| S4430 |
HCQ (Hydroxychloroquine) Sulfate
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Hydroxychloroquine (HCQ) Sulfate is an antimalarial agent used for the treatment of systemic lupus erythematosus, rheumatoid arthritis and other autoimmune, inflammatory and dermatologic conditions. Also acts as an inhibitor of autophagy and toll-like receptor (TLR) 7/9.
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EMBO J, 2025, 10.1038/s44318-025-00581-3
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iScience, 2025, 28(4):112054
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Int J Mol Sci, 2025, 26(2)588
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| S1396 |
Resveratrol (trans-Resveratrol)
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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. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis.
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PLoS One, 2026 Mar 16, e0344872
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PLoS One, 2026 Mar 16, e0344872
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Antioxidants, 2025 Oct 29, 1300
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| S1049 |
Y-27632 Dihydrochloride
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Y-27632 2HCl is a selective ROCK1 and ROCK2 inhibitor with a Ki of 140 nM and 300nM in a cell-free assay, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.
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Nature, 2025, 642(8066):143-153
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Cell, 2025, S0092-8674(25)00406-4
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Cell, 2025, S0092-8674(25)00807-4
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| S1263 |
CHIR-99021 (Laduviglusib)
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Laduviglusib (CHIR-99021, CT99021) is a GSK-3α and GSK-3β inhibitor with IC50 values of 10 nM and 6.7 nM, respectively. It does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) and shows a 350-fold selectivity toward GSK-3β compared to CDKs. This compound functions as a Wnt/β-catenin activator and induces autophagy.
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The Kaohsiung Journal of Medical Sciences, September 12, 2025, e70103
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Journal of the American Heart Association, October 2, 2017, e005295
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The American Journal of Sports Medicine, February 24, 2025, 1184-1194
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| S1060 |
AZD2281 (Olaparib)
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Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1/2 with IC50 of 5 nM/1 nM in cell-free assays, 300-times less effective against tankyrase-1. Olaparib induces significant autophagy that is associated with mitophagy in cells with BRCA mutations.
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Cell, 2025, 188(18):5081-5099.e27
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Cancer Cell, 2025, 43(8):1530-1548.e9
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Cancer Cell, 2025, 43(4):776-796.e14
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| S8048 |
ABT-199 (Venetoclax)
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Venetoclax (ABT-199, GDC-0199) is a Bcl-2-selective inhibitor with Ki of <0.01 nM in cell-free assays, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. Venetoclax is reported to induce cell growth suppression, apoptosis, cell cycle arrest, and autophagy in triple negative breast cancer MDA-MB-231 cells. Phase 3.
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Cell, 2025, S0092-8674(25)00689-0
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Cell, 2025, S0092-8674(25)01233-4
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Signal Transduct Target Ther, 2025, 10(1):161
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| S7655 |
Telaglenastat (CB-839)
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Telaglenastat (CB-839) is a potent, selective, and orally bioavailable glutaminase inhibitor with IC50 of 24 nM for recombinant human GAC. It induces autophagy and has antitumor activity. Phase 1.
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Signal Transduct Target Ther, 2025, 10(1):271
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Bone Res, 2025, 13(1):62
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Clin Mol Hepatol, 2025, 10.3350/cmh.2024.0694
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| S1378 |
Ruxolitinib (INCB18424)
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Ruxolitinib (INCB18424) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3. This compound kills tumor cells through toxic mitophagy. It induces autophagy and enhances apoptosis.
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Nature, 2025, 10.1038/s41586-025-08938-8
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Nat Commun, 2025, 16(1):8409
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Nat Commun, 2025, 16(1):492
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| S1039 |
Rapamycin (Sirolimus)
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Rapamycin is a specific mTOR inhibitor with IC50 of ~0.1 nM in HEK293 cells. This compound binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. It is an autophagy activator and an immunosuppressant.
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Nature, 2025, 10.1038/s41586-025-09018-7
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Signal Transduct Target Ther, 2025, 10(1):271
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Cell Metab, 2025, S1550-4131(25)00294-3
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| S2673 |
Trametinib (GSK1120212)
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Trametinib (GSK1120212, JTP-74057) is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM in cell-free assays, and it does not inhibit the kinase activities of c-Raf, B-Raf, ERK1/2. This compound activates autophagy and induces apoptosis.
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Cancer Cell, 2025, S1535-6108(25)00271-5
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Signal Transduct Target Ther, 2025, 10(1):161
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Signal Transduct Target Ther, 2025, 10(1):299
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