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Catalog No. Product Name Information Product Use Citations Product Validations
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.
Proc Natl Acad Sci U S A, 2021, 118(38)e2102423118
Int J Mol Sci, 2021, 22(21)11864
bioRxiv, 2021, 2021.04.15.440067
S1120 Everolimus (RAD001) Everolimus (RAD001, SDZ-RAD) 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, 2022, S1535-6108(21)00662-0
J Immunother Cancer, 2022, 10(1)e003766
Redox Biol, 2022, 51:102268
S5003 Tacrolimus (FK506) Tacrolimus (FK506, FR900506, Fujimycin, Prograf) 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.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Birth Defects Res, 2022, 10.1002/bdr2.2001
EMBO Mol Med, 2021, 13(3):e12834
S7091 Zotarolimus (ABT-578) Zotarolimus (ABT-578) is an analogue of rapamycin, and inhibits FKBP-12 binding with IC50 of 2.8 nM.
PLoS Biol, 2019, 17(5):e3000252
PLoS Biol, 2019, 17(5):e3000252
S8317 3BDO 3BDO, a butyrolactone derivative, could target FKBP1A and activate the mTOR signaling pathway. It inhibits autophagy in HUVECs. 3BDO inhibits oxLDL-induced apoptosis.
Front Oncol, 2021, 11:665420
Mol Med Rep, 2021, 24(2)592
Biomed Res Int, 2020, 2020:4035306
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.
S3469 Shield-1 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
S8487New AP20187 AP20187 (B/B Homodimerizer) is a chemical inducer of dimerization that activates FKBP-Casp8.
S9726New Rimiducid (AP1903) Rimiducid (AP1903) is a chemical protein dimerizer and binds tightly to the target FKBP fusion protein while binding minimally to the abundant natural FKBP. Rimiducid elicites potent and dose-dependent apoptosis of cells in culture expressing dimerizer-dependent Fas constructs, with an EC50 of ≈0.1 nM.
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.
Proc Natl Acad Sci U S A, 2021, 118(38)e2102423118
Int J Mol Sci, 2021, 22(21)11864
bioRxiv, 2021, 2021.04.15.440067
S1120 Everolimus (RAD001) Everolimus (RAD001, SDZ-RAD) 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, 2022, S1535-6108(21)00662-0
J Immunother Cancer, 2022, 10(1)e003766
Redox Biol, 2022, 51:102268
S5003 Tacrolimus (FK506) Tacrolimus (FK506, FR900506, Fujimycin, Prograf) 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.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Birth Defects Res, 2022, 10.1002/bdr2.2001
EMBO Mol Med, 2021, 13(3):e12834
S7091 Zotarolimus (ABT-578) Zotarolimus (ABT-578) is an analogue of rapamycin, and inhibits FKBP-12 binding with IC50 of 2.8 nM.
PLoS Biol, 2019, 17(5):e3000252
PLoS Biol, 2019, 17(5):e3000252
S8317 3BDO 3BDO, a butyrolactone derivative, could target FKBP1A and activate the mTOR signaling pathway. It inhibits autophagy in HUVECs. 3BDO inhibits oxLDL-induced apoptosis.
Front Oncol, 2021, 11:665420
Mol Med Rep, 2021, 24(2)592
Biomed Res Int, 2020, 2020:4035306
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.
S8487New AP20187 AP20187 (B/B Homodimerizer) is a chemical inducer of dimerization that activates FKBP-Casp8.
S9726New Rimiducid (AP1903) Rimiducid (AP1903) is a chemical protein dimerizer and binds tightly to the target FKBP fusion protein while binding minimally to the abundant natural FKBP. Rimiducid elicites potent and dose-dependent apoptosis of cells in culture expressing dimerizer-dependent Fas constructs, with an EC50 of ≈0.1 nM.