Autophagy

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

Chloroquine phosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator.

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.

Resveratrol has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases???LOX, IC50=2.7 μM???, kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects.

Aloe emodin is a anthraquinone present in aloe latex, an exudate from the aloe plant. It has a strong stimulant-laxative action.

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

MRT68921 is a potent and dual autophagy kinase ULK1/2 inhibitor with IC50 of 2.9 nM and 1.1 nM, respectively.

Emodin is a purgative resin, from rhubarb, the buckthorn and Japanese Knotweed (Fallopia japonica). It belongs to a family of compounds called anthraquinones, which have shown anti-inflammatory and anticancer effects

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 .

Berberine hydrochloride was novelly found that it has various beneficial effects on the cardiovascular system and significant anti-inflammatory activities. Berberine can effectively reduce intracellular superoxide levels in LPS-stimulated macrophages. Such a restoration of cellular redox by berberine is mediated by its selective inhibition of gp91phox expression and enhancement of SOD activity.

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.

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.

Pyrazinamide is an antimycobacterial compound that inhibits the growth of the human M. tuberculosis H37Rv strain.

STF-62247 is a small molecule agonist that induces autophagy and selectively causes lethality in renal cell carcinoma (RCC) cells that have lost the von Hippel-Lindau (VHL) tumor suppressor activity (IC50 = 625 nM).

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

740 Y-P (740YPDGFR; PDGFR 740Y-P) is a potent and cell-permeable PI3K activator. 740 Y-P readily binds GST fusion proteins containing both the N- and C- terminal SH2 domains of p85 but fails to bind GST alone.

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

EAD1 is a potent autophagy inhibitor with antiproliferative activity in lung and pancreatic cancer cells. EAD1 also induces apoptosis.

Tizoxanide is the active metabolite of Nitazoxanide, which is a thiazolide anti-infective compound against anaerobic bacteria, protozoa, and a range of viruses. Tizoxanide has anti-HIV-1 activities.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

Formosanin C is a diosgenin saponin that functions primarily as an apoptosis and autophagy inducer. It exhibits notable anti-tumor activities through mechanisms such as blocking the cell cycle, inhibiting metastasis, and promoting ferroptosis. Additionally, Formosanin C can suppress the NF-κB signaling pathway, providing anti-inflammatory effects while enhancing immune cell activity. This compound is relevant for research in anti-inflammatory, antifungal, and anti-cancer applications, particularly concerning lung, liver, breast, and colorectal cancers.

(E,E)-Bisdemethoxycurcumin is an autophagy inducer derived from curcumin, exhibiting significant anti-inflammatory and anticancer properties. This compound has been shown to enhance cellular autophagy processes, making it a valuable tool for research into cancer biology and potential therapeutic strategies. Its ability to modulate inflammatory pathways also positions it as a candidate for studies relating to chronic inflammatory diseases.

Cys-C-cGMP is an autophagy tag designed for AUTACs that facilitates the selective degradation of target proteins through autophagy. It enhances K63-linked ubiquitination of mitochondria in HeLa cells, thereby promoting cellular quality control and elimination of damaged organelles. This compound is valuable for studying autophagy-related pathways and the development of targeted protein degradation strategies.