Autophagy Signaling

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  1. retinoic acid metabolism inhibitor

    (-)-Talarozole is a potent inhibitor of retinoic acid metabolism extracted from patent WO 1997049704 A1.
  2. sulfasalazine analog

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

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

    LRRK2 inhibitor 1 is a potent, selective and oral LRRK2 inhibitor with an pIC50 of 6.8 nM.
  6. 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.
  7. 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.
  8. 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.
  9. 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.
  10. Nrf2 activator

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

    IT1t is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM.
  12. 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.
  13. EN6

    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.
  14. Xanthocillin is a marine agent extracted from Penicillium commune, induces autophagy through inhibition of the MEK/ERK pathway.
  15. 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.
  16. 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.
  17. LRRK2 inhibitor

    PFE-360, also known asd PF-06685360, is a potent and selective inhibitor of LRRK2 kinase.
  18. 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.
  19. 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.
  20. 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.
  21. drug-linker conjugate for ADC

    AmPEG6C2-Aur0131 is a drug-linker conjugate for ADC (anti-CXCR4 ADC) with potent antitumor activity by using Aur0131 (an auristatin microtubule inhibitor), linked via the non-cleavable linker AmPEG6C2.
  22. drug-linker conjugate for ADC

    AcLys-PABC-VC-Aur0101 is a drug-linker conjugate for ADC (anti-CXCR4 ADC) with potent antitumor activity by using Aur0101 (an auristatin microtubule inhibitor), linked via the cleavable linker AcLys-PABC-VC.
  23. 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.
  24. CXCR7 modulator

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

    Monacolin J is an inhibitor of cholesterol biosynthesis, and inhibits the activity of HMG-CoA reductase.
  26. Polydatin, a natural precursor of resveratrol, induces β-defensin production and reduces inflammatory response.
  27. JAK inhibitor

    S-Ruxolitinib is the chirality of INCB018424, is a potent and selective small-molecule Janus kinase 1 (JAK1) and JAK2 inhibitor.
  28. CXCR4 antagonist

    AMD-070 hydrochloride is a potent and selective antagonist of CXCR4 with an IC50 value of 13 nM in a CXCR4 125I-SDF inhibition binding assay, inhibit the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs.
  29. CXCL8 receptor inhibitor

    Reparixin L-lysine salt is an inhibitor of CXCL8 receptor, also inhibit CXCR1 and CXCR2 activation,which has been shown to attenuate inflammatory responses in various injury models.
  30. CXCL chemokines antagonist

    UNBS5162 is a novel naphthalimide that decreases CXCL chemokine expression in experimental prostate cancers; the mean antiproliferative activity IC50 value is 17.9 uM for 9 cancer cell lines; hydrolysis product of UNBS3157.
  31. EGFR inhibitor

    AV-412 (MP412) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M and ErbB2, respectively.
  32. LRRK2 inhibitor

    PF-06447475 is a highly potent, selective, brain penetrant LRRK2 inhibitor with IC50 of 3 nM/11 nM for Wt LRRK2/G2019S LRRK2 respectively.
  33. LRRK2 inhibitor

    CZC-54252 is a potent inhibitor of LRRK2 with IC50s of 1.28 nM and 1.85 nM for wild-type and G2019S LRRK2 respectively.
  34. anti-cancer agent

    Falcarindiol (FAD, (3R,8S)-Falcarindiol, FaDOH) is a natural polyacetylene compound found rich in many plants of the Umbelliferae family. Falcarindiol suppresses LPS-stimulated expression of inducible nitric oxide synthase (iNOS), tumor necrosis factor alpha (TNFα), interleukin-6 (IL-6), and interleukin-1 beta (IL-1β). Falcarindiol attenuates the LPS-induced activation of JNK, ERK, STAT1, and STAT3 signaling molecules. Falnidamol is a pyrimido-pyrimidine compound with anti-cancer activity.
  35. anti-bacterial agent

    Pogostone is isolated from patchouli with anti-bacterial and anti-cancer activities. Pogostone inhibits both gram negative and gram positive bacteria, also show inhibitory effect on corynebacterium xerosis with a MIC value of 0.098 ?g/ml . Pogostone induces cell apoptosis and autophagy.
  36. anticancer agent

    Decursin is an anticancer agent, with potential anti-inflammatory activity.
  37. ULK1/2 Inhibitor

    MR-2088 is a selective, ATP-competitive inhibitor of ULK1 and ULK2, exhibiting pEC50 values of 8.3 and 8.7, respectively. This compound effectively inhibits autophagic flux and demonstrates a synergistic antiproliferative effect with MEK inhibitors in vitro, making it a valuable tool for studying non-small cell lung cancer (NSCLC). Its ability to modulate autophagy-related pathways provides insights into cancer biology and potential therapeutic strategies.
  38. Autophagy Inducer

    Paeonol-d3 is a deuterium-labeled derivative of Paeonol, serving as an autophagy inducer. It enhances the autophagic process, which is crucial for cellular homeostasis and survival under stress conditions. This reagent is primarily utilized in studies investigating autophagy-related pathways and their implications in various diseases.
  39. Tag-Linker Conjugate

    Amino-PEG3-2G degrader-1 is a tag-linker conjugate designed to induce the ubiquitin-proteasome system (UPS) through its PEG linker and pyrazole-linked FBnG tag. This compound facilitates the synthesis of autophagy-targeting chimeras (AUTACs), enabling targeted degradation of specific cellular proteins. Its application is significant in the study of protein homeostasis and cellular degradation pathways, making it a valuable tool for research in cellular biology and therapeutic development.
  40. Autophagy Enhancer

    Valechlorine is an iridoid that functions primarily as an autophagy enhancer. It demonstrates efficacy in mitigating fatty liver conditions by promoting the breakdown of lipid droplets through autophagy. This compound is particularly useful for research involving nonalcoholic fatty liver disease (NAFLD).
  41. Autophagy Activator

    Clematichinenoside AR is an autophagy activator derived from the traditional Chinese herb Clematis chinensis. This compound exhibits significant pharmacological effects, notably in the context of atherosclerosis and related diseases. Its ability to modulate autophagy makes it a valuable tool for research into cellular processes and potential therapeutic interventions.
  42. Autophagy Inhibitor

    Autophagy-IN-5 is a potent autophagy inhibitor, exhibiting an EC50 of 0.736 μM. This compound selectively targets the autophagy pathway, playing a crucial role in cellular homeostasis and degradation processes. It is suitable for research applications investigating the modulation of autophagy in various disease contexts, including cancer and neurodegenerative disorders.
  43. Autophagy

    SLLN-15 is a potent and selective enhancer of autophagy that primarily targets the autophagic pathway. It effectively activates cytostatic macroautophagy in triple-negative breast cancer (TNBC) cells, promoting cellular degradation and recycling processes. SLLN-15 is ideal for research focused on autophagy modulation and its implications in cancer therapy, particularly in challenging malignancies like TNBC.
  44. Kif15/ULK1 Inhibitor

    (Z/E)-GW406108X serves as a selective inhibitor of Kif15, a member of the Kinesin-12 family, with an IC50 of 0.82 µM. This compound is instrumental in studying the dynamics of mitotic processes and cellular transport mechanisms. Additionally, it may have implications in cancer research, specifically in the investigation of tumor cell proliferation and migration.
  45. Autophagy

    MRT 68601 is a potent inhibitor of TBK1, predominantly influencing autophagy processes. It effectively inhibits autophagosome formation in lung cancer cells, underscoring its therapeutic potential in cancer research. Additionally, MRT 68601 may impact host-dependent factors implicated in SARS-CoV-2 infection, offering a foundation for the development of broad-spectrum antiviral therapies linked to known FDA-approved drugs and compounds currently in clinical trials.
  46. Autophagy Inducer

    Butylate is an autophagy inducer that plays a significant role in platelet research. It is involved in the activation of platelets, which can trigger autophagic processes mediated by the AMPK-MTOR signaling pathway and is associated with sphingolipid metabolism. This compound serves as a valuable tool for investigating the interplay between autophagy and metabolic pathways in hematological studies.
  47. Autophagy Inducer

    NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2), exhibiting an IC50 of 200 nM in a cell-free assay. This compound selectively inhibits Chk2 while displaying lesser activity against Brk, c-Met, IGFR, and LCK at higher concentrations. NSC 109555 disrupts Chk2 autophosphorylation and histone H1 phosphorylation with an IC50 of 240 nM. Its biological activity includes inducing autophagy and inhibiting growth in L1210 leukemia cells, as well as enhancing gemcitabine-induced cytotoxicity and increasing reactive oxygen species levels in various pancreatic cancer cell lines.
  48. Antitumor Agent

    Antitumor agent-82 is a potent antitumor compound that primarily exerts its effects through the induction of autophagy via the ATG5/ATG7 signaling pathway. This compound demonstrates significant anti-proliferative activity against various cancer cell lines, making it a valuable tool for cancer research. Antitumor agent-82 can be utilized in studies aimed at understanding autophagy's role in tumor progression and therapeutic resistance.
  49. Autophagy Inducer

    BRD5631 is an autophagy inducer that enhances the autophagic process through an mTOR-independent pathway. It has been shown to impact various cellular disease phenotypes associated with autophagy, including protein aggregation, cell survival mechanisms, bacterial replication, and the production of inflammatory cytokines. This compound is suitable for research applications exploring the roles of autophagy in disease modulation and therapeutic development.

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