Autophagy Signaling

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  1. 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.
  2. 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.
  3. 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.
  4. Ambroxol is a secretolytic agent used in the treatment of respiratory diseases associated with viscid or excessive mucus.
  5. CoA reductase inhibitor

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

    Deferoxamine mesylate is an iron chelator that binds free iron in a stable complex, preventing it from engaging in chemical reactions.
  7. 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.
  8. 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.
  9. PCSK9 antagonist

    SBC-115076 is an anti-proprotein convertase subtilisin kexin type 9 (anti-PCSK9) compounds, for the treatment and/or prevention of cardiovascular diseases.
  10. LRRK2 inhibitor

    JH-II-127 is a highly potent, selective, and brain penetrant LRRK2 inhibitor, with IC50 of 6.6 nM, 2.2 nM ,47.7 nM for LRRK2-wild-type, LRRK2-G2019S, LRRK2-A2016T.
  11. EGFR inhibitor

    Olafertinib (CK-101, RX518) is an epidermal growth factor receptor (EGFR) inhibitor.

     
  12. Autophagy Activator

    SMER28 is a small-molecule enhancer (SMER) of autophagy, inducing autophagy independently of rapamycin in mammalian cells.
  13. Autophagy Inhibitor

    Vps34-PIK-III (PIK-III) is a selective inhibitor of VPS34 enzymatic activity.

  14. CXCR2 antagonist

    AZD-5069 is a potent and selective CXCR2 antagonist with the potential to inhibit neutrophil migration into the airways in patients with COPD.
  15. CXCR4 agonist

    ATI-2341, pepducin targeting the C-X-C chemokine receptor type 4 (CXCR4) (EC50 = 194 nM, is an allosteric agonist activating the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization.
  16. 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.
  17. Azithromycin Dihydrate is an acid stable orally administered macrolide antimicrobial drug, structurally related to erythromycin.
  18. glucocorticoid receptor agonist

    Dexamethasone acetate (Dexamethasone 21-acetate) is a glucocorticoid receptor agonist.
  19. 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.
  20. 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.
  21. 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.
  22. Mitochonic Acid 5 is a derivative of the plant hormone indole-3-acetic acid.
  23. CXCR3 antagonist

    SCH 546738 is a potent, orally active and non-competitive CXCR3 antagonist, the affinity constant (Ki) of SCH 546738 binding to human CXCR3 receptor is determined to be 0.4 nM in multiple experiments.
  24. ULK1/ULK2 inhibitor

    MRT68921 dihydrochloride is the most potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively.
  25. lysosomal autophagy inhibitor

    Lys01 trihydrochloride (Lys05) is a novel lysosomal autophagy inhibitor with IC50 values of 3.6, 3.8, 6 and 7.9 μM for 1205Lu, c8161, LN229 and HT-29 cell line in the MTT assay.
  26. CXCR3 antagonist

    AMG 487 S-enantiomer is the S enantiomer of AMG 487. AMG 487 is an antagonist of the chemokine receptor CXCR3.
  27. non-peptide CCR1 antagonist

    BX471 hydrochloride (ZK-811752 hydrochloride) is a potent, selective non-peptide CCR1 antagonist with Ki of 1 nM for human CCR1, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.
  28. CXCR4 antagonist

    LY2510924 is a potent and selective CXCR4 antagonist that blocks SDF-1 binding to CXCR4 with an IC50 of 0.079 nM.
  29. CXCR4 antagonist

    IT1t dihydrochloride is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM.
  30. Sevelamer is a phosphate binding drug used to treat hyperphosphatemia in patients with chronic kidney disease; consists of polyallylamine that is crosslinked with epichlorohydrin.
  31. mHTT-LC3 linker compound

    LC3-mHTT-IN-AN1 (Compound AN1) is a mHTT-LC3 linker compound, which interacts with both mutant huntingtin protein (mHTT) and LC3B but not with wtHTT or irrelevant control proteins.
  32. dual ULK1/ULK2 autophagy inhibitor

    SBP-7455 is a potent, high affinity and orally active dual ULK1/ULK2 autophagy inhibitor with IC50s of 13 nM and 476 nM in the ADP-Glo assays, respectively.
  33. lysosomal exocytosis inhibitor

    Vacuolin-1 is a potent and cell-permeable lysosomal exocytosis inhibitor.
  34. inhibitor of quinone reductase 2 (QR2)

    S29434 (NMDPEF) is a potent, competitive, selective and cell-permeable inhibitor of quinone reductase 2 (QR2), with IC50s ranging from 5 to 16 nM for human QR2 at different organizational levels, and has good selectivity for QR2 over QR1.
  35. allosteric inhibitor of CXCR1 and CXCR2

    SX-682 is an orally bioavailable, potent allosteric inhibitor of CXCR1 and CXCR2.
  36. ULK1 activator

    LYN-1604 dihydrochloride is a potent UNC-51-like kinase 1 (ULK1) activator (EC50=18.94 nM) for the research of triple negative breast cancer (TNBC).
  37. CXCR4 antagonist

    Motixafortide (BKT140 4-fluorobenzoyl) is a novel CXCR4 antagonist with an IC50 vakue of ??1 nM.
  38. Autophagy inducer

    Tomatidine hydrochloride acts as an anti-inflammatory agent by blocking NF-κB and JNK signaling. Tomatidine hydrochloride activates autophagy either in mammal cells or C elegans.
  39. ULK1 activator

    BL-918 is an orally active UNC-51-like kinase 1 (ULK1) activator with an EC50 of 24.14 nM.
  40. antineoplastic agent

    ABTL-0812 (α-Hydroxylinoleic acid) induces endoplasmic reticulum (ER) stress-mediated autophagy. ABTL-0812 is a first-in-class small molecule with anti-cancer activity.
  41. natural pterostilbene analogue

    3'-Hydroxypterostilbene, a natural pterostilbene analogue, effectively inhibits the growth of human colon cancer cells (IC50s of 9.0, 40.2, and 70.9 ?M for COLO 205, HCT-116, and HT-29 cells, respectively) by inducing apoptosis and autophagy.
  42. antioxidant agent

    Ferulic acid methyl ester (Methyl Ferulate, Methyl 4'-hydroxy-3'-methoxycinnamate) is a lipophilic derivative of ferulic acid, which is a hydroxycinnamic acid that is abundant in plants. It shows the strongest antioxidant activity and can protect against inflammation and cancer.
  43. VPS34 inhibitor

    VPS34 inhibitor 1 (Compound 19, PIK-III analogue) is a potent and selective inhibitor of VPS34 with an IC50 of 15 nM.
  44. anti-tumor agent

    Sophocarpine (monohydrate) is one of the significant alkaloid extracted from the traditional herb medicine Sophora flavescens which has many pharmacological properties such as anti-virus, anti-tumor, anti-inflammatory.
  45. 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.
  46. 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.
  47. late-stage autophagy inhibitor

    PHY34 is a late-stage autophagy inhibitor with nanomolar potency and significant antitumor efficacy as a single agent against HGSOC in vivo.
  48. 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.
  49. CXCR2 receptor antagonist

    Nicotinamide N-oxide, an in vivo nicotinamide metabolite, is a potent, and selective antagonist of the CXCR2 receptor.
  50. p110β inhibitor

    Rac)-AZD 6482 ((Rac)-KIN-193) is a less active racemate of AZD 6482. AZD 6482 is a potent and selective p110β inhibitor with an IC50 of 0.69 nM.

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