-1 expression and protects rat brains against focal ischemia.
  27. 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.
  28. Autophagy activator

    EN6 is a novel covalent autophagy activator, targeting cysteine 277 in the ATP6V1A subunit of the lysosomal v-ATPase, which activates mTORC1 via the Rag guanosine triphosphatases.
  29. Xanthocillin is a marine agent extracted from Penicillium commune, induces autophagy through inhibition of the MEK/ERK pathway.
  30. autophagy receptor

    ALLO-1, an autophagy receptor, is essential for autophagosome formation around paternal organelles and directly binds to the worm LC3 homologue LGG-1 through its LC3-interacting region (LIR) motif.
  31. CXCR4 receptor antagonist

    USL311 is a CXCR4 receptor antagonist which prevents the binding of stromal-cell derived factor-1 (SDF-1 or CXCL12) to CXCR4.
  32. LRRK2 inhibitor

    PFE-360, also known asd PF-06685360, is a potent and selective inhibitor of LRRK2 kinase.
  33. Autophagy inhibitor

    Aumitin is an autophagy inhibitor, targeting mitochondrial complex I. Aumitin inhibits starvation- and rapamycin induced autophagy dose dependently with IC50s of 0.12 μM and 0.24 μM, respectively.
  34. 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.
  35. Autophagy inhibitor

    EACC is a reversible autophagy inhibitor, which can block autophagic flux. EACC selectively inhibits the translocation of autophagosome-specific SNARE Stx17 thereby blocking autophagosome-lysosome fusion.
  36. Human CXCR3 agonist

    PS372424, a three amino-acid fragment of CXCL10, is a specific human CXCR3 agonist with anti-inflammatory activity, which inhibits the binding of CXCR3 ligand CXCL10 to CXCR3 receptor with IC50 of 42 nM.
  37. CXCR7 modulator

    CXCR7 modulator 1 (compound 25) is a potent and orally bioavailable peptoid hybrid CXCR7 modulator, with a Ki of 9 nM.
  38. Cholesterol biosynthesis inhibitor

    Monacolin J is an inhibitor of cholesterol biosynthesis, and inhibits the activity of HMG-CoA reductase.
  39. sulfasalazine analog

    Ipsalazide is a novel sulfasalazine analog designed to release 5-aminosalicylic acid and a nontoxic carrier molecule in the gastrointestinal tract.
  40. macroautophagy/autophagy inhibitor

    CA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion.
  41. Oxyphenisatin acetate, the pro-drug of oxyphenisatin, is used to be a laxative.
  42. LRRK2 inhibitor

    LRRK2 inhibitor 1 is a potent, selective and oral LRRK2 inhibitor with an pIC50 of 6.8 nM.
  43. Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt.
  44. GPR35/CXCR8 antagonist

    ML 145 is a selective GPR35/CXCR8 antagonist with an IC50/EC50 of 20.1 nM, but not for the related GPR55 orphan receptor. GPR35 is expressed by various cells of the immune system and it may has potential as a therapeutic target in inflammatory disease.
  45. GPR35/CXCR8 agonist

    Kynurenic acid sodium, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid sodium is also an agonist of GPR35/CXCR8.
  46. Lysosomotropic autophagy inhibitor

    IITZ-01 is a potent lysosomotropic autophagy inhibitor with single-agent antitumor activity, with an IC50 of 2.62 μM for PI3Kγ.
  47. Nrf2 activator

    TBHQ (tert-Butylhydroquinone) is a widely used Nrf2 activator, protects against Doxorubicin (DOX)-induced cardiotoxicity through activation of Nrf2.
  48. CXCR4 antagonist

    IT1t is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM.
  49. 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.
  50. brain penetrant LRRK2 inhibitor

    MLi-2 is a potent, highly selective, orally available, brain penetrant inhibitor of LRRK2 with an IC50 of 0.76 nM.

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