research use only
Cat.No.S2391
| Related Targets | Akt mTOR GSK-3 ATM/ATR DNA-PK AMPK PDPK1 PTEN PP2A PDK |
|---|---|
| Other PI3K Inhibitors | LY294002 Buparlisib (BKM120) SAR405 Eganelisib (IPI-549) XL147 analogue Paxalisib (GDC-0084) Tersolisib (STX-478) 3-Methyladenine (3-MA) Dactolisib (BEZ235) Pictilisib (GDC-0941) |
| Cell Lines | Assay Type | Concentration | Incubation Time | Formulation | Activity Description | PMID |
|---|---|---|---|---|---|---|
| Walker 256 | Antitumor assay | In vivo antitumor activity against rat Walker 256 cells | 469554 | |||
| RBI-1 | Function assay | In vitro inhibition of 5-lipoxygenase (5-lo) from the 20000 g supernatant of RBI-1 cells, IC50=0.3μM | 2066989 | |||
| MCF-7 | Cytotoxicity assay | Cytotoxic effect on MCF-7 human breast carcinoma cells, IC50=24μM | 8201603 | |||
| ANN-1 | Cytotoxicity assay | Cytotoxic effect on v-abl transformed murine ANN-1 cells, IC50=32.5μM | 8201603 | |||
| 3T3 | Cytotoxicity assay | Cytotoxic effect on 3T3 cells, IC50=39.5μM | 8201603 | |||
| WiDr human colon cells | Cytotoxicity assay | Cytotoxic effect on WiDr human colon cells, IC50=40.2μM | 8201603 | |||
| RBL-1 | Function assay | In vitro inhibition against 5-lipoxygenase in RBL-1 cells was determined, IC50=0.2μM | 8254620 | |||
| HEK293 | Function assay | Displacement of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK293 cells, Ki=30μM | 8576921 | |||
| L929 | Function assay | 15 mins | Inhibition of recombinant human TNF-alpha-induced cytotoxicity of mouse L929 cells assessed as survivality preincubated for 15 mins before TNFalpha addition measured after 24 hrs by crystal violet staining, EC50=20μM | 9287415 | ||
| L929 | Function assay | 15 mins | Inhibition of recombinant human TNF-alpha-induced cytotoxicity of mouse L929 cells assessed as survivality preincubated for 15 mins before TNFalpha addition measured after 24 hrs by [methyl-3H]thymidine incorporation assay, EC50=26μM | 9287415 | ||
| L929 | Function assay | 2 hrs | Inhibition of recombinant human TNF-alpha-induced cytotoxicity of mouse L929 cells assessed as survivality treated with drug after 2 hrs of TNFalpha treatment | 9287415 | ||
| L929 | Function assay | 2 hrs | Potentiation of recombinant human TNF-alpha-induced cytotoxicity of mouse L929 cells assessed as survivality treated with drug after 2 hrs of TNFalpha treatment | 9287415 | ||
| 3T3/A31 | Growth inhibition assay | 10 to 100 ug/mL | 72 hrs | Growth inhibition of BALB/c mouse cloned 3T3/A31 cells at 10 to 100 ug/mL after 72 hrs by nigrosin assay | 10096863 | |
| HeLa | Function assay | TP_TRANSPORTER: inhibition of LTC4 uptake in membrane vesicle from MRP1-expressing HeLa cells, Ki=8.1μM | 11306701 | |||
| RAW264.7 | Function assay | Inhibition of LPS and INF-gamma-induced NO production in mouse RAW264.7 cells, IC50=26.8μM | 15043424 | |||
| RAW264.7 | Function assay | Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells, IC50=26.8μM | 16378364 | |||
| HT22 | Function assay | Inhibition of glutamate-induced oxytosis of mouse hippocampal HT22 cells, EC50=2.98μM | 16392814 | |||
| Jurkat T | Function assay | Activity against hydrogen peroxide induced DNA damage in Jurkat T cells, IC50=5μM | 16392814 | |||
| BM | Antioxidant assay | Antioxidant activity in BALB/c mouse BM cells assessed as inhibition of ROS production, IC25=3.5μM | 17166721 | |||
| Sf21 | Function assay | Inhibition of human recombinant COX2 expressed in insect Sf21 cells by EIA assay, IC50=28.6μM | 17378609 | |||
| LNCaP | Function assay | Decrease in androgen receptor protein expression in LNCaP cells by Western blotting, EC50=25μM | 17383188 | |||
| SKBR3 | Antiapoptotic assay | 72 hrs | Inhibition of HSP70-mediated antiapoptotic activity in human SKBR3 cells assessed as induction of cell growth arrest after 72 hrs by propidium iodide staining-based flow cytometry | 17603540 | ||
| SKBR3 | Antiapoptotic assay | 24 hrs | Inhibition of HSP70-mediated antiapoptotic activity in human SKBR3 cells assessed as increase in caspase-3 activity after 24 hrs by Western blot analysis | 17603540 | ||
| SKBR3 | Antiapoptotic assay | 24 hrs | Inhibition of HSP70-mediated antiapoptotic activity in human SKBR3 cells assessed as induction of caspase-3 cleavage after 24 hrs by Western blot analysis | 17603540 | ||
| SKBR3 | Antiapoptotic assay | 24 hrs | Inhibition of HSP70-mediated antiapoptotic activity in human SKBR3 cells assessed as induction of PARP cleavage after 24 hrs by Western blot analysis | 17603540 | ||
| BGC823 | Function assay | 50 uM | Effect on cell morphology in human BGC823 cells assessed as chromosomal condensations at 50 uM | 17997321 | ||
| BGC823 | Apoptosis assay | 50 uM | 48 hrs | Induction of apoptotic bodies in human BGC823 cells at 50 uM after 48 hrs | 17997321 | |
| BGC823 | Apoptosis assay | 50 uM | 48 hrs | Induction of apoptosis in human BGC823 cells assessed as increase in DNA fragmentation at 50 uM after 48 hrs | 17997321 | |
| BGC823 | Apoptosis assay | 100 uM | 48 hrs | Induction of apoptosis in human BGC823 cells assessed as increase in DNA fragmentation at 100 uM after 48 hrs | 17997321 | |
| RAW264.7 | Function assay | 16 hrs | Inhibition of LPS and INF-alpha-induced nitric oxide production in mouse RAW264.7 cells after 16 hrs, IC50=25μM | 18027905 | ||
| RAW264.7 | Function assay | Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells, IC50=26.8μM | 18027905 | |||
| BV2 | Function assay | Inhibition of LPS-induced NO production in mouse BV2 cells, IC50=29.6μM | 18178435 | |||
| HL60 | Antiproliferative assay | 30 uM | 48 hrs | Antiproliferative activity against human HL60 cells at 30 uM after 48 hrs by MTS assay | 18258440 | |
| Jurkat | Function assay | 50 ug/mL | 1 hr | Inhibition of heat-induced HSP70 expression in human Jurkat cells at 50 ug/mL treated for 1 hr before heat induction by Western blot | 19296652 | |
| HeLa | Function assay | 50 ug/mL | 1 hr | Enhancement of HSP27 Ser78 phosphorylation in human HeLa cells at 50 ug/mL treated for 1 hr | 19296652 | |
| Jurkat | Function assay | 50 ug/mL | 1 hr | Inhibition of HSF1 binding to heat shock element DNA assessed as HSF1/HSE complex formation in human Jurkat cells at 50 ug/mL treated for 1 hr before heat induction | 19296652 | |
| Jurkat | Function assay | 50 ug/mL | 1 hr | Inhibition of of heat-induced increase in nuclear HSF1 protein phosphorylation in human Jurkat cells assessed as decrease in protein mobility at 50 ug/mL treated for 1 hr before heat induction by EMSA | 19296652 | |
| HeLa | Function assay | 50 ug/mL | 1 hr | Inhibition of of heat-induced increase in nuclear HSF1 protein phosphorylation in human HeLa cells assessed as decrease in protein mobility at 50 ug/mL treated for 1 hr before heat induction by EMSA | 19296652 | |
| RAW264.7 | Antiinflammatory assay | 24 hrs | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess reagent assay, IC50=9.6μM | 19555124 | ||
| MCF7 | Function assay | 0.5 uM to 10 uM | 24 hrs | Induction of CYP1A1 expression in human MCF7 cells at 0.5 uM to 10 uM after 24 hrs by RT PCR and DNA electrophoresis | 19601638 | |
| HeLa | Function assay | Inhibition of MRP1 transfected in human HeLa cells assessed as inhibition of [3H]LTC4 transport by rapid filtration assay, Ki=2.4μM | 19725578 | |||
| MDCK | Antiviral assay | Antiviral activity against influenza A virus H1N1 A/PR/8/34 infected in MDCK cells assessed as reduction in virus-induced cytopathic effect, EC50=43.1μM | 19729316 | |||
| RAW264.7 | Antiinflammatory assay | 24 hrs | Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced nitrite accumulation after 24 hrs by Griess reagent method, IC50=11.4μM | 19778086 | ||
| Vero | Cytotoxicity assay | 3 days | Cytotoxicity against african green monkey Vero cells after 3 days by MTT assay, MNCC<20μM | 19778089 | ||
| Vero | Cytotoxicity assay | 3 days | Cytotoxicity against african green monkey Vero cells after 3 days by MTT assay, MNCC<20μM | 20092288 | ||
| RAW264.7 | Antiinflammatory assay | 24 hrs | Antiinflammatory activity against mouse RAW264.7 cells assessed as Inhibition of LPS-induced nitric oxide production after 24 hrs by ELISA, IC50=32.1μM | 20121165 | ||
| Sf9 | Function assay | Inhibition of rat ecto-5'-nucleotidase expressed in Sf9 cells by capillary electrophoresis method, Ki=0.0453μM | 20146483 | |||
| B16-4A5 | Function assay | 72 hrs | Inhibition of theophylline-stimulated melanogenesis in mouse B16-4A5 cells after 72 hrs, IC50=15μM | 20189399 | ||
| HUVEC | Cytoprotective assay | Cytoprotective activity against H2O2-induced cell injury in HUVEC cells, EC50=18μM | 20621727 | |||
| HEK293 FS | Function assay | Inhibition of NOX4 expressed in HEK293 FS cells assessed as H2O2 production by H2O2/Tyr/LPO assay, IC50=0.68μM | 20731357 | |||
| 3T3L1 | Function assay | 10 uM | Induction of AMPK phosphorylation in mouse 3T3L1 cells at 10 uM by Western blotting | 20822902 | ||
| 3T3L1 | Function assay | 10 uM | Induction of AMPK-mediated ACC phosphorylation in mouse 3T3L1 cells at 10 uM by Western blotting | 20822902 | ||
| 3T3L1 | Function assay | Inhibition of AMPK-mediated adipocyte differentiation in mouse 3T3L1 cells | 20822902 | |||
| 3T3L1 | Function assay | Inhibition of PPAR-gamma-mediated adipocyte differentiation in mouse 3T3L1 cells | 20822902 | |||
| RAW264.7 | Antiinflammatory assay | 24 hrs | Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NO production after 24 hrs, IC50=34.5μM | 20825224 | ||
| HCT116 | Function assay | 5 uM | 1 hr | Cellular uptake in human HCT116 cells assessed a bright fluorescence light at 5 uM after 1 hr by fluorescence microscopic analysis | 21090565 | |
| MCF7 | Function assay | 10 uM | 5 hrs | Cellular uptake in human MCF7 cells assessed as formation of quercetin glucuronide in cell lysates at 10 uM after 5 hrs by HPLC-mass spectrophotometric analysis | 21090565 | |
| MCF7 | Function assay | 10 uM | 5 hrs | Cellular uptake in human MCF7 cells assessed as formation of quercetin sulphate in cell lysates at 10 uM after 5 hrs by HPLC-mass spectrophotometric analysis | 21090565 | |
| MCF7 | Function assay | 10 uM | 5 hrs | Cellular uptake in human MCF7 cells assessed as formation of oxidised quercetin in cell lysates at 10 uM after 5 hrs by HPLC-mass spectrophotometric analysis | 21090565 | |
| MCF7 | Function assay | 10 uM | 5 hrs | Cellular uptake in human MCF7 cells assessed as formation of methylated quercetin in cell lysates at 10 uM after 5 hrs by HPLC-mass spectrophotometric analysis | 21090565 | |
| RAW264.7 | Antiinflammatory assay | 1 to 100 uM | 24 hrs | Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as nitrite level at 1 to 100 uM after 24 hrs by Griess method, Activity=1.38μM | 21353543 | |
| MDCK | Function assay | Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining, IC50=6.9μM | 21354800 | |||
| MCF-7 MX | Function assay | Inhibition of BCRP expressed in MCF-7 MX cells using Hoechst 33342 staining, IC50=7.6μM | 21354800 | |||
| HepG2(2.2.15) | Cytotoxicity assay | 8 days | Cytotoxicity against human HepG2(2.2.15) cells after 8 days by MTT assay, CC50=38.1μM | 21401115 | ||
| MDA-MB-231 | Function assay | 20 uM | 30 mins | Increase in c-Fos protein expression in human MDA-MB-231 cells at 20 uM within 30 mins by Western blot analysis | 21652208 | |
| MDA-MB-231 | Function assay | 20 uM | 30 mins | Increase in Egr-1 protein expression in human MDA-MB-231 cells at 20 uM within 30 mins by Western blot analysis | 21652208 | |
| MDA-MB-231 | Apoptosis assay | 20 uM | 12 hrs | Induction of apoptosis in human MDA-MB-231 cells assessed as cleaved caspase-7 accumulation at 20 uM after 12 hrs by Western blot analysis | 21652208 | |
| HepG2 | Cytotoxicity assay | Cytotoxicity against human HepG2 cells by MTT assay, IC50=30.9μM | 21726077 | |||
| Jurkat | Function assay | 145 uM | 8 hrs | Inhibition of heat shock-induced HSP70 expression in human Jurkat cells at 145 uM treated 2 hrs before beat shock challenge measured after 8 hrs by Western blotting | 21798748 | |
| HepG2 | Function assay | 24 hrs | Inhibition of oleic acid-induced triglyceride over-accumulation in human HepG2 cells incubated for 24 hrs relative to untreated control, IC30=14.9μM | 21824690 | ||
| HepG2 | Antioxidant assay | 24 hrs | Antioxidant activity in human HepG2 cells assessed as reduction of oleic acid-induced ROS generation incubated for 24 hrs by DHCF-DA based fluorimetric assay relative to untreated control, IC30=30.8μM | 21824690 | ||
| MDCK | Antiviral assay | 4 days | Antiviral activity against influenza A virus (A/swine/OH/511445/2007(H1N1)) Oh7 infected in MDCK cells assessed as inhibition of viral replication after 4 days by quantitative RT-PCR, ED50=48.2μM | 22115591 | ||
| HCT116 | Growth inhibition assay | 48 hrs | Growth inhibition of human HCT116 cells overexpressing PI3Kalpha H1047R mutant after 48 hrs by MTT assay, IC50=5.7μM | 22212721 | ||
| HCT116 | Growth inhibition assay | 48 hrs | Growth inhibition of human HCT116 cells after 48 hrs by MTT assay, IC50=6.7μM | 22212721 | ||
| HCT116 | Growth inhibition assay | 48 hrs | Growth inhibition of human HCT116 cells overexpressing PI3Kalpha after 48 hrs by MTT assay, IC50=23μM | 22212721 | ||
| HCT116 | Function assay | 25 uM | 10 mins | Inhibition of PI3Kalpha in human HCT116 cells using [32P]ATP at 25 uM after 10 mins | 22212721 | |
| HCT116 | Function assay | 25 uM | 10 mins | Inhibition of PI3Kalpha H1047R mutant in human HCT116 cells using [32P]ATP at 25 uM after 10 mins | 22212721 | |
| HCT116 | Function assay | 25 uM | Inhibition of PI3Kalpha in human HCT116 cells assessed as inhibition of Akt Ser473 phosphorylation at 25 uM by immunoblot analysis | 22212721 | ||
| HCT116 | Function assay | 25 uM | Inhibition of PI3Kalpha H1047R mutant in human HCT116 cells assessed as inhibition of Akt Ser473 phosphorylation at 25 uM by immunoblot analysis | 22212721 | ||
| human mast cells | Function assay | Inhibition of SYK in human mast cells assessed as reduction in mast cell degranulation, EC50=35μM | 22257213 | |||
| Huh7.5.1 | Antiviral assay | 72 hrs | Antiviral activity against HCV JFH-1 J399EM infected in Human Huh7.5.1 cells assessed as suppression of viral replication after 72 hrs by EGFP assay, EC50=19.8μM | 22445328 | ||
| HT22 | Neuroprotective assay | 25 uM | 24 hrs | Neuroprotective activity against glutamate induced oxidative stress in mouse hippocampal HT22 cells assessed as cell viability at 25 uM after 24 hrs by MTT assay | 22624880 | |
| 22Rv1 | Antiproliferative assay | Antiproliferative activity against human 22Rv1 cells incubated up to 144 hrs by Coulter particle count and size analyzer, IC50=15.5μM | 22789812 | |||
| RAW264.7 | Function assay | 50 uM | 3 hrs | Activation of Nrf2 in mouse RAW264.7 cells assessed as cytosolic accumulation at 50 uM after 3 hrs by Western blotting analysis | 23294286 | |
| RAW264.7 | Function assay | 50 uM | 3 hrs | Activation of Nrf2 in mouse RAW264.7 cells assessed as nuclear accumulation at 50 uM after 3 hrs by Western blotting analysis | 23294286 | |
| ARPE19 | Function assay | 20 uM | 18 days | Inhibition of intracellular A2E photooxidation in human ARPE19 cells at 20 uM after 18 days | 23346866 | |
| MV4-11 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MV4-11 cells harboring FLT3 mutation after 72 hrs by tetrazolium based Ez CyTox cell viability assay, GI50=13.1μM | 23411073 | ||
| RS4:11 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human RS4:11 cells harboring wild type FLT3 after 72 hrs by tetrazolium based Ez CyTox cell viability assay, GI50=21.6μM | 23411073 | ||
| HCT116 | Cytotoxicity assay | 1 to 100 uM | 12 hrs | Cytotoxicity against human HCT116 cells at 1 to 100 uM after 12 hrs by MTT assay | 23434132 | |
| MCF7 | Cytotoxicity assay | 1 to 100 uM | 12 hrs | Cytotoxicity against human MCF7 cells at 1 to 100 uM after 12 hrs by MTT assay | 23434132 | |
| HTLA | Function assay | 20 mins | Inhibition of CX3CL1-stimulated CX3CR1 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay, IC50=4.5μM | 23437772 | ||
| HTLA | Function assay | 20 mins | Inhibition of CX3CL1-stimulated CX3CR1 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay, IC50=5.01187μM | 23437772 | ||
| HTLA | Function assay | 20 mins | Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay, IC50=6.30957μM | 23437772 | ||
| HTLA | Function assay | 20 mins | Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay, IC50=7μM | 23437772 | ||
| HTLA | Function assay | 20 mins | Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay, IC50=10μM | 23437772 | ||
| HTLA | Function assay | 20 mins | Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay, IC50=10.2μM | 23437772 | ||
| HTLA | Function assay | 20 mins | Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay, IC50=15.2μM | 23437772 | ||
| HTLA | Function assay | 20 mins | Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay, IC50=15.8489μM | 23437772 | ||
| HTLA | Function assay | 20 mins | Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay, IC50=37.8μM | 23437772 | ||
| HTLA | Function assay | 20 mins | Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay, IC50=39.8107μM | 23437772 | ||
| RAW264.7 | Function assay | 24 hrs | Inhibition of iNOS-mediated nitric oxide production in LPS-stimulated mouse RAW264.7 cells after 24 hrs by Griess reaction analysis, IC50=16.4μM | 23517145 | ||
| RAW264.7 | Function assay | 24 hrs | Inhibition of LPS-induced NO production in mouse RAW264.7 cells after 24 hrs, IC50=1.3μM | 23540981 | ||
| 3T3L1 | Antiobesity assay | 100 uM | Antiobesity activity in mouse 3T3L1 cells assessed as reduction of fat accumulation at 100 uM by oil Red O staining-based ELISA | 23642481 | ||
| HT22 | Neuroprotective assay | 40 uM | 3 hrs | Neuroprotective activity in mouse HT22 cells assessed as t-BOOH-induced toxicity at 40 uM preincubated for 3 hrs followed by t-BOOH induction measured after 9 hrs by MTT assay | 24245939 | |
| HT22 | Neuroprotective assay | 40 uM | 3 hrs | Neuroprotective activity in mouse HT22 cells assessed as reduction of t-BOOH-induced oxidative stress at 40 uM preincubated for 3 hrs followed by t-BOOH induction measured after 20 hrs by MTT assay | 24245939 | |
| HepG2 | Antioxidant assay | 1 hr | Antioxidant activity in human HepG2 cells assessed as inhibition of ABAP-induced intracellular peroxyl radical scavenging activity by measuring ROS production measured every 5 mins for 1 hr by absorbance assay, IC50=11μM | 24471493 | ||
| HT22 | Neuroprotective assay | 24 hrs | Neuroprotective activity in mouse HT22 cells assessed as protection against glutamate-induced oxidative damage after 24 hrs by MTT assay, EC50=3.13μM | 24602904 | ||
| HT22 | Cytotoxicity assay | 24 hrs | Cytotoxicity against mouse HT22 cells after 24 hrs by MTT assay, EC50=11.52μM | 24602904 | ||
| RAW264.7 | Antiinflammatory assay | 10 uM | 18 hrs | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha secretion at 10 uM after 18 hrs by sandwich ELISA | 24679441 | |
| BV2 | Antiinflammatory assay | Antiinflammatory activity in human BV2 cells assessed as inhibition of LPS-induced nitric oxide production by Griess assay, IC50=10μM | 24707938 | |||
| HT22 | Neuroprotective assay | 5 uM | 48 hrs | Neuroprotection against glutamate challenged mouse HT22 cells assessed as reduction in cell viability at 5 uM after 48 hrs by MTT assay | 24819955 | |
| HT22 | Neuroprotective assay | 25 uM | 24 hrs | Neuroprotective activity against glutamate-induced oxidative stress in mouse HT22 cells assessed as reduction of intracellular ROS formation at 25 uM after 24 hrs by MTT assay | 24900407 | |
| U2OS | Function assay | 5 hrs | Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay, EC50=5.93μM | 24900447 | ||
| HT-29 | Function assay | 10 mins | Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay, EC50=8.02μM | 24900447 | ||
| HT-29 | Function assay | 10 mins | Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins, IC50=15.4μM | 24900447 | ||
| HT-29 | Function assay | 10 mins | Partial agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay | 24900447 | ||
| PC12 | Neuroprotective assay | 5 uM | 24 hrs | Neuroprotective activity in rat PC12 cells assessed as inhibition H2O2-induced reduction of cell viability at 5 uM after 24 hrs by MTT assay | 24941128 | |
| HLF1 | Function assay | 2 to 5 uM | 24 hrs | Inhibition of H2O2-induced oxidative stress in human HLF1 cells assessed as increase in cell viability at 2 to 5 uM pretreated for 24 hrs followed by addition of 300 uM H2O2 for 2.5 hrs | 24996137 | |
| HL60 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HL60 cells after 72 hrs by MTT assay, IC50=47μM | 25014747 | ||
| HT22 | Neuroprotective assay | 25 uM | Neuroprotective activity in mouse HT22 cells assessed as reduction in glutamate-induced cytotoxicity at 25 uM by MTT assay | 25059502 | ||
| RAW264.7 | Antiinflammatory assay | 3 uM | 24 hrs | Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as reduction in nitric oxide production at 3 uM after 24 hrs by Griess method based ELISA (Rvb = 52.4 +/- 0.9 uM), Activity=13.5μM | 25106885 | |
| RAW264.7 | Antiinflammatory assay | 1.5 uM | 24 hrs | Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as reduction in nitric oxide production at 1.5 uM after 24 hrs by Griess method based ELISA (Rvb = 52.4 +/- 0.9 uM), Activity=20.8μM | 25106885 | |
| BV2 | Function assay | 24 hrs | Inhibition of LPS-stimulated NO production in human BV2 cells after 24 hrs by Griess assay, IC50=4.3μM | 25127164 | ||
| HeLa | Anticancer assay | Anticancer activity against human HeLa cells by HTS assay, IC50=3.56μM | 25139569 | |||
| NCI-H1792 | Anticancer assay | Anticancer activity against human NCI-H1792 cells by HTS assay, IC50=3.85μM | 25139569 | |||
| LOXIMVI | Anticancer assay | Anticancer activity against human LOXIMVI cells by HTS assay, IC50=4.65μM | 25139569 | |||
| NCI-H522 | Anticancer assay | Anticancer activity against human NCI-H522 cells by HTS assay, IC50=5.77μM | 25139569 | |||
| NCI-H157 | Anticancer assay | Anticancer activity against human NCI-H157 cells by HTS assay, IC50=6μM | 25139569 | |||
| A549 | Anticancer assay | Anticancer activity against human A549 cells by HTS assay, IC50=6.2μM | 25139569 | |||
| HOP62 | Anticancer assay | Anticancer activity against human HOP62 cells by HTS assay, IC50=7.52μM | 25139569 | |||
| H460 | Anticancer assay | Anticancer activity against human H460 cells by HTS assay, IC50=9.62μM | 25139569 | |||
| NCI-H1944 | Anticancer assay | Anticancer activity against human NCI-H1944 cells by HTS assay, IC50=10.18μM | 25139569 | |||
| M14 | Anticancer assay | Anticancer activity against human M14 cells by HTS assay, IC50=12.77μM | 25139569 | |||
| H1299 | Anticancer assay | Anticancer activity against human H1299 cells by HTS assay, IC50=13.6μM | 25139569 | |||
| SKBR | Anticancer assay | Anticancer activity against human SKBR cells by HTS assay, IC50=16.71μM | 25139569 | |||
| H266 | Anticancer assay | Anticancer activity against human H266 cells by HTS assay, IC50=16.87μM | 25139569 | |||
| M4E | Anticancer assay | Anticancer activity against human M4E cells by HTS assay, IC50=21.71μM | 25139569 | |||
| Calu1 | Anticancer assay | Anticancer activity against human Calu1 cells by HTS assay, IC50=23.58μM | 25139569 | |||
| MDA-MB-231 | Function assay | 5 uM | 16 hrs | Inhibition of PMA-stimulated NF-kappaB signaling (unknown origin) expressed in MDA-MB-231 cells at 5 uM incubated for 16 hrs by luciferase reporter gene assay | 25190466 | |
| MDA-MB-231 | Function assay | 25 uM | Inhibition of basal NF-kappaB signaling in human MDA-MB-231 cells assessed as reduction in MMP9 mRNA expression at 25 uM by quantitative RT-PCR method relative to untreated control | 25190466 | ||
| MDA-MB-231 | Function assay | 25 uM | Inhibition of NF-kappaB signaling in human MDA-MB-231 cells assessed as reduction in PMA-stimulated MMP9 mRNA expression at 25 uM pre-incubated before PMA stimulation by quantitative RT-PCR method relative to untreated control | 25190466 | ||
| MDA-MB-231 | Function assay | 25 uM | Inhibition of basal NF-kappaB signaling in human MDA-MB-231 cells assessed as reduction in COX2 mRNA expression at 25 uM by quantitative RT-PCR method relative to untreated control | 25190466 | ||
| MDA-MB-231 | Function assay | 25 uM | Inhibition of NF-kappaB signaling in human MDA-MB-231 cells assessed as reduction in PMA-stimulated COX2 mRNA expression at 25 uM pre-incubated before PMA stimulation by quantitative RT-PCR method relative to untreated control | 25190466 | ||
| MDA-MB-231 | Function assay | 25 uM | Inhibition of NF-kappaB signaling in human MDA-MB-231 cells assessed as reduction in PMA-stimulated MMP9 mRNA expression at 25 uM pre-incubated before PMA stimulation by quantitative RT-PCR method | 25190466 | ||
| MDA-MB-231 | Function assay | 25 uM | Inhibition of NF-kappaB signaling in human MDA-MB-231 cells assessed as reduction in PMA-stimulated COX2 mRNA expression at 25 uM pre-incubated before PMA stimulation by quantitative RT-PCR method | 25190466 | ||
| MDA-MB-231 | Apoptosis assay | 3.125 to 25 uM | 48 hrs | Induction apoptosis in PMA-stimulated human MDA-MB-231 cells assessed as mitochondrial disruption 3.125 to 25 uM after 48 hrs by JC1 staining based fluorescence assay | 25190466 | |
| RAW264.7 | Anti-inflammatory assay | 24 hrs | Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of lipopolysaccharide-induced nitric oxide production incubated for 24 hrs by Griess reagent based assay, IC50=16.6μM | 25245917 | ||
| HCT116 | Cytotoxicity assay | 1.25 to 20 uM | 96 hrs | Cytotoxicity against human HCT116 cells at 1.25 to 20 uM after 96 hrs by MTT assay | 25397870 | |
| HCT116 | Apoptosis assay | 20 uM | 72 hrs | Induction of apoptosis in human HCT116 cells assessed as PARP cleavage at 20 uM after 72 hrs by immunoblotting | 25397870 | |
| HCT116 | Antitumor assay | 80 uM | 4 days | Antitumor activity against human HCT116 cells xenografted in 48 hpf zebrafish embryo assessed as inhibition of cancer cell proliferation at 80 uM treated for 4 days | 25397870 | |
| C6 | Function assay | 72 hrs | Inhibition of cell proliferation of rat C6 cells assessed as cell viability after 72 hrs by sulforhodamine B assay, IC50=18.38μM | 25442304 | ||
| HCT15 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HCT15 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50=16.35μM | 25906385 | ||
| MCF7 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MCF7 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50=20.9μM | 25906385 | ||
| 2008 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human 2008 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50=21.18μM | 25906385 | ||
| A431 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A431 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50=23.04μM | 25906385 | ||
| BxPC3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human BxPC3 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50=24.12μM | 25906385 | ||
| A375 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A375 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50=25.13μM | 25906385 | ||
| A431 | Cytotoxicity assay | 72 hrs | Cytotoxicity against cisplatin-resistant human A431 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50=34.37μM | 25906385 | ||
| C13 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human C13 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50=37.62μM | 25906385 | ||
| B16-4A5 | Function assay | 72 hrs | Inhibition of melanogenesis in theophylline-stimulated mouse B16-4A5 cells after 72 hrs by microplate reader analysis, IC50=15μM | 25987378 | ||
| RAW264.7 | Anti-inflammatory assay | 24 hrs | Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production incubated for 24 hrs by Griess reagent based assay, IC50=1.8μM | 26143931 | ||
| BV2 | Anti-inflammatory assay | 24 hrs | Antiinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-stimulated nitric oxide production after 24 hrs by Griess assay, IC50=17.4μM | 26327273 | ||
| LNCAP | Cytotoxicity assay | 3 days | Cytotoxicity against human androgen-dependent LNCAP cells assessed as inhibition of cell viability after 3 days by WST-1 cell proliferation assay, IC50=45.5μM | 26341135 | ||
| BV2 | Antineuroinflammatory assay | 24 hrs | Antineuroinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-stimulated NO production after 24 hrs by Griess assay, EC50=11μM | 26473791 | ||
| BL21 | Function assay | 20 uM | 15 mins | Inhibition of recombinant human N-terminal His6-tagged AKR1B10 expressed in Escherichia coli BL21 cells using all-trans-retinal as substrate at 20 uM incubated for 15 mins by HPLC method | 26529431 | |
| BV2 | Function assay | 24 hrs | Inhibition of LPS-induced nitric oxide production in human BV2 cells after 24 hrs by Griess assay, IC50=8.7μM | 26696523 | ||
| HT22 | Neuroprotective assay | 25 uM | 24 hrs | Neuroprotective activity against glutamate-induced oxycytotic cell death in mouse HT22 cells assessed as cell viability at 25 uM after 24 hrs by MTT assay | 26886849 | |
| RAW264.7 | Anti-inflammatory assay | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production by Griess assay, IC50=15μM | 26928174 | |||
| HepG2 | Antioxidant assay | 2.5 hrs | Antioxidant activity in human HepG2 cells assessed as decrease in fluorescence level after 2.5 hrs measured every 5 mins for 1 hr by DCFH-DA staining based fluorescence assay, EC50=4.63μM | 26974372 | ||
| RF/6A | Antimigratory assay | 24 hrs | Antimigratory activity in rhesus monkey RF/6A cells measured after 24 hrs by wound assay, IC50=40μM | 27015547 | ||
| RAW264.7 | Function assay | 24 hrs | Inhibition of LPS-induced NO production in mouse RAW264.7 cells after 24 hrs by Griess assay, IC50=15.9μM | 27177824 | ||
| BV2 | Antiinflammatory assay | 24 hrs | Antiinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced NO production incubated for 24 hrs measured after 15 mins by Griess assay, IC50=15.13μM | 27335254 | ||
| PC12 | Function assay | 5 uM | 2 hrs | Protective effect against H2O2-induced cell death in rat PC12 cells at 5 uM preincubated for 2 hrs followed by H2O2 addition for 24 hrs by MTT assay | 27343850 | |
| PC12 | Antioxidant assay | 2.5 uM | 2 hrs | Antioxidant activity in rat PC12 cells assessed as decrease of H2O2-induced ROS production at 2.5 uM preincubated for 2 hrs followed by H2O2 addition for 24 hrs by DCFH-DA /DAPI-based fluorescence assay | 27343850 | |
| LNCAP | Antiproliferative assay | 3 days | Antiproliferative activity against human LNCAP cells after 3 days by WST1 assay, IC50=45.5μM | 27476422 | ||
| BV2 | Antineuroinflammatory assay | 24 hrs | Antineuroinflammatory activity in human BV2 cells assessed as inhibition of LPS-induced NO production after 24 hrs in presence of LPS by Griess reaction, IC50=39.46μM | 27623545 | ||
| N9 | Antineuroinflammatory assay | 24 hrs | Antineuroinflammatory activity in mouse N9 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay, IC50=10.22μM | 28073678 | ||
| Escherichia coli competent cells | Function assay | overnight | Inhibition of amyloid beta (1 to 42) aggregation in Escherichia coli competent cells BL21 (DE3) after overnight incubation by Thioflavin-S steady-state fluorescence assay, IC50=15.3μM | 28128562 | ||
| BV2 | Antiinflammatory assay | 24 hrs | Antiinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced nitrite production after 24 hrs by Griess assay, IC50=19.11μM | 28165740 | ||
| RAW264.7 | Function assay | 1 hr | Inhibition of LPS-induced NO production in mouse RAW264.7 cells preincubated for 1 hr followed by LPS stimulation measured after 24 hrs by Griess assay, IC50=4.41μM | 28427811 | ||
| LLC-PK1 | Renoprotective assay | 10 to 100 uM | 2 hrs | Renoprotective activity in pig LLC-PK1 cells assessed as inhibition of cisplatin-induced damage by measuring increase in cell viability at 10 to 100 uM preincubated for 2 hrs followed by cisplatin addition after 24 hrs by Ez-Cytox reagent based assay | 28487074 | |
| human red blood cells | Antiplasmodial assay | 48 hrs | Antiplasmodial activity against asexual erythrocyte stage of chloroquine-sensitive Plasmodium falciparum 3D7 infected in human red blood cells after 48 hrs by lactate dehydrogenase assay, IC50=17.54μM | 28557449 | ||
| PC12 | Function assay | 10 uM | Inhibition of human amyloid beta (1 to 42) assessed as neuroprotective activity against amyloid beta (1 to 42)-induced toxicity in rat PC12 cells by measuring reduction in cell viability at 10 uM incubated 15 mins prior to amyloid beta (1 to 42) addition | 28559058 | ||
| T47D | Cytotoxicity assay | 48 hrs | Cytotoxicity against human T47D cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50=11μM | 28654265 | ||
| NCI-H460 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human NCI-H460 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50=12μM | 28654265 | ||
| SK-MEL-2 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human SK-MEL-2 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50=12μM | 28654265 | ||
| LN229 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human LN229 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50=12μM | 28654265 | ||
| A549 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human A549 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50=13μM | 28654265 | ||
| MML1 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MML1 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50=15μM | 28654265 | ||
| BxPC3 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human BxPC3 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50=16μM | 28654265 | ||
| HT-29 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HT-29 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50=18μM | 28654265 | ||
| COLO201 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human COLO201 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50=19μM | 28654265 | ||
| MDA-MB-231 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MDA-MB-231 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50=20μM | 28654265 | ||
| U87 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human U87 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50=23μM | 28654265 | ||
| LNCAP | Antiproliferative assay | 3 days | Antiproliferative activity against human LNCAP cells after 3 days by WST-1 assay, IC50=45.46μM | 28760528 | ||
| PC12 | Neuroprotective assay | 10 uM | 3 hrs | Neuroprotective activity in rat PC12 cells assessed as decrease in H2O2 mediated apoptosis at 10 uM preincubated for 3 hrs followed by H2O2 challenge measured after 24 hrs by MTT assay | 28803044 | |
| SH-SY5Y | Neuroprotective assay | 100 uM | 12 hrs | Neuroprotective activity against H2O2-induced cell death in human SH-SY5Y cells assessed as increase in cell viability at 100 uM pretreated for 12 hrs followed by H2O2 challenge measured after 3 hrs by MTT assay | 28988761 | |
| BV2 | Antiinflammatory assay | Antiinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-stimulated nitric oxide production by Griess reagent based spectrophotometric analysis, IC50=16.3μM | 29122483 | |||
| MDA-MB-468 | Function assay | 6.6 uM | Inhibition of human CYP1B1 expressed in MDA-MB-468 cells assessed as potentiation of cisplatin-induced cytotoxicity by measuring cisplatin EC50 at 6.6 uM (Rvb = 6.70+/- 0.7 uM), EC50=1.1μM | 29150398 | ||
| HEK293 | Function assay | Inhibition of human CYP1B1 expressed in HEK293 cells by fluorescence assay, IC50=2.2μM | 29150398 | |||
| MDA-MB-468 | Function assay | Inhibition of human CYP1B1 expressed in MDA-MB-468 cells assessed as cell toxicity, IC50=2.2μM | 29150398 | |||
| HEK293 | Function assay | 20 uM | Inhibition of human CYP1A1 transfected in HEK293 cells assessed as protection against CYP1A1 mediated B[a]P toxicity by measuring B[a]P EC50 at 20 uM by MTT assay (Rvb =1.2+/- 0.3 uM), EC50=8.8μM | 29150398 | ||
| HEK293 | Function assay | Inhibition of human CYP1A expressed in HEK293 cells by fluorescence assay, IC50=9.9μM | 29150398 | |||
| HEK293 | Function assay | Inhibition of human CYP1A1 transfected in HEK293 cells assessed as cell toxicity, IC50=9.9μM | 29150398 | |||
| BV2 | Antiinflammatory assay | 24 hrs | Antiinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by griess assay, IC50=7.2μM | 29303577 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | |||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | |||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | |||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | |||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | |||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | |||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | |||
| K562 | Cytotoxicity assay | 5 days | Cytotoxicity against human K562 cells assessed as inhibition of cell growth after 5 days by MTT assay, IC50=2.5μM | 29553260 | ||
| HepG2 | Antioxidant assay | 60 mins | Antioxidant activity in human HepG2 cells assessed as inhibition of ABAP-induced peroxyl radical generation incubated for 60 mins measured for 60 mins by DCFH-DA probe based fluorescence assay, IC50=12μM | 29553260 | ||
| RAW264.7 | Cytoprotective assay | 1 pM | 2 hrs | Cytoprotective activity against H2O2-induced oxidative stress in mouse RAW264.7 cells assessed as increase in cell viability at 1 pM incubated for 2 hrs prior to H2O2 addition measured after 24 hrs by MTT assay | 29681148 | |
| BV2 | Antiinflammatory assay | 24 hrs | Antiinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay, IC50=4.3μM | 30119995 | ||
| BV2 | Function assay | 24 hrs | Inhibition of LPS-induced nitric oxide production in mouse BV2 cells after 24 hrs by Griess assay, IC50=2.4μM | 30132670 | ||
| MCF10A | Cytotoxicity assay | 3 days | Cytotoxicity against human MCF10A cells assessed as decrease in cell viability after 3 days by WST-1 assay, IC50=11.97μM | 30165345 | ||
| PWR-1E | Cytotoxicity assay | 3 days | Cytotoxicity against human PWR-1E cells assessed as decrease in cell viability after 3 days by WST-1 assay, IC50=15.08μM | 30165345 | ||
| LNCAP | Antiproliferative assay | 3 days | Antiproliferative activity against human LNCAP cells after 3 days by WST-1 assay, IC50=45.5μM | 30165345 | ||
| HCT116 | Function assay | 2.5 uM | 30 mins | Inhibition of IP6K2 in human [3H]-inositol-labelled HCT116 cells assessed as reduction in insp7 levels at 2.5 uM after 30 mins by HPLC analysis | 30624931 | |
| HEK293 | Function assay | 2.5 uM | 3.5 hrs | Inhibition of IP6K2 in [3H]-inositol-labelled HEK293 cells assessed as reduction in insp7 levels at 2.5 uM after 3.5 hrs by HPLC analysis relative to control | 30624931 | |
| 3T3-L1 | Function assay | 2.5 uM | 3 hrs | Activation of AKT activity in mouse 3T3-L1 cells assessed as increase in AKT phosphorylation at T308 residues at 2.5 uM after 3 hrs by Western blot analysis | 30624931 | |
| 3T3-L1 | Function assay | 1 uM | 3 hrs | Inhibition of IP6K2 in mouse 3T3-L1 cells assessed as AKT phosphorylation at T308 at 1 uM after 3 hrs by Western blot analysis | 30624931 | |
| HCT116 | Function assay | 2.5 uM | 3.5 hrs | Inhibition of IP6K2 in human [3H]-inositol-labelled HCT116 cells assessed as reduction in insp7 levels at 2.5 uM after 3.5 hrs by HPLC analysis relative to control | 30624931 | |
| Jurkat | Function assay | 24 hrs | Inhibition of chymotrypsin-like activity of human 26S proteasome in human Jurkat cells assessed as decrease in AMC hydrolysis using Z-Gly-Gly-Leu-AMC as substrate after 24 hrs by fluorescence based method, IC50=2μM | 30776692 | ||
| Jurkat | Function assay | 2 hrs | Inhibition of chymotrypsin-like activity of purified human 20S proteasome expressed in human Jurkat cells assessed as decrease in AMC hydrolysis using Suc-Leu-Leu-Val-Tyr-AMC as substrate incubated for 2 hrs by fluorescence based method, IC50=3.5μM | 30776692 | ||
| CGN | Neuroprotective assay | 5 to 100 uM | 24 hrs | Neuroprotective activity in Sprague-Dawley rat CGN cells assessed as protection against H2O2-induced cytotoxicity by measuring increase in cell viability at 5 to 100 uM pre-incubated for 24 hrs before H2O2 stimulation for 24 hrs by MTT assay | 30935792 | |
| HEK293 | Function assay | 30 mins | Inhibition of human TRPC5 expressed in HEK293 cells assessed as reduction in gadolinium-induced calcium entry after 30 mins by fluo-4 dye based fluorescence assay, IC50=6.5μM | 30943030 | ||
| EPG85-257RDB | Function assay | 72 hrs | Downregulation of ABCB1 gene expression in human EPG85-257RDB cells after 72 hrs by RT-PCR analysis, IC50=12μM | 31103904 | ||
| PC12 | Neuroprotective assay | 10 uM | 3 hrs | Neuroprotective activity in rat PC12 cells assessed as protection against H2O2-induced cytotoxicity at 10 uM pre-incubated for 3 hrs before H2O2 addition and measured after 12 hrs by MTT assay | 31128990 | |
| SH-SY5Y | Neuroprotective assay | 100 uM | 1 hr | Neuroprotective activity against H2O2-induced oxidative stress in human SH-SY5Y cells assessed as reduction in ROS generation at 100 uM preincubated for 1 hr followed by DCFH-DA addition for 30 mins and subsequent co-treatment with compound and H2O2 for 3 | 31158754 | |
| HT22 | Neuroprotective assay | 25 uM | 24 hrs | Neuroprotection against glutamate-induced cell death in mouse HT22 cells assessed as increase in cell viability at 25 uM measured after 24 hrs by MTT assay | 31609115 | |
| HT22 | Neuroprotective assay | 25 uM | 24 hrs | Neuroprotective activity at mouse HT22 cells assessed as reduction in glutamate-induced oxidative stress by measuring cell viability at 25 uM incubated for 24 hrs by MTT assay | 31609608 | |
| PANC1 | Anti-austerity assay | 24 hrs | Anti-austerity activity against nutrient-deprived human PANC1 cells assessed as cell death incubated for 24 hrs by WST-8 assay, PC50=21.8μM | 31682126 | ||
| Click to View More Cell Line Experimental Data | ||||||
|
In vitro |
DMSO
: 60 mg/mL
(198.51 mM)
Water : Insoluble Ethanol : Insoluble |
|
In vivo |
|||||
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
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Note: 1. Please make sure the liquid is clear before adding the next solvent.
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| Molecular Weight | 302.24 | Formula | C15H10O7 |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 117-39-5 | Download SDF | Storage of Stock Solutions |
|
|
| Targets/IC50/Ki |
Sirtuin
Src
PKC
PI3Kγ
(Cell-free assay) 2.4 μM
PI3Kδ
(Cell-free assay) 3.0 μM
PI3Kβ
(Cell-free assay) 5.4 μM
|
|---|---|
| In vitro |
Quercetin is a type of plant-based chemical, or phytochemical, known as a flavonol and a plant-derived flavonoid found in fruits, vegetables, leaves and grains. It also may be used as an ingredient in supplements, beverages or foods. In several studies, it may have anti-inflammatory and antioxidant properties, and it is being investigated for a wide range of potential health benefits. This compound is a PI3K inhibitor with IC50 of 2.4 – 5.4 μM. It strongly abrogated PI3K and Src kinases, mildly inhibited Akt1/2, and slightly affected PKC, p38 and ERK1/2. This chemical inhibits TNF-induced LDH% release, EC-dependent neutrophils adhesion to bovine pulmonary artery endothelial cells (BPAEC), and BPAEC DNA synthesis and proliferation. |
| In vivo |
Combination of Quercetin (75 mg/kg) and 2-Methoxyestradiol enhances inhibition of human prostate cancer LNCaP and PC-3 cells xenograft tumor growth. LD50: >3000mg/kg (i.g.) |
References |
|
| Methods | Biomarkers | Images | PMID |
|---|---|---|---|
| Western blot | Bcl-2 / Bax / Bcl-xl p-p53 / p53 / p21 p-JAK1 / p-STAT3 / STAT3 / VEGF Her-2 / p-PI3K / p-Akt / Akt |
|
27175602 |
| Growth inhibition assay | Cell viability Cell viability |
|
27175602 |
(data from https://clinicaltrials.gov, updated on 2024-05-22)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06003270 | Recruiting | Chronic Obstructive Pulmonary Disease|Emphysema|Chronic Bronchitis With Airway Obstruction |
Temple University|National Center for Complementary and Integrative Health (NCCIH)|Quercegen Pharmaceuticals |
November 1 2023 | Phase 2 |
| NCT04907253 | Active not recruiting | Coronary Artery Disease |
Montreal Heart Institute |
June 4 2021 | Phase 2 |
| NCT04474626 | Withdrawn | Sickle Cell Disease|Sickle Cell-Beta0-Thalassemia |
Jeffrey Zwicker MD|Quercegen Pharmaceuticals|Dana-Farber Cancer Institute |
December 2020 | Phase 2 |
| NCT04063124 | Completed | Alzheimer Disease |
The University of Texas Health Science Center at San Antonio|Mayo Clinic |
February 14 2020 | Phase 1|Phase 2 |
| NCT03989271 | Recruiting | Chronic Obstructive Pulmonary Disease |
Temple University|National Institutes of Health (NIH)|Quercegen Pharmaceuticals|National Center for Complementary and Integrative Health (NCCIH) |
October 1 2019 | Phase 1|Phase 2 |
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