FKBP

阻害剤の選択性比較

カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
S1120 Everolimus (RAD001) <1 mg/mL 100 mg/mL '7 mg/mL
S5003 Tacrolimus (FK506) <1 mg/mL 94 mg/mL 83 mg/mL
S1022 Ridaforolimus (Deforolimus, MK-8669) <1 mg/mL 198 mg/mL <1 mg/mL
S7091 Zotarolimus (ABT-578) <1 mg/mL 100 mg/mL 100 mg/mL
S8317 3BDO <1 mg/mL 65 mg/mL 49 mg/mL
S0713 S107 hydrochloride 49 mg/mL 24 mg/mL '''10 mg/mL
S3469 Shield-1 <1 mg/mL 100 mg/mL '''100 mg/mL
S9726 Rimiducid (AP1903) <1 mg/mL 100 mg/mL ''100 mg/mL

亜型選択性的な製品

FKBP製品

製品コード 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 (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.

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.

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.

S7091

Zotarolimus (ABT-578)

Zotarolimus (ABT-578) is an analogue of rapamycin, and inhibits FKBP-12 binding with IC50 of 2.8 nM.

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.

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 high-affinity ligand of FK506-binding protein-12 (FKBP).

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.

製品コード 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 (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.

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.

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.

S7091

Zotarolimus (ABT-578)

Zotarolimus (ABT-578) is an analogue of rapamycin, and inhibits FKBP-12 binding with IC50 of 2.8 nM.

製品コード 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
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.

2021, 11:665420

2021, 24(2)592

2020, 2020:4035306

製品コード 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
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.

製品コード 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
S3469

Shield-1

Shield-1 is a specific cell-permeant high-affinity ligand of FK506-binding protein-12 (FKBP).

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.