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Literature summary for 2.7.10.2 extracted from

  • Lipka, D.B.; Hoffmann, L.S.; Heidel, F.; Markova, B.; Blum, M.C.; Breitenbuecher, F.; Kasper, S.; Kindler, T.; Levine, R.L.; Huber, C.; Fischer, T.
    LS104, a non-ATP-competitive small-molecule inhibitor of JAK2, is potently inducing apoptosis in JAK2V617F-positive cells (2008), Mol. Cancer Ther., 7, 1176-1184.
    View publication on PubMed
Search for more literature for 2.7.10.2

Cloned(Commentary)

Cloned (Comment) Organism
the V617F mutant is expressed in Ba/F3 cells Homo sapiens

Protein Variants

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

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/ Products (Substrates)

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

Organism UniProt Comment Textmining
Homo sapiens O60674
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + a [protein]-L-tyrosine
-
 Homo sapiens ADP + a [protein]-L-tyrosine phosphate
-
 ?

Synonyms

Synonyms Comment Organism
JAK2
-
 Homo sapiens
Janus kinase 2
-
 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
 Homo sapiens

IC50 Value

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