Cloned (Comment) | Organism |
---|---|
the V617F mutant is expressed in Ba/F3 cells | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
V617F | the activating JAK2mutation has been described in the majority of patients with Philadelphia chromosome-negative myeloproliferative disorders, the incidence of the JAK2V617F mutation is about 50% in both essential thrombocythemia and primary myelofibrosis and over 90% in polycythemia vera | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
JAK-inhibitor I | 40% JAK2 residual activity in the presence of 0.002 mM JAK-inhibitor I and 0.02 mM ATP | Homo sapiens | |
LS104 | i.e. [(E,E)-2-(benzylaminocarbonyl)-3-(3,4-dihydroxystyryl)acrylonitrite], non-ATP-competitive small-molecule inhibitor of JAK2, 20% residual activity of mutant V617F in the resence of 0.02 mM LS104 and 0.02 mM ATP | Homo sapiens | |
additional information | JAK2 is not inhibited by STI571 | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + a [protein]-L-tyrosine | Homo sapiens | - |
ADP + a [protein]-L-tyrosine phosphate | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | O60674 | - |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + a [protein]-L-tyrosine | - |
Homo sapiens | ADP + a [protein]-L-tyrosine phosphate | - |
? |
Synonyms | Comment | Organism |
---|---|---|
JAK2 | - |
Homo sapiens |
Janus kinase 2 | - |
Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00093 | - |
in the presence of 0.02 mM ATP and 0.00015 mM substrate peptide | Homo sapiens | LS104 | |
0.00193 | - |
in the presence of 0.02 mM ATP and 0.0003 mM substrate peptide | Homo sapiens | LS104 | |
0.00252 | - |
in the presence of 0.02 mM ATP and 0.0015 mM substrate peptide | Homo sapiens | LS104 |