(Rac)-BRD0705 |
| Catalog No.GC39058 |
(Rac)-BRD0705는 BRD0705의 덜 활동적인 라세미체입니다. BRD0705는 IC50이 66nM이고 Kd가 4.8μM인 강력한 파라로그 선택적 경구 활성 GSK3α 억제제입니다. BRD0705는 GSK3β(515nM의 IC50)에 비해 GSK3α(8배)에 대한 증가된 선택성을 나타냅니다. BRD0705는 급성 골수성 백혈병(AML)에 사용할 수 있습니다.
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.
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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.
Average Rating: 5 (Based on Reviews and 32 reference(s) in Google Scholar.)
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