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SML2003

Sigma-Aldrich

GSK621

≥98% (HPLC)

Synonym(s):

6-Chloro-5-(2′-hydroxy-3′-methoxy-[1,1′-biphenyl]-4-yl)-3-(3-methoxyphenyl)-1,5-dihydro-2H-pyrrolo[3,2-d]pyrimidine-2,4(3H)-dione, 6-Chloro-5-(2′-hydroxy-3′-methoxy[1,1′-biphenyl]-4-yl)-3-(3-methoxyphenyl)-1H-pyrrolo[3,2-d]pyrimidine-2,4(3H,5H)-dione

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About This Item

Empirical Formula (Hill Notation):
C26H20ClN3O5
CAS Number:
1346607-05-3
Molecular Weight:
489.91
MDL number:
MFCD28502280
UNSPSC Code:
51111800
NACRES:
NA.77

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

O=C(NC1=C2N(C3=CC=C(C4=C(O)C(OC)=CC=C4)C=C3)C(Cl)=C1)N(C5=CC=CC(OC)=C5)C2=O

Application

GSK621 has been used as an AMP-activated kinase α (AMPK α) activator to study the antiviral role of AMPK in Zika virus (ZIKV) infection. It has also been used as an AMPK α activator to study its protective effect on myocardial cells against oxygen-glucose deprivation-re-oxygenation (OGD/R).

Biochem/physiol Actions

GSK621 is a direct AMPK activator that exhibits anti-leukemic (300 μM; MOLM-14, HL-60, OCI-AML3) and anti-glioma (Effec. conc. 10-100 μM; U87MG and U251MG) activity, while displaying little cytotoxicity toward normal hematopoietic progenitors, primary human astrocytes, or HCN-1a neuronal cells. When administered via intraperitoneal injection, GSK621 (30 mg/kg twice daily) is shown to reduce leukemia growth and significantly extend the survival of mice xenografted with MOLM-14 cells. AMPK activation by GSK621 leads to mTOR inhibition and Tetraspanin 8 (Tspan8) downregulation in glioma cells, while GSK621-induced cytotoxicity in acute myeloid leukemia (AML) cells is the result of synthetic lethality, where co-activation of AMPK and mTORC1 activates the eIF2a signaling pathway, which in turn triggers autophagic cell death.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Pierre Sujobert et al.
Cell reports, 11(9), 1446-1457 (2015-05-26)
AMPK is a master regulator of cellular metabolism that exerts either oncogenic or tumor suppressor activity depending on context. Here, we report that the specific AMPK agonist GSK621 selectively kills acute myeloid leukemia (AML) cells but spares normal hematopoietic progenitors.
Hong Jiang et al.
PloS one, 11(8), e0161017-e0161017 (2016-08-18)
Here, we studied the anti-glioma cell activity by a novel AMP-activated protein kinase (AMPK) activator GSK621. We showed that GSK621 was cytotoxic to human glioma cells (U87MG and U251MG lines), possibly via provoking caspase-dependent apoptotic cell death. Its cytotoxicity was
Pierre Sujobert et al.
Molecular & cellular oncology, 3(4), e1071303-e1071303 (2016-09-22)
We report the therapeutic potential of GSK621, an AMP-activated protein kinase (AMPK) agonist, in acute myeloid leukemia (AML). GSK621-induced cytotoxicity is restricted to AML cells compared to normal hematopoietic progenitors due to a unique synthetic lethal interaction of co-activation of
Li Ting-Ting et al.
Biochemical and biophysical research communications, 514(3), 826-834 (2019-05-14)
Recent studies have implied that activation of AMP-dependent protein kinase (AMPK) could protect myocardial cells from oxygen glucose deprivation-re-oxygenation (OGD/R). The aim of the present study is to test whether GSK621, a novel and direct AMPK activator, could exert myocardial
Sneha Singh et al.
Journal of immunology (Baltimore, Md. : 1950), 204(7), 1810-1824 (2020-02-23)
Viruses are known to perturb host cellular metabolism to enable their replication and spread. However, little is known about the interactions between Zika virus (ZIKV) infection and host metabolism. Using primary human retinal vascular endothelial cells and an established human

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