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Autophagy activators/inhibitors

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Cat.No. Product Name Information Product Use Citations Product Validations
S1049 Y-27632 Dihydrochloride 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.
Nature, 2025, 642(8066):143-153
Cell, 2025, S0092-8674(25)00406-4
Cell, 2025, S0092-8674(25)00807-4
Verified customer review of Y-27632 Dihydrochloride
S1263 CHIR-99021 (Laduviglusib) 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.
Cancer Cell, 2025, 43(4):776-796.e14
Circulation, 2025, 151(20):1436-1448
Circulation, 2025, 151(20):1436-1448
Verified customer review of CHIR-99021 (Laduviglusib)
S1060 AZD2281 (Olaparib) 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.
Cell, 2025, 188(18):5081-5099.e27
Cancer Cell, 2025, 43(8):1530-1548.e9
Cancer Cell, 2025, 43(4):776-796.e14
Verified customer review of AZD2281 (Olaparib)
S8048 ABT-199 (Venetoclax) 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.
Cell, 2025, S0092-8674(25)00689-0
Cell, 2025, S0092-8674(25)01233-4
Signal Transduct Target Ther, 2025, 10(1):161
Verified customer review of ABT-199 (Venetoclax)
S7655 Telaglenastat (CB-839) 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.
Signal Transduct Target Ther, 2025, 10(1):271
Bone Res, 2025, 13(1):62
Clin Mol Hepatol, 2025, 10.3350/cmh.2024.0694
Verified customer review of Telaglenastat (CB-839)
S1378 Ruxolitinib (INCB18424) 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.
Nature, 2025, 10.1038/s41586-025-08938-8
Nat Commun, 2025, 16(1):8409
Nat Commun, 2025, 16(1):492
Verified customer review of Ruxolitinib (INCB18424)
S1039 Rapamycin (Sirolimus) 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.
Nature, 2025, 10.1038/s41586-025-09018-7
Signal Transduct Target Ther, 2025, 10(1):271
Cell Metab, 2025, S1550-4131(25)00294-3
Verified customer review of Rapamycin (Sirolimus)
S2673 Trametinib (GSK1120212) 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.
Cancer Cell, 2025, S1535-6108(25)00271-5
Signal Transduct Target Ther, 2025, 10(1):161
Signal Transduct Target Ther, 2025, 10(1):299
Verified customer review of Trametinib (GSK1120212)
S2924 Laduviglusib (CHIR-99021) Hydrochloride 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.
Cell, 2025, 188(11):2974-2991.e20
Cell, 2025, S0092-8674(25)00807-4
Protein Cell, 2025, pwaf098
Verified customer review of Laduviglusib (CHIR-99021) Hydrochloride
S1250 MDV3100 (Enzalutamide) Enzalutamide is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. Enzalutamide is shown to increase autophagy.
Cancer Cell, 2025, 43(5):891-904.e10
Nat Genet, 2025, 57(10):2468-2481
Nat Genet, 2025, 57(12):3027-3038
Verified customer review of MDV3100 (Enzalutamide)

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