Referencia número: HY-10249

GSK-690693

42 Cited Publications

Revisión del cliente

Based on 42 publication(s) in Google Scholar

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.

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Pureza: 98.47%
No. CAS: 937174-76-0
Fòrmula: C₂₁H₂₇N₇O₃
Peso molecular:425.48

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

GSK-690693 Chemical Structure

No. CAS: 937174-76-0

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (42)
Solvente y solubilidad
- In Vitro
- In Vivo
Protocolo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

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

Ver todos los productos específicos de isoformas Akt :

Ver todos los productos específicos de isoformas AMPK :

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]
A549	IC₅₀	11.83 μM Compound: GSK690693	Cytotoxicity against human A549 cells incubated for 24 hrs by MTT assay Cytotoxicity against human A549 cells incubated for 24 hrs by MTT assay	[PMID: 39047611]
BT-474	IC₅₀	0.05 μM Compound: 3g, GSK-690693	Antiproliferative activity against human BT474 cells Antiproliferative activity against human BT474 cells	[PMID: 18800763]
BT-474	IC₅₀	0.14 μM Compound: 3g, GSK-690693	Inhibition of AKT-mediated GSK3-beta phosphorylation in human BT474 cells Inhibition of AKT-mediated GSK3-beta phosphorylation in human BT474 cells	[PMID: 18800763]
BT-474	IC₅₀	138 nM Compound: GSK-690693	Inhibition of GSK3-beta phosphorylation in human BT474 cells Inhibition of GSK3-beta phosphorylation in human BT474 cells	[PMID: 19179070]
BT-474	IC₅₀	69 nM Compound: GSK-690693	Antiproliferative activity against human BT474 cells Antiproliferative activity against human BT474 cells	[PMID: 19179070]
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]
HFF	IC₅₀	16.3 μM Compound: 3g, GSK-690693	Cytotoxicity against HFF cells Cytotoxicity against HFF cells	[PMID: 18800763]
HFF	IC₅₀	>23000 nM Compound: GSK-690693	Antiproliferative activity against human HFF cells Antiproliferative activity against human HFF cells	[PMID: 19179070]
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]
LNCaP	IC₅₀	0.02 μM Compound: 3g, GSK-690693	Antiproliferative activity against human LNCaP cells Antiproliferative activity against human LNCaP cells	[PMID: 18800763]
LNCaP	IC₅₀	21 nM Compound: GSK-690693	Antiproliferative activity against human LNCAP cells Antiproliferative activity against human LNCAP cells	[PMID: 19179070]
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	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]
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]
Sf9	IC₅₀	0.89 μM Compound: 3g, GSK-690693	Inhibition of human recombinant ROCK1 expressed in Sf9 cells Inhibition of human recombinant ROCK1 expressed in Sf9 cells	[PMID: 18800763]
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]

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].

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

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].

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

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 937174-76-0
Appearance Solid
Peso molecular 425.48
Fòrmula C₂₁H₂₇N₇O₃
Color Off-white to yellow
SMILES

CC(O)(C)C#CC1=NC=C(OC[C@@H]2CNCCC2)C3=C1N=C(C4=NON=C4N)N3CC
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (42)

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Journal Impact Factor

Nat Commun

Domain-specific p53 mutants activate EGFR by distinct mechanisms exposing tissue-independent therapeutic vulnerabilities. [Abstract]

2023 Mar 28;14(1):1726. PMID: 36977662
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
J Exp Clin Cancer Res

ZIP10 drives osteosarcoma proliferation and chemoresistance through ITGA10-mediated activation of the PI3K/AKT pathway. [Abstract]

2021 Oct 27;40(1):340. PMID: 34706747

GSK-690693 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2021 Oct 27;40(1):340. [Abstract]

GSK-690693 (10 μM) attenuated the chemoresistance of 143B cells induced by ZIP10 overexpression.

GSK-690693 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2021 Oct 27;40(1):340. [Abstract]

GSK-690693 (30 mg/kg; i.p.; once daily) attenuated the promotion of tumor growth and chemoresistance by ZIP10 overexpression in 143B xenograft mice.

GSK-690693 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2021 Oct 27;40(1):340. [Abstract]

GSK-690693 (30 mg/kg; i.p.; once daily) decreased the protein levels of p-AKT increased by the overexpression of ZIP10 in 143B cell-derived xenografts.

GSK-690693 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2021 Oct 27;40(1):340. [Abstract]

GSK-690693 (30 mg/kg; i.p.; once daily) prevented the ZIP10 overexpression-induced increases in Ki67 and p-AKT expression in 143B cell-derived xenograft tissues under cisplatin treatment.

GSK-690693 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2021 Oct 27;40(1):340. [Abstract]

GSK-690693 (30 mg/kg; i.p.; once daily). IHC staining analysis of Ki67, ZIP10, ITGA10, p-AKT and cleaved caspase 3 in 143B cell-derived xenograft tissues without cisplatin treatment.
EBioMedicine

Augmenting the therapeutic efficacy of adenosine against pancreatic cancer by switching the Akt/p21-dependent senescence to apoptosis. [Abstract]

2019 Sep;47:114-127. PMID: 31495718
Cell Rep Med

Signaling-induced systematic repression of miRNAs uncovers cancer vulnerabilities and targeted therapy sensitivity. [Abstract]

2023 Oct 17;4(10):101200. PMID: 37734378
Int J Surg

Melatonin attenuates oxidative stress-induced ferroptosis of nucleus pulposus cells and intervertebral disc degeneration via PI3K/AKT-mTOR pathway. [Abstract]

2026 Feb 24. PMID: 41729690
Burns Trauma

2025.
Apoptosis

Ambra1 regulates apoptosis and chemosensitivity in breast cancer cells through the Akt-FoxO1-Bim pathway. [Abstract]

2022 Jun;27(5-6):329-341. PMID: 35257265
Cell Rep

Fibrillarin regulates epithelial integrity via EZH2-mediated modulation of scribble expression. [Abstract]

2025 Nov 25;44(12):116608. PMID: 41296560
Antioxidants (Basel)

Blue Light Alters the Composition of the Jejunal Microbiota and Promotes the Development of the Small Intestine by Reducing Oxidative Stress. [Abstract]

2022 Jan 29;11(2):274. PMID: 35204158
Mol Med

Triolein alleviates ischemic stroke brain injury by regulating autophagy and inflammation through the AKT/mTOR signaling pathway. [Abstract]

2024 Dec 6;30(1):242. PMID: 39639187
Biochem Pharmacol

Ginsenoside Rh4 suppresses aerobic glycolysis and the expression of PD-L1 via targeting AKT in esophageal cancer. [Abstract]

2020 Aug;178:114038. PMID: 32422139
Cells

Follicle-Stimulating Hormone Alleviates Ovarian Aging by Modulating Mitophagy- and Glycophagy-Based Energy Metabolism in Hens. [Abstract]

2022 Oct 18;11(20):3270. PMID: 36291137
Pharmaceuticals (Basel)

Activity of New Synthetic (2-Chloroethylthio)-1,4-naphthoquinones in Prostate Cancer Cells. [Abstract]

2021 Sep 22;14(10):949. PMID: 34681173
Int J Cancer

Effects of Metformin on the virus/host cell crosstalk in human papillomavirus-positive cancer cells. [Abstract]

2021 Sep 1;149(5):1137-1149. PMID: 33844847
J Cereb Blood Flow Metab

Activin A alleviates neuronal injury through inhibiting cGAS-STING-mediated autophagy in mice with ischemic stroke. [Abstract]

2023 May;43(5):736-748. PMID: 36537048
FASEB J

GLCCI1-Deficiency Facilitates Persistent Eosinophilic Lung Inflammation in Asthma via Upregulation of CCL5. [Abstract]

2026 Jan 15;40(1):e71389. PMID: 41460639
Exp Neurol

RvE1/ChemR23 facilitates hematoma clearance and promotes M2 polarization of macrophages/microglia in intracerebral hemorrhage. [Abstract]

2025 Jan 30:115173. PMID: 39892453
iScience

β-adrenergic receptor regulates embryonic epithelial extensibility through actomyosin inhibition. [Abstract]

2023 Nov 15;26(12):108469. PMID: 38213788
Cell Signal

ANXA2 promotes chondrocyte differentiation and fracture healing by regulating the phosphorylation of STAT3 and PI3K/AKT signaling pathways. [Abstract]

2025 Jan 23:127:111617. PMID: 39863030
Breast Cancer (Dove Med Press)

Ambra1 Deficiency Inhibits the Proliferation of Breast Cancer Cells Through the Akt-FoxO1-p27 Pathway. [Abstract]

2025 Oct 21:17:949-965. PMID: 41141217
Toxicol Appl Pharmacol

Lycorine relieves the CCl4-induced liver fibrosis mainly via the JAK2/STAT3 and PI3K/AKT signaling pathways. [Abstract]

2024 Jun 24:117017. PMID: 38925513
Cardiovasc Ther

KCa3.1 Promotes Proinflammatory Exosome Secretion by Activating AKT/Rab27a in Atrial Myocytes during Rapid Pacing. [Abstract]

2023 Mar 30:2023:3939360. PMID: 37035755
Arch Biochem Biophys

Identification and characterization of human PEIG-1/GPRC5A as a 12-O-tetradecanoyl phorbol-13-acetate (TPA) and PKC-induced gene. [Abstract]

2020 Jul 15;687:108375. PMID: 32339486
Vet Microbiol

Epidermal growth factor receptor (EGFR) promotes uptake of bovine parainfluenza virus type 3 into MDBK cells. [Abstract]

2022 Aug:271:109488. PMID: 35691094
PLoS One

The ginsenoside Rk3 exerts anti-esophageal cancer activity in vitro and in vivo by mediating apoptosis and autophagy through regulation of the PI3K/Akt/mTOR pathway. [Abstract]

2019 May 15;14(5):e0216759. PMID: 31091245
PLoS One

Targeting the mTOR Complex by Everolimus in NRAS Mutant Neuroblastoma. [Abstract]

2016 Jan 28;11(1):e0147682. PMID: 26821351
Oncologie

2024 Feb 23.
Reprod Sci

Modulation of Autophagy Through Regulation of 5'-AMP-Activated Protein Kinase Affects Mitophagy and Mitochondrial Function in Primary Human Trophoblasts. [Abstract]

2021 Aug;28(8):2314-2322. PMID: 33619701
Acta Histochem

Normal dermal mesenchymal stem cells improve the functions of psoriatic keratinocytes by inducing autophagy. [Abstract]

2025 Jan 25;127(1):152229. PMID: 39864345
Biomed Res Int

Molecular Mechanism of Gleditsiae Spina for the Treatment of High-Grade Serous Ovarian Cancer Based on Network Pharmacology and Pharmacological Experiments. [Abstract]

2022 Mar 8:2022:5988310. PMID: 35299895
Exp Ther Med

MTHFD2 facilitates breast cancer cell proliferation via the AKT signaling pathway. [Abstract]

2021 Jul;22(1):703. PMID: 34007312
J Mol Histol

Deficiency of METTL3 alleviates excessive autophagy and apoptosis in mice with slow transit constipation and glutamic acid-induced interstitial cells of Cajal via the activation of PI3K/AKT pathway. [Abstract]

2026 Jan 7;57(1):29. PMID: 41495570
Anticancer Drugs

Isovanillin regulates gastric cancer cells apoptosis and metastasis by targeting ROS-mediated MAPK and PI3K signaling pathways. [Abstract]

2026 Jan 14. PMID: 41546559
J Stroke Cerebrovasc Dis

VEGF-A ameliorates ischemia hippocampal neural injury via regulating autophagy and Akt/CREB signaling in a rat model of chronic cerebral hypoperfusion. [Abstract]

2023 Sep 19;32(11):107367. PMID: 37734181
Hematology

AKT inhibition sensitizes acute leukemia cells to S63845-induced apoptosis. [Abstract]

2023 Dec;28(1):2214465. PMID: 37222135
University of Washington

2025.
Research Square Preprint

2022 Feb.
Patent

US20210299273A1.
Universidad de Granada

2020 Sep.
Oxid Med Cell Longev

Cyclophilin A Protects Cardiomyocytes against Hypoxia/Reoxygenation-Induced Apoptosis via the AKT/Nox2 Pathway. [Abstract]

2019 Apr 28:2019:2717986. PMID: 31182989
Oncotarget

Dual inhibition of AKT/FLT3-ITD by A674563 overcomes FLT3 ligand-induced drug resistance in FLT3-ITD positive AML. [Abstract]

2016 May 17;7(20):29131-42. PMID: 27074558

Solvente y solubilidad

In Vitro:

DMSO : 20 mg/mL (47.01 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3503 mL

11.7513 mL

23.5026 mL

5 mM

0.4701 mL

2.3503 mL

4.7005 mL

10 mM

0.2350 mL

1.1751 mL

2.3503 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 2 mg/mL (4.70 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2 mg/mL.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2 mg/mL (4.70 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 20% HP-β-CD/10 mM Citrate pH 2.0

Solubility: 10 mg/mL (23.50 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocolo

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.

MedChemExpress (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.

MedChemExpress (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.

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (284 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Rhodes N, et al. Characterization of an Akt kinase inhibitor with potent pharmacodynamic and antitumor activity. Cancer Res, 2008, 68(7), 2366-2374. [Content Brief]

[2]. Levy DS, et al. AKT inhibitor, GSK690693, induces growth inhibition and apoptosis in acute lymphoblastic leukemia cell lines. Blood, 2009, 113(8), 1723-1729. [Content Brief]

[3]. Altomare DA, et al. GSK690693 delays tumor onset and progression in genetically defined mouse models expressing activated Akt. Clin Cancer Res, 2010, 16(2), 486-496. [Content Brief]

[4]. Konno H, et al. Pro-inflammation Associated with a Gain-of-Function Mutation (R284S) in the Innate Immune Sensor STING. Cell Rep. 2018 Apr 24;23(4):1112-1123. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
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
	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

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GSK-690693

42 Cited Publications

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GSK-690693

Epigenetics Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

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Publications Citing Use of MedChemExpress (MCE) GSK-690693

Ver todos los productos específicos de isoformas Akt

Ver todos los productos específicos de isoformas AMPK

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Complete Stock Solution Preparation Table

GSK-690693 Related Classifications

HY-10249 Related Classifications