GSK321

Research use only, not for human use.

GSK321 is a selective and potent mutant isocitrate dehydrogenase 1 (IDH1) inhibitor that inhibits lipid synthesis and blocks cell proliferation in OPA1-deficient MEFs and prevents cytoplasmic glutamine reductive carboxylation.GSK321 has been used in the study of leukemia.

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.

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Metabolic Enzyme/Protease

Dehydrogenase

Dehydrogenase

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1816331-63-1

501.55

C28H28FN5O3

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (498.45 mM; Ultrasonic )

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

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(-20℃)

With Ice Pack

≥ 2 years