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SML2003

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
UNSPSC Code:
51111800
NACRES:
NA.77
MDL number:
MFCD28502280
Assay:
≥98% (HPLC)
Form:
powder
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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

InChI

1S/C26H20ClN3O5/c1-34-18-6-3-5-17(13-18)30-25(32)23-20(28-26(30)33)14-22(27)29(23)16-11-9-15(10-12-16)19-7-4-8-21(35-2)24(19)31/h3-14,31H,1-2H3,(H,28,33)

InChI key

KURYSXLJGKKDHT-UHFFFAOYSA-N

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

A direct AMPK activator with anti-leukemic and anti-glioma efficacy.
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.

wgk

WGK 3

Storage Class

11 - Combustible Solids

flash_point_f

Not applicable

flash_point_c

Not applicable

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