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  • Autophagy Signaling

Autophagy Signaling

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Items 1-50 of 190

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  1. A10373
    Etoposide (VP-16)

    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.
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  2. A14396
    Telaglenastat (CB-839)

    Glutaminase inhibitor

    CB-839 an is orally bioavailable inhibitor of glutaminase, with potential antineoplastic activity. CB-839 (Telaglenastat) also inudces autophagy and has antitumor activity.

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  3. A12942
    Spautin-1

    Autophagy Inhibitor

    Spautin-1 is a novel autophagy inhibitor, IM inhibited the growth of K562 cells with IC50 of 1.03μM. In contrast, co-treatment with Spautin-1 increased IM-induced inhibition of cell viability with IC50 of 0.45 μM.
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  4. A14403
    Doxorubicin

    Topoisomerase II inhibitor

    Doxorubicin is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage and apoptosis.
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  5. A17323
    Valproic acid

    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.
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  6. A10741
    (E/Z)-Polydatin ((E/Z)-Piceid)

    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.
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  7. A10957
    U0126-EtOH

    MEK inhibitor

    U0126-EtOH is an inhibitor of both MEK1 and MEK2 with an IC50 of 72 nM and 58 nM respectively.
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  8. A10255
    ABT-737

    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).
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  9. A10746
    PP242 (Torkinib)

    mTOR Inhibitor

    PP242 is a potent and selective mTOR inhibitor in both mTORC1 and mTORC2.
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  10. A17858
    Sunitinib

    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.
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  11. A11041
    INCB018424 (Ruxolitinib)

    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;
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  12. A11151
    3-Methyladenine

    Autophagy/PI3K Inhibitor

    3-Methyladenine is an inhibitor of class III phosphatidylinositol 3-kinase (PI 3-kinase).
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  13. A15880
    MRT68921

    Autophagy ULK1/2 inhibitor

    MRT68921 is a potent and dual autophagy kinase ULK1/2 inhibitor with IC50 of 2.9 nM and 1.1 nM, respectively.
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  14. A11052
    Crenolanib (CP-868596)

    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.
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  15. A12383
    Reparixin

    CXCL8/CXCR1/2 Inhibitor

    Reparixin is a potent inhibitor of both CXCL8 receptors CXCR1/2, it inhibits weakly CXCR2-mediated cell migration (IC50=100 nM), whereas it strongly blocks CXCR1-mediated chemotaxis (IC50=1 nM).
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  16. A10979
    Vorinostat (SAHA)

    HDAC inhibitor

    Vorinostat is an inhibitor of HDACs, inhibiting deacetylation and leading to an accumulation of both hyperacetylated histones and transcription factors.
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  17. A10880
    Sunitinib Malate

    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).
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  18. A15795
    SBI-0206965

    ULK1 inhibitor

    SBI-0206965 is a potent, selective and cell permeable autophagy kinase ULK1 inhibitor with IC50 of 108 nM for ULK1 kinase activity and 711 nM for the highly related kinase ULK2 .
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  19. A10766
    Quercetin (Sophoretin)

    MAO-B inhibitor

    Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C.
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  20. A14316
    Mdivi-1

    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.
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  21. A14149
    GNE 9605

    LRRK2 inhibitor

    GNE-9605 is a highly potent and selective leucine-rich repeat kinase 2 (LRRK2) inhibitor with Ki and IC50 of 2 nM and 19 nM, respectively.
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  22. A10737
    Pitavastatin calcium (Livalo)

    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.
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  23. A10662
    TAE684

    ALK Inhibitor

    TAE684 is a inhibitor of ALK and also a potent inhibitor of LRRK2 kinase activity (IC(50) of 7.8nM against wild-type LRRK2, 6.1nM against the G2019S mutant).
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  24. A10111
    Olaparib (AZD2281)

    PARP inhibitor

    Olaparib (AZD2281) is an inhibitor of poly ADP ribose polymerase (PARP), an enzyme involved in DNA repair.
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  25. A11024
    PF-04691502

    PI3K/mTOR Inhibitor

    PF-04691502 is a PI3K/mTOR kinase inhibitor, is also an agent targeting the phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) in the PI3K/mTOR signaling pathway.
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  26. A10603
    Monensin sodium

    autophagy inhibitor

    Monensin sodium is an ionophore and inhibitor of autophagy commercially used in livestock feed. It inhibits autophagy, interfering with the fusion of the autophagosome and the lysosome.
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  27. A10698
    Parthenolide ((-)-Parthenolide)
    Parthenolide ((-)-Parthenolide) is a sesquiterpene lactone which occurs naturally in the plant feverfew (Tanacetum parthenium).
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  28. A10765
    Quercetin dihydrate (Sophoretin)

    MAO-B inhibitor

    Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C.
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  29. A10845
    Simvastatin

    HMG-CoA reductase inhibitor

    Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM.
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  30. A10855
    Valproic acid sodium salt

    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.
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  31. A10383
    Felodipine

    Calcium channel antagonist

    Felodipine is a 1,4-dihydropyridine antagonist and calcium channel protein inhibitor.

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  32. A22582
    Ethyl pyruvate

    HMGB1 release inhibitor

    Ethyl pyruvate is a simple derivative of the endogenous metabolite, pyruvic acid. Ethyl pyruvate is an anti-inflammatory agent.
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  33. A22586
    EAD1

    autophagy inhibitor

    EAD1 is a potent autophagy inhibitor with antiproliferative activity in lung and pancreatic cancer cells. EAD1 also induces apoptosis.
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  34. A22595
    PF-06454589

    LRRK2 inhibitor

    PF-06454589 is a potent and selective LRRK2 inhibitor.
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  35. A10784
    Reserpine

    Autophagy Inhibitor

    Reserpine acts as an inhibitor of vesicular monoamine transporter 2 (VMAT2), thereby influencing neurotransmitter storage and release. This compound is widely utilized in research studies focusing on autophagy inhibition and its implications in various neurodegenerative disorders. Additionally, reserpine's effects on monoamine levels make it a valuable tool in the investigation of psychiatric conditions and the biochemical pathways involved in these diseases.
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  36. A14463
    Leonurine

    Autophagy Inhibitor

    Leonurine is an alkaloid derived from Leonurus artemisia, functioning predominantly as an autophagy inhibitor. This compound exhibits notable antioxidative and anti-inflammatory properties, making it valuable for research focused on cellular stress responses and neuroprotection. Its ability to modulate autophagy can be explored in studies related to aging, neurodegenerative diseases, and inflammation-related conditions.
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  37. A18292
    Irinotecan hydrochloride

    Topoisomerase I Inhibitor

    Irinotecan hydrochloride is a potent inhibitor of topoisomerase I, an enzyme crucial for DNA replication and transcription. This compound exhibits significant anti-tumor activity, primarily in the treatment of colorectal cancers. Its mechanism involves the stabilization of the enzyme-DNA complex, leading to apoptosis in cancer cells. Irinotecan hydrochloride is widely utilized in cancer research to elucidate cellular response mechanisms and to develop novel therapeutic strategies.
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  38. A31140
    ULK1-IN-2

    ULK1 Inhibitor

    ULK1-IN-2 is a potent inhibitor of ULK1, a key regulator of autophagy. This compound exhibits significant cytotoxic effects against cancer cell lines, demonstrating an IC50 of 1.94 μM in A549 cells. ULK1-IN-2 not only induces apoptosis but also effectively inhibits autophagy, making it a valuable tool for research applications in non-small cell lung cancer (NSCLC) studies.
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  39. A31206
    Autophagy-IN-1

    Autophagy Inhibitor

    Autophagy-IN-1 is a selective autophagy and mitophagy inhibitor that operates by enhancing autophagic flux while obstructing the fusion of autophagosomes and lysosomes in cancer cells. This compound demonstrates significant biological activity by inducing apoptosis and facilitating cell cycle arrest. Research applications include investigating its effects on tumor growth, particularly in colorectal cancer models, as evidenced by its ability to inhibit tumor growth in an HCT116 xenograft mouse model with minimal toxicity.
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  40. A30107
    Britannin

    Autophagy Inducer, NLRP3 Inhibitor

    Britannin is an autophagy inducer and NLRP3 inflammasome inhibitor with an IC50 of 3.630 μM. It exhibits significant anti-inflammatory effects by disrupting the interaction between NLRP3 and NEK7, effectively preventing NLRP3 activation and assembly. Additionally, Britannin shows antitumor properties by inhibiting tumor cell proliferation through interference with the interaction of HIF-1α and Myc, leading to reduced PD-L1 expression and enhanced activity of cytotoxic T lymphocytes. This compound also promotes apoptosis and autophagy in liver cancer cells via activation of ROS-regulated AMPK, making it a valuable tool for research in anti-inflammatory and oncology studies.
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  41. A24524
    DCC-3116

    ULK1/2 inhibitor

    DCC-3116 is an orally active inhibitor of ULK1/2 that suppresses autophagy in lung cancer cells. By targeting ULK1/2, DCC-3116 inhibits KRAS^G12C-driven signaling pathways, leading to reduced cell proliferation and demonstrating anti-tumor activity in KRAS-mutant lung cancer models.
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  42. A24357
    Liensinine Diperchlorate

    Autophagy inhibitor

    Liensinine diperchlorate is a major isoquinoline alkaloid extracted from the seed embryo of *Nelumbo nucifera* Gaertn. It inhibits late-stage autophagy and mitophagy by blocking the fusion of autophagosomes with lysosomes. Liensinine diperchlorate exhibits a broad spectrum of biological activities, including anti-arrhythmic, antihypertensive, anti-pulmonary fibrosis effects, and vascular smooth muscle relaxation, making it a valuable compound for research in cardiovascular and pulmonary diseases, as well as autophagy-related disorders.
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  43. A24017
    HS-276

    TAK1 inhibitor

    HS-276 is an orally bioavailable, potent, and highly selective inhibitor of transforming growth factor-β–activated kinase 1 (TAK1), with a Kᵢ of 2.5 nM. It exhibits strong inhibition of TAK1 and moderate activity against a panel of other kinases, including CLK2, GCK, ULK2, MAP4K5, IRAK1, NUAK, CSNK1G2, CAMKKβ-1, and MLK1, with respective IC₅₀ values ranging from 8.25 to 5585 nM. HS-276 is a valuable tool for investigating TAK1-mediated signaling pathways and holds therapeutic potential for inflammatory conditions such as rheumatoid arthritis (RA).
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  44. A25800
    Alborixin

    PI3K-AKT Inhibitor

    Alborixin is a potent inhibitor of the PI3K-AKT signaling pathway that promotes autophagy. It facilitates the clearance of intracellular and extracellular amyloid-β by upregulating key autophagy-related proteins such as BECN1, ATG5, and ATG7, while enhancing lysosomal activity. This mechanism yields a reduction in amyloid-β-mediated neurotoxicity, positioning Alborixin as a valuable tool for research related to Alzheimer's disease and other neurodegenerative conditions.
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  45. A25838
    Hit 14

    CXCR4 Inhibitor

    Hit 14 is a selective inhibitor of C-X-C chemokine receptor type 4 (CXCR4), demonstrating an IC50 value of 254 nM. This compound effectively inhibits the migration and invasion of MDA-MB-231 cells, highlighting its potential in cancer research. Furthermore, Hit 14 modulates Akt phosphorylation and exhibits anti-inflammatory properties, demonstrating efficacy in reducing ear swelling and damage in mouse models. Its diverse biological activities make it a valuable tool for studies related to cancer metastasis and inflammation.
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  46. A27836
    Corydalmine

    CXCR Inhibitor

    Corydalmine, a CXCR inhibitor, demonstrates significant antifungal activity by inhibiting spore germination in various plant pathogenic and saprophytic fungi. Additionally, it serves as an oral analgesic agent, exhibiting potent analgesic effects. Corydalmine has been shown to alleviate Vincristine-induced neuropathic pain in murine models through the inhibition of the NF-κB-dependent CXCL1/CXCR2 signaling pathway, making it a valuable tool for pain research and therapeutic applications.
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  47. A28139
    Corydalmine hydrochloride

    CXCR Inhibitor

    Corydalmine hydrochloride is a potent CXCR inhibitor that demonstrates significant biological activity by inhibiting spore germination in certain plant pathogenic and saprophytic fungi. Additionally, it exhibits notable analgesic properties, effectively alleviating Vincristine-induced neuropathic pain in murine models. This effect is mediated through the inhibition of the NF-κB-dependent CXCL1/CXCR2 signaling pathway, highlighting its potential applications in pain management research and fungal inhibition studies.
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  48. A30936
    ARN5187 trihydrochloride

    REV-ERB/Autophagy Inhibitor

    ARN5187 trihydrochloride is a selective REV-ERBβ ligand that functions as an autophagy inhibitor. It exerts dual inhibitory effects on REV-ERB-mediated transcription and autophagy processes, demonstrating significant lysosomotropic properties. Additionally, ARN5187 trihydrochloride can induce apoptosis, making it a valuable tool for research in cellular metabolism and programmed cell death. Its biological activity positions it as a critical reagent for studies investigating the interplay between autophagy and transcriptional regulation.
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  49. A42450
    RNF5 inhibitor inh-02

    E3 ubiquitin ligase RNF5 Inhibitor

    RNF5 inhibitor inh-02 is a selective inhibitor of the E3 ubiquitin ligase RNF5/RMA1, demonstrating significant biological activity by restoring F508del-CFTR function in F508del-CFTR-expressing immortalized cell lines (CFBE41o⁻, EC50 = 2.6 μM; FRT, EC50 = 2.2 μM). This compound promotes autophagy through increased LC3IIB expression and enhanced autophagic vacuole formation by reducing ATG4B ubiquitylation. RNF5 inhibitor inh-02 is valuable for research into cystic fibrosis and related cellular mechanisms.
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  50. A46124
    ULK-101

    ULK1 Inhibitor

    ULK-101 is a highly selective inhibitor of ULK1, demonstrating an IC50 of 1.6 nM for ULK1 and 30 nM for ULK2. This compound effectively suppresses autophagy processes, making it valuable for cancer research, particularly in studies focused on nutrient stress sensitivity in cancer cells. ULK-101 is suitable for applications requiring modulation of autophagy and exploration of related signaling pathways.
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