GSK-690693

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].

Product Specifications

CAS Number

[937174-76-0]

UNSPSC

12352005

Hazard Statement

H301

Target

Akt; AMPK; Autophagy

Type

Reference compound

Related Pathways

Autophagy; Epigenetics; PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/GSK-690693.html

Concentration

10mM

Purity

99.05

Solubility

DMSO : 20 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

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

Molecular Formula

C21H27N7O3

Molecular Weight

425.48

Precautions

H301

References & Citations

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