Compound_ID |
Target |
Gene_Name |
Gene_ID |
Cancer |
Cell_lines |
IC50 Value |
EC50 Value |
ED50 Value |
GI50 Value |
Remarks |
References |
MMP-AC0109 |
BAX |
BCL2-associated X protein |
581 |
Prostate Cancer |
LNCaP |
- |
- |
- |
- |
The deregulation of apoptosis is studied by the expression of Bax and Bcl2. Bax is proapoptotic protein, there was a significant increase in the protein expression of Bax with a dose-dependent on treatment of LNCaP and CWR22Rm1 cells with butein. |
22114764 |
MMP-AC0109 |
BAX |
BCL2-associated X protein |
581 |
Prostrate Carcinoma |
CWR22Rm1 |
- |
- |
- |
- |
The deregulation of apoptosis is studied by the expression of Bax and Bcl2. Bax is proapoptotic protein, there was a significant increase in the protein expression of Bax with a dose-dependent on treatment of LNCaP and CWR22Rm1 cells with butein. |
22114764 |
MMP-AC0109 |
BAX |
BCL2-associated X protein |
581 |
Human promyelocytic leukemia |
HL-60 |
- |
- |
- |
- |
The treatment of HL-60 cells with butein increased the expression of Bax protein |
11393587 |
MMP-AC0109 |
BCL2 |
B-cell CLL/lymphoma 2 |
596 |
Prostate Cancer |
LNCaP |
- |
- |
- |
- |
The deregulation of apoptosis is studied by the expression of Bax and Bcl2. Bcl2 is anti-apoptotic, there was a significant decrease in the protein expression of Bcl2 on treatment of LNCaP and CWR22Rm1 cells with butein. |
22114764 |
MMP-AC0109 |
BCL2 |
B-cell CLL/lymphoma 2 |
596 |
Prostrate Carcinoma |
CWR22Rm1 |
- |
- |
- |
- |
The deregulation of apoptosis is studied by the expression of Bax and Bcl2. Bcl2 is anti-apoptotic, there was a significant decrease in the protein expression of Bcl2 on treatment of LNCaP and CWR22Rm1 cells with butein. |
22114764 |
MMP-AC0109 |
BCL2 |
B-cell CLL/lymphoma 2 |
596 |
Human promyelocytic leukemia |
HL-60 |
- |
- |
- |
- |
The treatment of HL-60 cells with butein decreased the expression of Bcl-2 protein |
11393587 |
MMP-AC0109 |
CASP3 |
caspase 3, apoptosis-related cysteine peptidase |
836 |
Human promyelocytic leukemia |
HL-60 |
- |
- |
- |
- |
The treatment of the cells with butein increased the caspase-3 activity |
11393587 |
MMP-AC0109 |
CASP3 |
caspase 3, apoptosis-related cysteine peptidase |
836 |
Prostate Cancer |
LNCaP |
- |
- |
- |
- |
Treatment of LNCaP cells with butein (10-30 µM) caused an increase in the activation of caspases-3, -8, and -9 dose dependently. |
22114764 |
MMP-AC0109 |
CASP8 |
caspase 8, apoptosis-related cysteine peptidase |
841 |
Prostate Cancer |
LNCaP |
- |
- |
- |
- |
Treatment of LNCaP cells with butein (10-30 µM) caused an increase in the activation of caspase-8 dose dependently. |
22114764 |
MMP-AC0109 |
CASP9 |
caspase 9, apoptosis-related cysteine peptidase |
842 |
Prostate Cancer |
LNCaP |
- |
- |
- |
- |
Treatment of LNCaP cells with butein (10-30 µM) caused an increase in the activation of caspase-9 dose dependently. |
22114764 |
MMP-AC0109 |
CCND1 |
cyclin D1 |
595 |
Prostate Cancer |
LNCaP |
- |
- |
- |
- |
LNCaP cells with butein (10-30 µM; 48 h) caused a dose-dependent decrease in the protein expression of cyclinsD1 by using immunoblot analysis. Treatment of CWR22Rm1 cells with butein (10-30 µM; 48 h) also caused an inhibition of cyclin D1,suggesting that the effects of butein on prostrate cancer(PCa) cells are not limited for one-cell type. |
22114764 |
MMP-AC0109 |
CCND1 |
cyclin D1 |
595 |
Prostrate Carcinoma |
CWR22Rm1 |
- |
- |
- |
- |
LNCaP cells with butein (10-30 µM; 48 h) caused a dose-dependent decrease in the protein expression of cyclinsD1 by using immunoblot analysis. Treatment of CWR22Rm1 cells with butein (10-30 µM; 48 h) also caused an inhibition of cyclin D1,suggesting that the effects of butein on prostrate cancer(PCa) cells are not limited for one-cell type. |
22114764 |
MMP-AC0109 |
CCND2 |
Cyclin D2 |
894 |
Prostate Cancer |
LNCaP |
- |
- |
- |
- |
LNCaP cells with butein (10-30 µM; 48 h) caused a dose-dependent decrease in the protein expression of cyclin D2 by using immunoblot analysis. |
22114764 |
MMP-AC0109 |
CCNE1 |
cyclin E1 |
898 |
Prostate Cancer |
LNCaP |
- |
- |
- |
- |
LNCaP cells with butein (10-30 µM; 48 h) caused a dose-dependent decrease in the protein expression of cyclin E by using immunoblot analysis. |
22114764 |
MMP-AC0109 |
CDK2 |
cyclin-dependent kinase 2 |
1017 |
Prostate Cancer |
LNCaP |
- |
- |
- |
- |
LNCaP cells with butein (10-30 µM; 48 h) caused a dose-dependent decrease in the protein expression of cdk2 using immunoblot analysis. Treatment of CWR22Rm1 cells with butein (10-30 µM; 48 h) also caused an inhibition of cdk 2,suggesting that the effects of butein on prostrate cancer(PCa) cells are not limited for one-cell type. |
22114764 |
MMP-AC0109 |
CDK2 |
cyclin-dependent kinase 2 |
1017 |
Prostrate Carcinoma |
CWR22Rm1 |
- |
- |
- |
- |
LNCaP cells with butein (10-30 µM; 48 h) caused a dose-dependent decrease in the protein expression of cdk2 using immunoblot analysis. Treatment of CWR22Rm1 cells with butein (10-30 µM; 48 h) also caused an inhibition of cdk 2,suggesting that the effects of butein on prostrate cancer(PCa) cells are not limited for one-cell type. |
22114764 |
MMP-AC0109 |
CDK4 |
cyclin-dependent kinase 4 |
1019 |
Prostate Cancer |
LNCaP |
- |
- |
- |
- |
LNCaP cells with butein (10-30 µM; 48 h) caused a dose-dependent decrease in the protein expression of cdk4 using immunoblot analysis. |
22114764 |
MMP-AC0109 |
CDK6 |
cyclin-dependent kinase 6 |
1021 |
Prostate Cancer |
LNCaP |
- |
- |
- |
- |
LNCaP cells with butein (10-30 µM; 48 h) caused a dose-dependent decrease in the protein expression of cdk4 using immunoblot analysis. |
22114764 |
MMP-AC0109 |
CDKN1A |
cyclin-dependent kinase inhibitor 1A (p21, Cip1) |
1026 |
Prostate Cancer |
LNCaP |
- |
- |
- |
- |
Treatment with butein resulted in an induction of WAF1/p21 even at the lowest concentration of 10 lM with a significant increase at the highest concentration of 30 µM. Treatment of CWR22Rm1 cells with butein (10-30 µM; 48 h) also caused an increase in WAF1/p21, suggesting that the effects of butein on prostrate cancer(PCa) cells are not limited for one-cell type. |
22114764 |
MMP-AC0109 |
CDKN1B |
cyclin-dependent kinase inhibitor 1B (p27, Kip1) |
1027 |
Prostate Cancer |
LNCaP |
- |
- |
- |
- |
Treatment with butein resulted in an induction of WAF1/p21 even at the lowest concentration of 10 lM with a significant increase at the highest concentration of 30 µM. Treatment of CWR22Rm1 cells with butein (10-30 µM; 48 h) also caused an increase in WAF1/p21, suggesting that the effects of butein on prostrate cancer(PCa) cells are not limited for one-cell type. |
22114764 |
MMP-AC0109 |
CHUK |
conserved helix-loop-helix ubiquitous kinase |
1147 |
Prostate Cancer |
LNCaP |
- |
- |
- |
- |
IKKalpha protein level was measured to evaluate the possible inhibitory mechanism of butein on IkBalpha protein degradation. Immunoblot analysis showed that pretreatment of LNCaP cells with butein inhibited IKKa in a dose-dependent manner. |
22114764 |
MMP-AC0109 |
GRB2 |
growth factor receptor-bound protein 2 |
2885 |
Liver Carcinoma |
SK-HEP-1 |
- |
- |
- |
- |
Western blotting analysis indicated that butein decreased the levels of GRB2 in SK-HEP-1 cell. |
21770460 |
MMP-AC0109 |
IL6 |
interleukin 6 |
3569 |
Murine monocyte/macrophage line derived from ascitic tumour induced with Abelson leukaemai virus |
Raw264 |
0.9 µM |
- |
- |
- |
IL-6 production in LPS-stimulated RAW264 cells was found to be suppressed by butein. |
21372424 |
MMP-AC0109 |
JUN |
jun proto-oncogene |
3725 |
Liver Carcinoma |
SK-HEP-1 |
- |
- |
- |
- |
Western blotting analysis indicated that butein decreased the levels of MMP-2, -7, and -9, uPA, Ras, Rho A, ROCK1, ERK1/2,JNK1/2, p-p38, and p-c-Jun in SK-HEP-1 cell. |
21770460 |
MMP-AC0109 |
MAPK1 |
mitogen-activated protein kinase 1 |
5594 |
Liver Carcinoma |
SK-HEP-1 |
- |
- |
- |
- |
Western blotting analysis indicated that butein decreased the levels of p38 in SK-HEP-1 cells. And butein at 62.5 and 125 µM suppressed the p38 activity. |
21770460 |
MMP-AC0109 |
MAPK8 |
mitogen-activated protein kinase 8 |
5599 |
Liver Carcinoma |
SK-HEP-1 |
- |
- |
- |
- |
Western blotting analysis indicated that butein decreased the levels of p38 in SK-HEP-1 cells. And butein at 62.5 and 125 µM suppressed the p38 activity. |
21770460 |
MMP-AC0109 |
MMP9 |
matrix metallopeptidase 9 (gelatinase B, 92kDa gelatinase, 92kDa type IV collagenase) |
4318 |
Liver Carcinoma |
SK-HEP-1 |
- |
- |
- |
- |
The gelatin zymography assay indicated that butein inhibited the activity of matrix metalloproteinases 2 (MMP-2). Gelationlytic activity of MMP-2 in the zymogram was inhibited by butein in a dose-dependent manner. Thus, MMP 2 was down-regulated in butein-treated SK-HEP-1 cells. |
21770460 |
MMP-AC0109 |
MMP7 |
matrix metallopeptidase 7 (matrilysin, uterine) |
4316 |
Carcinoma |
SK-HEP-1 |
- |
- |
- |
- |
The gelatin zymography assay indicated that butein inhibited the activity of matrix metalloproteinases 2 (MMP-2). Gelationlytic activity of MMP-2 in the zymogram was inhibited by butein in a dose-dependent manner. Thus, MMP 2 was down-regulated in butein-treated SK-HEP-1 cells. |
21770460 |
MMP-AC0109 |
MMP-AC0109 |
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 |
4790 |
Liver Carcinoma |
SK-HEP-1 |
- |
- |
- |
- |
Butein at 50 µM might inhibit theNF-kB activity, which is able to involve cell migration and invasion of SK-HEP-1 cells. |
21770460 |
MMP-AC0109 |
NFKBIA |
nuclear factor of kappa light polypeptide gene enhancer in B-cells inhibitor, alpha |
4792 |
Prostate Cancer |
LNCaP |
- |
- |
- |
- |
A significant dose-dependent inhibition in the phosphorylation of IkBalpha protein on treatment of LNCaP cells with butein. |
22114764 |
MMP-AC0109 |
NOS2 |
nitric oxide synthase 2, inducible |
4843 |
Murine monocyte/macrophage line derived from ascitic tumour induced with Abelson leukaemai virus |
Raw264 |
5±2 µM |
- |
- |
- |
suppressed the TNF-a production in LPS-stimulated RAW264 cell. |
21372424 |
MMP-AC0109 |
PARP1 |
poly (ADP-ribose) polymerase 1 |
142 |
Prostate Cancer |
LNCaP |
- |
- |
- |
- |
On treatment of LNCaP cells with butein, they found that there was an increase in the protein expression of the 85 KD fragment of PARP, while there was a decrease in the protein expression of full-size PARP (116 KD) protein. And PARP has several cellular functions including DNA recombination and repair, cellular proliferation, apoptosis in ischemic conditions, and necrotic cell deat. |
22114764 |
MMP-AC0109 |
PLAU |
plasminogen activator, urokinase |
5328 |
Liver Carcinoma |
SK-HEP-1 |
- |
- |
- |
- |
Western blotting analysis indicated that butein decreased the level of uPA in SK-HEP-1 cells. |
21770460 |
MMP-AC0109 |
PTK2 |
PTK2 protein tyrosine kinase 2 |
5747 |
Liver Carcinoma |
SK-HEP-1 |
- |
- |
- |
- |
Western blotting analysis indicated that butein decreased the levels of FAK in SK-HEP-1 cell. |
21770460 |
MMP-AC0109 |
RHOA |
ras homolog family member A |
387 |
Liver Carcinoma |
SK-HEP-1 |
- |
- |
- |
- |
Western blotting analysis indicated that butein decreased the levels of Rho A in SK-HEP-1 cells. |
21770460 |
MMP-AC0109 |
ROCK1 |
Rho-associated, coiled-coil containing protein kinase 1 |
6093 |
Liver Carcinoma |
SK-HEP-1 |
- |
- |
- |
- |
Western blotting analysis indicated that butein decreased the levels of Rho A in SK-HEP-1 cells. |
21770460 |
MMP-AC0109 |
SOS1 |
son of sevenless homolog 1 (Drosophila) |
6654 |
Liver Carcinoma |
SK-HEP-1 |
- |
- |
- |
- |
Western blotting analysis indicated that butein decreased the levels of SOS1 in SK-HEP-1 cells. |
21770460 |
MMP-AC0109 |
VEGFA |
vascular endothelial growth factor A |
7422 |
Liver Carcinoma |
SK-HEP-1 |
- |
- |
- |
- |
Western blotting analysis indicated that butein decreased the levels of SOS1 in SK-HEP-1 cells. |
21770460 |
MMP-AC0109 |
TNF |
tumor necrosis factor |
7124 |
Murine monocyte/macrophage line derived from ascitic tumour induced with Abelson leukaemai virus |
Raw264 |
8±4 µM |
- |
- |
- |
TNF-a suppressive alkaloids also inhibited NO production in RAW264 cell. |
21372424 |