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Literature summary for 2.7.10.2 extracted from

  • Burger, R.; Le Gouill, S.; Tai, Y.T.; Shringarpure, R.; Tassone, P.; Neri, P.; Podar, K.; Catley, L.; Hideshima, T.; Chauhan, D.; Caulder, E.; Neilan, C.L.; Vaddi, K.; Li, J.; Gramatzki, M.; Fridman, J.S.; Anderson, K.C.
    Janus kinase inhibitor INCB20 has antiproliferative and apoptotic effects on human myeloma cells in vitro and in vivo (2009), Mol. Cancer Ther., 8, 26-35.
    View publication on PubMedView publication on EuropePMC
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Inhibitors

Inhibitors Comment Organism Structure
AG490
-
 Homo sapiens
INCB20 potently inhibits all members of the JAK family with a 100-1000fold selectivity for JAKs over more than 70 other kinases, potent and specific Pan-JAK inhibitor Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
INA-6 cell
-
 Homo sapiens
-
myeloma cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + EQEDEPEGDYFEWLE
-
 Homo sapiens ADP + EQEDEPEGDpYFEWLE
-
 ?

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
0.0000003
-
 TYK2, in 50 mM, Tris-HCl (pH 7.8), 100 mM NaCl, 5 mM dithiothreitol, and 0.1 mg/ml bovine serum albumin, at 25°C Homo sapiens INCB20
0.0000005
-
 JAK2, in 50 mM, Tris-HCl (pH 7.8), 100 mM NaCl, 5 mM dithiothreitol, and 0.1 mg/ml bovine serum albumin, at 25°C Homo sapiens INCB20
0.0000005
-
 JAK3, in 50 mM, Tris-HCl (pH 7.8), 100 mM NaCl, 5 mM dithiothreitol, and 0.1 mg/ml bovine serum albumin, at 25°C Homo sapiens INCB20
0.0000009
-
 JAK1, in 50 mM, Tris-HCl (pH 7.8), 100 mM NaCl, 5 mM dithiothreitol, and 0.1 mg/ml bovine serum albumin, at 25°C Homo sapiens INCB20
0.0102
-
 JAK1, in 50 mM, Tris-HCl (pH 7.8), 100 mM NaCl, 5 mM dithiothreitol, and 0.1 mg/ml bovine serum albumin, at 25°C Homo sapiens AG490
0.0112
-
 JAK2, in 50 mM, Tris-HCl (pH 7.8), 100 mM NaCl, 5 mM dithiothreitol, and 0.1 mg/ml bovine serum albumin, at 25°C Homo sapiens AG490
0.0154
-
 JAK3, in 50 mM, Tris-HCl (pH 7.8), 100 mM NaCl, 5 mM dithiothreitol, and 0.1 mg/ml bovine serum albumin, at 25°C Homo sapiens AG490