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Drug-Target Interaction

Drug

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PubChem ID:3973
Structure:
Synonyms:
"insolution™ ly 294002"
"ly 294002; 2-(4-morpholino)-8-phenyl-4h-1-benzopyran-4-one"
154447-36-6
1yi3
2-(4-Morpholino)-8-phenyl-4H-1-benzopyran-4-one
2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one
2-MORPHOLIN-4-YL-7-PHENYL-4H-CHROMEN-4-ONE
2-morpholin-4-yl-8-phenyl-4H-chromen-4-one
2-morpholin-4-yl-8-phenylchromen-4-one
4H-1-Benzopyran-4-one, 2-(4-morpholinyl)-8-phenyl
4H-1-Benzopyran-4-one, 2-(4-morpholinyl)-8-phenyl-
4H-1-Benzopyran-4-one, 2-(4-morpholinyl)-8-phenyl- (9CI)
8-Phenyl-2-(morpholin-4-yl)-chromen-4-one
AC1L1H4N
AC1Q6CLU
AIDS-223867
AIDS223867
AR-1J3542
BCBcMAP01_000117
Bio1_000332
Bio1_000821
Bio1_001310
Bio2_000442
Bio2_000922
BiomolKI2_000037
BiomolKI_000029
BMK1-D5
BRD-K27305650-001-05-9
BSPBio_001223
C085911
C15195
CBiol_002046
CCG-100633
CHEMBL98350
DB02656
EC-000.2341
H-1-Benzopyran-4-one, 2-(4-morpholinyl)-8-phenyl- (9CI)
HMS1362M05
HMS1792M05
HMS1990M05
HMS3229G17
HSCI1_000206
IDI1_002197
IN1266
IN1268
InSolution&trade
InSolution™ LY 294002
K00235
KBio2_000563
KBio2_003131
KBio2_005699
KBio3_001005
KBio3_001006
KBioGR_000563
KBioSS_000563
Kinome_3543
Lopac-L-9908
Lopac0_000710
LS-39828
LY 294002
LY 294002; 2-(4-Morpholino)-8-phenyl-4H-1-benzopyran-4-one
LY-294,002
LY-294,002 hydrochloride
LY-294002
LY-924002
LY2
LY294002
LY294002-Supplied by Selleck Chemicals
Lys 294002
NCGC00015622-01
NCGC00015622-02
NCGC00015622-03
NCGC00015622-04
NCGC00015622-05
NCGC00015622-06
NCGC00015622-07
NCGC00025020-01
NCGC00025020-02
NCGC00025020-03
NCGC00025020-04
NCGC00179253-01
nchembio790-comp36
NCI60_034712
NSC697286
S1105_Selleck
Tocris-1130
ZINC00006014

Target

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Uniprot ID:AKT1_MOUSE
Synonyms:
AKT1 kinase
C-AKT
PKB
Protein kinase B
RAC-alpha serine/threonine-protein kinase
RAC-PK-alpha
Thymoma viral proto-oncogene
EC-Numbers:2.7.11.1
Organism:Mouse
Mus musculus
PDB IDs:-

Binding Affinities:

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

References:

17433610
Inhibition of phosphatidylinositol 3-kinase causes cell death in rat osteoblasts through inactivation of Akt.. Yun Zhang; Le Zhang; Ming Yan; Xiaoxiang Zheng (2007) Biomedicine & pharmacotherapy display abstract
Previous evidences indicated that phosphatidylinositol 3-kinase (PI3-kinase) is an important regulatory molecule that is involved in the cell growth and survival, and inhibition of the PI3-kinase activity enhances apoptotic cell death. However, the relationship between PI3-kinase activity and osteoblasts, capable of new bone formation, remained unknown. In the present study, pharmacological inhibitor of PI3-kinase LY294002 was used to observe the role of the PI3-kinase in the growth of rat osteoblasts. To identify its molecular mechanism, Western blots analysis and immunocytochemistry were applied to examine changes of Akt phosphorylation and its distribution. Our data showed that inhibition of PI3-kinase activity significantly triggered the decrease of cell growth, cell apoptosis and loss of mitochondrial membrane potential (Deltapsi(m)). Osteoblastic dysfunction stimulated by LY294002 was accompanied by inactivation of Akt and its redistribution. In all these results demonstrated that inhibition of PI3-kinase induced apoptotic cell death, which was mediated by inactivation of Akt pathway in rat osteoblasts.