Autophagy Signaling

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  1. Anti-Insect Agent

    Methyl Eugenol is an anti-insect agent primarily effective against the oriental fruit fly (Bactrocera dorsalis). In addition to its insecticidal properties, Methyl Eugenol exhibits anti-cancer and anti-inflammatory activities, making it a versatile compound for biological research. It has been shown to induce autophagy in cells and can be utilized in studies related to intestinal ischemia/reperfusion injury.
  2. Iron Chelator

    Deferoxamine (Deferoxamine B) is an iron chelator (binds to Fe(III) and many other metal cations), is widely used to reduce iron accumulation and deposition in tissues. Deferoxamine upregulates HIF-1α levels with good antioxidant activity. Deferoxamine also shows anti-proliferative activity, can induce apoptosis and autophagy in cancer cells. Deferoxamine can be used in studies of diabetes, neurodegenerative diseases as well as anti-cancer and anti-COVID-19.
  3. 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.
  4. 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.
  5. Apoptosis Inducer

    Sanguinarine chloride is a benzophenanthridine alkaloid that functions as an apoptosis inducer primarily through the generation of reactive oxygen species (ROS). This compound is known to activate key signaling pathways, specifically JNK and NF-κB, facilitating programmed cell death. Sanguinarine chloride is widely utilized in cancer research and studies investigating apoptotic mechanisms.
  6. 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.
  7. CXCR4 Antagonist

    Nef-M1 is a CXCR4 antagonist peptide derived from the myristoylated protein encoded by the nef gene in HIV. It induces apoptosis by enhancing caspase-3 levels in cancer cells and inhibits critical processes associated with tumor progression, including angiogenesis and epithelial-mesenchymal transition (EMT). Nef-M1 reduces levels of VEGF-A, phosphorylated GSK-3β, and vimentin while promoting E-cadherin expression. This compound is valuable for research applications focused on colorectal cancer and breast cancer.
  8. Apoptosis Inducer/Autophagy Inhibitor

    Kumatakenin is a potent apoptosis inducer and autophagy inhibitor that targets ATG5 with a Kd value of 2.94 μM. It effectively enhances the activity of caspases 3, 8, and 9, leading to caspase-dependent apoptosis in ovarian cancer cells while modulating chemokines and pro-oncogenic factors. Kumatakenin also reduces M2 macrophage polarization, inhibits tumor progression in esophageal cancer by targeting FASN, and interacts with Eno3 to mitigate ferroptosis and alleviate intestinal inflammation. This compound is valuable for studies in ovarian cancer, esophageal cancer, depression, and colitis research.
  9. ULK1 Inhibitor

    XST-14 is a potent and selective inhibitor of ULK1, demonstrating an IC50 of 26.6 nM. This compound effectively inhibits autophagy by decreasing the phosphorylation of ULK1 downstream substrates. XST-14 has been shown to induce apoptosis in hepatocellular carcinoma (HCC) cells, providing significant antitumor effects and contributing to ongoing cancer research and therapeutic studies.
  10. Autophagy Inducer

    Bigelovin is a sesquiterpene lactone derived from Inula hupehensis, functioning as a selective agonist of the retinoid X receptor α. It induces autophagy and apoptosis, effectively suppressing tumor growth through the inhibition of the mTOR pathway, which is modulated by reactive oxygen species (ROS) generation. This compound is valuable for research applications focused on cancer biology and the mechanisms of autophagy modulation.
  11. Autophagy Inducer

    ZPCK is a proagent of gemcitabine that functions as an autophagy inducer. It is designed to enhance oral bioavailability, facilitating more efficient delivery in research applications. ZPCK is relevant for studies exploring cancer therapies that utilize autophagy modulation to improve treatment outcomes.
  12. LRRK2 Inhibitor

    LRRK2-IN-8 is a selective inhibitor of the leucine-rich repeat kinase 2 (LRRK2), effectively targeting both wild-type LRRK2 and the G2019S mutant with IC50 values under 10 nM. Additionally, this compound demonstrates inhibitory activity against TYK2 and NUAK1 with IC50 values ranging from 10 to 100 nM. LRRK2-IN-8 is valuable for research focused on neurodegenerative diseases linked to LRRK2, as well as studies aimed at exploring the functionality of TYK2 and NUAK1 in various cellular processes.
  13. LRRK2/NUAK1/TYK2 Inhibitor

    LRRK2/NUAK1/TYK2-IN-1 is a potent inhibitor of LRRK2, NUAK1, and TYK2, exhibiting IC50 values under 10 nM for LRRK2 (Wt), LRRK2 (G2019), TYK2, and NUAK1. This compound is valuable for research in autoimmune diseases, providing insights into the mechanisms of inflammation and immune response modulation. Its high selectivity and efficacy make it a crucial tool for studying the roles of these kinases in various biological pathways.
  14. Anticancer Agent

    Bufothionine is a natural alkaloid with anticancer properties, isolated from Cinobufacini. It induces apoptosis through a mitochondria-mediated pathway and effectively reduces serum IL-6 levels while suppressing the expression of p-Stat3tyr705, p-Stat3ser727, and Jak2. Bufothionine also promotes autophagy by upregulating key autophagy-related proteins Atg5, Atg7, and LC3Ⅱ, while inhibiting PIM3 expression. Its efficacy in preclinical models demonstrates significant anti-cancer activity against gastric cancer and highlights its potential role in therapeutic applications.
  15. 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.
  16. 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.
  17. Autophagy Inducer

    Sanguinarine is a benzophenanthridine alkaloid that acts as an autophagy inducer. It is derived from the root of Sanguinaria canadensis and can stimulate apoptosis through the production of reactive oxygen species (ROS). The pro-apoptotic effects of sanguinarine are linked to the activation of the JNK and NF-κB signaling pathways, making it a valuable tool for research in cancer biology and cellular stress responses.
  18. Autophagy Inducer

    ZX-29 is a selective autophagy inducer that targets the ALK pathway, exhibiting potent inhibition with IC50 values of 2.1 nM, 1.3 nM, and 3.9 nM for wild-type ALK and its L1196M and G1202R mutations, respectively. This compound triggers apoptosis through the induction of endoplasmic reticulum stress while effectively overcoming resistance associated with ALK mutations. Additionally, ZX-29 promotes protective autophagy and demonstrates significant antitumor activity, making it a valuable tool for research into cancer therapies targeting the ALK signaling pathway.
  19. Autophagy Inducer

    Quercetin-d5, a deuterated form of Quercetin, serves as an autophagy inducer by modulating key signaling pathways. This natural flavonoid enhances the activity of recombinant SIRT1 and exhibits inhibitory effects on phosphoinositide 3-kinases (PI3K), with IC50 values of 2.4 μM for PI3K γ, 3.0 μM for PI3K δ, and 5.4 μM for PI3K β. Quercetin-d5 is utilized in research applications exploring autophagy modulation and the consequences on cellular metabolism and longevity.
  20. 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.
  21. Stable Isotope

    Kynurenic acid-d5 is a deuterium-labeled analog of kynurenic acid, an endogenous metabolite of tryptophan. It acts as a broad-spectrum antagonist of NMDA and glutamate receptors, as well as the α7 nicotinic acetylcholine receptor. Additionally, kynurenic acid-d5 serves as an agonist for GPR35/CXCR8, making it valuable in studies related to neuropharmacology and neurotransmitter signaling pathways. This stable isotope is ideal for tracing and characterization studies in metabolic research.
  22. Autophagy Modulator

    Tea polyphenol primarily functions as an autophagy modulator. It demonstrates significant biological activities, including antioxidant properties, anti-cancer effects, inhibition of cell proliferation, induction of apoptosis, and cell cycle arrest. Additionally, tea polyphenol plays a role in modulating carcinogen metabolism, making it a valuable reagent for research in cancer biology and cellular physiology.
  23. Autophagy Inducer

    Soyasapogenol B is an autophagy inducer derived from soy. It enhances autophagy and promotes apoptosis, contributing to its anti-inflammatory, antioxidant, and antitumor effects. This compound is valuable for research applications focused on cancer biology and the regulation of cellular processes linked to autophagy and inflammation.
  24. 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.
  25. Lipoteichoic acid is an orally active compound with anti-inflammatory and antitumor properties. It is a key immune molecule found in Gram-positive bacteria that activates the complement system by upregulating C3 and inhibiting CD55. Lipoteichoic acid modulates macrophage autophagy via the PI3K/Akt/mTOR pathway, induces lung injury in mouse models, and inhibits melanin production.
  26. Staurosporine Analog

    Stauprimide is a staurosporine analog that promotes embryonic stem cell (ESC) differentiation. It selectively binds to the MYC transcriptional regulator NME2, blocking its nuclear localization in ESCs and thereby downregulating MYC transcription.
  27. 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.
  28. (E/Z)-Sulfosuccinimidyl oleate sodium is a racemic mixture comprising (Z)- and (E)-isomers of sulfosuccinimidyl oleate sodium (Sulfo-N-succinimidyl oleate sodium), a long-chain fatty acid derivative. It functions as a potent and irreversible inhibitor of mitochondrial respiratory chain activity and inhibits fatty acid transport into cells. Sulfosuccinimidyl oleate sodium binds to the CD36 receptor on microglial cell surfaces and exhibits anti-inflammatory effects, making it a valuable tool for studying lipid metabolism, neuroinflammation, and mitochondrial function.
  29. Balixafortide (POL6326) is a potent, selective, and well-tolerated peptidic antagonist of the CXCR4 receptor, with IC50 values below 10 nM. It demonstrates over 1000-fold selectivity for CXCR4 compared to other receptors, including CXCR7. Balixafortide effectively blocks β-arrestin recruitment and calcium flux, and is a strong mobilizer of hematopoietic stem and progenitor cells (HSPCs). It also exhibits anti-cancer activity, making it a promising candidate for oncology and hematology research.
  30. Autophagy Modulator

    Pennogenin 3-O-β-chacotrioside is a bioactive saponin isolated from *Paris polyphylla* with demonstrated anti-colorectal cancer activity. It modulates autophagy by upregulating the expression of key autophagy-related proteins, including LC3 and Beclin-1, contributing to its anticancer effects.
  31. CXCR1/CXCR2 antagonist

    Ladarixin (DF 2156A free base) is an orally active, allosteric, non-competitive antagonist of the chemokine receptors CXCR1 and CXCR2. By blocking these receptors, Ladarixin inhibits neutrophil recruitment and inflammatory responses. It is under investigation for the treatment of inflammatory airway diseases such as chronic obstructive pulmonary disease (COPD) and asthma.
  32. CXCR antagonist

    LIT-927 is a locally and orally active CXCL12 neutraligand with anti-inflammatory properties. It binds to CXCL12 with a Ki of 267 nM, thereby preventing its interaction with the CXCR4 receptor. LIT-927 is a valuable tool for studying CXCL12/CXCR4-mediated signaling in inflammatory and immune-related conditions.
  33. Autophagy inducer

    Cearoin is a bioactive compound that promotes both autophagy and apoptosis by inducing reactive oxygen species (ROS) production and activating the ERK signaling pathway. Through this dual mechanism, cearoin contributes to the regulation of cellular stress responses and programmed cell death. Its ability to modulate these processes makes it a valuable candidate for research in cancer biology and other diseases involving dysregulated autophagy or apoptosis.
  34. Anticholinergic agent

    Penehyclidine hydrochloride (also known as Penequinine hydrochloride) is a selective anticholinergic agent that acts as an antagonist of muscarinic M1 and M3 receptors. It exerts anti-inflammatory effects by modulating immune signaling in lung tissue, notably through activation of the NF-κB pathway and inhibition of pro-inflammatory cytokine release. In preclinical studies, Penehyclidine hydrochloride has been shown to alleviate pulmonary inflammation in rat models of chronic obstructive pulmonary disease (COPD), particularly under conditions of mechanical ventilation. These properties suggest its potential utility in managing respiratory inflammatory conditions and improving outcomes in mechanically ventilated patients with COPD.
  35. SH498 is a novel antitumor agent that exerts its therapeutic effect through Bmi-1 inhibition. It demonstrates potent antiproliferative activity, making it a promising candidate for targeting Bmi-1–driven oncogenic pathways in cancer research and potential therapy development.
  36. QW24 is a potent anti-tumor compound that exerts its effects by downregulating the expression of BMI-1, a key oncogenic regulator involved in cancer stem cell maintenance and tumor progression. It has demonstrated significant efficacy in preclinical models and is being explored as a promising therapeutic agent for clinical research in colorectal cancer.
  37. 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).
  38. LRRK2 PROTAC

    XL01126 is a potent PROTAC degrader of LRRK2, with DC₅₀ values of 14 nM for the G2019S mutant and 32 nM for wild-type LRRK2. It is blood-brain barrier permeable, making it a valuable tool for Parkinson’s disease research. XL01126 enables investigation of both catalytic and non-catalytic functions of LRRK2.
  39. Anti-CXCR4 Antibody

    LY-2624587 is a humanized IgG4 monoclonal antibody that antagonizes CXCR4. By blocking the interaction between SDF-1 and CXCR4, it inhibits SDF-1-induced GTP binding, significantly reducing cell migration and promoting apoptosis in human lymphoma and leukemia cells. Additionally, LY-2624587 impedes CXCR4 and SDF-1-mediated signaling pathways, including the activation of MAPK and AKT. This reagent is valuable for research applications involving human hematological malignancies, particularly acute myeloid leukemia (AML).
  40. CXCR4 Antagonist.

    BPRCX807 is a selective and potent antagonist of the CXC chemokine receptor type 4 (CXCR4). It effectively inhibits CXCL12-mediated phosphorylation of ERK and Akt, leading to significant suppression of primary tumor growth. This compound is applicable for research in hepatocellular carcinoma, providing insights into its therapeutic potential in cancer treatment.
  41. 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.
  42. Apoptosis/Autophagy Inducer

    Momordicine I is a cucurbitane-type triterpenoid that functions as an apoptosis and autophagy inducer. It effectively suppresses glioma growth by promoting apoptosis and disrupting mitochondrial oxidative phosphorylation. In head and neck cancer cells, Momordicine I inhibits glycolysis and lipid metabolism while stimulating autophagy. Additionally, it alleviates isoproterenol-induced cardiomyocyte hypertrophy by suppressing PLA2G6 and DGK-ζ, offering cardiovascular benefits through the upregulation of nitric oxide and inhibition of angiotensin-converting enzyme (ACE). Momordicine I also shows potential in managing type 2 diabetes by inhibiting AKT1, IL-6, and SRC.
  43. 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.
  44. Autophagy/Apoptosis Inducer

    Autophagy Inducer 7 is an effective modulator of autophagy and apoptosis, primarily targeting the Akt/mTOR signaling pathway. This compound promotes autophagy by inhibiting pathway activity and downregulating associated proteins, leading to a reduction in DNA synthesis and inducing G0-G1 cell cycle arrest. Additionally, Autophagy Inducer 7 has demonstrated the ability to inhibit tumor cell proliferation, making it a valuable tool for research in cancer biology and therapeutic strategies involving autophagy.
  45. Autophagy Enhancer

    Corynoxine is a tetracyclic oxindole alkaloid derived from Uncaria rhynchophylla, acting primarily as an autophagy enhancer. It promotes the clearance of alpha-synuclein through the Akt/mTOR signaling pathway, making it a valuable tool for investigating neurodegenerative diseases and related cellular mechanisms. Its ability to modulate autophagy positions Corynoxine as a significant research reagent for studies focused on cellular stress responses and neuroprotection.
  46. Autophagy Inducer

    Diazoxide is an ATP-sensitive potassium channel activator that induces autophagy through modulation of cellular ion balance. This compound demonstrates potential therapeutic effects in conditions related to hyperinsulinism. It is commonly utilized in research applications focusing on autophagy pathways and metabolic regulation.
  47. 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.
  48. Autophagy Inducer

    Physalin B is a potent autophagy inducer derived from Cape gooseberry, known for its steroidal properties. It has been shown to induce cell cycle arrest and promote apoptosis in breast cancer cells by modulating the p53-dependent apoptotic pathway. Additionally, Physalin B inhibits the ubiquitin-proteasome pathway and elicits an incomplete autophagic response in human colon cancer cells in vitro, making it a valuable tool for cancer research and the study of autophagic mechanisms.
  49. Autophagy Inducer

    Loperamide hydrochloride is an opioid receptor agonist that functions primarily as an autophagy inducer. This compound selectively inhibits human intestinal carboxylesterases (hiCE), contributing to its anti-diarrheal properties. Its unique mechanism of action makes Loperamide hydrochloride a valuable reagent for studies related to gastrointestinal motility and autophagy modulation in various biological contexts.
  50. GPX4 Targeting AUTAC

    GPX4-AUTAC is a GPX4-targeting autophagy-mediated degrader designed to selectively induce degradation of GPX4 through autophagy. By promoting the ubiquitination of GPX4 via E3 ligase TRAF6, it enhances the interaction with p62, facilitating the autophagy-dependent degradation process. GPX4-AUTAC has been shown to significantly induce ferroptosis and exhibit notable anti-cancer activity in breast cancer cells, breast cancer-derived organoids, and in the MDA-MB-231 tumor xenograft model. Additionally, it demonstrates potent synergistic effects when used in combination with drugs such as Sulfasalazine or traditional chemotherapy agents like Paclitaxel or Cisplatin.

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