FKBP

亜型選択性的な製品

FKBP製品

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  • FKBP阻害剤 (4)
  • FKBP活性剤(1)
  • FKBPモジュレータ(1)
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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)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
Mol Metab, 2024, 80:101876
Cancer Cell, 2023, 41(1):139-163.e17
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.
Cell Metab, 2022, 34(5):667-680.e6
Cell Metab, 2022, S1550-4131(22)00191-7
Nat Struct Mol Biol, 2022, (9):863-870.
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 Commun, 2023, 14(1):3928
Cell Commun Signal, 2023, 21(1):25
JCI Insight, 2023, 8(14)e157027
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.
Adv Sci (Weinh), 2023, 10(13):e2205436
Research Square, 2023, 10.21203/rs.3.rs-3629594/v1
J Cancer, 2022, 13(4):1203-1213
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.
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)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
Mol Metab, 2024, 80:101876
Cancer Cell, 2023, 41(1):139-163.e17
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.
Cell Metab, 2022, 34(5):667-680.e6
Cell Metab, 2022, S1550-4131(22)00191-7
Nat Struct Mol Biol, 2022, (9):863-870.
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 Commun, 2023, 14(1):3928
Cell Commun Signal, 2023, 21(1):25
JCI Insight, 2023, 8(14)e157027
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.
Adv Sci (Weinh), 2023, 10(13):e2205436
Research Square, 2023, 10.21203/rs.3.rs-3629594/v1
J Cancer, 2022, 13(4):1203-1213
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.

FKBP阻害剤の選択性比較

Tags: FKBP inhibitor|FKBP agonist|FKBP activator|FKBP inducer|FKBP antagonist|FKBP signaling pathway|FKBP assay kit