(Rac)-BRD0705 |
| رقم الكتالوجGC39058 |
(Rac) -BRD0705 هو زميل سباق أقل نشاطًا من BRD0705BRD0705 هو مثبط GSK3α قوي وانتقائي وفعال عن طريق الفم مع IC50 من 66 نانومتر و Kd 4.8 ميكرومتريعرض BRD0705 انتقائية متزايدة لـ GSK3α (8 أضعاف) مقابل GSK3β (IC50 من 515 نانومتر)يمكن استخدام BRD0705 لابيضاض الدم النقوي الحاد (AML)
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Cas No.: 1597440-03-3
Sample solution is provided at 25 µL, 10mM.
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(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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