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Drug-Target Interaction

Drug

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PubChem ID:4713
Structure:
Synonyms:
"2′-amino-3′-methoxyflavone"
167869-21-8
2′-Amino-3′-methoxyflavone
2'-AMINO-3'-METHOXYFLAVONE
2-(2'-amino-3'-methoxyphenyl)oxanaphthalen-4-one
2-(2-Amino-3-methoxyphenyl)-4H-1-benzopyran-4-one
2-(2-Amino-3-methoxyphenyl)-chromen-4-one
2-(2-amino-3-methoxyphenyl)chromen-4-one
4H-1-Benzopyran-4-one, 2-(2-amino-3-methoxyphenyl)-
4H-1-Benzopyran-4-one, 2-(2-amino-3-methoxyphenyl)- & Z-100
AC1L1ISD
AC1Q6AK0
AIDS-220091
AIDS220091
AR-1C6511
BCBcMAP01_000049
Bio1_000475
Bio1_000964
Bio1_001453
Bio2_000338
Bio2_000818
BiomolKI2_000011
BiomolKI_000001
BIP0711
BMK1-B1
BRD-K62810658-001-05-6
BSPBio_000996
C093973
CCG-100605
CHEBI:150222
CHEMBL35482
EC-000.2425
EU-0101028
HMS1362B17
HMS1792B17
HMS1990B17
HMS3229M08
HMS3263M17
IDI1_002093
IN1172
KBio2_000336
KBio2_002904
KBio2_005472
KBio3_000671
KBio3_000672
KBioGR_000336
KBioSS_000336
Lopac-P-215
Lopac0_001028
LS-182409
MolPort-000-005-902
NCGC00015790-01
NCGC00015790-02
NCGC00015790-03
NCGC00015790-04
NCGC00015790-05
NCGC00015790-06
NCGC00015790-07
NCGC00015790-08
NCGC00025045-01
NCGC00025045-02
NCGC00025045-03
NCGC00025045-04
NCGC00025045-05
NCGC00179347-01
nchembio.282-comp4
NCI60_028554
NSC679828
P-215
P215_SIGMA
PD 098059
PD 98,059
PD 98059
PD 98059 & Z-100
PD 98059, PD98059
PD-098059
PD-98059
PD098059
PD09859
PD98059
PD98059-Supplied by Selleck Chemicals
S1177_Selleck
SMP2_000052
Tocris-1213
ZINC01420826

Target

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Uniprot ID:MK03_HUMAN
Synonyms:
ERK-1
ERT2
Extracellular signal-regulated kinase 1
Insulin-stimulated MAP2 kinase
MAP kinase 1
MAPK 1
Microtubule-associated protein 2 kinase
Mitogen-activated protein kinase 3
p44-ERK1
p44-MAPK
EC-Numbers:2.7.11.24
Organism:Homo sapiens
Human
PDB IDs:2ZOQ
Structure:
2ZOQ

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----

References:

16982750
Inhibition of the janus kinase family increases extracellular signal-regulated kinase 1/2 phosphorylation and causes endoreduplication.. Gudrun Reiterer; Andrew Yen (2006) Cancer research display abstract
The role of Janus-activated kinase (JAK) signaling in cell cycle transit and maintenance of genomic stability was determined in HL-60 myeloblastic leukemia cells. Inhibition of JAKs, all JAKs (JAK1, JAK2, JAK3, and tyrosine kinase 2), JAK2, or JAK3, caused a significant reduction in cell growth with a major G2-M arrest evident 24 hours after treatment. Targeting all JAKs also caused endoreduplication 48 and 72 hours after treatment. We discovered mitotic cells in both G2 (4N DNA) and G4 (8N DNA) subpopulations of cells treated with an inhibitor of all JAKs as detected by phosphorylated histone H3 expression. Treatment with inhibitors of just JAK2 or JAK3 drastically reduced such mitotic cells. We observed a complete blockage of IFN-gamma and interleukin-6-induced signal transducer and activator of transcription (STAT)-1 and STAT-3 response when all JAKs were inhibited. At the same time, we found baseline phosphorylated extracellular signal-regulated kinase (ERK) 1/2 to be elevated by JAK inhibition, particularly when all JAKs were inhibited. The G2-M arrest and endoreduplication induced by JAK inhibitors were reduced in cells pretreated with PD98059 to inhibit ERK. PD98059 also increased back the expression of the MAD2 cell cycle checkpoint protein that was down-regulated during "all JAKs inhibitor"-mediated endoreduplication. These data suggest that JAK signaling is needed for G2-M transit with inhibition of ERK.