Name | GSK621 |
Synonyms | GSK621 GSK621 (GSK 621 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 1H-Pyrrolo[3,2-d]pyrimidine-2,4(3H,5H)-dione, 6-chloro-5-(2'-hydroxy-3'-methoxy[1,1'-biphenyl]-4-yl)-3-(3-methoxyphenyl)- |
CAS | 1346607-05-3 |
Molecular Formula | C26H20ClN3O5 |
Molar Mass | 489.91 |
Density | 1.41±0.1 g/cm3(Predicted) |
pKa | 9.01±0.40(Predicted) |
Storage Condition | 2-8°C |
biological activity | GSK621 is a specific AMPK agonist with an IC50 value of 13-30 μm for AML cell lines. GSK621 can induce autophagy and apoptosis. GSK621 induces phosphorylation of eiF2α, a marker of UPR activation. |
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. AML cell lines and primary AML samples. |
Concentration: | 0-30 μM. 30 μM. |
Incubation Time: | 4 d. 24 h. |
Result: | IC 50 values ranged from 13 to 30 μM. Reduced the proliferation of all 20 lines and increased apoptosis in 17 (85%) lines. Induced the formation of numerous intracytoplasmic vacuoles including autophagosomes. Reduced leukemia growth and significantly extended survival compared to vehicle-treated animals or those treated with 10 mg/kg twice daily. |
Animal Model: | MOLM-14 cells xenografted into nude mice. |
Dosage: | 30 mg/kg. |
Administration: | IP twice daily. |