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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.
- Beatriz Giesen, .et al. , Pharmaceutics, 2021, Feb 23;13(2):295 PMID: 33672398
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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.- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Yoon-Jin Kim, .et al. , Sci Adv, 2021, Feb 19;7(8) PMID: 33608268
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Autophagy/PI3K Inhibitor
3-Methyladenine is an inhibitor of class III phosphatidylinositol 3-kinase (PI 3-kinase).- Ming-Shan Chen, .et al. , Int J Med Sci, 2025, Jun 23;22(12):3120-3131 PMID: 40657389
- Enhui Gong, .et al. , J Pharm Pharmacol, 2024, Apr 3;76(4):354-367 PMID: 38330446
- Yu-Chih Hsu, .et al. , Int J Med Sci, 2023, 20(4): 444-454 PMID: 37057216
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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.- Mireia Nager, .et al. , J Cell Sci, 2025, Mar 19;138(9):jcs263408 PMID: 39912384
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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 .- SR Bonam, .et al. , Cells, 2020, May; 9(5): 1321 PMID: 32466347
- Altea Rocchi, .et al. , PLoS Genet, 2017, Aug; 13(8): e1006962 PMID: 28806762
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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.- Yusuke Murase, .et al. , Oncol Rep, 2022, Apr;47(4):61 PMID: 35088890
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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. -
Calcium channel antagonist
Felodipine is a 1,4-dihydropyridine antagonist and calcium channel protein inhibitor.
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HMGB1 release inhibitor
Ethyl pyruvate is a simple derivative of the endogenous metabolite, pyruvic acid. Ethyl pyruvate is an anti-inflammatory agent. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
PPT1 Inhibitor
Ezurpimtrostat (hydrochloride) is a potent and selective PPT1 inhibitor with multiple biological activities. It disrupts lysosomal function, modulates autophagy, and induces apoptosis, making it a valuable tool in cancer research and immunology. This compound has demonstrated efficacy in reducing inflammatory markers such as IFN-α and CRP, as well as in lowering viral loads of SARS-CoV-2. Ezurpimtrostat is suitable for investigating conditions such as systemic lupus erythematosus, hepatocellular carcinoma, fibrosis, and other related disorders. -
15-LO inhibitor
PD146176 (NSC168807) is a 15-Lipoxygenase (15-LO) inhibitor, which inhibits rabbit reticulocyte 15-LO with a Ki of 197 nM. PD146176 (NSC168807) has a dramatic effect in reducing atherogenesis. -
cell cycle inhibitor
Briciclib disodium salt is a benzyl styryl sulfone analog, and a disodium phosphate ester prodrug of ON 013100, with potential antineoplastic activity. -
Autophagy inhibitor
Autophinib is a novel potent autophagy inhibitor, inhibiting autophagy induced by starvation or Rapamycin by targeting the lipid kinase VPS34. -
CoA reductase inhibitor
Atorvastatin, (+/-)- is a Hydroxymethylglutaryl-CoA reductase inhibitor. -
Autophagy Inhibitor
Vps34-PIK-III (PIK-III) is a selective inhibitor of VPS34 enzymatic activity.
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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. -
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. -
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. -
lysosomal exocytosis inhibitor
Vacuolin-1 is a potent and cell-permeable lysosomal exocytosis inhibitor. -
VPS34 inhibitor
VPS34 inhibitor 1 (Compound 19, PIK-III analogue) is a potent and selective inhibitor of VPS34 with an IC50 of 15 nM. -
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. -
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. -
CYP26 inhibitor/RAMBA
Talarozole (R115866) is an oral systemic all-trans retinoic acid metabolism blocking agent (RAMBA) which increases intracellular levels of endogenous all-trans retinoic acid (RA). Talarozole inhibits both CYP26A1 and CYP26B1 with IC50s of 5.4 and 0.46 nM, respectively. -
retinoic acid metabolism inhibitor
(+)-Talarozole is a potent inhibitor of retinoic acid metabolism extracted from patent WO 1997049704 A1. -
retinoic acid metabolism inhibitor
(-)-Talarozole is a potent inhibitor of retinoic acid metabolism extracted from patent WO 1997049704 A1. -
Cholesterol biosynthesis inhibitor
Monacolin J is an inhibitor of cholesterol biosynthesis, and inhibits the activity of HMG-CoA reductase. -
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. -
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. -
Autophagy Inhibitor
ATG12-IN-1 is an autophagy inhibitor that effectively disrupts the ATG12-ATG3 protein-protein interaction, exhibiting an IC50 of 9 μM. This compound is valuable in cancer research, allowing for the exploration of autophagy dynamics and its implications in tumor biology. It provides a robust tool for investigating the role of autophagy in cancer progression and therapeutic resistance. -
Autophagy Inhibitor
Autophagy-IN-4 (Compound 34) is a potent autophagy inhibitor, demonstrating an EC50 of 0.5 μM in U2OS cells and an LD50 of 27 μM. This compound effectively interferes with the autophagic process, making it a valuable tool for researchers investigating the role of autophagy in various biological contexts and disease models. Its specificity and efficacy support its application in studies aimed at understanding autophagy-related pathways and potential therapeutic interventions. -
Autophagy Inhibitor
Autophagy-IN-3 is an autophagy inhibitor that enhances metabolic stress within the tumor microenvironment. By inhibiting autophagic processes, it significantly increases the efficacy of cytostatics in combination therapies. This compound is particularly valuable in cancer research, where modulating autophagy can influence tumor growth and treatment response.

