GSK321

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

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.

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.Western Blot Analysis 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 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 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.

——

——

Metabolic Enzyme/Protease

Dehydrogenase

Dehydrogenase

——

——

1816331-63-1

501.55

C28H28FN5O3

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 250 mg/mL (498.45 mM; 超声助溶 )

C(N1C2=C(C(C(NC3=CC([C@H](C)O)=CC=C3)=O)=N1)CN(C(=O)C4=CC=CN4)C[C@H]2C)C5=CC=C(F)C=C5

——

(-20℃)

With Ice Pack

≥ 2 years