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FKBP Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S5003 FK506 (Tacrolimus) Tacrolimus (FK506) is a 23-membered macrolide lactone, it reduces peptidyl-prolyl isomerase activity in T cells by binding to the immunophilin FKBP12 (FK506 binding protein) creating a new complex. Tacrolimus also inhibits the phosphatase activity of calcineurin. Tacrolimus induces vascular endothelial autophagy.
Proc Natl Acad Sci U S A, 2025, 122(4):e2418317122
J Nanobiotechnology, 2025, 23(1):32
PLoS Pathog, 2025, 21(1):e1012872
Verified customer review of FK506 (Tacrolimus)
S1120 RAD001 (Everolimus) Everolimus is an mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM in a cell-free assay. Everolimus induces cell apoptosis and autophagy and inhibits tumor cells proliferation.
Cancer Cell, 2025, 43(4):776-796.e14
Nat Commun, 2025, 16(1):8189
Cell Rep Med, 2025, 6(11):102425
Verified customer review of RAD001 (Everolimus)
S1022 Ridaforolimus (Deforolimus, MK-8669) Ridaforolimus (Deforolimus, MK-8669, AP23573) is a selective mTOR inhibitor with IC50 of 0.2 nM in HT-1080 cell line; while not classified as a prodrug, mTOR inhibition and FKBP12 binding is similar to rapamycin. Phase 3.
JCI Insight, 2025, e186456
Front Oncol, 2025, 15:1486671
Nat Commun, 2024, 15(1):3636
Verified customer review of Ridaforolimus (Deforolimus, MK-8669)
S7091 Zotarolimus (ABT-578) Zotarolimus (ABT-578, A 179578), an analogue of rapamycin, inhibits FKBP-12 binding with an IC50 of 2.8 nM.
Molecules, 2023, 28(6)2820
Molecules, 2023, 28(6), 2820
PLoS Biol, 2019, 17(5):e3000252