PDK
信号通路图
研究领域
- 抑制剂选择性比较
- 溶解性比较
| 目录号 | 产品目录 | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | 酒精 | ||
| S1106 | OSU-03012 (AR-12) | <1 mg/mL | 11 mg/mL | <1 mg/mL |
| S1274 | BX-795 | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S1275 | BX-912 | <1 mg/mL | 94 mg/mL | 94 mg/mL |
| S1556 | PHT-427 | <1 mg/mL | 82 mg/mL | 60 mg/mL |
| S7087 | GSK2334470 | <1 mg/mL | 90 mg/mL | 90 mg/mL |
- PDK抑制剂（5）
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1106 |
OSU-03012 (AR-12)OSU-03012 (AR-12)是一种有效的重组PDK-1(phosphoinositide-dependent kinase 1)抑制剂，无细胞试验中IC50为5 μM，比OSU-02067作用效果高2倍。 |
Serum-deprived HEK293-AT1A cells were pretreated with PD98059 (20 uM; 1 h) or OSU03012 (10 uM; 6 h) prior to 5 min stimulation with AngII (100 nm) or SII (50 uM). A, abundance of phospho-Akt T308 in whole cell detergent lysates. Representative phospho-Akt and total Akt immunoblots are shown above a bar graph depicting the mean ?S.E. of three biological replicates.
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| S1274 |
BX-795BX-795是一种有效的，特异性的PDK1抑制剂，在无细胞试验中IC50为6 nM，作用于PDK1比作用于PKA和PKC选择性分别高140和1600倍。同时，相比于 GSK3β，作用于PDK1的选择性高出100多倍。 |
(A) Washed human platelets were untreated or pretreated with the PDK1 inhibitor BX-795 (1 μM) for 5 min, and this was followed by stimulation with 2-methylthio-ADP (2MeSADP) (50 nM) under stirring for 5 min. Western blots were then probed for phosphorylated Akt (Thr308), Akt (Ser473), glycogen synthase kinase 3b (GSK3b) (Ser9), mitogen-activated protein kinase kinase 1/2 (MEK1/2) (Ser217/221), extracellular signal-regulated kinase 1/2 (ERK1/2) (Thr202/Tyr204), and cytosolic phospholipase A2 (cPLA2) (Ser505). The western blots shown are representative of three independent experiments.
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| S1275 |
BX-912BX-912是一种有效的，特异性的PDK1抑制剂，无细胞试验中IC50为12 nM，作用于PKD1比作用于PKA和PKC选择性分别高9和105倍。与 GSK3β相比，对 PDK1的选择性是600倍。 |
Inhibition of PDK1 or MEK1/2 abrogated Erk1/2 phosphorylation. Cells were treated with pharmacological inhibitors of Raf (AZ 628, PLX4032), MEK1/2 (AZD6244), p90RSK (BI-D1870), PI3Kδ (X-370), PDK1 (BX-912), Akt (MK-2206), mTOR (AZD8055) or mTORC1 (Rapamycin) respectively and indicated proteins were detected. |
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| S1556 |
PHT-427PHT-427是作用于Akt和PDPK1的双重抑制剂，对Akt和PDPK1的PH结构域具有高度亲和力，Ki分别为2.7 μM和5.2 μM。 |
Luciferase reporter assays. 32D/BCR-ABL cells transfected with the reporter construct containing 1548 bp of the Atf5 promoter were treated with either DMSO, imatinib (5 μM for 24 hours), LY294002 (20 μM for 48 hours), PHT-427 (20 μM for 24 hours), or JAK inhibitor I (10 μM for 24 hours). Error bars represent SD. |
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| S7087 |
GSK2334470GSK2334470是一种新型的PDK1抑制剂，无细胞试验中IC50约为10 nM，对其他密切相关的AGC-激酶无活性。 |
(G) Effect of the PDK1 inhibitor GSK2334470 on MYC and P70 phosphorylation in CNE2/235 cell line by immunoblotting analysis. (H) Sensitivity to GSK2334470 in CNE2/235 cells after treatment with GSK2334470 for 5 d using the MTT assay. (I) Inhibitory effect of GSK2334470 in combination with BEZ235 on cell proliferation in CNE2/235 cells using the MTT assay. (J) IC50 values of BEZ235 with or without GSK2334470 in CNE2 and CNE2/235 cell lines. The data shown are representative of 3 individual experiments.
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