FKBP
抑制剂选择性比较
特异性亚型抑制剂
FKBP产品
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1120 |
Everolimus (RAD001)Everolimus (RAD001, SDZ-RAD)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。 |
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.
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| S5003 |
Tacrolimus (FK506)Tacrolimus (FK506, FR900506, Fujimycin, Prograf) 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。 |
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, AP23573)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。 |
Breast cancer cells were pretreated with 100ng/ml EGF for 15 min and then treated with the indicated concentrations of Deforolimus for 24 hours.
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| 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。 |
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| S8317 |
3BDO3BDO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。3BDO 还可抑制oxLDL诱导的凋亡。 |
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| S0713 |
S107 hydrochlorideS107 hydrochloride 是一种 RyR2 (type 2 ryanodine receptor)/FKBP12.6 (FK506 binding protein 12.6) complex 的特异性稳定剂，会影响 Ca2+ 信号传导。 |
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| S3469 |
Shield-1Shield-1 是 FK506-binding protein-12 (FKBP) 的特异性细胞渗透性高亲和力配体。 |
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| S8487New |
AP20187AP20187 (B/B Homodimerizer, HY-13992) 是一种二聚化的化学诱导剂，可激活 FKBP-Casp8。 |
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| S9726New |
Rimiducid (AP1903)Rimiducid (AP1903) 是一种化学蛋白二聚体，可与 FKBP 融合蛋白 紧密结合，同时与丰富的天然 FKBP 结合最少。Rimiducid 在表达二聚体依赖的 Fas 构建体的培养物中引发有效且剂量依赖的细胞凋亡，EC50 约为 0.1 nM。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1120 |
Everolimus (RAD001)Everolimus (RAD001, SDZ-RAD)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。 |
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, FR900506, Fujimycin, Prograf) 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。 |
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, AP23573)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。 |
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。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S8317 |
3BDO3BDO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。3BDO 还可抑制oxLDL诱导的凋亡。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S0713 |
S107 hydrochlorideS107 hydrochloride 是一种 RyR2 (type 2 ryanodine receptor)/FKBP12.6 (FK506 binding protein 12.6) complex 的特异性稳定剂，会影响 Ca2+ 信号传导。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S3469 |
Shield-1Shield-1 是 FK506-binding protein-12 (FKBP) 的特异性细胞渗透性高亲和力配体。 |
||
| S8487New |
AP20187AP20187 (B/B Homodimerizer, HY-13992) 是一种二聚化的化学诱导剂，可激活 FKBP-Casp8。 |
||
| S9726New |
Rimiducid (AP1903)Rimiducid (AP1903) 是一种化学蛋白二聚体，可与 FKBP 融合蛋白 紧密结合，同时与丰富的天然 FKBP 结合最少。Rimiducid 在表达二聚体依赖的 Fas 构建体的培养物中引发有效且剂量依赖的细胞凋亡，EC50 约为 0.1 nM。 |
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