Description
A cell-permeable pyridinylbutanone compound that inhibits cellular autophosphorylation of both the wild-type Jak2 and the constitutively active V167F mutant (IC50 = 15 & 28 µM, respectively, with WT- & V617F-transfected BSC-40 cells), while exhiting no effect against cellular Tyk2 autophosphorylation in COS cells or c-Src kinase in cell-free kinase assays. Z3 suppresses the Jak2-V167F-dependent proliferation of the erythroleukemia cell line HEL by blocking the G1-S transition and is shown to effectively reduce the cytokine-stimulated growth of both Jak2-V617F-positive and Jak2-F537I-positive primary hematopoietic progenitor cells from myeloproliferative disorder patients.
Abbr
JAK2 Inhibitor V, Z3(JAK2, the constitutively active V167F mutant)
Storage
+2 centigrade to +8 centigrade
Targets
Jak2, the constitutively active V167F mutant
Molecular Formula
C23H24N2O
Chemical Name
2-Methyl-1-phenyl-4-pyridin-2-yl-2-(2-pyridin-2-ylethyl)butan-1-one