IDH889 |
| Catalog No.GC38640 |
IDH889는 이소시트레이트 탈수소효소 1(IDH1)의 경구 사용 가능한 뇌 침투성 알로스테릭 및 돌연변이 특이적 억제제입니다. IDH889는 IDH1R132* 돌연변이에 대해 강력한 선택성을 가지며, IC50은 IDH1R132H, IDH1R132C 및 IDH1wt에 대해 각각 0.02μM, 0.072μM 및 1.38μM입니다. IDH889는 0.014μM의 IC50으로 R-2-하이드록시글루타레이트(2-HG) 생산의 강력한 세포 억제를 보여줍니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1429179-07-6
Sample solution is provided at 25 µL, 10mM.
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IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC50s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1R132H, IDH1R132C and IDH1wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC50 of 0.014 μM[1].
[1]. Levell JR, et al. Optimization of 3-Pyrimidin-4-yl-oxazolidin-2-ones as Allosteric and Mutant Specific Inhibitors of IDH1. ACS Med Chem Lett. 2016 Dec 16;8(2):151-156.
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