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Drug-Target Interaction

Drug

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PubChem ID:5280442
Structure:
Synonyms:
00017_FLUKA
4'-Methoxy-5,7-dihydroxyflavone
4'-Methoxyapigenin
480-44-4
4H-1-Benzopyran-4-one, 5,7-dihydroxy-2-(4-methoxyphenyl)-
5,7-Dihydroxy-2-(4-methoxyphenyl)-4-benzopyrone
5,7-dihydroxy-2-(4-methoxyphenyl)-4H-chromen-4-one
5,7-dihydroxy-2-(4-methoxyphenyl)chromen-4-one
5,7-DIHYDROXY-4'-METHOXY FLAVONE
5,7-Dihydroxy-4'-methoxyflavone
5,7-Dioxy-4'-methoxyflavone
5-18-04-00575 (Beilstein Handbook Reference)
AC1NQX12
Acacetin
Acacetine
Acaceztin
ACAETIN
AIDS-014771
AIDS014771
Akatsetin
Apigenin 4'-dimethyl ether
Apigenin 4'-methyl ether
Apisenin 4'-methyl ether
BCBcMAP01_000082
BE7185D3-6331-4E84-8C8E-5D10E505E37A
BPBio1_000935
BRD-K77685744-001-03-6
BRN 0277879
BSPBio_000849
Buddleoflavonol
C01470
CAS-480-44-4
CHEBI:15335
CHEMBL243664
DivK1c_000878
EINECS 207-552-3
Flavone, 5,7-dihydroxy-4'-methoxy-
Flavone, 5,7-dihydroxy-4'-methoxy- (8CI)
HMS1570K11
HMS1922P12
HMS2097K11
HMS2234J17
HMS502L20
IDI1_000878
KBio1_000878
KBio2_000595
KBio2_003163
KBio2_005731
KBioSS_000595
Kinome_3212
Linarigenin
Linarisenin
LMPK12110468
LS-39600
MLS002153960
MLS002693970
MolPort-003-665-819
NCGC00016458-01
NCGC00016458-02
NCGC00016458-03
NCGC00016458-04
NCGC00016458-05
NCGC00095213-01
NCGC00095213-02
NCGC00095213-03
NCGC00179402-01
NINDS_000878
NSC 76061
NSC-76061
NSC76061
Prestwick0_000695
Prestwick1_000695
Prestwick2_000695
Prestwick3_000695
Prestwick_49
SMP1_000001
SMR001233299
SPBio_002770
SPECTRUM200499
Spectrum5_000930
Spectrum_000135
ST066889
WLN: T66 BO EVJ CR DO1& GQ IQ
ZINC03871358

Target

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Uniprot ID:ICE_DROME
Synonyms:
Caspase
drICE
EC-Numbers:3.4.22.-
Organism:Drosophila melanogaster
Fruit fly
PDB IDs:-

Binding Affinities:

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

References:

17846503
Acacetin-induced apoptosis of human breast cancer MCF-7 cells involves caspase cascade, mitochondria-mediated death signaling and SAPK/JNK1/2-c-Jun activation.. Hye-Young Shim; Jong-Hwa Park; Hyun-Dong Paik; Seung-Yeol Nah; Darrick S H L Kim; Ye Sun Han (2007) Molecules and cells display abstract
The mechanism of acacetin-induced apoptosis of human breast cancer MCF-7 cells was investigated. Acacetin caused 50% growth inhibition (IC50) of MCF-7 cells at 26.4% 0.7% M over 24 h in the MTT assay. Apoptosis was characterized by DNA fragmentation and an increase of sub-G1 cells and involved activation of caspase-7 and PARP (poly-ADP-ribose polymerase). Maximum caspase 7 activity was observed with 100 microM acacetin for 24 h. Caspase 8 and 9 activation cascades mediated the activation of caspase 7. Acacetin caused a reduction of Bcl-2 expression leading to an increase of the Bax:Bcl-2 ratio. It also caused a loss of mitochondrial membrane potential that induced release of cytochrome c and apoptosis inducing factor (AIF) into the cytoplasm, enhancing ROS generation and subsequently resulting in apoptosis. Pretreatment of cells with N-acetylcysteine (NAC) reduced ROS generation and cell growth inhibition, and pretreatment with NAC or a caspase 8 inhibitor (Z-IETD-FMK) inhibited the acacetin-induced loss of mitochondrial membrane potential and release of cytochrome c and AIF. Stress-activated protein kinase/c-Jun NH4-terminal kinase 1/2 (SAPK/ JNK1/2) and c-Jun were activated by acacetin but extracellular-regulated kinase 1/2 (Erk1/2) nor p38 mitogen-activated protein kinase (MAPK) were not. Our results show that acacetin-induced apoptosis of MCF-7 cells is mediated by caspase activation cascades, ROS generation, mitochondria-mediated cell death signaling and the SAPK/JNK1/2-c-Jun signaling pathway, activated by acacetin-induced ROS generation.