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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.
bioRxiv, 2026, 2026.01.12.699082
bioRxiv, 2026, 2026.05.29.728765
Proc Natl Acad Sci U S A, 2025, 122(4):e2418317122
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.
Signal Transduct Target Ther, 2026, 11(1)79
Sci Rep, 2026, 16(1):4339
Oncol Rep, 2026, 55(5)94
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.
Journal of Lipid Research, May 2014, 919-928
JCI Insight, 2025, e186456
Front Oncol, 2025, 15:1486671
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.
PLOS Biology, May 21, 2019, e3000252
Pharmaceutical Chemistry Journal, March 2019, 1011–1015
Molecules, 2023, 28(6)2820