Compound_ID |
Target |
Gene_Name |
Gene_ID |
Cancer |
Cell_lines |
IC50 Value |
EC50 Value |
ED50 Value |
GI50 Value |
Remarks |
References |
MMP-AC0014 |
AKT1 |
v-akt murine thymoma viral oncogene homolog 1 |
207 |
Lung adenocarcinoma |
A549 |
- |
- |
- |
- |
Apigenin has been shown to inhibit AKT activation . |
15947208 |
MMP-AC0014 |
CCNB1 |
cyclin B1 |
891 |
Colon Cancer |
SW-480 |
- |
- |
- |
- |
The steady-state level of cyclin B1 was significantly reduced after apigenintreatment for 48 h at doses of 30 mM and higher. |
10900467 |
MMP-AC0014 |
MMP-AC0014 |
cyclin-dependent kinase 1 |
983 |
Human Melanoma |
OCM-1 |
- |
- |
- |
- |
Apigenin inhibited CDK-1 in OCM-1 cell line. |
11322924 |
MMP-AC0014 |
CDK1 |
cyclin-dependent kinase 1 |
983 |
Colon Cancer |
HT-29 |
- |
- |
- |
- |
p34cdc2 kinase activity was significantly reduced by apigenin, at least in the high concentrations of 50-80 mM, for 24 h in each of three cell lines in comparison with the vehicle controls |
10900467 |
MMP-AC0014 |
CDK1 |
cyclin-dependent kinase 1 |
983 |
Colon Cancer |
SW-480 |
- |
- |
- |
- |
p34cdc2 kinase activity was significantly reduced by apigenin, at least in the high concentrations of 50-80 mM, for 24 h in each of three cell lines in comparison with the vehicle controls |
10900467 |
MMP-AC0014 |
CDK1 |
cyclin-dependent kinase 1 |
983 |
Colorectal Adenocarcinoma |
CaCo-2 |
- |
- |
- |
- |
p34cdc2 kinase activity was significantly reduced by apigenin, at least in the high concentrations of 50-80 mM, for 24 h in each of three cell lines in comparison with the vehicle controls |
10900467 |
MMP-AC0014 |
CDKN1B |
cyclin-dependent kinase inhibitor 1B (p27, Kip1) |
1027 |
Human Melanoma |
OCM-1 |
- |
- |
- |
- |
The flavone apigenin which arrest cells in G2/M but were without effect on CDK2 activity, affected only marginally the level of p27KIP1 and did not induce p21CIP. |
11322924 |
MMP-AC0014 |
COX-1 |
cytochrome c oxidase subunit I |
4512 |
Murine monocyte/macrophage line derived from ascitic tumour induced with Abelson leukaemai virus |
RAW264.7 |
100 µM |
- |
- |
- |
It inhibits cyclooxygenase 1 (Cox-1) activity and it is an anti-inflammatory mechanism. |
Phytochemistry Reviews 1: 369-377, 2002 |
MMP-AC0014 |
CYP19A1 |
cytochrome P450, family 19, subfamily A, polypeptide 1 |
1588 |
Adrenocortical Carcinoma |
H295R |
20 µM |
- |
- |
- |
Apigenin inhibited aromatase activity concentration dependently in H295R cells after a 24 h exposure.A key enzyme in the synthesis of estrogens from androgens is aromatase(cytochromeP45019;CYP19. |
15319488 |
MMP-AC0014 |
CYP19A1 |
cytochrome P450, family 19, subfamily A, polypeptide 1 |
1588 |
Breast adenocarcinoma |
MCF-7 |
1 µM |
- |
- |
- |
Apigenin inhibited aromatase activity with IC50 value of about 1µM. |
22209285 |
MMP-AC0014 |
CYPIA1 |
cytochrome P450, family 1, subfamily A, polypeptide 1 |
1543 |
Murine monocyte/macrophage line derived from ascitic tumour induced with Abelson leukaemai virus |
RAW264.7 |
0.02 µM |
- |
- |
- |
Apigenin potently inhibited Cyp1A activity with an IC50 of 0.02 µM Cyp1A, which is e.g. involved in the activation of carcinogens from grilled meat, as a model phase 1 enzyme, and measured the potential of beer constituents to inhibit its enzymatic activity. |
Phytochemistry Reviews 1: 369-377, 2002 |
MMP-AC0014 |
HIF1A |
hypoxia inducible factor 1 |
3091 |
Lung adenocarcinoma |
A549 |
- |
- |
- |
- |
Apigenin specifically inhibited expression of HIF-1alpha but not HIF-1Beta subunit. |
15947208 |
MMP-AC0014 |
IGF1 |
insulin-like growth factor 1 |
3479 |
Prostate Cancer |
PC-3 |
- |
- |
- |
- |
growth of PC-3 tumors in nude mice was significantly inhibited by administration of apigenin to mice |
18726972 |
MMP-AC0014 |
NOS2 |
nitric oxide synthase 2, inducible |
4843 |
Murine monocyte/macrophage line derived from ascitic tumour induced with Abelson leukaemai virus |
RAW264.7 |
17.5 µM |
- |
- |
- |
Nitric oxide (NO) synthase (iNOS) and consequently, enhance the generation of NO. Generally, NO is an important signaling molecule, long-term elevated levels of NO, however, have been linked to early steps in carcinogenesis.It cause inhibition of lipopolysaccharide (LPS)-mediated induction of inducible nitric oxide synthase , which is an anti-inflammatory mechanis. |
Phytochemistry Reviews 1: 369-377, 2002 |
MMP-AC0014 |
NQO1 |
NAD(P)H dehydrogenase, quinone 1 |
1728 |
Murine monocyte/macrophage line derived from ascitic tumour induced with Abelson leukaemai virus |
RAW264.7 |
RAW264.7 |
- |
- |
- |
It induces the QR activity.Induction of phases 2 enzymes contributes to chemopreventive activity. QR is not catalyzing a conjugation reaction, but it is induced co-ordinately with other phase 2 enzymes and contributes to detoxification by reduction of reactive quinones to less reactive hydroquinones. |
Phytochemistry Reviews 1: 369-377, 2002 |
MMP-AC0014 |
RPS6KB1 |
ribosomal protein S6 kinase, 70kDa, polypeptide 1 |
6198 |
Lung adenocarcinoma |
A549 |
- |
- |
- |
- |
Apigenin inhibited p70S6K1 expression and activation in the cells . p70S6K1 were recently shown to regulate HIF-1 and VEGF transcriptional activation. |
15947208 |
MMP-AC0014 |
VEGFA |
vascular endothelial growth factor A |
7422 |
Lung adenocarcinoma |
A549 |
- |
- |
- |
- |
Apigenin inhibited VEGF transcriptional activation through the hypoxia-inducible factor 1 (HIF-1) binding site and specifically decreased HIF-1alpha but not HIF-1Beta subunit expression in the cells. |
15947208 |