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。
| 生物活性 | GSK321 is a potent inhibitor of mutantisocitrate dehydrogenase1 (IDH1) enzymes. GSK321 has high inhibitory and selectivity for mutantIDH1enzymes. GSK321 can be used for the research of acute myeloid leukemia[1][2]. |
| IC50& Target | IC50 for mutant IDH1 enzymes: 4.6 nM (R132H), 3.8 nM (R132C), 2.9 nM (R132G)[1]. |
体外研究
(In Vitro) | GSK321 has high inhibitory for mutant IDH1 enzymes, with IC50values of 4.6 nM against R132H, 3.8 nM against R132C and 2.9 nM against R132G, respectively[1].
GSK321 (0, 0.5, 5 μM; 48 h) induces markedly decreased H3K9me2 levels[1].
GSK321 decreases intracellular 2-HG and affects proliferation of primary IDH1 mutant AML cells[1].
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[1].
GSK321 leads to genome-wide DNA cytosine hypomethylation in IDH1-mutant AML cells[1].
Western Blot Analysis[1] | Cell Line: | HT-1080 cells | | Concentration: | 0, 0.5, 5 μM | | Incubation Time: | 48 h | | Result: | Lead to the reduction of histone H3K9 dimethylation (H3K9me2). |
Cell Proliferation Assay[1] | Cell Line: | IDH1 mutant AML cells | | Concentration: | 3 μM | | Incubation Time: | 15 days | | Result: | Showed a significant, initial increase in cell numbers (2-fold to 15-fold) in IDH1 mutant AML cells. |
Cell Cycle Analysis[1] | Cell Line: | IDH1 mutant AML cells | | Concentration: | | | Incubation Time: | 7 days | | Result: | Observed a reproducible and significant decrease in quiescent (G0)-phase cells in R132G IDH1 and R132C IDH1 AML cells. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 溶解性数据 | In Vitro: DMSO : 250 mg/mL(498.45 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.9938 mL | 9.9691 mL | 19.9382 mL | | 5 mM | 0.3988 mL | 1.9938 mL | 3.9876 mL | | 10 mM | 0.1994 mL | 0.9969 mL | 1.9938 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
