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抑制剂选择性比较

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所有产品 PDK抑制剂(6) PDK激活剂(1) 新PDK产品

目录号	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。	Cell, 2019, 176(6):1379-1392 Nat Cell Biol, 2019, 21(6):778-790 Arthritis Res Ther, 2019, 21(1):153	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.
S1274	BX-795 BX-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。	Nature, 2019, 567(7747):262-266 Cell, 2019, 176(6):1447-1460 Nat Immunol, 2019, 20(1):18-28	Induction of basal p62 Ser403 phosphorylation in ULK1/2-deﬁcient MEF was suppressed by BX-795, an inhibitor of TBK1. WT ( Ulk1 +/+/Ulk2 +/+) and Ulk1 -/- /Ulk2 -/-(KO) MEF were treated with NaCl/Pi (Con) or 10 uM BX-795 for 6 h, and subjected to immunoblotting with indicated antibodies.
S1275	BX-912 BX-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。	Cancer Cell, 2019, 36(2):179-193 Cell, 2019, 36(2):179-193 Nat Cell Biol, 2019, 21(6):778-790	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.
S1556	PHT-427 PHT-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，K_i分别为2.7 μM和5.2 μM。	FEBS Lett, 2019, 593(2):175-186 Nat Commun, 2018, 9(1):2434 Nutrients, 2018, 10(10)	The inhibition of PI3K/Akt pathway is involved in ATG-induced FOXO3a dephosphorylation in PDGF-BB-activated HSCs. Serum-starved LX-2 human HSCs were pretreated with or without DMSO (vehicle) or ATG (0.5 uM) for 4 h, in the absence or presence of PI3K inhibitor LY294002 (20 uM) or Akt inhibitor PHT-427 (20 uM), and then incubated with or without 50 ng/ml PDGF-BB for 4 h. After treatment, aliquots of whole cell lysates were collected and subjected to Western blotting analysis. The experiments were repeated three times with similar results and a representative blot was shown for each protein. Total protein levels of Akt and FOXO3a served as internal controls.
S7087	GSK2334470 GSK2334470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。	Nat Cell Biol, 2019, 21(6):778-790 Br J Pharmacol, 2019, 176(3):416-435 Biochem J, 2019, 476(20):3081-3107	(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.
S6504^New	BX517 BX517是有效的、选择性PDK1抑制剂，可与该蛋白的ATP结合口袋结合，IC50为6 nM。
S2272^New	Indoprofen Indoprofen是一种非甾体类抗炎药（NSAID）和 cyclooxygenase (COX) 抑制剂。Indoprofen通过激活 PDK1/AKT pathway 来防止衰老小鼠的肌肉萎缩。Indoprofen选择性地增加 SMN2-luciferase reporter protein 和 endogenous SMN protein。

目录号	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。	Cell,2019, 176(6):1379-1392 Nat Cell Biol,2019, 21(6):778-790 Arthritis Res Ther,2019, 21(1):153	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.
S1274	BX-795 BX-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。	Nature,2019, 567(7747):262-266 Cell,2019, 176(6):1447-1460 Nat Immunol,2019, 20(1):18-28	Induction of basal p62 Ser403 phosphorylation in ULK1/2-deﬁcient MEF was suppressed by BX-795, an inhibitor of TBK1. WT ( Ulk1 +/+/Ulk2 +/+) and Ulk1 -/- /Ulk2 -/-(KO) MEF were treated with NaCl/Pi (Con) or 10 uM BX-795 for 6 h, and subjected to immunoblotting with indicated antibodies.
S1275	BX-912 BX-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。	Cancer Cell,2019, 36(2):179-193 Cell,2019, 36(2):179-193 Nat Cell Biol,2019, 21(6):778-790	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.
S1556	PHT-427 PHT-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，K_i分别为2.7 μM和5.2 μM。	FEBS Lett,2019, 593(2):175-186 Nat Commun,2018, 9(1):2434 Nutrients,2018, 10(10)	The inhibition of PI3K/Akt pathway is involved in ATG-induced FOXO3a dephosphorylation in PDGF-BB-activated HSCs. Serum-starved LX-2 human HSCs were pretreated with or without DMSO (vehicle) or ATG (0.5 uM) for 4 h, in the absence or presence of PI3K inhibitor LY294002 (20 uM) or Akt inhibitor PHT-427 (20 uM), and then incubated with or without 50 ng/ml PDGF-BB for 4 h. After treatment, aliquots of whole cell lysates were collected and subjected to Western blotting analysis. The experiments were repeated three times with similar results and a representative blot was shown for each protein. Total protein levels of Akt and FOXO3a served as internal controls.
S7087	GSK2334470 GSK2334470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。	Nat Cell Biol,2019, 21(6):778-790 Br J Pharmacol,2019, 176(3):416-435 Biochem J,2019, 476(20):3081-3107	(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.
S6504^New	BX517 BX517是有效的、选择性PDK1抑制剂，可与该蛋白的ATP结合口袋结合，IC50为6 nM。

目录号

产品描述

文献引用

实验数据

S2272^New

Indoprofen

Indoprofen是一种非甾体类抗炎药（NSAID）和 cyclooxygenase (COX) 抑制剂。Indoprofen通过激活 PDK1/AKT pathway 来防止衰老小鼠的肌肉萎缩。Indoprofen选择性地增加 SMN2-luciferase reporter protein 和 endogenous SMN protein。

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