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BRENDA support

Literature summary for 2.7.10.2 extracted from

  • Li, J.; Favata, M.; Kelley, J.A.; Caulder, E.; Thomas, B.; Wen, X.; Sparks, R.B.; Arvanitis, A.; Rogers, J.D.; Combs, A.P.; Vaddi, K.; Solomon, K.A.; Scherle, P.A.; Newton, R.; Fridman, J.S.
    INCB16562, a JAK1/2 selective inhibitor, is efficacious against multiple myeloma cells and reverses the protective effects of cytokine and stromal cell support (2010), Neoplasia, 12, 28-38.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
INCB16562 selective, and orally bioavailable small-molecule inhibitor of JAK1 and JAK2 markedly selective over JAK3 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
INA-6 cell
-
Homo sapiens
-
MM1-S cell
-
Homo sapiens
-
myeloma cell
-
Homo sapiens
-
NCI-H929 cell
-
Homo sapiens
-
plasma cell primary CD138+ plasma cell Homo sapiens
-
RPMI-8226 cell
-
Homo sapiens
-
TF-1 BCR-ABL cell
-
Homo sapiens
-
TF-1 cell
-
Homo sapiens
-
U-266 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + STAT3
-
Homo sapiens ADP + phospho-L-tyrosinyl-STAT3
-
?

Synonyms

Synonyms Comment Organism
Jak1
-
Homo sapiens
JAK2
-
Homo sapiens
Jak3
-
Homo sapiens
Janus kinase
-
Homo sapiens
Tyk2
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000025
-
JAK2 Homo sapiens INCB16562
0.0000022
-
JAK1 Homo sapiens INCB16562
0.0000027
-
TYK2 Homo sapiens INCB16562
0.0000101
-
JAK3 Homo sapiens INCB16562