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抑制剂描述:

产品名称:PS48

产品别名:见爱必信官网

英文别名:PS48

靶点:PDK-1

CAS:1180676-32-7

纯度:≥98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

PS48是一小分子PDK1激动剂,Kd值为10.3uM,特异性结合PDK1的PIF-binding pocket,区别于ATP结合位点。

溶解性:10 mM in DMSO

体外研究:

PS48 activates full length PDK1 (His-PDK1- FL) and PDK1 50-359 (His-PDK1 dm) with AC50s (the concentrations required to reach 50% of the maximal activation) of 7.95±0.2 and 10.0±2.0 μM, respectively. PS48 binds to PDK150–359 with a 1:1 stoichiometry and a binding affinity in the micromolar range (Kd=10.3 μM). PDK1 activator, PS48, has the ability to reverse the cell proliferation inhibition role of triptolide (TP) in vitro. The inhibition role of TP in cell number is significantly reversed by PS48. TP significantly increases the cell proportion in G0-G1 phase and decreases the cell proportion in G2-M and S phase. However, the effect of TP on cell cycle distribution is all reversed by PS48. In addition, suppression of PDK1/Akt/mTOR pathway by TP in high glucose (HG)-treated human renal mesangial cells (HRMCs) is also reversed by PS48, as well as the expression of Ki-67 and proliferating cell nuclear antigen (PCNA).

体内研究:

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