BX795是一种高效、选择性的PDK1抑制剂,IC50为6 nM。它还有效抑制TBK1和IKKε,IC50值分别为6 nM和41 nM。BX795阻止S6K1、Akt、PKCδ和GSK3β的磷酸化,但对酶如PKA、PKC、c-Kit和GSK3β的选择性较低。此外,BX795调节自噬。
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产品名称 | PDK1 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
OSU-03012 |
++
PDK-1, IC50: 5 μM |
99%+ | |||||||||||||||||
BX-912 |
+++
PDK-1, IC50: 12 nM |
PKA | 99%+ | ||||||||||||||||
GSK2334470 |
+++
PDK-1, IC50: 10 nM |
99%+ | |||||||||||||||||
BX795 |
++++
PDK-1, IC50: 6 nM |
c-Kit | 99%+ | ||||||||||||||||
PHT-427 |
+
PDK1, Ki: 5.2 μM |
Akt | 99%+ | ||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
产品名称 | NF-κB ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
PDTC ammonium | ✔ | 98% | |||||||||||||||||
QNZ |
++++
NF-κB, IC50: 11 nM |
99%+ | |||||||||||||||||
Sodium 4-Aminosalicylate Dihydrate | ✔ | 98% | |||||||||||||||||
Sodium Salicylate | ✔ | 95% | |||||||||||||||||
Parthenolide | ✔ | p53 | 97% HPLC | ||||||||||||||||
JSH-23 |
+
NF-κB, IC50: 7.1 μM |
98% | |||||||||||||||||
Phenethyl caffeate | ✔ | 98% | |||||||||||||||||
Andrographolide | ✔ | 98+% | |||||||||||||||||
Curcumin | ✔ | HDAC,Nrf2 | 98% | ||||||||||||||||
SC75741 |
+++
NF-κB, EC50: 200 nM |
99%+ | |||||||||||||||||
CBL0137 HCl |
++
NF-κB, EC50: 0.47 μM |
p53 | 99%+ | ||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | The phosphoinositide 3-kinase/3-phosphoinositide-dependent kinase 1 (PDK1)/Akt signaling pathway plays a key role in cancer cell growth, survival, and tumor angiogenesis and represents a promising target for anticancer drugs[3]. BX-912 is a direct, selective, and ATP-competitive PDK1 inhibitor with an IC50 value of 26 nM. BX-912 blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induces apoptosis[3]. When treating asynchronously growing cultures of tumor cells for 18 h with 10 μM BX-912, it promoted a pronounced increase in the population of MDA-468 cells with 4 N DNA content, indicative of a block at the G2/M phase of the cell cycle. BX-912 also potently inhibited the growth of HCT-116 and PC-3 cells in soft agar, showing a 96% inhibitory effect at a dose of 1 μM for HCT-116 and IC50 value of 0.32 μM for PC-3[3]. |
作用机制 | BX-795 is a competitive inhibitor of PDK1 activity with respect to its substrate, ATP, suggesting that it binds to the ATP binding pocket of PDK1[2]. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
human 5637 cell | Growth inhibition assay | Inhibition of human 5637 cell growth in a cell viability assay, IC50=8.07904 μM | SANGER | ||
human 697 cell | Growth inhibition assay | Inhibition of human 697 cell growth in a cell viability assay, IC50=1.01623 μM | SANGER | ||
human 8-MG-BA cell | Growth inhibition assay | Inhibition of human 8-MG-BA cell growth in a cell viability assay, IC50=1.95744 μM | SANGER | ||
human A172 cell | Growth inhibition assay | Inhibition of human A172 cell growth in a cell viability assay, IC50=4.4457 μM | SANGER | ||
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.69mL 0.34mL 0.17mL |
8.45mL 1.69mL 0.85mL |
16.91mL 3.38mL 1.69mL |
CAS号 | 702675-74-9 |
分子式 | C23H26IN7O2S |
分子量 | 591.468 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,2-8°C |
溶解度 |
DMSO: 35 mg/mL(59.17 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |
2% DMSO+30% PEG +2% Tween 80+water 4 mg/mL |