产品
编 号：F225976
分子式：C28H28FN5O3
分子量：501.55
分子式：C28H28FN5O3
分子量：501.55
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
50mg
询价
询价
结构图
CAS No: 1816331-63-1
产品详情
生物活性：
GSK321 is a potent inhibitor of mutant isocitrate dehydrogenase 1 (IDH1) enzymes. GSK321 has high inhibitory and selectivity for mutant IDH1 enzymes. GSK321 can be used for the research of acute myeloid leukemia.
体外研究：
GSK321 has high inhibitory for mutant IDH1 enzymes, with IC50 values of 4.6 nM against R132H, 3.8 nM against R132C and 2.9 nM against R132G, respectively.GSK321 (0, 0.5, 5 μM; 48 h) induces markedly decreased H3K9me2 levels.GSK321 decreases intracellular 2-HG and affects proliferation of primary IDH1 mutant AML cells.GSK321 has inhibition activity for mutant IDH1 that overcomes the pathognomonic differentiation block of AML cells, and induces myeloid differentiation of IDH1 mutant cells at the level of leukemic blasts and more stem-like cells.GSK321 leads to genome-wide DNA cytosine hypomethylation in IDH1-mutant AML cells.
GSK321 is a potent inhibitor of mutant isocitrate dehydrogenase 1 (IDH1) enzymes. GSK321 has high inhibitory and selectivity for mutant IDH1 enzymes. GSK321 can be used for the research of acute myeloid leukemia.
体外研究：
GSK321 has high inhibitory for mutant IDH1 enzymes, with IC50 values of 4.6 nM against R132H, 3.8 nM against R132C and 2.9 nM against R132G, respectively.GSK321 (0, 0.5, 5 μM; 48 h) induces markedly decreased H3K9me2 levels.GSK321 decreases intracellular 2-HG and affects proliferation of primary IDH1 mutant AML cells.GSK321 has inhibition activity for mutant IDH1 that overcomes the pathognomonic differentiation block of AML cells, and induces myeloid differentiation of IDH1 mutant cells at the level of leukemic blasts and more stem-like cells.GSK321 leads to genome-wide DNA cytosine hypomethylation in IDH1-mutant AML cells.
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