Sf9 cells |
Function assay |
|
|
|
Inhibition of His-tagged bovine PI3K expressed in Sf9 cells, IC50=10 μM. |
10998351 |
HeLa cells |
Binding affinity assay |
|
|
|
Binding affinity for PI3-kinase isolated from HeLa cells, Ki=6 μM |
15658870 |
HeLa cells |
Function assay |
|
|
|
Inhibition of mTOR protein isolated from HeLa cells, IC50=2.5 μM. |
15658870 |
HeLa (human carcinoma) cells. |
Function assay |
|
|
|
In vitro inhibition of DNA-dependent protein kinase(DNA-PK) from HeLa (human carcinoma) cells, IC50=1.4 μM. |
15658870 |
human PC3 cells |
Proliferation assay |
25 μM |
120 h |
|
Antiproliferative activity against human PC3 cells at 25 uM after 120 hrs by MTT assay relative to DMSO |
16680159 |
human BJ cells |
Function assay |
25 μM |
2 h |
|
Activation of Akt phosphorylation at Thr308 in PDGF-stimulated serum starved human BJ cells at 25 uM treated 2 hrs before PDGF challenge by immunoblotting |
16767085 |
human BJ cells |
Function assay |
25 μM |
2 h |
|
Inhibition of PI3K signaling in PDGF-stimulated serum starved human BJ cells transfected with plasmid EGFP/PH domain of Akt assessed as suppression of PH-EGFP redistribution to plasma membrane at 25 uM treated 2 hrs before PDGF challenge by confocal microscopy |
16767085 |
mouse mast cells |
Function assay |
20 μM |
|
|
Inhibition of SCF-induced PKB/Akt phosphorylation in mouse mast cells at 20 μM |
16789742 |
THP1 cells |
Function assay |
|
|
|
Inhibition of MCP1-induced chemotaxis of THP1 cells, IC50=37 μM. |
16789742 |
mouse Raw264 macrophage |
Function assay |
|
|
|
Inhibition of C5a-mediated PKB/Akt phosphorylation in mouse Raw264 macrophage, IC50=10 μM. |
16789742 |
THP1 cells |
Function assay |
|
|
|
Inhibition of MCP1-induced PKB/Akt phosphorylation in THP1 cells, IC50=1.65 μM. |
16789742 |
THP1 cells |
Function assay |
|
|
|
Inhibition of SCF1-induced PKB/Akt phosphorylation in THP1 cells, IC50=1.01 μM. |
16789742 |
human A375 cells |
Proliferation assay |
|
46 h |
|
Antiproliferative activity against human A375 cells after 46 hrs, IC50=8.4 μM. |
17049248 |
HeLa cells |
Function assay |
|
|
|
Inhibition of AX-7503 binding to recombinant Plk3 expressed in HeLa cells by Western blot, IC5=3 μM. |
17135248 |
human SW480 cells |
Function assay |
20 μM |
24 h |
|
Decrease in survivin expression in human SW480 cells at 20 uM after 24 hrs by immunoblot analysis |
17472962 |
human A375 cells |
Proliferation assay |
|
|
|
Inhibition of serum-induced proliferation of human A375 cells, IC50=8.4 μM. |
17601739 |
human A2780 cells |
Apoptosis assay |
2 μM |
12 h |
|
Induction of apoptosis in cisplatin-resistant human A2780 cells assessed as decrease in phosphorylated Akt level at 2 uM after 12 hrs by immunoblot analysis. |
17684018 |
human H4 cells |
Function assay |
|
2 h |
|
Decrease in FYVE-RFP+ vesicle intensity per cell in human H4 cells after 2 hrs relative to control |
18024584 |
Sf9 cells |
Function assay |
|
|
|
Inhibition of CK2 expressed in Sf9 cells, IC50=6.9 μM. |
18321716 |
rat RBL2H3 cells |
Function assay |
|
|
|
Inhibition of A23187-induced degranulation in rat RBL2H3 cells |
18328716 |
human U87MG cells |
Function assay |
|
|
|
Inhibition of GSK3-beta in human U87MG cells by ELISA, IC50=8.1 μM. |
18345609 |
human H460 cells |
Function assay |
30 μM |
|
|
Inhibition of PI3K in human H460 cells assessed as Akt phosphorylation at Ser 473 up to 30 uM |
18501601 |
human U251HRE cells |
Function assay |
|
|
|
Inhibition of hypoxia-induced HIF1 activation in human U251HRE cells by cell based reporter gene assay |
18501601 |
human 184B5 cells |
Cytotoxic assay |
|
|
|
Cytotoxicity against human 184B5 cells by SRB assay, GI50=39.37 μM. |
18691894 |
human MDA-MB-468 cells |
Cytotoxic assay |
|
|
|
Cytotoxicity against human MDA-MB-468 cells by SRB assay, IC50=10.4 μM. |
18691894 |
human MDA-MB-468 cells |
Cytotoxic assay |
|
|
|
Cytotoxicity against human MDA-MB-468 cells in presence of 10 uM chloroquine by SRB assay, GI50=8.2 μM. |
18691894 |
MDA-MB-231 cells |
Cytotoxic assay |
|
|
|
Cytotoxicity against human MDA-MB-231 cells by SRB assay, GI50=6.71 μM. |
18691894 |
human MDA-MB-468 cells |
Cytotoxic assay |
|
|
|
Cytotoxicity against human MDA-MB-468 cells in presence of 20 uM chloroquine by SRB assay, IC50=4.76 μM. |
18691894 |
human MDA-MB-231 cells |
Cytotoxic assay |
|
|
|
Cytotoxicity against human MDA-MB-231 cells in presence of 10 uM chloroquine by SRB assay, GI50=4.35 μM. |
18691894 |
human MDA-MB-231 cells |
Cytotoxic assay |
|
|
|
Cytotoxicity against human MDA-MB-231 cells in presence of 20 μM chloroquine by SRB assay, GI=3.32 μM. |
18691894 |
human MCF7 cells |
Cytotoxic assay |
|
|
|
Cytotoxicity against human MCF7 cells by SRB assay, GI=3.16 μM. |
18691894 |
human MCF7 cells |
Cytotoxic assay |
|
|
|
Cytotoxicity against human MCF7 cells in presence of 10 uM chloroquine by SRB assay, GI50=3.08 μM. |
18691894 |
human MCF7 cells |
Cytotoxic assay |
|
|
|
Cytotoxicity against human MCF7 cells in presence of 20 μM chloroquine by SRB assay, GI50=2.63 μM. |
18691894 |
Sf21 cells |
Function assay |
|
|
|
Inhibition of mouse recombinant PI3Kalpha expressed in baculovirus-infected Sf21 cells, IC50=0.5 μM. |
19748269 |
Sf9 cells |
fluorescent polarization assay |
|
|
|
Inhibition of human PI3Kgamma expressed in Sf9 cells by fluorescent polarization assay |
21121631 |
Sf9 cells |
Fluorescent polarization assay |
|
|
|
Inhibition of human PI3Kalpha expressed in Sf9 cells by fluorescent polarization assay, IC50=0.55 μM. |
21121631 |
human IGROV1 cells |
Function assay |
|
24 h |
|
Cell cycle arrest in human IGROV1 cells assessed as accumulation at G1 phase at 5 fold IC50 after 24 hrs by flow cytometry |
21216151 |
human IGROV1 cells |
Function assay |
|
24 h |
|
Cell cycle arrest in human IGROV1 cells assessed as accumulation at G1 phase at 1 fold IC50 after 24 hrs by flow cytometry |
21216151 |
human IGROV1 cells |
Function assay |
|
24/48 h |
|
Inhibition of PI3K/Akt in human IGROV1 cells assessed as decrease in cyclin D1 level at 1 to 5 times IC50 after 24 to 48 hrs by Western blot analysis |
21216151 |
human IGROV1 cells |
Function assay |
|
24/48 h |
|
Inhibition of PI3K/Akt in human IGROV1 cells assessed as decrease in phosphorylated AKT level at 1 to 5 times IC50 after 24 to 48 hrs by Western blot analysis |
21216151 |
human HCT116 cells |
Cytotoxic assay |
|
72 h |
|
Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50=56.01 μM. |
21945250 |
human KB cells |
Cytotoxic assay |
|
72 h |
|
Cytotoxicity against human KB cells after 72 hrs by MTT assay, IC50=44.76 μM. |
21945250 |
HUVEC |
Function assay |
10-25 μM |
30 min |
|
Inhibition of TNFalpha-stimulated human ICAM-1 promoter activity expressed in HUVEC assessed as beta-galactosidase activity at 10 to 25 uM pretreated for 30 mins before TNFalpha challenge measured after 5 hrs by luciferase reporter gene assay |
22026410 |
HUVEC |
Function assay |
10-25 μM |
16 h |
|
Inhibition of TNFalpha-stimulated ICAM-1 mRNA expression in HUVEC at 10 to 25 uM pretreated for 16 hrs before TNFalpha challenge measured after 6 hrs by RT-PCR analysis |
22026410 |
human HCT116 cells |
Function assay |
10 μM |
|
|
Inhibition of Akt expression in human HCT116 cells at 10 uM by immunoblot analysis |
22212721 |
human HCT116 cells |
Function assay |
10 μM |
|
|
Inhibition of PI3Kalpha H1047R mutant in human HCT116 cells assessed as inhibition of Akt Ser473 phosphorylation at 10 uM by immunoblot analysis |
22212721 |
human HCT116 cells |
Function assay |
10 μM |
|
|
Inhibition of PI3Kalpha in human HCT116 cells assessed as inhibition of Akt Ser473 phosphorylation at 10 uM by immunoblot analysis |
22212721 |
human HCT116 cells |
Function assay |
10 μM |
10 min |
|
Inhibition of PI3Kalpha H1047R mutant in human HCT116 cells using [32P]ATP at 10 uM after 10 mins |
22212721 |
human HCT116 cells |
Function assay |
10 μM |
10 min |
|
Inhibition of PI3Kalpha in human HCT116 cells using [32P]ATP at 10 uM after 10 mins |
22212721 |
human HCT116 cells |
Growth inhibition assay |
|
48 h |
|
Growth inhibition of human HCT116 cells overexpressing PI3Kalpha after 48 hrs by MTT assay, IC50=6.7 μM. |
22212721 |
human HCT116 cells |
Growth inhibition assay |
|
48 h |
|
Growth inhibition of human HCT116 cells after 48 hrs by MTT assay, IC50=5.8 μM. |
22212721 |
human HCT116 cells |
Growth inhibition assay |
|
48 h |
|
Growth inhibition of human HCT116 cells overexpressing PI3Kalpha H1047R mutant after 48 hrs by MTT assay, IC50=5.3 μM |
22212721 |
human A549 cells |
Cytotoxic assay |
|
72 h |
|
Cytotoxicity against human A549 cells after 72 hrs by MTT assay |
22480851 |
human PC3 cells |
Cytotoxic assay |
|
72 h |
|
Cytotoxicity against human PC3 cells after 72 hrs by MTT assay, IC50=61.35 μM. |
22480851 |
human HL60 cells |
Cytotoxic assay |
|
72 h |
|
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay, IC50=9.94 μM. |
22480851 |
Sf21 cells |
Function assay |
|
|
|
Inhibition of mouse wild type PI3Kalpha expressed in Sf21 cells co-expressing N-terminal His-tagged human p85a using L-alpha-phosphatidylinositol substrate by TLC based phosphor imaging, IC50=0.5 μM |
22520630 |
HEK293 cells |
Function assay |
|
1.5 h |
|
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting |
22537153 |
human H1299 cells |
Function assay |
0.1-30 μM |
24 h |
|
Induction of JNK-mediated CHOP expression in human H1299 cells at 0.1 to 30 uM after 24 hrs by Western blot analysis |
22622069 |
human H1299 cells |
Function assay |
0.1-30 μM |
24 h |
|
Induction of DR5 expression in human H1299 cells at 0.1 to 30 uM after 24 hrs by Western blot analysis |
22622069 |
human H1299 cells |
Function assay |
0.1-30 μM |
24 h |
|
Down regulation of cIAP2 expression in human H1299 cells at 0.1 to 30 uM after 24 hrs by Western blot analysis in presence of 100 ug/ml TRAIL and PI3K inhibitor LY294002 |
22622069 |
human H1299 cells |
Function assay |
0.1-30 μM |
24 h |
|
Down regulation of cIAP2 expression in human H1299 cells at 0.1 to 30 uM after 24 hrs by Western blot analysis |
22622069 |
MDA-MB-231 cells |
Cell invasion assay |
|
24 h |
|
Inhibition of epithelial growth factor-induced cell migration of human MDA-MB-231 cells pre-incubated for 24 hrs by cell invasion assay, IC50=0.38 μM. |
22804108 |
human LNCAP cells |
Function assay |
0.1-30 μM |
24 h |
|
Downregulation of survivin expression in human LNCAP cells at 0.1 to 30 uM after 24 hrs by Western blot analysis |
22832316 |
human LNCAP cells |
Function assay |
0.1-30 μM |
30 min |
|
Inhibition of Akt phosphorylation in human LNCAP cells at 0.1 to 30 uM after 30 mins by Western blot analysis |
22832316 |
human PC3 cells |
Function assay |
50 μM |
8 h |
|
Induction of p21 protein expression in human PC3 cells at 50 uM incubated for 8 hrs by Western blotting relative to untreated control |
22998472 |
human BT474 cell |
Proliferation assay |
|
72 h |
|
Inhibition of human BT474 cell proliferation after 72 hrs by spectrophotometric analysis, IC50=20.7 μM. |
23410005 |
human PC3 cell |
Proliferation assay |
|
72 h |
|
Inhibition of human PC3 cell proliferation after 72 hrs by spectrophotometric analysis, IC50=12.1 μM. |
23410005 |
human PC3 cells |
Function assay |
|
30 min |
|
Inhibition of PI3K in human PC3 cells assessed as decrease in AKT phosphorylation at serine 473 after 30 mins by ELISA, IC50=1.3μM. |
23410005 |
human MGC803 cells |
Function assay |
25 μM |
48 h |
|
Cell cycle arrest in human MGC803 cells assessed as accumulation at G2/M phase at 25 uM after 48 hrs using propidium iodide staining after 48 hrs by flow cytometer relative to control |
24119869 |
mouse RAW264.7 cells |
Function assay |
25 μM |
20 h |
|
Inhibition of PI3K/AKT in mouse RAW264.7 cells assessed as inhibition of LPS-induced iNOS protein expression at 25 μM after 20 hrs by Western blot analysis |
24299616 |
human A549 cells |
Proliferation assay |
|
72 h |
|
Antiproliferative activity against human A549 cells assessed as inhibition of absorbance after 72 hrs by MTT assay, IC50=82.32 μM. |
25693787 |
human HuH7 cells |
Proliferation assay |
|
72 h |
|
Antiproliferative activity against human HuH7 cells assessed as inhibition of absorbance after 72 hrs by MTT assay, IC50=67.18 μM. |
25693787 |
human HCT116 cells |
Proliferation assay |
|
72 h |
|
Antiproliferative activity against human HCT116 cells assessed as inhibition of absorbance after 72 hrs by MTT assay, IC50=51.82 μM. |
25693787 |
human HL60 cells |
Proliferation assay |
|
72 h |
|
Antiproliferative activity against human HL60 cells assessed as inhibition of absorbance after 72 hrs by MTT assay, IC50=18.43 μM. |
25693787 |
Sf9 cells |
Function assay |
|
|
|
Inhibition of His-tagged human CK2 expressed in Sf9 cells, IC50 = 6.9 μM. |
10998351 |
HeLa cells |
Function assay |
|
|
|
In vitro inhibition of DNA-dependent protein kinase(DNA-PK) from HeLa (human carcinoma) cells., IC50 = 1.4 μM. |
12941339 |
HeLa cells |
Function assay |
|
|
|
Inhibition of DNA dependent protein kinase isolated from HeLa cells, IC50 = 1.5 μM. |
15658870 |
Sf21 cells |
Function assay |
|
|
|
Inhibition of human recombinant PI3Kbeta expressed in baculovirus-infected Sf21 cells, IC50 = 0.9 μM. |
19748269 |
Sf21 cells |
Function assay |
|
|
|
Inhibition of bovine recombinant PI3Kgamma expressed in baculovirus-infected Sf21 cells, IC50 = 7 μM. |
19748269 |
HeLa cells |
Function assay |
|
|
|
Activity at PI3K in human HeLa cells by ELISA, EC50 = 1.5 μM. |
20092323 |
Sf21 cells |
Function assay |
|
|
|
Inhibition of PI3Kdelta expressed in cells co-expressing N-terminal His-tagged human p85a using L-alpha-phosphatidylinositol substrate by TLC based phosphor imaging, IC50 = 0.57 μM. |
22520630 |
Sf21 cells |
Function assay |
|
|
|
Inhibition of human wild type PI3Kbeta expressed in Sf21 cells co-expressing N-terminal His-tagged human p85a using L-alpha-phosphatidylinositol substrate by TLC based phosphor imaging, IC50 = 0.97 μM. |
22520630 |
HL60 cells |
Antiproliferative assay |
|
3 days |
|
Antiproliferative activity against human HL60 cells measured after 3 days by MTS assay, IC50 = 14 μM. |
26945110 |
U937 cells |
Antiproliferative assay |
|
3 days |
|
Antiproliferative activity against human U937 cells measured after 3 days by MTS assay, IC50 = 14 μM. |
26945110 |
Jurkat cells |
Antiproliferative assay |
|
3 days |
|
Antiproliferative activity against human Jurkat cells measured after 3 days by MTS assay, IC50 = 22 μM. |
26945110 |
K562 cells |
Antiproliferative assay |
|
3 days |
|
Antiproliferative activity against human K562 cells measured after 3 days by MTS assay, IC50 = 38 μM. |
26945110 |
U266 cells |
Antiproliferative assay |
|
3 days |
|
Antiproliferative activity against human U266 cells measured after 3 days by MTS assay, IC50 = 46 μM. |
26945110 |
MDA-MB-231 cells |
Antimigratory assay |
|
24 hrs |
|
Antimigratory activity against EGF induced chemotaxis in human MDA-MB-231 cells preincubated for 24 hrs followed by EGF addition for 3.5 hrs by light microscopy, IC50 = 0.38 μM. |
27598237 |
MDA-MB-231 cells |
Antiinvasive assay |
|
3.5 hrs |
|
Antiinvasive activity in human MDA-MB-231 cells assessed as inhibition of EGF-induced cell invasion after 3.5 hrs, IC50 = 0.38 μM. |
28009521 |
HEK293T cells |
Function assay |
|
1 hr |
|
Inhibition of immobilized N-LY294002 bead binding to PI3Kbeta (unknown origin) expressed in HEK293T cells incubated for 1 hr by LC-MS/MS analysis, IC50 = 0.42 μM. |
28280261 |
HEK293T cells |
Function assay |
|
1 hr |
|
Inhibition of immobilized N-LY294002 bead binding to PI3Kdelta (unknown origin) expressed in HEK293T cells incubated for 1 hr by LC-MS/MS analysis, IC50 = 1.53 μM. |
28280261 |
HEK293T cells |
Function assay |
|
1 hr |
|
Inhibition of immobilized N-LY294002 bead binding to PI3Kalpha (unknown origin) expressed in HEK293T cells incubated for 1 hr by LC-MS/MS analysis, IC50 = 2.37 μM. |
28280261 |
MDA-MB-231 cells |
Function assay |
|
|
|
Inhibition of EGF-induced invasion of human MDA-MB-231 cells by MTT assay, IC50 = 0.38 μM. |
28302401 |
MCF7 cells |
Function assay |
10 uM |
1 hr |
|
Inhibition of IGF1R phosphorylation at Tyr1161 residue in human MCF7 cells at 10 uM after 1 hr by Hoechst 33258 staining based immunohistochemical analysis |
28557430 |
SKOV3 cells |
Function assay |
20 uM |
24 hrs |
|
Inhibition of BDNF-induced invasion in human SKOV3 cells at 20 uM after 24 hrs in by matrigel invasion assay |
29122484 |
SKOV3 cells |
Antimigratory assay |
20 uM |
24 hrs |
|
Antimigratory activity against human SKOV3 cells assessed as inhibition of BDNF-induced cell migration at 20 uM after 24 hrs by scratch wound healing assay |
29122484 |
NB1643 cells |
qHTS assay |
|
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells |
29435139 |
OHS-50 cells |
qHTS assay |
|
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells |
29435139 |
SJ-GBM2 cells |
qHTS assay |
|
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells |
29435139 |
SK-N-MC cells |
qHTS assay |
|
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells |
29435139 |
J774 cells |
Antiinflammatory assay |
|
24 hrs |
|
Antiinflammatory activity in mouse J774 cells assessed as reduction in LPS-induced MCP1 expression after 24 hrs by ELISA, IC50 = 3.7 μM. |
29726680 |
J774 cells |
Antiinflammatory assay |
|
24 hrs |
|
Antiinflammatory activity in mouse J774 cells assessed as reduction in LPS-induced IL6 expression after 24 hrs by ELISA, IC50 = 5.1 μM. |
29726680 |
J774 cells |
Antiinflammatory assay |
|
24 hrs |
|
Antiinflammatory activity in mouse J774 cells assessed as reduction in LPS-induced nitric oxide production after 24 hrs by Griess assay, IC50 = 8.9 μM. |
29726680 |
J774 cells |
Function assay |
10 uM |
4 hrs |
|
Inhibition of PI3K/Akt in mouse J774 cells assessed as reduction in LPS-induced Akt phosphorylation at Ser473 at 10 uM after 4 hrs by Western blot analysis |
29726680 |