| S1041 |
STF-62247
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STF-62247 is a molecule targeting VHL-deficient renal cell carcinoma that induces autophagy. This compound shows selective toxicity and growth inhibition of renal cells lacking VHL; 25-fold greater sensitivity observed for cells with VHL deficiency compared to wild-type (VHL+).
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ACS Nano, 2021, 8267-8282
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Neuropsychiatr Dis Treat, 2015, 11:2091-9
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Neuropsychiatric Disease and Treatment, 2015, 2091-2099
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| E3586 |
Myristica fragrans Extract
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Myristica Fragrans Extract is extracted from Myristica Fragrans, which has autophagy modulating activity.
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| E3141 |
Codonopsis Pilosula Extract
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Codonopsis Pilosula Extract is obtained from Codonopsis pilosula, exhibits not only an anti-melanogenic effect in normal melanocytes, but also a cytoprotective effect in melanocytes subjected to oxidative stress by inducing autophagy and microphthalmia-associated transcription factor (MITF) expression.
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| E4692 |
THZ-P1-2
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THZ-P1-2 is an inhibitor of PI5P4K, which covalently binds to cysteines on a disordered loop in PI5P4Kα/β/γ. It inhibits PI5P4Kα kinase activity with an IC50 of 190 nM and disrupts autophagy by impairing autophagosome clearance and increasing TFEB nuclear localization.
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| S2924 |
Laduviglusib (CHIR-99021) Hydrochloride
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Laduviglusib (CHIR-99021; CT99021) HCl is hydrochloride of CHIR-99021, which is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs Cdc2 and ERK2. CHIR-99021 is a potent pharmacological activators of the Wnt/beta-catenin signaling pathway. CHIR-99021 significantly rescues light-induced autophagy and augments GR, RORα and autophagy-related proteins.
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Circulation Research, September 08, 2023, 772-788
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Blood, November 28, 2019, 1983-1995
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Cell, 2025, 188(11):2974-2991.e20
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| S2215 |
DAPT
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DAPT is a novel γ-secretase inhibitor, which inhibits Aβ production with IC50 of 20 nM in HEK 293 cells. DAPT enhances the apoptosis of human tongue carcinoma cells and regulates autophagy.
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Frontiers in Neuroscience, September 4, 2019, 867
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Investigative Ophthalmology & Visual Science, September 1, 2022, 14
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Protein & Cell, February 18, 2019, 249-271
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| S1241 |
Vincristine (Leurocristine) Sulfate
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Vincristine sulfate is an inhibitor of polymerization of microtubules by binding to tubulin with IC50 of 32 μM in a cell-free assay. Vincristine sulfate induces apoptosis.
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International Journal of Molecular Sciences, October 25, 2023, 15571
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eLife, November 19, 2019, e50036
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Oncotarget, November 05, 2019, 6403-6417
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| S7153 |
10058-F4
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10058-F4 is a c-Myc inhibitor that specificallly inhibits the c-Myc-Max interaction and prevents transactivation of c-Myc target gene expression. 10058-F4 promotes a caspase-3-dependent apoptosis and modulates autophagy.
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Nat Commun, 2025, 16(1):138
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Int J Biol Sci, 2025, 21(6):2762-2779
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Cell Death Dis, 2025, 16(1):601
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| S1274 |
BX-795
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BX-795 is a potent and specific PDK1 inhibitor with IC50 of 6 nM, 140- and 1600-fold more selective for PDK1 than PKA and PKC in cell-free assays, respectively. Meanwhile, in comparison to GSK3β more than 100-fold selectivity observed for PDK1. BX-795 modulates autophagy via inhibiting ULK1. BX-795 also is a potent TBK1 inhibitor that blocks both TBK1 and IKKε with IC 50 values of 6 nM and 41 nM, respectively.
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Cancer Res, 2025, 10.1158/0008-5472.CAN-25-1791
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Cell Rep, 2025, 44(7):115972
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EMBO J, 2024, 10.1038/s44318-024-00244-9
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| S7980 |
VPS34-IN1
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Vps34-IN1 is a potent and highly selective Vps34 inhibitor with IC50 of 25 nM invitro,which does not significantly inhibit the isoforms of class I as well as class II PI3Ks. Vps34-IN1 modulates autophagy.
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Cell Res, 2025, 10.1038/s41422-025-01085-9
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Cell Rep, 2025, 44(1):115115
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J Cell Biol, 2025, 224(5)e202404009
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| S1204 |
Melatonin
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Melatonin is a MT receptor agonist, used as a dietary supplement. This compound is a selective ATF-6 inhibitor and downregulates COX-2. It enhances mitophagy and regulates the homeostasis of apoptosis and autophagy.
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Antioxidants (Basel), 2025, 14(5)528
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Sci Rep, 2025, 15(1):8451
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Biochem Biophys Res Commun, 2025, 760:151706
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| S3592 |
4-PBA (4-Phenylbutyric acid)
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4-PBA (4-Phenylbutyric acid) is a histone deacetylase (HDAC) inhibitor and a key epigenetic inducer of anti-HCV hepatic hepcidin. This compound inhibits LPS-induced inflammation through regulating endoplasmic-reticulum (ER) stress and autophagy in acute lung injury models.
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Nat Commun, 2025, 16(1):50
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Adv Sci (Weinh), 2025, 12(46):e08991
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Phytomedicine, 2025, 145:156939
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| S1627 |
Nitazoxanide
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Nitazoxanide is a synthetic nitrothiazolyl-salicylamide derivative and an antiprotozoal agent(IC50 for canine influenza virus ranges from 0.17 to 0.21 μM). This compound modulates autophagy and inhibits mTORC1 signaling.
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Viruses, February 12, 2024, 282
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Frontiers in Pharmacology, December 09, 2021, 781640
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iScience, 2025, 28(4):112218
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| S2271 |
Berberine chloride
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Berberine chloride is a quaternary ammonium salt from the group of isoquinoline alkaloids. This compound activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. It decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. This chemical induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. It is a dual topoisomerase I and II inhibitor. It is also a potential autophagy modulator.
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J Cardiovasc Dev Dis, 2025, 12(7)278
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Adv Healthc Mater, 2023, e2300591.
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Transl Oncol, 2023, 35:101712
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| S5144 |
Neferine
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Neferine ((R)-1,2-Dimethoxyaporphine), a natural component of Nelumbo nucifera, has antitumor efficiency. It induces apoptosis in renal cancer cells. This compound prevents autophagy through activation of Akt/mTOR pathway and Nrf2 in muscle cells. It strongly inhibits NF-κB activation. It possesses a number of therapeutic effects such as anti-diabetic, anti-aging, anti-microbial, anti-thrombotic, anti-arrhythmic, anti-inflammatory and even anti-HIV.
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上海交通大学学报(医学版), 2025, 261-270
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J Cosmet Dermatol, 2024, 10.1111/jocd.16587
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Bone Res, 2022, 10(1):27
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| S6889 |
Monomethyl Fumarate
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Monomethyl Fumarate (MMF, Monomethylfumarate, Fumaric acid monomethyl ester, Methyl hydrogen fumarate), the active metabolite of the psoriasis drug Fumaderm, is a potent GPR109A agonist. This compound prevents major dysfunctions associated with neurodegenerative diseases: oxidative stress, mitochondrial dysfunction, apoptosis and autophagy.
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Frontiers in Oncology, January 28, 2020, 22
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Cell Cycle, December 8, 2022, 818-828
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Cell Cycle, 2023, 818-828
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