Akt
信号通路图
研究领域
抑制剂选择性比较
特异性亚型抑制剂
Akt产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1078 |
MK-2206 2HClMK-2206 2HCl是一种高度选择性的Akt1/2/3抑制剂，在无细胞试验中IC50分别为8 nM/12 nM/65 nM；对250种其他蛋白激酶没有抑制活性。Phase 2。 |
Inhibition of AKT signaling abolishes MKK4 phosphorylation on Ser78 in injured axons. Cultures of sensory neurons were treated with 5 µM MK-2206 or 5 µM GDC-0068 for 1 hr prior to axotomy. Axonal proteins harvested at indicated time points after axotomy were subjected to immunoblot analysis.
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| S1037 |
Perifosine (KRX-0401)Perifosine (KRX-0401)是一种新型的Akt抑制剂，在MM.1S细胞中IC50为4.7 μM，靶向作用于Akt的pleckstrin同源结构域。Phase 3。 |
Tumor growth of 827 GSC-derived xenografts
treated with an AKT inhibitor perifosine (30 mg/kg
body weight). Twenty-three days after tumor
implantation in mice, perifosine was administered
by intraperitoneal injection (daily for 5 days). Error
bars represent SD. Five mice per group, *p < 0.01.
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| S1113 |
GSK690693GSK690693是 一种泛Akt抑制剂，靶向作用于Akt1/2/3，在无细胞试验中IC50为2 nM/13 nM/9 nM，也对AGC激酶家族:PKA，PrkX和PKC同工酶敏感。Phase 1。 |
UPN cells were treated with GSK690693 or MK2206 (1 uM) for 1h followed by LPA (10 uM), EGF or IGF-1 (10 ng/ml) for another 1h and Western blot was performed. Band intensities of phospho-AKT (p-AKTS473), phospho-S6 (p-S6S240/S244), phospho-YB-1 (p-YB-1S102) and YB-1 were quantified and normalized to the intensity of ERK2. It directly determined the role of AKT using two potent, AKT inhibitors with distinct actions—a catalytic domain inhibitor, GSK690693, and an allosteric inhibitor, MK2206 -in UPN and SKOV3 cells, which showed appreciable AKT and YB-1 phosphorylation upon growth factor stimulation. GSK690693 increased basal and growth factor-induced AKT phosphorylation due to blocking a negative feedback loop downstream of AKT, whereas MK2206 abolished both basal and growth-factor-induced AKT phosphorylation.
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| S2808 |
Ipatasertib (GDC-0068)Ipatasertib (GDC-0068)是一种高选择性的pan-Akt抑制剂，靶向作用于Akt1/2/3，在无细胞试验中IC50为5 nM/18 nM/8 nM，比 |