GSK621 是特异性的 AMPK 激动剂，其对 AML 细胞系的IC50 值为13-30 μM。GSK621 可诱导自噬和凋亡。GSK621 可诱导eiF2α 磷酸化 (UPR 激活的一个标志)。 Information GSK621 GSK621 is a specific and potent AMPK activator. Targets AMPK (Cell-free assay) In vitro In AML cell lines and primary AML samples, GSK621 markedly increases phosphorylation at AMPKα T172, a marker of AMPK activation. In a set of 20 cell lines, GSK621 reduces the proliferation of all 20 lines with IC50 ranged from 13-30 μM, and increases apoptosis in 17 (85%) lines. In addition, GSK621 also triggers autophagy, which partially contributes to AML cell death. In vivo In nude mice bearing MOLM-14 xenografts, GSK621 (30 mg/kg, i.p.) reduces leukemia growth and significantly extends survival by enhancing AMPK activity and the induction of apoptosis. Cell Research(from reference) Cell lines：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 cell lines Concentrations：~30 μM Incubation Time：~4 d
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GSK621
CAS number：1346607-05-3 molecular formula：C26H20ClN3O5
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| Chinese alias | - | ||
| English alias | 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 | ||
| CAS number | 1346607-05-3 | molecular formula | C26H20ClN3O5 |
| molecular weight | 489.91 g/mol | Exact mass | 10mM in DMSO |
| PSA | 93.000 Ų | logp | 5.1 |
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