SML2003
GSK621
≥98% (HPLC)
别名:
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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关于此项目
经验公式（希尔记法）:
C26H20ClN3O5
化学文摘社编号:
分子量:
489.91
UNSPSC Code:
51111800
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
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
存储类别
11 - Combustible Solids
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
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
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
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| SML2003-25MG | 04061833247815 |
| SML2003-5MG | 04061833247822 |