Home PI3K/Akt/mTOR AMPK activator GSK621 For research use only.

GSK621

GSK621 is a specific and potent AMPK activator.

GSK621 Chemical Structure

GSK621 Chemical Structure

CAS No. 1346607-05-3

Purity & Quality Control

GSK621 Related Products

Signaling Pathway

AMPK Signaling Pathways

AMPK Signaling Pathway

Biological Activity

Description GSK621 is a specific and potent AMPK activator.
Targets
AMPK [1]
(Cell-free assay)
In vitro
In vitro In AML cell lines and primary AML samples, GSK621 markedly increases phosphorylation at AMPKα T172, a marker of AMPK activation. In a set of 20 cell lines, GSK621 reduces the proliferation of all 20 lines with IC50 ranged from 13-30 μM, and increases apoptosis in 17 (85%) lines. In addition, GSK621 also triggers autophagy, which partially contributes to AML cell death. [1]
Kinase Assay AMPK enzymatic assay
HEPG2 cells are treated with increasing doses of A-769662 or GSK621, and ACC S79 phosphorylation is assessed as a surrogate marker for AMPK activation using a commercially available ELISA kit.
Cell Research Cell lines MV4-11, OCI-AML3, OCI-AML2, HL-60, Kasumi, HEL, UT7, NB4, TF-1, KG1A, Nomo p28, SKM-1, U937, YHP1, MOLM-14, Mo7e, K562, MOLM-13, EOL-1, SET-2 cell lines
Concentrations ~30 μM
Incubation Time ~4 d
Method

Twenty AML cell lines are treated with log10 dilutions of GSK621 and relative viability is determined by CellTiter-Glo?assay. IC50 of GSK621 among these 20 cell lines is calculated using the Prism software and are presented as log[C] with [C] in mol/l (M). Results are presented for 5 different cell lines per panel.
Experimental Result Images Methods Biomarkers Images PMID
Growth inhibition assay Cell viability pS6K1 / S6K1 / p4EBP1 / 4EBP1 / Tspan8 / Cyclin D1 pACC / ACC1 27532105
In Vivo
In vivo In nude mice bearing MOLM-14 xenografts, GSK621 (30 mg/kg, i.p.) reduces leukemia growth and significantly extends survival by enhancing AMPK activity and the induction of apoptosis. [1]
Animal Research Animal Models NUDE Mice bearing MOLM-14 Xenografts
Dosages 30 mg/kg, twice daily
Administration i.p.

Chemical Information & Solubility

Molecular Weight 489.91 Formula

C26H20ClN3O5
CAS No. 1346607-05-3 SDF Download GSK621 SDF
Smiles COC1=CC=CC(=C1)N2C(=O)C3=C(C=C(N3C4=CC=C(C=C4)C5=C(C(=CC=C5)OC)O)Cl)NC2=O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 97 mg/mL ( (197.99 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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