(Rac)-BRD0705 |
Catalog No.GC39058 |
(Rac)-BRD0705 est un racémate moins actif de BRD0705. BRD0705 est un puissant inhibiteur de GSK3α paralogue sélectif et actif par voie orale avec une IC50 de 66 nM et un Kd de 4,8 μM. BRD0705 affiche une sélectivité accrue pour GSK3α (8 fois) par rapport À GSK3β (IC50 de 515 nM). BRD0705 peut être utilisé pour la leucémie myéloÏde aiguë (LMA).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1597440-03-3
Sample solution is provided at 25 µL, 10mM.
(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 to treat acute myeloid leukemia (AML)[1][2].
[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. [2]. Edward Scolnick, et al. Uses of paralog-selective inhibitors of gsk3 kinases. US20160375006A1.
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