PDK
The 3-phosphoinositide-dependent protein kinase-1 (PDK1) has emerged as a master regulator of the AGC family of protein kinases. It acts as an upstream protein kinase phosphorylating and activating several AGC-family members implicated in the control of cell growth, proliferation, survival and metabolism regulation. These include protein kinase B (PKB)/Akt, p70 ribosomal S6 kinase (S6K), p90 ribosomal S6 kinase (RSK), the serum and glucocorticoid-induced protein kinase (SGK), as well as several protein kinase C (PKC) isoforms. PDK1 is ubiquitously expressed in cells and surprisingly for an enzyme that regulates at least 23 agoniststimulated AGC kinases, it is constitutively active. PKB like PDK1 possesses a PtdIns(3,4,5)P3 binding PH domain. Following growth factor or insulin stimulation, the phosphoinositide 3-kinase (PI 3-kinase) is activated and PDK1 and PKB are presumed to co-localise at the membrane due to their mutual ability to bind the newly generated PtdIns(3,4,5)P3 second messenger. These AGC kinases have evolved a distinct mechanism to interact with PDK1 that involves the phosphorylation of a C-terminal, non-catalytic hydrophobic motif, by distinct non-PDK1 upstream kinases, such as the mTOR complexes. Phosphorylation of the hydrophobic motif is required for PDK1 to interact and phosphorylate the non-PKB AGC kinases and functions as the gatekeeper controlling the activation of these enzymes by PDK1. PDK1 is an attractive target for cancer therapy due to its peculiar role in the regulation of cell motility, a fundamental process both in physiological and in pathological situations.
References
1.Bayascas JR.Cell Cycle. 2008;7(19):2978–2982.
2.Di Blasio L,et al. Cancers (Basel). 2017;9(3):25.
References
1.Bayascas JR.Cell Cycle. 2008;7(19):2978–2982.
2.Di Blasio L,et al. Cancers (Basel). 2017;9(3):25.
PI3K/Akt/mTOR signaling
PDK
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6-Bromo-4-methoxypyrazolo[1,5-a]pyridine-3-carbonitrile
产品货号 : M37049
cas no: 1207836-10-9
6-Bromo-4-methoxypyrazolo[1,5-a]pyridine-3-carbonitrile is a PDK1 inhibitor with anticancer and antiproliferative activity that can be used to study angiosarcoma, adenocarcinoma, multiple myeloma, psoriasis, prostate cancer, and Alzheimer's disease. -
RS1-PDK1 inhibitor
产品货号 : M34021
cas no: 1643958-85-3
RS1-PDK1 inhibitor (RS 1) is a selective inhibitor of the protein kinase PDK1 that can be used to treat and prevent disease or disorders. -
M77976
产品货号 : M33422
cas no: 394237-61-7
M77976 是一种特异性的,ATP 竞争性的丙酮酸脱氢酶激酶 PDK4 抑制剂,其作用的 IC50 值为 648 μM。M77976 有用于肥胖症和糖尿病研究的潜力。 -
KPLH1130
产品货号 : M24944
cas no: 906669-07-6
KPLH1130 改善 HFD 喂养小鼠的葡萄糖耐量。 KPLH1130 是一种特异性丙酮酸脱氢酶激酶 (PDK) 抑制剂,可阻断巨噬细胞极化并减弱促炎反应。 -
VER-246608
产品货号 : M23757
cas no: 1684386-71-7
VER-246608 是一种有效的 ATP 竞争性丙酮酸脱氢酶激酶抑制剂。