Home PI3K/Akt/mTOR AMPK activator GSK621

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GSK621 AMPK activator

Cat.No.S7898

GSK621 is a specific and potent AMPK activator.
GSK621 AMPK activator Chemical Structure

Chemical Structure

Molecular Weight: 489.91

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Quality Control

Batch: Purity: 99.05%
99.05

Solubility

In vitro
Batch:

DMSO : 97 mg/mL (197.99 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
Batch:

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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. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Chemical Information, Storage & Stability

Molecular Weight 489.91 Formula

C26H20ClN3O5

 Storage (From the date of receipt)
CAS No. 1346607-05-3 Download SDF Storage of Stock Solutions

Synonyms N/A 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

Mechanism of Action

Targets/IC50/Ki
AMPK
(Cell-free assay)
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, this compound reduces the proliferation of all 20 lines with IC50 ranged from 13-30 μM, and increases apoptosis in 17 (85%) lines. In addition, it also triggers autophagy, which partially contributes to AML cell death.
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.
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.
References

Applications

Methods Biomarkers Images PMID
Growth inhibition assay Cell viability pS6K1 / S6K1 / p4EBP1 / 4EBP1 / Tspan8 / Cyclin D1 pACC / ACC1
S7898-viability1
27532105

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