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Isoform-selective Products

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)
S9813 dTAG-13 dTAG-13(FKBP12 PROTAC dTAG-13) is an ortho-substituted, heterobifunctional selective degrader of FKBP12F36V that effectively engage FKBP12F36V and CRBN leading to rapid and selective CRBN-mediated degradation of FKBP12F36V.It can useful for target validation in the context of drug discovery.
S9726 Rimiducid (AP1903) Rimiducid (AP1903) is a chemical protein dimerizer that binds tightly to the target FKBP fusion protein while binding minimally to the abundant natural FKBP. This compound elicits potent and dose-dependent apoptosis of cells in culture expressing dimerizer-dependent Fas constructs, with an EC50 of ≈0.1 nM.
S3469 Shield-1 (Shld1) Shield-1 is a specific, cell-permeant and high-affinity ligand of FK506-binding protein-12 (FKBP). Shield-1 reverses the instability by binding to mutated FKBP (mtFKBP), allowing conditional expression of mtFKBP-fused proteins. Shield-1 stabilizes the entire fusion protein.
Cell Rep, 2022, 38(12):110536
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)
S8487 AP20187 (B/B Homodimerizer) AP20187 (B/B Homodimerizer) is a chemical inducer of dimerization that activates FKBP-Casp8.
Front Immunol, 2022, 13:1110322
S0713 S107 hydrochloride S107 hydrochloride is a specific stabilizer of RyR2 (type 2 ryanodine receptor)/FKBP12.6 (FK506 binding protein 12.6) complex that affects Ca2+ signaling.
E8289New dTAGV-1 TFA dTAGV-1 TFA is a degrader of FKBP12F36V-tagged proteins that functions as a PROTAC. It mediates the degradation of FKBP12F36V-Nluc in vivo. (Pink: Target Protein Ligand ; Black: Linker ; Blue: VHL Ligand ; VHL Ligand+Linker (A))
S9966New SAFit2 SAFit2 is a highly potent and selective antagonist of FK506-binding protein 51 (FKBP51) with a Ki of 6 nM. It exhibits anxiolytic and antidepressant-like effects, regulates AKT2-AS160 signaling and metabolic function, and may be useful in research on stress-related disorders and type 2 diabetes.
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)