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GSK621 (GSK 621;GSK-621)

  Cat. No.:  DC29234   Featured
Chemical Structure
1346607-05-3
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More than 5000 active chemicals with high quality for research!
Field of application
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 phosphoryl
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1346607-05-3
Chemical Name: 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
SMILES: O=C1NC2=C(N(C3=CC=C(C4=CC=CC(OC)=C4O)C=C3)C(Cl)=C2)C(N1C5=CC=CC(OC)=C5)=O
Formula: C26H20ClN3O5
M.Wt: 489.91
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: GSK621 is a specific AMPK activator, with IC50 values of 13-30 μM for AML cells. GSK621 induces autophagy and apoptosis. GSK621 induces eiF2α phosphorylation-a hallmark of UPR activation[1].
In Vivo: GSK621 (30 mg/kg, ip twice daily) exhibits significant anti-tumor activity in MOLM-14 cells xenograft[1]. Animal Model: MOLM-14 cells xenografted into nude mice[1]. Dosage: 30 mg/kg. Administration: IP twice daily. Result: Reduced leukemia growth and significantly extended survival compared to vehicle-treated animals or those treated with 10 mg/kg twice daily.
In Vitro: GSK621 (30 μM) induces AMPKα T172, ACC (S79) and ULK1 (S555) phosphorylation[1]. GSK621 (30 μM) induces autophagy and apoptosis[1]. GSK621 treatment also induces PERK phosphorylation, a marker of ER stress, in AML cells[1]. Cell Proliferation Assay[1] Cell Line: 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 AML cell lines.0-30 μM. Concentration: 0-30 μM. Incubation Time: 4 d. Result: IC50 values ranged from 13 to 30 μM. Reduced the proliferation of all 20 lines and increased apoptosis in 17 (85%) lines. Cell Autophagy Assay[1]. Cell Line: AML cell lines and primary AML samples. Concentration: 30 μM. Incubation Time: 24 h. Result: Induced the formation of numerous intracytoplasmic vacuoles including autophagosomes.
References: [1]. Pierre Sujobert, et al. Co-activation of AMPK and mTORC1 Induces Cytotoxicity in Acute Myeloid Leukemia. Cell Rep. 2015 Jun 9;11(9):1446-57.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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