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GSK621

Chemical Structure : GSK621

CAS No.: 1346607-05-3

GSK621 (GSK 621;GSK-621)

Catalog No.: PC-35414Not For Human Use, Lab Use Only.

GSK621 (GSK-621) is a potent, specific AMPK agonist (activator), induces cytotoxicity in AML (IC50=13-30 uM) but not in normal hematopoietic cells.

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Biological Activity

GSK621 (GSK-621) is a potent, specific AMPK agonist (activator), induces cytotoxicity in AML (IC50=13-30 uM) but not in normal hematopoietic cells.
GSK621 is more potent than A-769662 at inducing AMPK activation, as measured by the level of ACC phosphorylation, markedly increases phosphorylation at AMPKα T172 in AML cell lines (MOLM-14, HL-60, and OCI-AML3) and primary AML samples.
Cytotoxicity in AML cells from GSK621 involves the eIF2α/ATF4 signaling pathway that specifically results from mTORC1 activation.

Physicochemical Properties

M.Wt 489.912
Formula C26H20ClN3O5
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

20 mM in DMSO (9.7 mg/mL) ultrasonic

Chemical Name/SMILES

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

References

1. Sujobert P, et al. Cell Rep. 2015 Jun 9;11(9):1446-57.

2. Jiang H, et al. PLoS One. 2016 Aug 17;11(8):e0161017.

3. Chen L, et al. Biochem Biophys Res Commun. 2016 Nov 25;480(4):515-521.

4. Liu W, et al. Oncotarget. 2017 Feb 7;8(6):10543-10552.

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