Janus Kinase 2 (JAK2)Targeted Library |
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Ligand in JAK2 active site. Docking example from JAK2 Targeted Library.
The detection of H-bonds between ligand and key JAK2 residue (Leu932) was used for the library preparation.
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In humans, the Janus protein tyrosine kinase family (JAKs) contains four members: JAK1, JAK2, JAK3 and TYK2. JAKs phosphorylate signal transducers and activators of transcription (STATs) simultaneously with other phosphorylations required for activation, and there are several cellular mechanisms in place to inhibit JAK/STAT signaling. That one might be able to modulate selected JAK/STAT-mediated cellular signals by inhibiting JAK kinase activity to effect a positive therapeutic outcome is a tantalizing prospect, as yet incompletely realized. While current data suggest no therapeutic use for JAK1 and TYK2 inhibition, JAK2 inhibition seems a promising but not definitively tested mechanism for treatment of leukemia.
The designed JAK2 Targeted Library comprises only drug-like compounds (PAINS compounds is filtered off). It provides a perfect basis for drug discovery projects related with leukemia.
All compounds are in stock, cherry-picking is available.
The JAK2 Targeted Library (DB, SD, XLS, PDF format) as well as the price-list is available on request. Feel free to contact us or use on-line form below to send an inquiry if you are interested to obtain this library or if you need more information.
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