Product Data Sheet

GSK321

Catalog No. A24746

main product photo
GSK321 is a potent and selective inhibitor of mutant isocitrate dehydrogenase 1 (IDH1), showing IC50 values of 2.9, 3.8, 4.6, and 46 nM for the R132G, R132C, R132H, and wild-type IDH1 variants, respectively, with over 100-fold selectivity for IDH2. This compound effectively reduces intracellular levels of α-Hydroxyglutaric acid (2-HG), disrupts the myeloid differentiation block, and promotes granulocytic differentiation in leukemic blasts and stem-like cells. GSK321 is valuable for research on acute myeloid leukemia (AML) and various other malignancies.
Chemical Information
Catalog NumA24746
M. Wt501.55
FormulaC28H28FN5O3
Purity>98%
Storageat -20 °C 3 years (powder form); at -20 °C 6 months (Solution base)
CAS No.1816331-63-1
SynonymsGSK-321, GSK 321
SMILESO=C(C1=CC=CN1)N2C[C@@H](C)C(N(CC3=CC=C(F)C=C3)N=C4C(NC5=CC([C@H](C)O)=CC=C5)=O)=C4C2
Biological Activity
DescriptionGSK321 is a potent and selective inhibitor of mutant isocitrate dehydrogenase 1 (IDH1), showing IC50 values of 2.9, 3.8, 4.6, and 46 nM for the R132G, R132C, R132H, and wild-type IDH1 variants, respectively, with over 100-fold selectivity for IDH2. This compound effectively reduces intracellular levels of α-Hydroxyglutaric acid (2-HG), disrupts the myeloid differentiation block, and promotes granulocytic differentiation in leukemic blasts and stem-like cells. GSK321 is valuable for research on acute myeloid leukemia (AML) and various other malignancies.
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SHIPPING AND STORAGE
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