Bone marrow cell
|
EC50 |
100 nM
Compound: 1-alpha, 25-(OH)2D3
|
Effect on osteoclast formation in ddY mouse bone marrow cells co cultured with primary osteoclasts after 3 days relative to 1-alpha, 25-(OH)2D3
Effect on osteoclast formation in ddY mouse bone marrow cells co cultured with primary osteoclasts after 3 days relative to 1-alpha, 25-(OH)2D3
|
[PMID: 18539034]
|
Bone marrow cell
|
EC50 |
2 nM
Compound: 1-alpha, 25-(OH)2D3
|
Effect on osteoclast formation in ddY mouse bone marrow cells co cultured with primary osteoclasts after 3 days
Effect on osteoclast formation in ddY mouse bone marrow cells co cultured with primary osteoclasts after 3 days
|
[PMID: 18539034]
|
BXPC-3
|
IC50 |
21.07 μM
Compound: 3; 1,25(OH)2D3
|
Antiproliferative activity against human BxPC3 cells after 24 hrs by MTT assay
Antiproliferative activity against human BxPC3 cells after 24 hrs by MTT assay
|
[PMID: 30193216]
|
Caco-2
|
EC50 |
223.4 nM
Compound: 1,25(OH)2D3
|
Activation of VDR in human Caco2 cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay
Activation of VDR in human Caco2 cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay
|
[PMID: 27070779]
|
Caco-2
|
IC50 |
4.4 μM
Compound: Calcitriol
|
Antipoliferative activity against human Caco2 cells after 48 hrs by MTT assay
Antipoliferative activity against human Caco2 cells after 48 hrs by MTT assay
|
[PMID: 26562542]
|
Caco-2
|
IC50 |
4.46 μM
Compound: Calcitriol
|
Antiproliferative activity against human Caco2 cells after 48 hrs by MTT assay
Antiproliferative activity against human Caco2 cells after 48 hrs by MTT assay
|
[PMID: 29518319]
|
Caco-2
|
EC50 |
515.2 nM
Compound: 1,25(OH)2D3
|
Transactivation of VDR in human Caco2 cells after 24 hrs by luciferase reporter gene assay
Transactivation of VDR in human Caco2 cells after 24 hrs by luciferase reporter gene assay
|
[PMID: 26367019]
|
COS-7
|
EC50 |
50 nM
Compound: 1, 1,25-(OH)2D3
|
Agonist activity at human VDR in COS7 cells assessed as induction of transcriptional transactivation after 24 hrs by mouse osteopontin luciferase reporter gene assay
Agonist activity at human VDR in COS7 cells assessed as induction of transcriptional transactivation after 24 hrs by mouse osteopontin luciferase reporter gene assay
|
[PMID: 17904370]
|
COS-7
|
EC50 |
500 pM
Compound: 1, 1,25-(OH)2D3
|
Induction of transactivation of human VDR responsive gene in COS7 cells by rat osteopontin luciferase reporter gene assay
Induction of transactivation of human VDR responsive gene in COS7 cells by rat osteopontin luciferase reporter gene assay
|
[PMID: 17298045]
|
HaCaT
|
EC50 |
249.7 nM
Compound: 1,25(OH)2D3
|
Activation of VDR in human HaCaT cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay
Activation of VDR in human HaCaT cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay
|
[PMID: 27070779]
|
HaCaT
|
EC50 |
321.5 nM
Compound: 1,25(OH)2D3
|
Transactivation of VDR in human HaCaT cells after 24 hrs by luciferase reporter gene assay
Transactivation of VDR in human HaCaT cells after 24 hrs by luciferase reporter gene assay
|
[PMID: 26367019]
|
HCT-116
|
IC50 |
0.01 nM
Compound: 1b, calcitriol
|
Cytotoxicity against human HCT116 assessed as decrease in cell count after 120 hrs
Cytotoxicity against human HCT116 assessed as decrease in cell count after 120 hrs
|
[PMID: 22926068]
|
HEK293
|
IC50 |
> 10 μM
Compound: 1, 1,25-VD3
|
Antagonist activity at human androgen receptor expressed in HEK293 cells assessed as inhibition of transcriptional activity by luciferase and beta-galactosidase reporter gene assay
Antagonist activity at human androgen receptor expressed in HEK293 cells assessed as inhibition of transcriptional activity by luciferase and beta-galactosidase reporter gene assay
|
[PMID: 23462715]
|
HEK293
|
EC50 |
0.003 μM
Compound: 1, 1,25-VD3
|
Agonist activity at CMX-GAL4 tagged human VDR expressed in HEK293 cells assessed as increase in transcriptional activity by luciferase reporter gene assay
Agonist activity at CMX-GAL4 tagged human VDR expressed in HEK293 cells assessed as increase in transcriptional activity by luciferase reporter gene assay
|
[PMID: 23462715]
|
HEK293
|
IC50 |
0.1 nM
Compound: 1; 1,25(OH)2D3
|
Agonist activity at VDR (unknown origin) expressed in HEK293 cells cotransfected with NCoR assessed as decrease in NCoR recruitment by two-hybrid assay
Agonist activity at VDR (unknown origin) expressed in HEK293 cells cotransfected with NCoR assessed as decrease in NCoR recruitment by two-hybrid assay
|
[PMID: 26613420]
|
HEK293
|
EC50 |
0.12 nM
Compound: 1; 1,25(OH)2D3
|
Agonist activity at VDR in human HEK293 cells assessed as transcriptional activity after 16 to 24 hrs by luciferase reporter gene assay
Agonist activity at VDR in human HEK293 cells assessed as transcriptional activity after 16 to 24 hrs by luciferase reporter gene assay
|
[PMID: 26613420]
|
HEK293
|
EC50 |
0.6 nM
Compound: 1; 1,25(OH)2D3
|
Agonist activity at VDR (unknown origin) expressed in HEK293 cells cotransfected with RXRalpha assessed as RXRalpha recruitment by two-hybrid assay
Agonist activity at VDR (unknown origin) expressed in HEK293 cells cotransfected with RXRalpha assessed as RXRalpha recruitment by two-hybrid assay
|
[PMID: 26613420]
|
HEK293
|
EC50 |
1 nM
Compound: 1, 1,25-(OH)2D3
|
Agonist activity at human VDR in HEK293 cells assessed as induction of transcriptional transactivation after 24 hrs by mouse osteopontin luciferase reporter gene assay
Agonist activity at human VDR in HEK293 cells assessed as induction of transcriptional transactivation after 24 hrs by mouse osteopontin luciferase reporter gene assay
|
[PMID: 17904370]
|
HEK293
|
EC50 |
7.28 x 10 -10 M
Compound: 1,25(OH)2D3, Calcitriol
|
Antiproliferative activity against NHEK cells incubated for 24 hrs by [3H]thymidine incorporation assay
Antiproliferative activity against NHEK cells incubated for 24 hrs by [3H]thymidine incorporation assay
|
[PMID: 22404326]
|
HeLa
|
EC50 |
1 nM
Compound: calcitriol, [1alpha,25(OH)2D3]
|
Transactivation of GAL4-fused VDR ligand binding domain expressed in human HeLa cells after 16 hrs by luciferase reporter gene assay
Transactivation of GAL4-fused VDR ligand binding domain expressed in human HeLa cells after 16 hrs by luciferase reporter gene assay
|
[PMID: 22957834]
|
HeLa
|
EC50 |
2.5 nM
Compound: calcitriol, [1alpha,25(OH)2D3]
|
Transactivation of full length human VDR expressed in human HeLa cells assessed as increase in CYP24 transcription after 18 hrs by luciferase reporter gene assay
Transactivation of full length human VDR expressed in human HeLa cells assessed as increase in CYP24 transcription after 18 hrs by luciferase reporter gene assay
|
[PMID: 22957834]
|
HepG2
|
IC50 |
> 50 μM
Compound: Calcitriol
|
Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
|
[PMID: 29518319]
|
HepG2
|
IC50 |
> 50 μM
Compound: Calcitriol
|
Antipoliferative activity against human HepG2 cells after 48 hrs by MTT assay
Antipoliferative activity against human HepG2 cells after 48 hrs by MTT assay
|
[PMID: 26562542]
|
HL-60
|
EC50 |
0.009 μM
Compound: Calcitriol
|
Agonist activity at vitamin D3 receptor in human HL-60 cells assessed as induction of cell differentiation after 96 hrs by NBT dye-based microscopic analysis
Agonist activity at vitamin D3 receptor in human HL-60 cells assessed as induction of cell differentiation after 96 hrs by NBT dye-based microscopic analysis
|
[PMID: 26562542]
|
HL-60
|
IC50 |
0.05 μM
Compound: 1, 1,25(OH)2D3, calcitriol
|
Induction of cell differentiation of human HL60 cells incubated for 144 hrs by Wst-1 dye based assay
Induction of cell differentiation of human HL60 cells incubated for 144 hrs by Wst-1 dye based assay
|
[PMID: 25180926]
|
HL-60
|
EC50 |
17.9 nM
Compound: Calcitriol
|
Induction of human HL60 cell differentiation after 4 days by NBT reduction assay
Induction of human HL60 cell differentiation after 4 days by NBT reduction assay
|
[PMID: 24035340]
|
HL-60
|
ED50 |
2 nM
Compound: 1, calcitriol, 1alpha,25-(OH)2D3
|
Induction of differentiation of human HL60 promyelocytes to monocytes after 4 days by nitro blue tetrazolium reduction assay
Induction of differentiation of human HL60 promyelocytes to monocytes after 4 days by nitro blue tetrazolium reduction assay
|
[PMID: 26206427]
|
HL-60
|
ED50 |
2 nM
Compound: 1, calcitriol, 1alpha,25-(OH)2D3
|
Induction of human HL60 cell differentiation after 4 days by NBT reduction assay
Induction of human HL60 cell differentiation after 4 days by NBT reduction assay
|
[PMID: 22490010]
|
HL-60
|
EC50 |
2 nM
Compound: 1, 1alpha,25-(OH)2D3, calcitriol
|
Induction of differentiation of human HL60 promyelocytes into monocytes after 4 days by NBT reduction assay
Induction of differentiation of human HL60 promyelocytes into monocytes after 4 days by NBT reduction assay
|
[PMID: 19819702]
|
HL-60
|
EC50 |
2 nM
Compound: 1, 1alpha,25(OH)2D3, calcitriol
|
Induction of differentiation of human HL-60 cells promyelocytes to monocytes after 4 days by NBT reduction assay
Induction of differentiation of human HL-60 cells promyelocytes to monocytes after 4 days by NBT reduction assay
|
[PMID: 18722130]
|
HL-60
|
EC50 |
2 nM
Compound: 1, calcitriol
|
Induction of differention of human HL60 cells into monocytes by NBT reduction assay
Induction of differention of human HL60 cells into monocytes by NBT reduction assay
|
[PMID: 17960924]
|
HL-60
|
EC50 |
2150 pM
Compound: 1, 1,25-(OH)2D3
|
Induction of human HL60 cell differentiation to monocytes by NBT reduction assay
Induction of human HL60 cell differentiation to monocytes by NBT reduction assay
|
[PMID: 17298045]
|
HL-60
|
EC50 |
3 nM
Compound: 1, Calcitriol, 1alpha,25-(OH)2D3
|
Induction of human HL60 cell differentiation after 4 days by nitro blue tetrazolium reduction assay
Induction of human HL60 cell differentiation after 4 days by nitro blue tetrazolium reduction assay
|
[PMID: 22018918]
|
HL-60
|
ED50 |
3 nM
Compound: 1; calcitriol; 1alpha,25-(OH)2D3
|
Induction of human HL60 cell differentiation assessed as differentiation from promyelocytes to monocytes by NBT assay
Induction of human HL60 cell differentiation assessed as differentiation from promyelocytes to monocytes by NBT assay
|
[PMID: 26630444]
|
HL-60
|
ED50 |
3 nM
Compound: 1, 1alpha,25-(OH)2D3,calcitriol
|
Induction of human HL60 cell differentiation into monocytes after 4 days by NBT reduction assay
Induction of human HL60 cell differentiation into monocytes after 4 days by NBT reduction assay
|
[PMID: 19402630]
|
HL-60
|
EC50 |
3 nM
Compound: 1, calcitriol
|
Induction of cell differentiation of human HL60 cells to monocytes by NBT reduction assay
Induction of cell differentiation of human HL60 cells to monocytes by NBT reduction assay
|
[PMID: 19167893]
|
HN12
|
IC50 |
4.68 nM
Compound: 1b, calcitriol
|
Cytotoxicity against human HN12 assessed as decrease in cell count after 120 hrs
Cytotoxicity against human HN12 assessed as decrease in cell count after 120 hrs
|
[PMID: 22926068]
|
HN12
|
IC50 |
553 nM
Compound: calcitriol
|
Antiproliferative activity against human HN12 cells assessed as decrease in cell number after 72 hrs by WST assay
Antiproliferative activity against human HN12 cells assessed as decrease in cell number after 72 hrs by WST assay
|
[PMID: 24900339]
|
HOS
|
EC50 |
0.01 nM
Compound: 1alpha,25(OH)2D3
|
Activity at human VDR expressed in human HOS cells transfected with pGL3-hOc, pCDNA-hVDR and phRL-TK assessed as assessed as transcriptional activation measured 24 hrs post infection by luciferase reporter gene assay
Activity at human VDR expressed in human HOS cells transfected with pGL3-hOc, pCDNA-hVDR and phRL-TK assessed as assessed as transcriptional activation measured 24 hrs post infection by luciferase reporter gene assay
|
[PMID: 21889334]
|
HOS
|
EC50 |
0.011 nM
Compound: 1-alpha,25(OH)2D3
|
Agonist activity at human VDR expressed in HOS cells co-expressing human RXR by Dual-Glo luciferase reporter gene assay
Agonist activity at human VDR expressed in HOS cells co-expressing human RXR by Dual-Glo luciferase reporter gene assay
|
[PMID: 30446437]
|
Huh-7
|
EC50 |
0.0003 μM
Compound: 1alpha,25-dihydroxyvitamin D3
|
Agonist activity at VDR expressed in human HuH7 cells after 24 hrs by pDR3-luciferase reporter gene assay
Agonist activity at VDR expressed in human HuH7 cells after 24 hrs by pDR3-luciferase reporter gene assay
|
[PMID: 27145071]
|
Jurkat
|
EC50 |
3.936 nM
Compound: 1,25(OH)2D3
|
Activation of VDR in human Jurkat cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay
Activation of VDR in human Jurkat cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay
|
[PMID: 27070779]
|
L02
|
IC50 |
0.67 μM
Compound: Calcitriol
|
Antiproliferative activity against human L02 cells after 48 hrs by MTT assay
Antiproliferative activity against human L02 cells after 48 hrs by MTT assay
|
[PMID: 29518319]
|
L02
|
IC50 |
0.67 μM
Compound: Calcitriol
|
Cytotoxicity against human L02 cells after 48 hrs by MTT assay
Cytotoxicity against human L02 cells after 48 hrs by MTT assay
|
[PMID: 26562542]
|
L02
|
IC50 |
48 μM
Compound: 1; 1,25(OH)2D3
|
Cytotoxicity against human LO2 cells assessed as reduction in cell viability after 24 hrs by MTT assay
Cytotoxicity against human LO2 cells assessed as reduction in cell viability after 24 hrs by MTT assay
|
[PMID: 30579121]
|
MCF7
|
IC50 |
> 50 μM
Compound: 3; 1,25(OH)2D3
|
Antiproliferative activity against human MCF7 cells expressing VDR siRNA assessed as reduction in BrdU incorporation after 16 hrs by ELISA
Antiproliferative activity against human MCF7 cells expressing VDR siRNA assessed as reduction in BrdU incorporation after 16 hrs by ELISA
|
[PMID: 30193216]
|
MCF7
|
IC50 |
11.1 μM
Compound: 1; 1,25(OH)2D3
|
Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay
Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay
|
[PMID: 30579121]
|
MCF7
|
IC50 |
11.43 μM
Compound: 3; 1,25(OH)2D3
|
Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay
Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay
|
[PMID: 30193216]
|
MCF7
|
IC50 |
12.5 μM
Compound: 1alpha,25-dihydroxyvitamin D3
|
Antiproliferative activity against human MCF7 cells assessed as inhibition of proliferation after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of proliferation after 72 hrs by MTT assay
|
[PMID: 25127149]
|
MCF7
|
EC50 |
3.28 nM
Compound: 1, 1alpha,25-(OH)2D3, 1,25D, calcitriol
|
Agonist activity at VDR in human MCF7 cells assessed as transcription of CYP24A1 gene after 24 hrs by luciferase reporter gene assay
Agonist activity at VDR in human MCF7 cells assessed as transcription of CYP24A1 gene after 24 hrs by luciferase reporter gene assay
|
[PMID: 22989379]
|
MCF7
|
EC50 |
5.2 x 10 -2 μM
Compound: 1
|
Antiproliferative activity against human MCF7 cells after 72 hrs by [3H]thymidine incorporation assay
Antiproliferative activity against human MCF7 cells after 72 hrs by [3H]thymidine incorporation assay
|
[PMID: 19739672]
|
MCF7
|
EC50 |
5.5 nM
Compound: 1alpha,25(OH)2D3
|
Agonist activity at zebrafish gal4-VDR LBD expressed in human MCF7 cells by luciferase reporter gene based transactivation assay
Agonist activity at zebrafish gal4-VDR LBD expressed in human MCF7 cells by luciferase reporter gene based transactivation assay
|
[PMID: 22180837]
|
MCF7
|
IC50 |
5.59 μM
Compound: Calcitriol
|
Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay
|
[PMID: 29518319]
|
MCF7
|
IC50 |
5.6 μM
Compound: Calcitriol
|
Antipoliferative activity against human MCF7 cells after 48 hrs by MTT assay
Antipoliferative activity against human MCF7 cells after 48 hrs by MTT assay
|
[PMID: 26562542]
|
Medulloblastoma cell
|
GI50 |
|
Antiproliferative activity against medulloblastoma cells derived from conditional patched knockout mouse after 48 hrs by [3H]-thymidine incorporation assay
Antiproliferative activity against medulloblastoma cells derived from conditional patched knockout mouse after 48 hrs by [3H]-thymidine incorporation assay
|
[PMID: 30471551]
|
PBMC
|
IC50 |
|
Inhibition of LPS-induced IL12/23p40 production in human PBMC after 24 hrs by ELISA
Inhibition of LPS-induced IL12/23p40 production in human PBMC after 24 hrs by ELISA
|
[PMID: 19309155]
|
PBMC
|
IC50 |
1.2 x 10 -2 μM
Compound: 1
|
Inhibition of LPS-induced IL6 production in human PBMC after 24 hrs by ELISA
Inhibition of LPS-induced IL6 production in human PBMC after 24 hrs by ELISA
|
[PMID: 19309155]
|
PBMC
|
IC50 |
|
Inhibition of LPS-induced TNFalpha production in human PBMC after 24 hrs by ELISA
Inhibition of LPS-induced TNFalpha production in human PBMC after 24 hrs by ELISA
|
[PMID: 19309155]
|
PBMC
|
IC50 |
|
Inhibition of IFN-gamma production in human PBMC after 5 days by ELISA-based mixed lymphocyte reaction assay
Inhibition of IFN-gamma production in human PBMC after 5 days by ELISA-based mixed lymphocyte reaction assay
|
[PMID: 19309155]
|
PC-3
|
IC50 |
17.2 μM
Compound: Calcitriol
|
Antipoliferative activity against human PC3 cells after 48 hrs by MTT assay
Antipoliferative activity against human PC3 cells after 48 hrs by MTT assay
|
[PMID: 26562542]
|
PC-3
|
IC50 |
17.25 μM
Compound: Calcitriol
|
Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay
Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay
|
[PMID: 29518319]
|
PC-3
|
IC50 |
9.53 μM
Compound: 3; 1,25(OH)2D3
|
Antiproliferative activity against human PC3 cells after 24 hrs by MTT assay
Antiproliferative activity against human PC3 cells after 24 hrs by MTT assay
|
[PMID: 30193216]
|
SW480
|
IC50 |
|
Anticancer activity against human SW480 cells assessed as reduction in cell proliferation incubated for 2 days by CCK-8 assay
Anticancer activity against human SW480 cells assessed as reduction in cell proliferation incubated for 2 days by CCK-8 assay
|
[PMID: 33445154]
|
T47D
|
IC50 |
1.3 nM
Compound: calcitriol
|
Antiproliferative activity against human T47D cells assessed as decrease in cell number after 72 hrs by WST assay
Antiproliferative activity against human T47D cells assessed as decrease in cell number after 72 hrs by WST assay
|
[PMID: 24900339]
|
THP-1
|
EC50 |
|
Activation of VDR in human THP1 cells assessed as increase in 25-hydroxyvitamin D-24-hydroxylase mRNA expression by RT-PCR
Activation of VDR in human THP1 cells assessed as increase in 25-hydroxyvitamin D-24-hydroxylase mRNA expression by RT-PCR
|
[PMID: 19309155]
|
THP-1
|
EC50 |
|
Activation of VDR in human THP1 cells assessed as increase in cathelicidin antimicrobial peptide mRNA expression by RT-PCR
Activation of VDR in human THP1 cells assessed as increase in cathelicidin antimicrobial peptide mRNA expression by RT-PCR
|
[PMID: 19309155]
|