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Catalog No. Product Name Information Product Use Citations Product Validations
S1120 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.
Cell, 2024, 187(3):712-732.e38
Cell, 2024, 187(3):712-732.e38
Kidney Int, 2024, S0085-2538(24)00627-6
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.
Nat Commun, 2024, 15(1):3636
Sci Rep, 2024, 14(1):9070
Cell Metab, 2022, 34(5):667-680.e6
S5003 Tacrolimus (FK506) 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.
Nat Immunol, 2024, 25(5):860-872
Int J Antimicrob Agents, 2024, 63(5):107116
Cell Commun Signal, 2024, 22(1):428
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.
NPJ Parkinsons Dis, 2024, 10(1):52
Adv Sci (Weinh), 2023, 10(13):e2205436
Research Square, 2023, 10.21203/rs.3.rs-3629594/v1
S7091 Zotarolimus (ABT-578) Zotarolimus (ABT-578,A 179578) is an analogue of rapamycin, and inhibits FKBP-12 binding with IC50 of 2.8 nM.
Molecules, 2023, 28(6)2820
Molecules, 2023, 28(6), 2820
PLoS Biol, 2019, 17(5):e3000252
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
S8487 AP20187 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.
S9726 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.
S9813New 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.
S1120 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.
Cell, 2024, 187(3):712-732.e38
Cell, 2024, 187(3):712-732.e38
Kidney Int, 2024, S0085-2538(24)00627-6
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.
Nat Commun, 2024, 15(1):3636
Sci Rep, 2024, 14(1):9070
Cell Metab, 2022, 34(5):667-680.e6
S5003 Tacrolimus (FK506) 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.
Nat Immunol, 2024, 25(5):860-872
Int J Antimicrob Agents, 2024, 63(5):107116
Cell Commun Signal, 2024, 22(1):428
S7091 Zotarolimus (ABT-578) Zotarolimus (ABT-578,A 179578) is an analogue of rapamycin, and inhibits FKBP-12 binding with IC50 of 2.8 nM.
Molecules, 2023, 28(6)2820
Molecules, 2023, 28(6), 2820
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.
NPJ Parkinsons Dis, 2024, 10(1):52
Adv Sci (Weinh), 2023, 10(13):e2205436
Research Square, 2023, 10.21203/rs.3.rs-3629594/v1
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.
S9813New 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.

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