FKBP

抑制剂选择性比较

FKBP产品

所有产品 FKBP抑制剂(4) FKBP激活剂(1)

目录号	产品描述	文献引用	实验数据
S1120	Everolimus (RAD001) Everolimus (RAD001)是一种mTOR抑制剂，作用于FKBP12，在无细胞试验中IC50为1.6-2.4 nM。Everolimus 可诱导细胞凋亡及自噬并抑制肿瘤细胞的增殖。	Cancer Cell, 2020, 37(2):183-199 Nat Commun, 2020, 26;11(1):2641 Neuro Oncol, 2020, 15;22(4):563-574	Cytoskeleton organisation of 786-O SuR treated with NVP-LDE225 (2.5 uM), everolimus (1 uM), and their combination for 24 h was analysed by confocal microscopy. Actin-based structures were revealed by rhodaminated phalloidin staining (red fluorescence). Localisation of focal adhesion points was obtained by immunofluorescent staining of p-paxillin (green fluorescence). Merged row images show overlapping of p-paxillin and actin signals. Moreover, all captures were shown in transmitted light. Scale bars, 10 um.
S5003	Tacrolimus (FK506) Tacrolimus (FK506) 是一种23元大环内酯物，通过结合到抑免蛋白FKBP12 (FK506 结合蛋白)产生新的复合物，从而降低T细胞中肽酰脯氨酰异构酶活性。Tacrolimus 也可抑制calcineurin钙调磷酸酶的磷酸酶活性。Tacrolimus 可诱导血管内皮细胞的自噬。	Blood, 2020, 2;135(1):28-40 Cancer Lett, 2020, 10;482:8-18 Signal Transduct Target Ther, 2020, 5:23	Effect of FK506 on cytosolic calcium homeostasis induced by TG and thrombin in human platelets. (A-B) Human platelets were suspended in a Ca 2+-free medium (100 µM of EGTA was added as indicated by arrowhead), and preincubated for 5 min at 37oC in the absence (solid black traces) or presence of increased concentrations (0.01-100 µM) of FK506 (light-doted and dark solid-grey traces, respectively). Cells were then stimulated with TG (200 nM; A) or Thr (0.1 U/mL; B) and 3 min later 300 μM of CaCl2 was added to extracellular medium to visualize calcium entry.
S1022	Ridaforolimus (Deforolimus, MK-8669) Ridaforolimus (Deforolimus, MK-8669)是一种选择性mTOR抑制剂，在HT-1080细胞中IC50为0.2 nM；不被分类为一种前药，mTOR抑制和FKBP12结合与rapamycin相似。Phase 3。	PLoS Biol, 2019, 17(5):e3000252 Sci Signal, 2019, 12(589) Int J Mol Med, 2019, 43(1):47-56	Breast cancer cells were pretreated with 100ng/ml EGF for 15 min and then treated with the indicated concentrations of Deforolimus for 24 hours.
S7091	Zotarolimus(ABT-578) Zotarolimus (ABT-578)是rapamycin的类似物,可以抑制FKBP-12结合的IC50为2.8nM。	PLoS Biol, 2019, 17(5):e3000252 PLoS Biol, 2019, 17(5):e3000252
S8317	3BDO 3BDO是一种丁内酯衍生物，可靶向FKBP1A并激活mTOR信号通路，抑制HUVECs自噬。	Biomater Sci, 2019, 7(9):3779-3787 Front Neurosci, 2019, 13:1225

目录号	产品描述	文献引用	实验数据
S1120	Everolimus (RAD001) Everolimus (RAD001)是一种mTOR抑制剂，作用于FKBP12，在无细胞试验中IC50为1.6-2.4 nM。Everolimus 可诱导细胞凋亡及自噬并抑制肿瘤细胞的增殖。	Cancer Cell,2020, 37(2):183-199 Nat Commun,2020, 26;11(1):2641 Neuro Oncol,2020, 15;22(4):563-574	Cytoskeleton organisation of 786-O SuR treated with NVP-LDE225 (2.5 uM), everolimus (1 uM), and their combination for 24 h was analysed by confocal microscopy. Actin-based structures were revealed by rhodaminated phalloidin staining (red fluorescence). Localisation of focal adhesion points was obtained by immunofluorescent staining of p-paxillin (green fluorescence). Merged row images show overlapping of p-paxillin and actin signals. Moreover, all captures were shown in transmitted light. Scale bars, 10 um.
S5003	Tacrolimus (FK506) Tacrolimus (FK506) 是一种23元大环内酯物，通过结合到抑免蛋白FKBP12 (FK506 结合蛋白)产生新的复合物，从而降低T细胞中肽酰脯氨酰异构酶活性。Tacrolimus 也可抑制calcineurin钙调磷酸酶的磷酸酶活性。Tacrolimus 可诱导血管内皮细胞的自噬。	Blood,2020, 2;135(1):28-40 Cancer Lett,2020, 10;482:8-18 Signal Transduct Target Ther,2020, 5:23	Effect of FK506 on cytosolic calcium homeostasis induced by TG and thrombin in human platelets. (A-B) Human platelets were suspended in a Ca 2+-free medium (100 µM of EGTA was added as indicated by arrowhead), and preincubated for 5 min at 37oC in the absence (solid black traces) or presence of increased concentrations (0.01-100 µM) of FK506 (light-doted and dark solid-grey traces, respectively). Cells were then stimulated with TG (200 nM; A) or Thr (0.1 U/mL; B) and 3 min later 300 μM of CaCl2 was added to extracellular medium to visualize calcium entry.
S1022	Ridaforolimus (Deforolimus, MK-8669) Ridaforolimus (Deforolimus, MK-8669)是一种选择性mTOR抑制剂，在HT-1080细胞中IC50为0.2 nM；不被分类为一种前药，mTOR抑制和FKBP12结合与rapamycin相似。Phase 3。	PLoS Biol,2019, 17(5):e3000252 Sci Signal,2019, 12(589) Int J Mol Med,2019, 43(1):47-56	Breast cancer cells were pretreated with 100ng/ml EGF for 15 min and then treated with the indicated concentrations of Deforolimus for 24 hours.
S7091	Zotarolimus(ABT-578) Zotarolimus (ABT-578)是rapamycin的类似物,可以抑制FKBP-12结合的IC50为2.8nM。	PLoS Biol,2019, 17(5):e3000252 PLoS Biol,2019, 17(5):e3000252

目录号

产品描述

文献引用

实验数据

S8317

3BDO

3BDO是一种丁内酯衍生物，可靶向FKBP1A并激活mTOR信号通路，抑制HUVECs自噬。

Biomater Sci, 2019, 7(9):3779-3787

Front Neurosci, 2019, 13:1225