GSK621

Catalog No.S7898

For research use only.

GSK621 is a specific and potent AMPK activator.

GSK621 Chemical Structure

CAS No. 1346607-05-3

Selleck's GSK621 has been cited by 12 Publications

3 Customer Reviews

Purity & Quality Control

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Biological Activity

Description GSK621 is a specific and potent AMPK activator.
Targets
AMPK [1]
(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, 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]

Assay
Methods Test Index PMID
Growth inhibition assay Cell viability ; pS6K1 / S6K1 / p4EBP1 / 4EBP1 / Tspan8 / Cyclin D1 ; pACC / ACC1 27532105
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]

Protocol (from reference)

Kinase Assay:

[1]

  • 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:

[1]

  • 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.

Animal Research:

[1]

  • Animal Models: NUDE Mice bearing MOLM-14 Xenografts
  • Dosages: 30 mg/kg, twice daily
  • Administration: i.p.

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.

5mg/mL

Chemical Information

Molecular Weight 489.91
Formula

C26H20ClN3O5

CAS No. 1346607-05-3
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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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