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CAS No. : 1816331-63-1
MCE 国际站:GSK321
产品活性:GSK321 是突变异柠檬酸脱氢酶 1 (IDH1) 酶的有效抑制剂。GSK321 对突变的 IDH1 酶具有高抑制性和选择性。GSK321 可用于急性髓性白血病的研究。
研究领域:Metabolic Enzyme/Protease
作用靶点:Isocitrate Dehydrogenase (IDH)
In Vitro: 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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