GSK621

Catalog No.S7898 Batch:S789802

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Technical Data

Formula

C26H20ClN3O5
Molecular Weight 489.91 CAS No. 1346607-05-3
Solubility (25°C)* In vitro DMSO 100 mg/mL (204.11 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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]
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 Assay:

[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 Study:

[1]
  • Animal Models

    NUDE Mice bearing MOLM-14 Xenografts

  • Dosages

    30 mg/kg, twice daily

  • Administration

    i.p.

Customer Product Validation

Data from [Data independently produced by , , Haematologica, 2018, doi:10.3324/haematol.2018.191403]

Data from [Data independently produced by , , J Cell Mol Med, 2018, doi:10.1111/jcmm.13975]

Data from [Data independently produced by , , PLoS One, 2016, 11(8):e0161017.]

Selleck's GSK621 has been cited by 14 publications

Redefining the role of AMPK in autophagy and the energy stress response [ Nat Commun, 2023, 14(1):2994] PubMed: 37225695
AMPK Stimulation Inhibits YAP/TAZ Signaling to Ameliorate Hepatic Fibrosis [ Research Square, 2023, 10.21203/rs.3.rs-3727864/v1] PubMed: none
AMPK-PERK axis represses oxidative metabolism and enhances apoptotic priming of mitochondria in acute myeloid leukemia [ Cell Rep, 2022, 38(1):110197] PubMed: 34986346
GPR120 induces regulatory dendritic cells by inhibiting HK2-dependent glycolysis to alleviate fulminant hepatic failure [ Cell Death Dis, 2021, 13(1):1] PubMed: 34911928
Effects of (Pro)renin Receptor on Diabetic Cardiomyopathy Pathological Processes in Rats via the PRR-AMPK-YAP Pathway [ Front Physiol, 2021, 12:657378] PubMed: 34122131
GPA peptide inhibits NLRP3 inflammasome activation to ameliorate colitis through AMPK pathway [ Aging (Albany NY), 2020, 12(18):18522-18544] PubMed: 32950971
Metformin induces lipogenic differentiation in myofibroblasts to reverse lung fibrosis [ Nat Commun, 2019, 10(1-:2987] PubMed: 31278260
Ubiquinol-cytochrome C reductase core protein II promotes tumorigenesis by facilitating p53 degradation. [ EBioMedicine, 2019, 40:92-105] PubMed: 30674441
Neuronal AMP-activated protein kinase hyper-activation induces synaptic loss by an autophagy-mediated process [ Cell Death Dis, 2019, 10(3):221] PubMed: 30833547
The Transcription Factors TFEB and TFE3 Link the FLCN-AMPK Signaling Axis to Innate Immune Response and Pathogen Resistance. [ Cell Rep, 2019, 26(13):3613-3628] PubMed: 30917316

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.