FKBP

亜型選択性的な製品

FKBP製品

• All (10)
• FKBP阻害剤 (4)
• FKBP活性剤(1)
• FKBPモジュレータ(1)
• 新製品

製品コード	製品名称	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S1120	Everolimus	エベロリムス (Everolimus (RAD001, SDZ-RAD)) は FKBP12 に結合することで形成した複合体により mTOR を阻害します。Cell-free assay における IC50 は1.6 ～ 2.4 ｎM です。エベロリムスは アポトーシス (apoptosis) と オートファジー (autophagy) を誘発することによりがん細胞の増殖を阻害します。	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 high-affinity ligand of FK506-binding protein-12 (FKBP).	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	エベロリムス (Everolimus (RAD001, SDZ-RAD)) は FKBP12 に結合することで形成した複合体により mTOR を阻害します。Cell-free assay における IC50 は1.6 ～ 2.4 ｎM です。エベロリムスは アポトーシス (apoptosis) と オートファジー (autophagy) を誘発することによりがん細胞の増殖を阻害します。	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.