BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor. BRD0705 can be used for acute myeloid leukemia.
BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML) research[1].
BRD0705 (30 mg/kg; oral gavage; twice daily; NSG mice) treatment impairs leukemia initiation and prolongs survival in AML mouse models[1].
| Animal Model: | 8-week-old male NSG mice injected with MLL-AF9 AML cells[1] |
| Dosage: | 30 mg/kg |
| Administration: | Oral gavage; twice daily |
| Result: | Mice survival was significantly improved.
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GSK3α: 66 nM (IC50); GSK3α: 4.8 μM (Kd); GSK-3β(WT): 515 nM (IC50)
[1] Wagner FF, et al. Exploiting an Asp-Glu "switch" in glycogen synthase kinase 3 to design paralog-selective inhibitors for use in acute myeloid leukemia. Sci Transl Med. 2018 Mar 7;10(431). pii: eaam8460. DOI:
10.1126/scitranslmed.aam8460
