| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T08391 | ||||
| Target Name | Tyrosine-protein kinase JAK2 | ||||
| Target Type | Successful |
||||
| Drug Potency against Target | NSC-1771 | Drug Info | IC50 = 223 nM | [531262] | |
| ITF2357 | Drug Info | IC50 = 1~10 nM | [552763] | ||
| Ruxolitinib | Drug Info | IC50 = 4.5 nM | |||
| Atropisomer 1 | Drug Info | IC50 = 270 nM | [530583] | ||
| Action against Disease Model | ITF2357 | The clonogenic activity of JAK2V617F mutated cells was inhibited by low concentrations of ITF2357 (IC50 0.001-0.01 mu M) | [552763] | Drug Info | |
| The Effect of Target Knockout, Knockdown or Genetic Variations | JAK2 knockout mice suffered embryonically lethal and no blood formation;Dificient INF-gamma,IL 3,IL-5,Epo,Tpo and GM-CSF in JAK2 knockout mice | [531262] | |||
| References | |||||
| Ref 531262 | Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. Epub 2010 Oct 21.In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). | ||||
| Ref 552763 | The histone deacetylase inhibitor ITF2357 selectively targets cells bearing mutated JAK2(V617F). Leukemia. 2008 Apr;22(4):740-7. Epub 2007 Dec 13. | ||||
| Ref 530583 | J Med Chem. 2009 Dec 24;52(24):7938-41.Janus kinase 2 inhibitors. Synthesis and characterization of a novel polycyclic azaindole. | ||||
| Ref 552763 | The histone deacetylase inhibitor ITF2357 selectively targets cells bearing mutated JAK2(V617F). Leukemia. 2008 Apr;22(4):740-7. Epub 2007 Dec 13. | ||||
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