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AutophagyATG
Autophagy-related proteins (ATG) constitute a class of proteins essential for cellular autophagy, participating in the regulation of intracellular degradation and recycling processes. The ATG protein family comprises numerous members, including ATG1, ATG3, ATG4, ATG5, ATG7, and ATG8, each performing distinct roles during different stages of autophagosome formation, extension, and maturation. For instance, ATG7 functions as an E1-like enzyme responsible for activating ubiquitin-like proteins ATG12 and ATG8, while ATG5 serves as the binding partner for ATG12; both jointly contribute to autophagosome expansion. Abnormal expression or dysfunction of ATG proteins is closely associated with the onset and progression of various diseases, including neurodegenerative disorders, cardiovascular diseases, and cancer.
ATG7-IN-1
T397052226229-87-2In house
ATG7-IN-1 is a selective ATG7 inhibitor with an IC50 of 62 nM.
- $329
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Pennogenin 3-O-beta-chacotrioside
T816655916-52-4
Pennogenin 3-O-beta-chacotrioside, isolated from *Paris polyphylla*, exhibits anti-colorectal cancer activity by modulating autophagy through increased expression of autophagy-related proteins LC3 and Beclin-1.
- $59
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FMK 9a
T153031955550-51-2In house
FMK 9a is an irreversible inhibitor of ATG4B with IC50 values of 80 and 73 nM in the TR-FRET and cellular-based LRA assays.
- $118
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Neriifolin
T124830466-07-9
Neriifolin (17β-Neriifolin), a cardiac glycoside extracted from the unripe fruit of Cerbera manghas, is a Na+K+-ATPase inhibitor with anticancer activity that inhibits cell proliferation by suppressing HOXA9-dependent gene expression and inducing apoptosis in the human acute myeloid cell line, THP-1. Neriifolin induces cell cycle arrest and apoptosis in human hepatocellular carcinoma HepG2 cells and can be used in prostate cancer research.
- $148
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AMDE-1
T23716478043-30-0
AMDE-1 is an autophagy modulator and triggers autophagy in an Atg5-dependent manner. AMDE-1 recruits Atg16 to the pre-autophagosomal site and causes LC3 lipidation.
- $84
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ARP 101
T22034849773-63-3
ARP 101 is an effective selective matrix metalloproteinase-2 (MMP-2) inhibitor with anti-cancer activity. It induces the inhibition of HCMV through non-classical chelate 1 (SQSTM1)/p62-Keap1-Nrf2 pathways and phosphorylation of the C-terminal domain of p62, regulating autophagy and inhibiting melanogenesis.
- $100
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RNF5 inhibitor inh-02
T35883324579-65-9
RNF5 inhibitor inh-02 is a selective inhibitor of the ubiquitin ligase RNF5/RMA1, which can significantly rescue F508del-CFTR (cystic fibrosis transmembrane conductance regulator with a deletion at position 508 of phenylalanine) and regulate ATG4B and paxillin, making it useful for studying cystic fibrosis (CF).
- $78
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CA-5f
T51811370032-19-1
CA-5f is a potent late-stage macroautophagy/autophagy inhibitor that works by inhibiting autophagosome-lysosome fusion.
- $40
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Bifendate
T327373536-69-3
Bifendate (Bifendatatum) is commonly used to treat the transaminase elevation that caused by viral hepatitis and drug-induced liver injury.
- $32
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NSC 185058
T521139122-38-8
NSC 185058, an inhibitor of ATG4B (a major cysteine protease), can also attenuate autophagic activity.
- $60
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LC3-mHTT-IN-AN2
T50707758-73-8
LC3-mHTT-IN-AN2 (5,7-Dihydroxy-4-phenylcoumarin) is found in the plant Passiflora serratodigitata with the antibacterial activity.
- $41
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2'-Aminoacetophenone
Fr14273551-93-9
Compound Fr14273 is a natural product for research related to life sciences. The catalog number is Fr14273 and the CAS number is 551-93-9.
- $29
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LC3-mHTT-IN-AN1
T8081486443-73-6
LC3-mHTT-IN-AN1 is a mHTT-LC3 linker compound that interacts with both mutant huntingtin protein (mHTT) and LC3B. LC3-mHTT-IN-AN1 targeted mHTT to autophagosomes reduces the levels of mHTT in an allele-selective manner in cultured Huntington disease (HD) mouse neurons.
- $35
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Atg4B-IN-2
T609672765008-88-4
Atg4B-IN-2. A potent, selective Atg4B inhibitor with anticancer activity, inhibits both Atg4B and PLA2, enabling autophagy that counteracts the anticancer activity of anti-desiccation-resistant prostate cancer drugs.
- $68
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DC-LC3in-D5
T618712868312-73-4
DC-LC3in-D5 is a potent and selective covalent inhibitor of LC3A/B that disrupts autophagy by covalently binding to Lys49 on LC3B (IC₅₀ = 200 nM), resulting in impaired LC3B lipidation, accumulation of the autophagy substrate p62, and a significant reduction in the formation of autophagosome vesicles.
- $100
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Manumycin A
T1601152665-74-4
Manumycin A is an antibiotic with anticancer activity and is a mammalian thioredoxin reductase-1 (TrxR-1) inhibitor.Manumycin A inhibits the production of IL-1β, IL-6, and IL-8 in TNF alpha-stimulated THP-1 cells and peripheral blood mononuclear cells in a dose-dependent manner, inducing apoptosis.
- $278
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LC3B recruiter 2
T205700380636-64-6
LC3B recruiter 2 (34R) is an LC3B recruiting agent incorporated into the autophagy-lysosome pathway degradation system (ATTEC, Autophagy-Tethering Compounds), with a direct binding affinity for LC3B. It connects via a linker to the CDK9 inhibitor SNS-032, creating an ATTEC capable of targeting and degrading the CDK9 and Cyclin T1 complex, while also inhibiting them. Consequently, LC3B recruiter 2 exerts its function through an LC3B-dependent autophagy-lysosome pathway, interfering with the cancer cell cycle progression, thereby demonstrating antitumor activity.
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Autophagy inducer 3
T615802691054-63-2
Autophagy Inducer 3 is a chemical compound that exhibits autophagy-induced activity, specifically inducing robust autophagic cell death in various cancer cells while sparing normal cells. This compound induces lethal autophagy through the formation of distinct autophagic vacuoles, LC3 puncta formation, and upregulation of signature autophagy markers such as Beclin and Atg family proteins [1].
- $734
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ALLO-1
T1918837468-32-9
ALLO-1 is a crucial autophagy receptor responsible for facilitating the formation of autophagosomes around paternal organelles. It directly interacts with the worm LC3 homologue, LGG-1, through its LC3-interacting region (LIR) motif.
- $355
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ATG7-IN-3
T615522226229-76-9
ATG7-IN-3 (compound 18) is an effective ATG7 inhibitor with an IC50 value of 0.048 μM, exhibiting inhibitory actions on autophagy and effectively hampering the development of endogenous LC3B puncta in the H4 neuroglioma cell line [1].
- $1,520
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XIE62-1004
T839452421146-32-7
XIE62-1004 is a chemical compound that induces the interaction between p62 and LC3 by binding to the ZZ domain of p62. This interaction promotes p62 self-aggregation and its subsequent interaction with LC3 on autophagosome membranes, thereby facilitating the delivery of cargo proteins to the autophagosome for degradation. XIE62-1004 is effective both in vitro and in vivo, displaying specificity for the wild type of p62 and exhibiting its actions in a concentration- and time-dependent manner. Additionally, it induces the degradation of mutant huntingtin in vitro and can be employed in AUTAC protein degradation systems to trigger autophagy via p62 self-aggregation and LC3 interaction.
- $620
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LC3B recruiter 1
T2045211281081-32-0
LC3B recruiter 1 (compound 33R) is an LC3B recruiting fragment. It directly interacts with LC3B, exhibiting a Kd value of 2.87 µM.
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Autophagy agonist-1
T205669
Autophagyagonist-1 (compound 22) is an autophagy agonist. It exhibits significant anticancer activity against HepG2 cells and normal cells, with IC50 values of 8.8 μM and > 50 μM, respectively. The compound induces G1 S phase cell cycle arrest, suppresses the expression of CDK4 and CyclinD1, and upregulates P21. Additionally, Autophagyagonist-1 enhances autophagosome, LC3, and PINK1 accumulation, thereby promoting autophagy and mitophagy in HepG2 cells.
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Microcolin H
TN77312408008-21-7
Microcolin H, a marine lipopeptide and phosphatidylinositol transfer protein ligand, targets PITPα β. It enhances the conversion of LC3I to LC3II and decreases p62 levels in cancer cells, inducing autophagy cell death (Autophagy). Furthermore, Microcolin H effectively inhibits tumor growth and exhibits anti-proliferative activity in nude mouse subcutaneous tumor models [1].
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