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Drug-Target Interaction

Drug

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PubChem ID:8515
Structure:
Synonyms:
"insolution™ jnk inhibitor ii"
1,9-Pyrazoloanthrone
129-56-6
14,15-diazatetracyclo[7.6.1.0^{2,7}.0^{13,16}]hexadeca-1(15),2(7),3,5,9,11
1pmv
2,6-DIHYDROANTHRA/1,9-CD/PYRAZOL-6-ONE
2H-Dibenzo[cd,g]indazol-6-one
AIDS-220090
AIDS220090
ANTHRA(1,9-cd)PYRAZOL-6(2H)-ONE
Anthra-1,9-pyrazol-6-none
Anthrapyrazolone
Anthra[1,9-cd]pyrazol-6(2H)-one
Anthra[1,9-cd]pyrazol-6(2H)-one & Z-100
BAS 00719687
BCBcMAP01_000053
Bio1_000335
Bio1_000824
Bio1_001313
Bio2_000373
Bio2_000853
BiomolKI2_000072
BiomolKI_000068
BRN 0746890
BSPBio_001066
C.I. 70300
C432165
CBiol_002049
dibenzo[cd,g]indazol-6(2H)-one
dihydroanthrapyrazole compound 4
EINECS 204-955-6
EU-0100473
HSCI1_000136
IDI1_002128
InSolution™ JNK Inhibitor II
JNK Inhibitor II
K00068
KBio2_000406
KBio2_002974
KBio2_005542
KBio3_000771
KBio3_000772
KBioGR_000406
KBioSS_000406
Lopac-S-5567
Lopac0_000473
LS-20607
MLS002153267
NCGC00015958-01
NCGC00025186-01
NCGC00025186-02
NCGC00025186-03
NCGC00025186-04
NCGC00025186-05
NSC 75890
NSC75890
Pyrazolanthrone
Pyrazoleanthrone
QTL1_000077
RH 00237
S5567_SIGMA
SAPK Inhibitor II
SBB000595
SMP2_000240
SMR000015440
SP 600125
SP 600125 & Z-100
SP600125
SR-01000637108-1
TL8000704
Tocris-1496
WLN: T C6665 1A P IV OMNJ
ZINC04335977

Target

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Uniprot ID:NOS3_HUMAN
Synonyms:
cNOS
Constitutive NOS
EC-NOS
Endothelial NOS
eNOS
Nitric oxide synthase, endothelial
NOS type III
NOSIII
EC-Numbers:1.14.13.39
Organism:Homo sapiens
Human
PDB IDs:1M9J 1M9K 1M9M 1M9Q 1M9R 3EAH 3NOS
Structure:
3NOS

Binding Affinities:

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

References:

17322004
Post-transcriptional regulation of human inducible nitric-oxide synthase expression by the Jun N-terminal kinase.. Riku Korhonen; Katrin Linker; Andrea Pautz; Ulrich F÷rstermann; Eeva Moilanen; Hartmut Kleinert (2007) Molecular pharmacology display abstract
Human inducible nitric-oxide synthase (iNOS) expression is regulated both at transcriptional and post-transcriptional levels. In the present study, the effect of Jun N-terminal kinase (JNK) on human iNOS expression was investigated. In A549/8 human alveolar epithelial cells, both the inhibition of JNK by a pharmacological inhibitor anthra[1,9-cd]pyrazol-6(2H)-one1,9-pyrazoloanthrone (SP600125) and small interfering RNA (siRNA)-mediated down-regulation of JNK led to a reduction of iNOS mRNA and protein expression. iNOS promoter activity was not affected by these treatments. Hence, JNK seems to regulate iNOS expression through post-transcriptional mechanisms by stabilizing iNOS mRNA. Our laboratory has shown recently that a cytokine-induced RNA binding protein tristetraprolin (TTP) is a major positive regulator of human iNOS expression by stabilizing iNOS mRNA. Therefore, the effect of JNK inhibition by SP600125 or down-regulation by siRNA on TTP expression was investigated. Both SP600125 and siRNA targeted at JNK resulted in a reduction of TTP protein expression without affecting the amount of TTP mRNA. These data suggest a post-transcriptional control of TTP expression by JNK. Moreover, the modulation of JNK signaling by SP600125 or siRNA did not change p38 phosphorylation. In summary, the results suggest that JNK regulates human iNOS expression by stabilizing iNOS mRNA possibly by a TTP-dependent mechanism.