(Rac)-BRD0705 Chemical Properties

Boiling point:

512.0±50.0 °C(Predicted)

Density 

1.22±0.1 g/cm3(Predicted)

pka

14.82±0.60(Predicted)

form 

Solid

color 

Light yellow to yellow

(Rac)-BRD0705 Usage And Synthesis

Uses

(Rac)-BRD0705 is a less active racemate of BRD0705. 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)[1][2].

References

[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
[2] Edward Scolnick, et al. Uses of paralog-selective inhibitors of gsk3 kinases. US20160375006A1.