rat neuronal cells |
Cytotoxicity assay |
10 uM |
24 hrs |
Cytotoxicity against rat neuronal cells at 10 uM after 24 hrs |
17276679 |
PP30 |
Function assay |
100 uM |
3 hrs |
Inhibition of human HSP90alpha expressed in yeast PP30 cells co-expressing HSF-lacZ reporter assessed as induction of heat shock response at 100 uM after 3 hrs |
21129982 |
MCF7 |
Function assay |
500 nM |
24 hrs |
Inhibition of Hsp90 in human MCF7 cells assessed as induction of Her2 degradation at 500 nM after 24 hrs by Western blot method |
21861487 |
MCF7 |
Function assay |
500 nM |
24 hrs |
Inhibition of Hsp90 in human MCF7 cells assessed as induction of Raf degradation at 500 nM after 24 hrs by Western blot method |
21861487 |
MCF7 |
Function assay |
500 nM |
24 hrs |
Inhibition of Hsp90 in human MCF7 cells assessed as induction of Akt degradation at 500 nM after 24 hrs by Western blot method |
21861487 |
SKBR3 |
Function assay |
0.5 uM |
18 hrs |
Inhibition of HSP90 in human SKBR3 cells assessed as aggregation of intracellular HER2 at 0.5 uM after 18 hrs by DAPI staining-based immunofluorescence microscopic analysis |
23859777 |
CL1-5 |
Function assay |
2 uM |
16 hrs |
Inhibition of HSP90 in human CL1-5 cells assessed as reduction of total Akt at 2 uM after 16 hrs by Western blotting analysis |
24428777 |
MDA-MB 231 |
Function assay |
0.5 uM |
24 hrs |
Inhibition Hsp90 in human MDA-MB 231 cells assessed as increase in HSP70 protein level at 0.5 uM incubated for 24 hrs by Western blot method |
25277067 |
PC12 |
Function assay |
10 uM |
3 to 16 hrs |
Inhibition of D-aspartate biosynthesis in rat PC12 cells assessed as reduction of intracellular D-aspartate content at 10 uM measured at 3 to 16 hrs by O-phthalaldehyde/N-acetyl-L-cysteine derivatization technique-based HPLC analysis relative to vehicle-t |
26642769 |
PC12 |
Function assay |
10 uM |
6 to 16 hrs |
Inhibition of D-aspartate biosynthesis in rat PC12 cells assessed as reduction of total D-aspartate content at 10 uM measured at 6 to 16 hrs by O-phthalaldehyde/N-acetyl-L-cysteine derivatization technique-based HPLC analysis relative to vehicle-treated c |
26642769 |
PC12 |
Function assay |
up to 10 uM |
24 hrs |
Inhibition of D-aspartate biosynthesis in rat PC12 cells assessed as reduction of D-aspartate level in cell culture medium up to 10 uM after 24 hrs by O-phthalaldehyde/N-acetyl-L-cysteine derivatization technique-based HPLC analysis |
26642769 |
A549 |
Function assay |
5 to 10 uM |
24 hrs |
Inhibition of HSP90alpha in human A549 cells assessed as upregulation of HSP90alpha expression at 5 to 10 uM after 24 hrs by Western blot analysis |
29486954 |
A549 |
Function assay |
5 to 10 uM |
24 hrs |
Inhibition of HSP90beta in human A549 cells assessed as upregulation of HSP90beta expression at 5 to 10 uM after 24 hrs by Western blot analysis |
29486954 |
Jurkat |
Function assay |
1 uM |
|
Inhibition of to HSP90 in FADD deficient human Jurkat cells assessed as RIP protein degradation at 1 uM by Western blot |
18408713 |
SK-BR-3 |
Function assay |
50 mg/kg |
|
Inhibition of oncogene product p185 erbB-2 from human breast cancer cells(SK-BR-3 cells) at 50 mg/kg dose, IC50=0.07μM |
7562911 |
SH-SY5Y |
Neuroprotection assay |
10 nM |
|
Neuroprotection against beta-amyloid peptide 1-42-induced toxicity in retinoic acid-differentiated human SH-SY5Y cells assessed as lactate dehydrogenase release at 10 nM |
19138859 |
MCF7 |
Function assay |
0.5 uM |
|
Inhibition of Hsp90 in human MCF7 cells assessed as Akt degradation at 0.5 uM by Western blot analysis |
21273068 |
MCF7 |
Function assay |
0.5 uM |
|
Inhibition of Hsp90 in human MCF7 cells assessed as Raf degradation at 0.5 uM by Western blot analysis |
21273068 |
MCF7 |
Function assay |
0.5 uM |
|
Inhibition of Hsp90 in human MCF7 cells assessed as Hsp90 degradation at 0.5 uM by Western blot analysis |
21273068 |
MCF7 |
Function assay |
0.5 uM |
|
Inhibition of Hsp90 in human MCF7 cells assessed as Her2 degradation at 0.5 uM by Western blot analysis |
21273068 |
MDA-MB 231 |
Function assay |
0.5 and 5 uM |
|
Inhibition of HSP90 in human MDA-MB 231 cells assessed increase in HSP70 protein levels at 0.5 and 5 uM by Western blot method |
25105924 |
KPL4 |
Function assay |
|
40 hrs |
Inhibition of Hsp90 in human KPL4 cells assessed as depletion of Raf-1 level after 40 hrs, MEC=0.33μM |
18243703 |
KPL4 |
Function assay |
|
40 hrs |
Inhibition of Hsp90 in human KPL4 cells assessed as depletion of ErbB2 level after 40 hrs, MEC=0.11μM |
18243703 |
P19 |
Cytotoxicity assay |
|
18 hrs |
Cytotoxicity against mouse P19 cells after 18 hrs, IC50=0.1μM |
17442565 |
SKBR3 |
Function assay |
|
24 hrs |
Inhibition of Hsp90-mediated HER2 degradation in human SKBR3 cells after 24 hrs by Western blot |
18816111 |
SKBR3 |
Function assay |
|
24 hrs |
Inhibition of Hsp90-mediated Raf degradation in human SKBR3 cells after 24 hrs by Western blot |
18816111 |
HuH7 |
Antiviral assay |
|
3 days |
Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human HuH7 cells assessed as GAPDH RNA or 18S rRNA level after 3 days by qRT-PCR analysis, EC50=0.00025μM |
18936191 |
HuH7 |
Antiviral assay |
|
3 days |
Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human HuH7 cells assessed as GAPDH RNA or 18S rRNA level after 3 days selected with 40 nM HCV-796 and 800 nM boceprevir by qRT-PCR analysis, EC50=0.0012μM |
18936191 |
SKBR3 |
Cytotoxicity assay |
|
72 hrs |
Cytotoxicity against human SKBR3 cells after 72 hrs by celltiter-glo assay, IC50=0.041μM |
19405528 |
A431 |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against human A431 cells after 72 hrs, IC50=0.2μM |
20655237 |
HCT116 |
Antiproliferative assay |
|
4 days |
Antiproliferative activity against human HCT116 cells measured on day 4 by Cell titer-glo assay, EC50=0.03μM |
21420297 |
MCF7 |
Cytotoxicity assay |
|
72 hrs |
Cytotoxicity against human MCF7 cells at 72 hrs by MTS assay, IC50=0.053μM |
22162786 |
SKBR3 |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against estrogen receptor deficient human SKBR3 cells after 72 hrs, IC50=0.0085μM |
23648180 |
MCF7 |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against human MCF7 cells expressing estrogen receptor after 72 hrs, IC50=0.0098μM |
23648180 |
A549 |
Cytotoxicity assay |
|
2 days |
Cytotoxicity against human A549 cells after 2 days by AlamarBlue assay, IC50=0.15μM |
23947794 |
L6 |
Cytotoxicity assay |
|
72 hrs |
Cytotoxicity against rat L6 cells after 72 hrs by Alamar Blue assay, IC50=6μM |
24580531 |
Sf9 |
Function assay |
|
16 hrs |
Displacement of GM-BODIPY from human full length HSP90 alpha expressed in baculovirus-infected Sf9 cells after 16 hrs by fluorescence polarization assay, IC50=0.074μM |
24751441 |
MDA-kb2 |
Function assay |
|
18 hrs |
Inhibition of HSP90 in human MDA-kb2 cells assessed as reduction in glucocorticoid receptor-dependent luciferase expression after 18 hrs by firefly luciferase reporter gene assay, IC50<0.01μM |
24984936 |
MCF7 |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTS/PMS assay, IC50=0.04μM |
25075762 |
MDA-MB-231 |
Cytotoxicity assay |
|
72 hrs |
Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50=0.05μM |
25105924 |
LNCAP |
Cytotoxicity assay |
|
72 hrs |
Cytotoxicity against human LNCAP cells after 72 hrs by MTT assay, IC50=0.43μM |
25105924 |
HUVEC |
Cytotoxicity assay |
|
72 hrs |
Cytotoxicity against HUVEC cells after 72 hrs by MTT assay, IC50=0.019μM |
25277067 |
A431 |
Cytotoxicity assay |
|
72 hrs |
Cytotoxicity against human A431 cells after 72 hrs by MTT assay, IC50=0.04μM |
25277067 |
BGC823 |
Cytotoxicity assay |
|
72 hrs |
Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay, IC50=0.04μM |
25277067 |
HepG2 |
Cytotoxicity assay |
|
72 hrs |
Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, IC50=0.04μM |
25277067 |
MDA-MB-231 |
Cytotoxicity assay |
|
72 hrs |
Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50=0.05μM |
25277067 |
A549 |
Cytotoxicity assay |
|
72 hrs |
Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50=0.097μM |
25277067 |
HL7702 |
Cytotoxicity assay |
|
72 hrs |
Cytotoxicity against human HL7702 cells after 72 hrs by MTT assay, IC50=0.141μM |
25277067 |
SW480 |
Cytotoxicity assay |
|
72 hrs |
Cytotoxicity against human SW480 cells after 72 hrs by MTT assay, IC50=0.31μM |
25277067 |
HeLa |
Cytotoxicity assay |
|
72 hrs |
Cytotoxicity against human HeLa cells after 72 hrs by MTT assay, IC50=0.798μM |
25277067 |
MCF7 |
Cytotoxicity assay |
|
72 hrs |
Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTS/PMS assay, IC50=0.0427μM |
25756299 |
MCF7 |
Function assay |
|
24 hrs |
Inhibition of HSP90 in human MCF7 cells assessed as pAkt degradation at 5 times IC50 after 24 hrs by Western blot analysis |
25756299 |
MCF7 |
Function assay |
|
24 hrs |
Inhibition of HSP90 in human MCF7 cells assessed as Her2 degradation at 5 times IC50 after 24 hrs by Western blot analysis |
25756299 |
MCF7 |
Function assay |
|
24 hrs |
Inhibition of HSP90 in human MCF7 cells assessed as Cdk6 degradation at 5 times IC50 after 24 hrs by Western blot analysis |
25756299 |
MCF7 |
Function assay |
|
24 hrs |
Inhibition of HSP90 in human MCF7 cells assessed as Raf degradation at 5 times IC50 after 24 hrs by Western blot analysis |
25756299 |
MCF7 |
Function assay |
|
24 hrs |
Change in Cdc37 expression in human MCF7 cells at 5 times IC50 after 24 hrs by Western blot analysis |
25756299 |
MCF7 |
Function assay |
|
24 hrs |
Change in p23 expression in human MCF7 cells at 5 times IC50 after 24 hrs by Western blot analysis |
25756299 |
MCF7 |
Function assay |
|
24 hrs |
Inhibition of HSP90 in human MCF7 cells assessed as induction of heat shock response-mediated HSP90 production at 5 times IC50 after 24 hrs by Western blot analysis relative to vehicle-treated control |
25756299 |
MCF7 |
Function assay |
|
24 hrs |
Inhibition of HSP90 in human MCF7 cells assessed as induction of heat shock response-mediated HSP70 production at 5 times IC50 after 24 hrs by Western blot analysis relative to vehicle-treated control |
25756299 |
MCF7 |
Function assay |
|
24 hrs |
Inhibition of HSP90 in human MCF7 cells assessed as induction of heat shock response-mediated HSP27 production at 5 times IC50 after 24 hrs by Western blot analysis relative to vehicle-treated control |
25756299 |
PC12 |
Function assay |
|
24 hrs |
Inhibition of D-aspartate biosynthesis in rat PC12 cells assessed as reduction of intracellular D-aspartate level up to 10 uM after 24 hrs by O-phthalaldehyde/N-acetyl-L-cysteine derivatization technique-based HPLC analysis |
26642769 |
A549 |
Function assay |
|
12 to 24 hrs |
Inhibition of Hsp90 in human A549 cells assessed as decrease in EGFR levels at five times IC50 value after 12 to 24 hrs by Western blot analysis |
26745854 |
A549 |
Function assay |
|
12 to 24 hrs |
Inhibition of Hsp90 in human A549 cells assessed as decrease in Her2 levels at five times IC50 value after 12 to 24 hrs by Western blot analysis |
26745854 |
A549 |
Function assay |
|
12 to 24 hrs |
Inhibition of Hsp90 in human A549 cells assessed as decrease in C-Raf levels at five times IC50 value after 12 to 24 hrs by Western blot analysis |
26745854 |
BA/F3 |
Function assay |
|
48 hrs |
Inhibition of imatinib-resistant BCR-ABL T315I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as decrease in cell viability after 48 hrs by trypan blue exclusion assay, IC50=1μM |
26844689 |
BA/F3 |
Function assay |
|
48 hrs |
Inhibition of imatinib-resistant BCR-ABL E255K mutant (unknown origin) expressed in mouse BA/F3 cells assessed as decrease in cell viability after 48 hrs by trypan blue exclusion assay, IC50=1μM |
26844689 |
BA/F3 |
Function assay |
|
48 hrs |
Inhibition of BCR-ABL (unknown origin) expressed in mouse BA/F3 cells assessed as decrease in cell viability after 48 hrs by trypan blue exclusion assay, IC50=5μM |
26844689 |
MDA-MB-231 |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTS/PMS assay, Activity=0.06μM |
27003516 |
MDA-MB-231 |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay, IC50=0.03μM |
27266997 |
HeLa |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against human HeLa cells after 72 hrs by SRB assay, IC50=0.06μM |
27266997 |
SNU638 |
Anticancer assay |
|
72 hrs |
Anticancer activity against human SNU638 cells measured after 72 hrs by SRB assay, IC50=0.03μM |
27283788 |
Caki1 |
Anticancer assay |
|
72 hrs |
Anticancer activity against human Caki1 cells measured after 72 hrs by SRB assay, IC50=0.056μM |
27283788 |
A549 |
Anticancer assay |
|
72 hrs |
Anticancer activity against human A549 cells measured after 72 hrs by SRB assay, IC50=0.109μM |
27283788 |
MDA-MB-231 |
Anticancer assay |
|
72 hrs |
Anticancer activity against human MDA-MB-231 cells measured after 72 hrs by SRB assay, IC50=0.11μM |
27283788 |
HCT116 |
Anticancer assay |
|
72 hrs |
Anticancer activity against human HCT116 cells measured after 72 hrs by SRB assay, IC50=0.15μM |
27283788 |
SKBR3 |
Antiproliferative assay |
|
1 to 3 days |
Antiproliferative activity against Her2-overexpressing human SKBR3 cells after 1 to 3 days by MTS assay, GI50=0.43μM |
27783977 |
NCI-H1975 |
Antiproliferative assay |
|
1 to 3 days |
Antiproliferative activity against gefitinib-resistant human NCI-H1975 cells after 1 to 3 days by MTS assay, GI50=0.56μM |
27783977 |
RPMI8226 |
Growth inhibition assay |
|
72 hrs |
Growth inhibition of human RPMI8226 cells after 72 hrs by MTS/PMS assay, GI50=0.003μM |
29057043 |
MDA-MB-231 |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay, IC50=0.06μM |
29172085 |
A549 |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against human A549 cells after 72 hrs by SRB assay, IC50=0.1μM |
29172085 |
NCI-H1975 |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against human NCI-H1975 cells after 72 hrs by Cell Titer 96 Aqueous One Solution cell proliferation assay, GI50=0.56μM |
29202402 |
SKBR3 |
Function assay |
|
24 hrs |
Inhibition of HSP90 at N-terminus in human SKBR3 cells assessed as induction of Raf1 protein degradation incubated for 24 hrs by Western blot analysis |
31591016 |
SKBR3 |
Function assay |
|
24 hrs |
Inhibition of HSP90 at N-terminus in human SKBR3 cells assessed as induction of CDK4 protein degradation incubated for 24 hrs by Western blot analysis |
31591016 |
SKBR3 |
Function assay |
|
24 hrs |
Inhibition of HSP90 at N-terminus in human SKBR3 cells assessed as induction of Her2 protein degradation incubated for 24 hrs by Western blot analysis |
31591016 |
SKBR3 |
Function assay |
|
24 hrs |
Inhibition of HSP90 at N-terminus in human SKBR3 cells assessed as induction of AKT protein degradation incubated for 24 hrs by Western blot analysis |
31591016 |
Jurkat |
Function assay |
|
|
Inhibition of TNF-alpha-induced NF-kappaB activation expressed in FADD deficient human Jurkat cells by luciferase reporter gene assay |
18408713 |
HEK293T |
Function assay |
|
|
Inhibition of TNF-alpha-induced NF-kappaB activation expressed in HEK293T cells by luciferase reporter gene assay |
18408713 |
A549 |
Growth inhibition assay |
|
|
Growth inhibition of human A549 cells, GI50=0.064μM |
18243703 |
KPL4 |
Growth inhibition assay |
|
|
Growth inhibition of human KPL4 cells, GI50=0.059μM |
18243703 |
DLD1 |
Growth inhibition assay |
|
|
Growth inhibition of human DLD1 cells, GI50=0.037μM |
18243703 |
HCT116 |
Growth inhibition assay |
|
|
Growth inhibition of human HCT116 cells, GI50=0.021μM |
18243703 |
MCF7 |
Growth inhibition assay |
|
|
Growth inhibition of human MCF7 cells after days by SRB assay, GI50=35.6μM |
17869098 |
LS174T |
Cytotoxicity assay |
|
|
Cytotoxicity against human LS174T cells by MTS assay, IC50=0.45μM |
17034135 |
HEK293 |
Function assay |
|
|
Inhibition of HSP90 expressed in HEK293 cells assessed as effect on Akt1:p27 interaction complexes by EYFP and/or YFP Venus fragment based reporter gene assay |
16680159 |
SKBR-3 |
Function assay |
|
|
Effective concentration for Her-2 degradation in SKBR-3 cells, Concentration=5μM |
15713410 |
MCF-7 |
Function assay |
|
|
Inhibition of steady-state expression of Raf-1 in MCF-7 breast cancer cells, IC50=0.2μM |
10340605 |
MCF-7 |
Function assay |
|
|
Inhibition of steady-state expression of ER in MCF-7 breast cancer cells, IC50=0.06μM |
10340605 |
MCF-7 |
Function assay |
|
|
Inhibition of steady-state expression of HER2 in MCF-7 breast cancer cells, IC50=0.05μM |
10340605 |
SK-BR-3 |
Function assay |
|
|
In vitro inhibition of p185 erbB-2 oncoprotein in human breast cancer SK-BR-3 cells, IC50=0.07μM |
7562912 |
HT-29 cell |
Growth inhibition assay |
|
|
Inhibitory concentration against human colorectal carcinoma HT-29 cell lines, IC50=24.5 nM |
15658879 |
K562 cell |
Growth inhibition assay |
|
|
Inhibitory concentration against human leukemia K562 cell lines, IC50=22.1 nM |
15658879 |
MCF-7 cell |
Growth inhibition assay |
|
|
Inhibitory concentration against human breast cancer MCF-7 cell lines, IC50=6.5 nM |
15658879 |
SW620 cell |
Growth inhibition assay |
|
|
Inhibitory concentration against human colorectal carcinoma SW620 cell lines, IC50=6.2 nM |
15658879 |
A2780 cells |
Proliferation assay |
|
|
Compound was evaluated for antiproliferative activity against human ovarian carcinoma cell line A2780, IC50=3.4 μM |
11514145 |
SH-SY5Y |
Neuroprotection assay |
|
|
Neuroprotection against beta-amyloid peptide 1-42-induced toxicity in human SH-SY5Y cells assessed as lactate dehydrogenase release, EC50=0.04269μM |
19138859 |
MCF7 |
Cytotoxicity assay |
|
|
Cytotoxicity against human MCF7 cells by SRB assay, IC50=9.6μM |
19560353 |
SK-BR-3 |
Antiproliferative assay |
|
|
Antiproliferative activity against human SK-BR-3 cells, IC50=0.0158μM |
19896848 |
MCF7 |
Antiproliferative assay |
|
|
Antiproliferative activity against human MCF7 cells, IC50=0.0161μM |
19896848 |
HCT116 |
Antiproliferative assay |
|
|
Antiproliferative activity against human HCT116 cells by luminescence assay, EC50=0.03μM |
21605975 |
U87 |
Antiproliferative assay |
|
|
Antiproliferative activity against human U87 cells by luminescence assay, EC50=0.089μM |
21605975 |
HCT116 |
Antiproliferative assay |
|
|
Antiproliferative activity against human HCT116 cells, IC50=0.03μM |
21715165 |
NCI-H1975 |
Antiproliferative assay |
|
|
Antiproliferative activity against human NCI-H1975 cells, IC50=0.036μM |
21715165 |
U87MG |
Antiproliferative assay |
|
|
Antiproliferative activity against human U87MG cells, IC50=0.089μM |
21715165 |
HepG2 |
Cytotoxicity assay |
|
|
Cytotoxicity against human HepG2 cells, IC50=0.37μM |
22849774 |
HepG2 |
Cytotoxicity assay |
|
|
Cytotoxicity against human HepG2 cells by MTT assay, IC50=0.3μM |
23656556 |
SKBR3 |
Function assay |
|
|
Inhibition of Hsp90 in human SKBR3 cells, IC50=0.07μM |
26844689 |