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.
| Molecular Weight | 489.91 |
| Formula | C26H20ClN3O5 |
| CAS Number | 1346607-05-3 |
| Solubility (25°C) | DMSO: 2 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[3] Lezi Chen, et al. AMPK activation by GSK621 inhibits human melanoma cells in vitro and in vivo
[4] Yong-Hong Wu, et al. GSK621 activates AMPK signaling to inhibit LPS-induced TNFα production
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