For research use only.

Catalog No.S7898

10 publications

GSK621 Chemical Structure

CAS No. 1346607-05-3

GSK621 is a specific and potent AMPK activator.

Selleck's GSK621 has been cited by 10 publications

3 Customer Reviews

  • GSK621 dose-dependent activation of AMPK in erythroblasts. Western Blot analysis of PT172 AMPKα1, PS79 ACC and PS555 ULK1 in primary erythroblasts incubated for 3 h with increasing doses of GSK621. Anti-HSC70 was used as a loading control.

    Haematologica, 2018, doi:10.3324/haematol.2018.191403. GSK621 purchased from Selleck.

    AMPK activation was essential for Drp1 expression and activation in HUVECs. The phosphorylation levels of AMPK and ACC as well as Drp1 and pDrp1 expression in HUVECs were evaluated by Western blot following cell exposure to GSK621, a specific AMPK activator. Data shown represent mean ± SD (n = 3‐6). *P<0.05 vs the normal group; # P < 0.05 vs the HG group or the diabetic control group. VLD, vildagliptin; HUVECs, human umbilical vein endothelial cells; HG, high glucose; Man, mannitol; pAMPK, phosphorylation of AMPK at Thr172; pACC, phosphorylation of ACC at Ser79; pDrp1, phosphorylation of Drp1 at Ser637.

    J Cell Mol Med, 2018, doi:10.1111/jcmm.13975. GSK621 purchased from Selleck.

  • Human glioma U87MG cells (A-C) and U251MG cells (D), as well as HCN-1a neuronal cells (D) or primary human astrocytes (“Astrocytes”, D) were either left untreated (“C”) or treated with applied concentrations of GSK621 for indicated periods of time, cell survival was tested by MTT assay (A and D) and clonogenicity assay (B); Cell death was also tested by the trypan blue staining assay (C). Experiments in this figure were repeated four times, and similar results were obtained. Data were presented as mean ± SD. * p <0.05 vs. “C”.

    PLoS One, 2016, 11(8):e0161017.. GSK621 purchased from Selleck.

Purity & Quality Control

Choose Selective AMPK Inhibitors

Biological Activity

Description GSK621 is a specific and potent AMPK activator.
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]

Methods Test Index PMID
Growth inhibition assay
Cell viability; 

PubMed: 27532105     

Human glioma U87MG cells were either left untreated (“C”) or treated with applied concentrations of GSK621 for indicated periods of time, cell survival was tested by MTT assay. Data were presented as mean ± SD. * p <0.05 vs. “C”.

pS6K1 / S6K1 / p4EBP1 / 4EBP1 / Tspan8 / Cyclin D1 ; 

PubMed: 27532105     

U87MG cells were either left untreated (“C”) or stimulated with GSK621 (25 μM) for applied periods of time, expressions of listed proteins were tested by Western blots (A and B).

pACC / ACC1 ; 

PubMed: 27532105     

U87MG cells were either left untreated (“C”) or treated with applied concentrations of GSK621 for 2 hours, phospho- (p-) and regular ACC expressions were tested by Western blots.

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]


Kinase Assay:


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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:


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  • 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.

    (Only for Reference)
Animal Research:


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

Solubility (25°C)

In vitro DMSO 97 mg/mL (197.99 mM)
Water Insoluble
Ethanol Insoluble
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.

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 489.91


CAS No. 1346607-05-3
Storage powder
in solvent
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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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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AMPK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID