GSK621

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

GSK621 (GSK-621) 是一种有效的、特异性的 AMPK 激动剂（激活剂），在 AML 中诱导细胞毒性 (IC50=13-30 uM)。

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.

GSK621 (30 μM) induces AMPKα T172, ACC (S79) and ULK1 (S555) phosphorylation.GSK621 (30 μM) induces autophagy and apoptosis.GSK621 treatment also induces PERK phosphorylation, a marker of ER stress, in AML cells. :Cell Proliferation AssayCell 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.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.

GSK621 (30 mg/kg, ip twice daily) exhibits significant anti-tumor activity in MOLM-14 cells xenograft. Animal Model:MOLM-14 cells xenografted into nude mice.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.

GSK 621 | GSK-621

Membrane Transporter/Ion Channel

AMPK

AMPK

Other Indications

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1346607-05-3

489.912

C26H20ClN3O5

>98% (HPLC)

In Vitro:?DMSO : 12.5 mg/mL (25.51 mM)

O=C1NC2=C(N(C3=CC=C(C4=CC=CC(OC)=C4O)C=C3)C(Cl)=C2)C(N1C5=CC=CC(OC)=C5)=O

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

(-20℃)

With Ice Pack

≥ 2 years