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GSK-690693

Catalog No. T6285 CAS 937174-76-0

Synonyms: GSK690693

GSK-690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. Phase 1.

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GSK-690693, CAS 937174-76-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 41.00
5 mg	In stock	$ 97.00
10 mg	In stock	$ 138.00
25 mg	In stock	$ 279.00
50 mg	In stock	$ 447.00
100 mg	In stock	$ 659.00
1 mL * 10 mM (in DMSO)	In stock	$ 97.00

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Purity: 100%

Purity: 98.78%

Purity: 97.54%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	GSK-690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. Phase 1.
Targets&IC50	PKCη:2 nM, Akt3:9 nM, PKCθ:2 nM, PRKX:5 nM, Akt1:2 nM
In vitro	GSK690693 exhibits high specificity for Akt isoforms compared to most other kinase families, though it shows lower selectivity for AGC kinase family members, including PKA, PrkX, and PKC isozymes, with IC50 values of 24 nM, 5 nM, and 2-21 nM, respectively. It also effectively inhibits AMPK and DAPK3 from the CAMK family and PAK4, 5, and 6 from the STE family, with IC50 values of 50 nM, 81 nM, 10 nM, 52 nM, and 6 nM, respectively. GSK690693 prevents GSK3β phosphorylation in tumor cells, with IC50 values ranging 43-150 nM, and promotes dose-dependent nuclear accumulation of FOXO3A. It strongly suppresses the proliferation of various cancer cell lines, including T47D, ZR-75-1, BT474, HCC1954, MDA-MB-453, and LNCaP, with IC50 values of 72 nM, 79 nM, 86 nM, 119 nM, 975 nM, and 147 nM, respectively, and induces apoptosis in LNCaP and BT474 cells at concentrations above 100 nM. [1] In alignment with AKT's role in cell survival, GSK690693 triggers apoptosis in sensitive ALL cell lines. [2]
In vivo	Administering a single dose of GSK690693 effectively inhibits GSK3β phosphorylation in human breast carcinoma (BT474) xenografts, with its impact varying by dose and time. It also leads to a decrease in phosphorylation of Akt substrates, including PRAS40 and FKHR/FKHRL1. Additionally, GSK690693 causes a temporary spike in blood glucose levels, which normalize within 8 to 10 hours post-administration. This compound not only significantly reduces phosphorylated Akt substrates in vivo but also powerfully restricts growth in various human carcinoma xenografts such as SKOV-3 ovarian, LNCaP prostate, and BT474 and HCC-1954 breast, achieving up to 58% to 75% growth inhibition at a 30 mg/kg/day dosage. Its effectiveness is consistent across different Akt activation mechanisms and notably excels in delaying tumor progression in Lck-MyrAkt2 mice, which express an always-active, membrane-bound form of Akt.
Kinase Assay	In vitro kinase assays: 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.
Cell Research	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.(Only for Reference)
Animal Research	Animal Models: Female CD1 Swiss Nude mice injected with LNCaP, SKOV-3, or PANC1 cells, and C.B-17 SCID mice with HCC1954, MDA-MB-453, or BT474 cellsFormulation: Formulated in either 4% DMSO/40% hydroxypropyl-β-cyclodextrin in water (pH 6.0) or 5% dextrose (pH 4.0)Dosages: ~30 mg/kg/dayAdministration: Administered via i.p.

Synonyms	GSK690693
Molecular Weight	425.48
Formula	C21H27N7O3
CAS No.	937174-76-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMF: soluble

DMSO: 21.3 mg/mL(50 mM)

References and Literature

1. Rhodes N, et al. Cancer Res, 2008, 68(7), 2366-2374. 2. Levy DS, et al. Blood, 2009, 113(8), 1723-1729. 3. Altomare DA, et al. Clin Cancer Res, 2010, 16(2), 486-496.

Citations

1. Liu H, Liu Y, Wang H, et al. Geometric Constraints Regulate Energy Metabolism and Cellular Contractility in Vascular Smooth Muscle Cells by Coordinating Mitochondrial DNA Methylation. Advanced Science. 2022: 2203995.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library TGF-beta/Smad Compound Library Kinase Inhibitor Library Anti-Cancer Drug Library Autophagy Compound Library Anti-Breast Cancer Compound Library Angiogenesis related Compound Library

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Keywords

GSK-690693 937174-76-0 Autophagy Chromatin/Epigenetic Cytoskeletal Signaling PI3K/Akt/mTOR signaling Proteases/Proteasome Akt Serine Protease AMPK PKC AMP-activated protein kinase GSK690693 Protein kinase B GSK 690693 inhibit PKB Inhibitor inhibitor

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