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

GSK-690693 是一種 ATP 競(jìng)爭(zhēng)型的泛 Akt 抑制劑，對(duì) Akt1， Akt2 和 Akt3 的 IC50 分別為 2 nM，13 nM，9 nM。GSK-690693 也是一種 AMPK 的抑制劑，影響 ULK1 的活性，并能顯著抑制 STING 依賴的 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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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥776
In-stock
1 mg ￥320
In-stock
5 mg ￥705
In-stock
10 mg ￥1045
In-stock
25 mg ￥2600
In-stock
50 mg ￥4500
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100 mg 現(xiàn)貨 詢價(jià)
200 mg   詢價(jià)  
500 mg   詢價(jià)  

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Other Forms of GSK-690693:

MCE 顧客使用本產(chǎn)品發(fā)表的 32 篇科研文獻(xiàn)

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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

 

細(xì)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]
體外研究
(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.
體內(nèi)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 號(hào)
性狀

固體

顏色

Light yellow to yellow

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 20 mg/mL (47.01 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

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

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

* 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過濾除菌后使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑： 10% DMSO    90% Corn Oil

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

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液，此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中，混合均勻。

  • 方案 二

    請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2 mg/mL (4.70 mM); 澄清溶液; 超聲助溶

    此方案可獲得 2 mg/mL的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 20.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。

以下溶解方案，請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比； 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶。

  • 方案 一

    請(qǐng)依序添加每種溶劑： 20% HP-β-CD/10 mM Citrate pH 2.0

    Solubility: 10 mg/mL (23.50 mM); 澄清溶液; 超聲助溶

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 98.46%

參考文獻(xiàn)
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.
參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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

* 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過濾除菌后使用。

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  • 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.

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產(chǎn)品名稱：
GSK-690693
目錄號(hào)：
HY-10249
需求量：