2. PI3K/Akt/mTOR Epigenetics Autophagy
  3. Akt AMPK Autophagy
  4. GSK-690693

GSK-690693 是一种 ATP 竞争型的泛 Akt 抑制剂，对 Akt1， Akt2 和 Akt3 的 IC50 分别为 2 nM，13 nM，9 nM。GSK-690693 也是一种 AMPK 的抑制剂，影响 ULK1 的活性，并能显著抑制 STING 依赖的 IRF3 的激活。

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GSK-690693 Chemical Structure

GSK-690693 Chemical Structure

CAS No. : 937174-76-0

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥776
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1 mg ￥320
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5 mg ￥705
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10 mg ￥1045
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25 mg ￥2600
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50 mg ￥4500
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Customer Review

Other Forms of GSK-690693:

GSK-690693 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 31 篇科研文献

查看 Akt 亚型特异性产品:

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Akt Akt1 Akt2 Akt3

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NUAK1 NUAK2 AMPK AMPK α1β1γ1 AMPK α2β1γ1 AMPK α1β2γ1 AMPK α2β2γ1

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

GSK-690693 is an ATP-competitive pan-Akt inhibitor with IC50s of 2 nM, 13 nM, 9 nM for Akt1, Akt2 and Akt3, respectively. GSK-690693 is also an AMPK inhibitor, affects Unc-51-like autophagy activating kinase 1 (ULK1) activity and robustly inhibits STING-dependent IRF3 activation[1][2][3].

IC50 & Target[1]

Akt1

2 nM (IC50)

Akt3

9 nM (IC50)

Akt2

13 nM (IC50)

PKCη

2 nM (IC50)

PKCθ

2 nM (IC50)

PrkX

5 nM (IC50)

PAK6

6 nM (IC50)

PAK4

10 nM (IC50)

PKCδ

14 nM (IC50)

PKCβ1

19 nM (IC50)

PKCε

21 nM (IC50)

PKA

24 nM (IC50)

PKG1β

33 nM (IC50)

AMPK

50 nM (IC50)

PAK5

52 nM (IC50)

DAPK3

81 nM (IC50)

Autophagy

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
105.33 μM
Compound: GSK690693
Cytotoxicity against human A549 cells assessed as decrease in cell viability after 24 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as decrease in cell viability after 24 hrs by MTT assay
[PMID: 29966916]
C6 IC50
14.5 μM
Compound: GSK690693
Cytotoxicity against rat C6 cells assessed as decrease in cell viability after 24 hrs by MTT assay
Cytotoxicity against rat C6 cells assessed as decrease in cell viability after 24 hrs by MTT assay
[PMID: 29966916]
HCT-116 IC50
8.2 μM
Compound: GSK690693
Growth inhibition of human HCT116 cells after 72 hrs by coulter counter method
Growth inhibition of human HCT116 cells after 72 hrs by coulter counter method
[PMID: 24900862]
JeKo-1 IC50
3 μM
Compound: GSK690693
Antiproliferative activity against human JeKo1 cells after 72 hrs by CellTiter Glo assay
Antiproliferative activity against human JeKo1 cells after 72 hrs by CellTiter Glo assay
[PMID: 28704757]
JVM-2 IC50
1.6 μM
Compound: GSK690693
Antiproliferative activity against human JVM2 cells after 72 hrs by CellTiter Glo assay
Antiproliferative activity against human JVM2 cells after 72 hrs by CellTiter Glo assay
[PMID: 28704757]
Maver1 IC50
5.1 μM
Compound: GSK690693
Antiproliferative activity against human Maver1 cells after 72 hrs by CellTiter Glo assay
Antiproliferative activity against human Maver1 cells after 72 hrs by CellTiter Glo assay
[PMID: 28704757]
NCI-H460 IC50
5.4 μM
Compound: GSK690693
Growth inhibition of human NCI-H460 cells after 72 hrs by coulter counter method
Growth inhibition of human NCI-H460 cells after 72 hrs by coulter counter method
[PMID: 24900862]
PC-3 IC50
14.1 μM
Compound: GSK690693
Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay
Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay
[PMID: 30151089]
PC-3 IC50
15.5 μM
Compound: GSK690693
Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay
Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay
[PMID: 24308997]
Z-138 IC50
3.1 μM
Compound: GSK690693
Antiproliferative activity against human Z138 cells after 72 hrs by CellTiter Glo assay
Antiproliferative activity against human Z138 cells after 72 hrs by CellTiter Glo assay
[PMID: 28704757]
体外研究
(In Vitro)

GSK690693 is very selective for the Akt isoforms versus the majority of kinases in other families. However, GSK690693 is less selective for members of the AGC kinase family including PKA, PrkX, and PKC isozymes with IC50 of 24 nM, 5 nM, and 2-21 nM, respectively. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively, and PAK4, 5, and 6 from the STE family with IC50 of 10 nM, 52 nM, and 6 nM, respectively. GSK690693 inhibits the phosphorylation of GSK3β in tumor cells with IC50 ranging from 43 nM to 150 nM. GSK690693 treatment leads to a dose-dependent increase in the nuclear accumulation of the transcription factor FOXO3A. GSK690693 potently inhibits the proliferation of T47D, ZR-75-1, BT474, HCC1954, MDA-MB-453, and LNCaP cells with IC50 of 72 nM, 79 nM, 86 nM, 119 nM, 975 nM, and 147 nM, respectively. GSK690693 treatment induces apoptosis at concentrations > 100 nM in both LNCaP and BT474 cells[1]. Consistent with the role of AKT in cell survival, GSK690693 induces apoptosis in sensitive ALL cell lines[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

GSK-690693 相关抗体:
体内研究
(In Vivo)

A single administration of GSK690693 inhibits GSK3β phosphorylation in human breast carcinoma (BT474) xenografts in a dose- and time-dependent manner. Similarly, GSK690693 induces a reduction in phosphorylation of the Akt substrates, PRAS40, and FKHR/FKHRL1. GSK690693 also results in an acute increase in blood glucose, returning to baseline 8 to 10 hours after drug administration. Administration of GSK690693 induces reductions in phosphorylated Akt substrates in vivo, and potently inhibits the growth of human SKOV-3 ovarian, LNCaP prostate, and BT474 and HCC-1954 breast carcinoma xenografts, with maximal inhibition of 58% to 75% at the dose of 30 mg/kg/day[1]. GSK690693 exhibits efficacy irrespective of the mechanism of Akt activation involved. GSK690693 is most effective in delaying tumor progression in Lck-MyrAkt2 mice expressing a membrane-bound, constitutively active form of Akt[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量

425.48

Formula

C21H27N7O3
CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 20 mg/mL (47.01 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H2O 中的溶解度 : 5 mg/mL (11.75 mM; ultrasonic and adjust pH to 5 with HCl)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3503 mL 11.7513 mL 23.5026 mL
5 mM 0.4701 mL 2.3503 mL 4.7005 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 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，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制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

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.88 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

  • 方案 二

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2 mg/mL (4.70 mM); 澄清溶液; 超声助溶

    此方案可获得 2 mg/mL的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制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。

  • 方案 一

    请依序添加每种溶剂： 20% HP-β-CD/10 mM Citrate pH 2.0

    Solubility: 10 mg/mL (23.50 mM); 澄清溶液; 超声助溶

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 98.46%

COA (195 KB) RP-HPLC (247 KB)

产品使用指南 (1538 KB)
参考文献
Kinase Assay
[1]

His-tagged full-length Akt1, 2, or 3 are expressed and purified from baculovirus. Activation is carried out with purified PDK1 to phosphorylate Thr308 and purified MK2 to phosphorylate Ser473. To more accurately measure time-dependent inhibition of Akt, activated Akt enzymes are incubated with GSK690693 at various concentrations at room temperature for 30 minutes before the reaction is initiated with the addition of substrate. Final reaction contains 5 nM to 15 nM Akt1, 2, and 3 enzymes; 2 μM ATP; 0.15 μCi/μL[γ-33P]ATP; 1 μM Peptide (Biotin-aminohexanoicacid-ARKR-ERAYSFGHHA-amide); 10 mM MgCl2; 25 mM MOPS (pH 7.5); 1 mM DTT; 1 mM CHAPS; and 50 mM KCl. The reactions are incubated at room temperature for 45 minutes, followed by termination with Leadseeker beads in PBS containing EDTA (final concentration, 2 mg/mL beads and 75 mM EDTA). The plates are then sealed, the beads are allowed to settle for at least 5 hours, and product formation is quantitated using a Viewlux Imager.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

Cells are plated at densities that allow untreated cells to grow logarithmically during the course of a 3-day assay. Briefly, cells are plated in 96- or 384-well plates and incubated overnight. Cells are then treated with GSK690693 (ranging from 30 μM-1.5 nM) and incubated for 72 hours. Cell proliferation is measured using the CellTiter Glo reagent. Data are analyzed using the XLFit curve-fitting tool for Microsoft Excel. IC50 values are obtained by fitting data to Eq, 2.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Tumors are initiated by injection of tumor cell suspension (HCC1954, MDA-MB-453, and LNCaP) or tumor fragments (BT474, SKOV-3, and PANC1) s.c. in 8- to 12-wk-old CD1 Swiss Nude mice (LNCaP, SKOV-3, and PANC1) or SCID mice (HCC1954, MDA-MB-453, and BT474). When tumors reach a volume of 100 to 200 mm3, mice are randomized and divided into groups of 8 to 12 mice per group. GSK690693 is administered once daily at 10, 20, and 30 mg/kg by i.p. administration. Animals are euthanized by inhalation of CO2 at the completion of the study. Tumor volume is measured twice weekly by calipers, using the equation: tumor volume (mm3)=(length × width2)/2. Results are reported as % inhibition on day 21 of treatment=100× [1-(average growth of the drug-treated population/average growth of vehicle-treated control population)]. Statistical analysis is done using two-tailed t test.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

GSK-690693 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 2.3503 mL 11.7513 mL 23.5026 mL 58.7566 mL
5 mM 0.4701 mL 2.3503 mL 4.7005 mL 11.7513 mL
10 mM 0.2350 mL 1.1751 mL 2.3503 mL 5.8757 mL
DMSO 15 mM 0.1567 mL 0.7834 mL 1.5668 mL 3.9171 mL
20 mM 0.1175 mL 0.5876 mL 1.1751 mL 2.9378 mL
25 mM 0.0940 mL 0.4701 mL 0.9401 mL 2.3503 mL
30 mM 0.0783 mL 0.3917 mL 0.7834 mL 1.9586 mL
40 mM 0.0588 mL 0.2938 mL 0.5876 mL 1.4689 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSK-690693937174-76-0GSK690693GSK 690693AktAMPKAutophagyPKBProtein kinase BAMP-activated protein kinaseInhibitorinhibitorinhibit

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