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产品名称 | Akt ↓ ↑ | Akt1 ↓ ↑ | Akt2 ↓ ↑ | Akt3 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Honokiol | ✔ | MEK | 98% | ||||||||||||||||
PF-04691502 |
++++
P-Akt (S473), IC50: 3.8 nM P-Akt (T308), IC50: 7.5 nM |
98+% | |||||||||||||||||
PHT-427 |
+
Akt, Ki: 2.7 μM |
99%+ | |||||||||||||||||
Deguelin | ✔ | PI3K | 99%+ | ||||||||||||||||
TIC10 isomer | ✔ | ERK | 98+% | ||||||||||||||||
Perifosine |
+
Akt, IC50: 4.7 μM |
98% | |||||||||||||||||
Miltefosine | ✔ | PI3K,PKC | 98% | ||||||||||||||||
Triciribine |
+
Akt, IC50: 130 nM |
99%+ | |||||||||||||||||
Uprosertib |
+
Akt1, IC50: 180 nM |
+
Akt2, IC50: 328 nM |
++
Akt3, IC50: 38 nM |
99%+ | |||||||||||||||
Afuresertib |
++++
Akt1, Ki: 0.08 nM |
++++
Akt2, Ki: 2 nM |
++++
Akt3, Ki: 2.6 nM |
99%+ | |||||||||||||||
Miransertib |
++++
Akt1, IC50: 5 nM |
++++
Akt2, IC50: 4.5 nM |
++
Akt3, IC50: 16 nM |
98+% | |||||||||||||||
GSK-690693 |
++++
Akt1, IC50: 2 nM |
+++
Akt2, IC50: 13 nM |
+++
Akt3, IC50: 9 nM |
99%+ | |||||||||||||||
AT7867 |
++
Akt1, IC50: 32 nM |
++
Akt2, IC50: 17 nM |
++
Akt3, IC50: 47 nM |
PKA | 99%+ | ||||||||||||||
AKT inhibitor VIII |
++
Akt1, IC50: 58 nM |
+
Akt2, IC50: 210 nM |
+
Akt3, IC50: 2119 nM |
97% | |||||||||||||||
MK-2206 2HCl |
+++
Akt1, IC50: 8 nM |
+++
Akt2, IC50: 12 nM |
+
Akt3, IC50: 65 nM |
99%+ | |||||||||||||||
Ipatasertib |
++++
Akt1, IC50: 5 nM |
++
Akt2, IC50: 18 nM |
+++
Akt3, IC50: 8 nM |
99%+ | |||||||||||||||
AT13148 |
++
Akt1, IC50: 38 nM |
+
Akt2, IC50: 402 nM |
++
Akt3, IC50: 50 nM |
PKA | 95% | ||||||||||||||
Capivasertib |
++++
Akt1, IC50: 3 nM |
+++
Akt2, IC50: 8 nM |
+++
Akt3, IC50: 8 nM |
99%+ | |||||||||||||||
A-674563 HCl |
+++
Akt1, Ki: 11 nM |
PKA | 99% | ||||||||||||||||
CCT128930 |
+++
Akt2, IC50: 6 nM |
PKA | 95% | ||||||||||||||||
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。 |
描述 | Akt/PKB is the major molecular in the PI3K pathway. It contains a PH domain that specifically binds PtdIns(3,4,5)P3 on the plasma membrane, which guides AKT to the cell membrane in a process mediated by interaction with the phospholipids then switches AKT to an active form. Elevation of Akt activation is an obvious clinical strategy to prevent progressive neuronal death in neurological diseases. SC79 is a pan-Akt activator, though it suppresses AKT PH-domain plasma membrane translocation. In multiple cell lines, treatment with 1-4ug/ml SC79 can dramatically increase p-AKT. SC79 treatment (4μg/ml) can reduce the hippocampal neuron death induced by glutamate. Intraperitoneal injection of 40mg/kg SC79 can prevent stroke induced Akt deactivation and neuronal death in brain of mouse ischemia model. This also hinted that SC79 was brain-penetrable[1]. |
作用机制 | SC79 can directly bind to AKT and convert AKT to an active conformation, which is more suitable to be phosphorylated by upstream kinases.[1] |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.74mL 0.55mL 0.27mL |
13.71mL 2.74mL 1.37mL |
27.41mL 5.48mL 2.74mL |
CAS号 | 305834-79-1 |
分子式 | C17H17ClN2O5 |
分子量 | 364.78 |
SMILES Code | O=C(OCC)C(C#N)C1C(C(OCC)=O)=C(N)OC2=CC=C(Cl)C=C12 |
别名 | |
运输 | 蓝冰 |
InChI Key | DXVKFBGVVRSOLI-UHFFFAOYSA-N |
Pubchem ID | 2810830 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C |
溶解方案 |
DMSO: 105 mg/mL(287.84 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 无水乙醇: 50 mg/mL(137.07 mM),配合低频超声助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
|
动物实验配方 |
2% DMSO+corn oil 5 mg/mL |