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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:JUN_MOUSE
Synonyms:
Activator protein 1
AH119
AP1
Jun A
Proto-oncogene c-jun
Transcription factor AP-1
V-jun avian sarcoma virus 17 oncogene homolog
EC-Numbers:-
Organism:Mouse
Mus musculus
PDB IDs:-

Binding Affinities:

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

References:

17372274
Humulone inhibits phorbol ester-induced COX-2 expression in mouse skin by blocking activation of NF-kappaB and AP-1: IkappaB kinase and c-Jun-N-terminal kinase as respective potential upstream targets.. Jung-Chul Lee; Joydeb K Kundu; Dal-Mi Hwang; Hye-Kyung Na; Young-Joon Surh (2007) Carcinogenesis display abstract
Humulone, a bitter acid derived from hop (Humulus lupulus L.), possesses antioxidative, anti-inflammatory and other biologically active activities. Although humulone has been reported to inhibit chemically induced mouse skin tumor promotion, the underlying mechanisms are yet to be elucidated. Since an inappropriate over-expression of cyclooxygenase-2 (COX-2) is implicated in carcinogenesis, we investigated effects of humulone on COX-2 expression in mouse skin stimulated with the tumor promoter 12-O-tetradecanoylphorbol-13-acetate (TPA). Topical application of humulone (10 mumol) significantly inhibited TPA-induced epidermal COX-2 expression. Humulone also diminished TPA-induced DNA binding of nuclear factor-kappaB (NF-kappaB) and activator protein-1 (AP-1). Pre-treatment with humulone attenuated TPA-induced phosphorylation of p65 and nuclear translocation of NF-kappaB subunit proteins. Humulone blunted TPA-induced activation of inhibitory kappaB (IkappaB) kinase (IKK) in mouse skin, which accounts for its suppression of phosphorylation and subsequent degradation of IkappaBalpha. An in vitro kinase assay revealed that humulone could directly inhibit the catalytic activity of IKKbeta. Humulone suppressed the activation of mitogen-activated protein kinases (MAPKs) in TPA-treated mouse skin. The roles of extracellular signal-regulated protein kinase-1/2 and p38 MAPK in TPA-induced activation of NF-kappaB in mouse skin had been defined in our previous studies. The present study revealed that topical application of SP600125, a pharmacological inhibitor of c-Jun-N-terminal kinase (JNK), abrogated the activation of AP-1 and the expression of COX-2 in TPA-treated mouse skin. Taken together, humulone suppressed TPA-induced activation of NF-kappaB and AP-1 and subsequent expression of COX-2 by blocking upstream kinases IKK and JNK, respectively, which may account for its antitumor-promoting effects on mouse skin carcinogenesis.