Home PI3K/Akt/mTOR ATM/ATR activator - Autophagy inhibitor - TLR inhibitor - Anti-infection inhibitor - COVID-19 inhibitor Chloroquine diphosphate For research use only.

Chloroquine diphosphate

Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. Chloroquine is also an inhibitor of toll-like receptors (TLRs).

Chloroquine diphosphate Chemical Structure

Chloroquine diphosphate Chemical Structure

CAS No. 50-63-5

Purity & Quality Control

Chloroquine diphosphate Related Products

Signaling Pathway

ATM/ATR Signaling Pathways

ATM/ATR Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human K562 cells Cytotoxic assay Cytotoxicity against human K562 cells by MTT assay, IC50=31.83 nM 18538567
human KB cells Cytotoxic assay Cytotoxicity against human KB cells by microplate method, IC50=0.6 μM 14640524
human MDA-MB-468 cells Cytotoxic assay 48 h Cytotoxicity against human MDA-MB-468 cells after 48 hrs by SRB assay in presence of 3.5 uM 4-(2-chloro-10H-phenoxazin-10-yl)-N,N-diethylbutan-1-amine hydrochloride, GI50=2.81 μM 19945197
human MCF7 cells Cytotoxic assay 48 h Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay in presence of 0.4 uM 1-(1-(4-(7-phenyl-1H-imidazo[4,5-g]quinoxalin-6-yl)benzyl)piperidin-4-yl)-1H-benzo[d]imidazol-2(3H)-one, GI50=5.51 μM 19945197
human MDA-MB-231 cells Cytotoxic assay 48 h Cytotoxicity against human MDA-MB-231 cells after 48 hrs by SRB assay in presence of 3.5 uM 4-(2-chloro-10H-phenoxazin-10-yl)-N,N-diethylbutan-1-amine hydrochloride, GI50=6.08 μM 19945197
human HeLa cells Cytotoxic assay Cytotoxicity against human HeLa cells assessed as growth inhibition by MTT assay, IC50=30 μM 24354322
human HepG2 cells Cytotoxic assay 48 h Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay, IC50=37.68 μM 23815186
mammary tumor FM3A Cytotoxicity assay Cytotoxicity of compound was tested against mouse mammary tumor FM3A cells, EC50 = 0.0000003 μM. 12570385
red blood cells Antiplasmodial assay 48 hrs Antiplasmodial activity against Plasmodium falciparum FcB1/Columbia infected in human red blood cells assessed as parasite growth inhibition after 48 hrs by [3H]-hypoxanthine incorporation assay, IC50 = 0.00011 μM. 25659770
red blood cells Antiplasmodial assay 48 hrs Antiplasmodial activity against chloroquine and pyrimethamine-resistant ring stage Plasmodium falciparum V1/S infected in human red blood cells after 48 hrs, IC50 = 0.0055 μM. 21207937
red blood cells Antimalarial assay Antimalarial activity against Plasmodium ovale ring stage infected in red blood cells in presence of AB+ human serum by drug susceptibility assay, IC50 = 0.0078 μM. 20937779
red blood cells Antimalarial assay 48 hrs Antimalarial activity against chloroquine-sensitive erythrocytic stage of Plasmodium falciparum NF54 infected in human red blood cells assessed as growth inhibition after 48 hrs by [3H]-hypoxanthine incorporation assay, IC50 = 0.0094 μM. 23685569
red blood cells Antimalarial assay 48 hrs Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 infected in human O positive red blood cells assessed as inhibition of [3H]-hypoxanthine uptake after 48 hrs, IC50 = 0.01 μM. 21155593
red blood cells Antimalarial assay Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 infected in red blood cells after 72 hrs by Malstat reagent based LDH assay, IC50 = 0.011 μM. 28222317
red blood cells Antimalarial assay 72 hrs Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in human type A-positive red blood cells assessed as growth inhibition after 72 hrs by spectrophotometrically, IC50 = 0.012 μM. 25311562
red blood cells Antimalarial assay Antimalarial activity against Plasmodium malariae ring stage infected in red blood cells in presence of AB+ human serum by drug susceptibility assay, IC50 = 0.014 μM. 20937779
red blood cells Antiplasmodial assay 48 hrs Antiplasmodial activity against chloroquine-sensitive, mefloquine-resistant ring stage Plasmodium falciparum D6 infected in human red blood cells after 48 hrs, IC50 = 0.0142 μM. 21207937
red blood cells Antiplasmodial assay 72 hrs Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 infected in human red blood cells after 72 hrs by parasite lactate dehydrogenase assay, IC50 = 0.0143 μM. 22917857
red blood cells Antiplasmodial assay 48 hrs Antiplasmodial activity against asexual erythrocyte stage of chloroquine-sensitive Plasmodium falciparum NF54 infected in human red blood cells after 48 hrs by lactate dehydrogenase assay, IC50 = 0.016 μM. 30296683
red blood cells Antimalarial assay 96 hrs Antimalarial activity against wild type early trophozoite stage of Plasmodium falciparum D6 in human red blood cells assessed as [3H]hypoxanthine uptake after 96 hrs, IC50 = 0.017 μM. 23448281
FM3A Function assay Selectivity for FM3A cells over Plasmodium falciparum as mean EC50 ratio, IC50 = 0.019 μM. 12408708
red blood cells Antimalarial assay 48 hrs Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in human O positive red blood cells assessed as inhibition of [3H]-hypoxanthine uptake after 48 hrs, IC50 = 0.02 μM. 21155593
red blood cells Antimalarial assay 72 hrs Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D10 infected in human type A-positive red blood cells assessed as growth inhibition after 72 hrs by spectrophotometrically, IC50 = 0.02 μM. 25311562
red blood cells Antimalarial assay Antimalarial activity against ring stage Plasmodium falciparum 3D7 infected with human red blood cells incubated for 48 hrs by SYBR Green method, IC50 = 0.023 μM. 25725608
red blood cells Antimalarial assay Antimalarial activity against Plasmodium ovale trophozoite stage infected in red blood cells in presence of AB+ human serum by drug susceptibility assay, IC50 = 0.0232 μM. 20937779
red blood cells Antimalarial assay Antimalarial activity against Plasmodium falciparum 3D7 A infected in red blood cells assessed as inhibition of [3H]hypoxanthine incorporation after 24 hrs by scintillation counting, IC50 = 0.024 μM. 24900261
red blood cells Antimalarial assay 48 hrs Antimalarial activity against chloroquine-sensitive Plasmodium falciparum Nigerian infected in human red blood cells after 48 hrs by [3H]-hypoxanthine incorporation assay, IC50 = 0.025 μM. 28800458
red blood cells Antiplasmodial assay 48 hrs Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in human red blood cells assessed as reduction in parasite growth after 48 hrs by Hoechst 33342 staining based flow cytometric analysis, IC50 = 0.026 μM. 30199706
HCT-8 Antimicrobial assay 48 hrs Antimicrobial activity against Cryptosporidium parvum infected in human HCT-8 cells after 48 hrs by ELISA, IC50 = 0.027 μM. 18591280
red blood cells Antimalarial assay 72 hrs Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D10 infected in human type A-positive red blood cells assessed as parasite lactate dehydrogenase activity after 72 hrs by spectrophotometric analysis, IC50 = 0.029 μM. 22054038
red blood cells Antimalarial assay 72 hrs Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D10 infected in human A-positive red blood cells after 72 hrs by lactate dehydrogenase assay, IC50 = 0.03 μM. 21123074
red blood cells Antimalarial assay Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in red blood cells after 72 hrs by SYBR green 1 staining based fluorometric assay, IC50 = 0.03 μM. 27692831
3D7 Antiplasmodial assay Antiplasmodial activity against Plasmodium falciparum 3D7 ring stage cells assessed as reduction parasitemia by Malstat assay, IC50 = 0.03 μM. 22858300
red blood cells Antimalarial assay Antimalarial activity against Plasmodium falciparum 3D7A infected in red blood cells assessed as inhibition of parasite growth after 24 hrs by [3H]hypoxanthine incorporation assay, IC50 = 0.036 μM. 25906200
red blood cells Antimalarial assay Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 infected in human red blood cells assessed as reduction in parasitic LDH activity by Malstat reagent based spectrophotometric method, IC50 = 0.04 μM. 28800458
red blood cells Antiplasmodial assay Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D6 infected in red blood cells after 72 hrs by Malstat reagent based LDH assay, IC50 = 0.04 μM. 28315598
red blood cells Antiplasmodial assay Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D6 infected in red blood cells after 72 hrs by parasitic LDH assay, IC50 = 0.04 μM. 24900509
Vero Antimalarial assay 72 hrs Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 infected in African green monkey (Cercopithecus aethiops) Vero cells assessed as parasite LDH activity after 72 hrs, IC50 = 0.05 μM. 19833520
red blood cells Antiplasmodial assay 4 hrs Antiplasmodial activity against Plasmodium falciparum in human red blood cells after 4 hrs, IC50 = 0.055 μM. 17990865
red blood cells Antiplasmodial assay 48 hrs Antiplasmodial activity against chloroquine-sensitive ring stage Plasmodium falciparum 3D7 infected in human red blood cells after 48 hrs, IC50 = 0.089 μM. 21207937
B-cells Function assay Concentration required for half-maximal inhibition of CpG-ODN effect on thymidine uptake by WEHI 231 murine B-cells in the presence of alpha-sIgM., EC50 = 0.11 μM. 10406648
red blood cells Antiplasmodial assay 48 hrs Antiplasmodial activity against chloroquine and pyrimethamine resistant Plasmodium falciparum K1 infected in human red blood cells assessed as reduction in parasite viability after 48 hrs by [3H]-hypoxanthine incorporation assay, IC50 = 0.12 μM. 25746816
red blood cells Antiplasmodial assay 48 hrs Antiplasmodial activity against chloroquine/pyrimethamine-resistant Plasmodium falciparum K1 infected in human red blood cells assessed as [3H]-hypoxanthine incorporation incubated for 48 hrs prior to [3H]-hypoxanthine addition measured after 24 hrs by li, IC50 = 0.125 μM. 24268543
red blood cells Antimalarial assay Antimalarial activity against Plasmodium malariae trophozoite stage infected in red blood cells in presence of AB+ human serum by drug susceptibility assay, IC50 = 0.1279 μM. 20937779
red blood cells Antimalarial assay 48 hrs Antimalarial activity against chloroquine-resistant Plasmodium falciparum FcB1 infected in human red blood cells after 48 hrs by [3H]-hypoxanthine incorporation assay, IC50 = 0.132 μM. 28800458
red blood cells Antiplasmodial assay 48 hrs Antiplasmodial activity against chloroquine-resistant ring stage Plasmodium falciparum W2 infected in human red blood cells after 48 hrs, IC50 = 0.138 μM. 21207937
red blood cells Antiplasmodial assay 48 hrs Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human red blood cells assessed as inhibition of ring-stage parasite growth after 48 hrs by flow cytometry, IC50 = 0.14 μM. 21295887
RPMI1640 Antiparasitic assay 72 hrs Antiparasitic activity against chloroquine-resistant erythrocytic stage of Plasmodium falciparum K1 infected in human RPMI1640 cells after 72 hrs by NBT staining based spectroscopic analysis, IC50 = 0.14 μM. 26922226
red blood cells Antiplasmodial assay 48 hrs Antiplasmodial activity against chloroquine/pyrimethamine resistant Plasmodium falciparum K1 infected in human red blood cells after 48 hrs by [3H]hypoxanthine incorporation assay, IC50 = 0.15 μM. 27344215
red blood cells Antiplasmodial assay 48 hrs Antiplasmodial activity against asexual erythrocyte stage of chloroquine-resistant Plasmodium falciparum Dd2 infected in human red blood cells after 48 hrs by lactate dehydrogenase assay, IC50 = 0.15 μM. 30296683
red blood cells Antimalarial assay 48 hrs Antimalarial activity against multidrug-resistant Plasmodium falciparum K1 infected in human red blood cells assessed as 3H-hypoxanthine incorporation after 48 hrs by liquid scintillation counting, IC50 = 0.17 μM. 21644541
L6 Antiparasitic assay 48 hrs Antiparasitic activity against Plasmodium falciparum K1 infected in rat L6 cells assessed as inhibition of parasite growth preincubated for 48 hrs before [3H]hypoxanthine addition measured after 24 hrs by [3H]hypoxanthine incorporation assay, IC50 = 0.178 μM. 21937228
L6 Cytotoxicity assay Cytotoxicity against rat L6 cells by alamar blue assay, IC50 = 0.1885 μM. 17178177
red blood cells Antiplasmodial assay 48 hrs Antiplasmodial activity against the multidrug-resistant Plasmodium falciparum FRC-3 infected in human red blood cells assessed as reduction in parasite growth after 48 hrs by Hoechst 33342 staining based flow cytometric analysis, IC50 = 0.207 μM. 30199706
red blood cells Antimalarial assay 48 hrs Antimalarial activity against chloroquine-resistant erythrocytic stage of Plasmodium falciparum K1 infected in human red blood cells assessed as growth inhibition after 48 hrs by [3H]-hypoxanthine incorporation assay, IC50 = 0.21 μM. 23685569
red blood cells Antiplasmodial assay 48 hrs Antiplasmodial activity against chloroquine- and pyrimethamine-resistant Plasmodium falciparum K1 infected in human red blood cells assessed as [3H]hypoxanthine incorporation after 48 hrs by liquid scintillation counting, IC50 = 0.22 μM. 21438586
red blood cells Antimalarial assay Antimalarial activity against ring stage Plasmodium falciparum W2 infected with human red blood cells incubated for 48 hrs by flow cytometry, IC50 = 0.229 μM. 25725608
L6 Antiparasitic assay Antiparasitic activity against chloroquine, pyrimethamine-resistant Plasmodium falciparum K1 erythrocyte stage infected rat L6 cells, IC50 = 0.23 μM. 17949068
L6 Antiplasmodial assay Antiplasmodial activity against chloroquine and pyrimethamine-resistant Plasmodium falciparum K1 infected in rat L6 cells, IC50 = 0.25 μM. 19942439
red blood cells Antimalarial assay 72 hrs Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human A-positive red blood cells after 72 hrs by lactate dehydrogenase assay, IC50 = 0.25 μM. 21123074
red blood cells Antimalarial assay 48 hrs Antimalarial activity against chloroquine-resistant Plasmodium falciparum FcM29 infected in human red blood cells after 48 hrs by [3H]-hypoxanthine incorporation assay, IC50 = 0.26 μM. 28800458
red blood cells Antimalarial assay 48 hrs Antimalarial activity against multidrug-resistant Plasmodium falciparum TM90-C2B infected in human O positive red blood cells assessed as inhibition of [3H]-hypoxanthine uptake after 48 hrs, IC50 = 0.28 μM. 21155593
red blood cells Antimalarial assay 48 hrs Antimalarial activity against ring stage Plasmodium falciparum Dd2 infected with human red blood cells incubated for 48 hrs by SYBR Green method, IC50 = 0.285 μM. 25725608
red blood cells Antimalarial assay 96 hrs Antimalarial activity against chloroquine and pyrimethamine-resistant early trophozoite stage of Plasmodium falciparum W2 in human red blood cells assessed as [3H]hypoxanthine uptake after 96 hrs, IC50 = 0.29 μM. 23448281
red blood cells Antimalarial assay 72 hrs Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human type A-positive red blood cells assessed as growth inhibition after 72 hrs by spectrophotometrically, IC50 = 0.316 μM. 25311562
red blood cells Antimalarial assay 72 hrs Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 infected in red blood cells after 72 hrs by Malstat reagent based LDH assay, IC50 = 0.317 μM. 28222317
red blood cells Antiplasmodial assay 72 hrs Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human red blood cells after 72 hrs by parasite lactate dehydrogenase assay, IC50 = 0.3171 μM. 22917857
red blood cells Antiplasmodial assay 72 hrs Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 infected in red blood cells after 72 hrs by parasitic LDH assay, IC50 = 0.39 μM. 24900509
red blood cells Antimalarial assay 48 hrs Antimalarial activity against chloroquine and pyrimethamine-resistant Plasmodium falciparum K1 infected in human O positive red blood cells assessed as inhibition of [3H]-hypoxanthine uptake after 48 hrs, IC50 = 0.4 μM. 21155593
red blood cells Antimalarial assay Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human red blood cells assessed as reduction in parasitic LDH activity by Malstat reagent based spectrophotometric method, IC50 = 0.42 μM. 28800458
red blood cells Antiplasmodial assay 72 hrs Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 infected in red blood cells after 72 hrs by Malstat reagent based LDH assay, IC50 = 0.43 μM. 28315598
Vero Antimalarial assay 72 hrs Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 infected in African green monkey (Cercopithecus aethiops) (Cercopithecus aethiops) Vero cells assessed as parasite LDH activity after 72 hrs, IC50 = 0.484 μM. 19833520
HEK293 Cytotoxicity assay 72 hrs Cytotoxicity against HEK293 cells after 72 hrs by resazurin dye based assay, IC50 = 0.49 μM. 29236492
red blood cells Antimalarial assay 72 hrs Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human type A-positive red blood cells assessed as parasite lactate dehydrogenase activity after 72 hrs by spectrophotometric analysis, IC50 = 0.52 μM. 22054038
red blood cells Antiplasmodial assay 48 hrs Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human red blood cells after 48 hrs by SYBR test, IC50 = 0.59 μM. 26988303
red blood cells Antimalarial assay 48 hrs Antimalarial activity against multidrug-resistant Plasmodium falciparum TM93-C1088 infected in human O positive red blood cells assessed as inhibition of [3H]-hypoxanthine uptake after 48 hrs, IC50 = 0.62 μM. 21155593
Dd2 Antiplasmodial assay Antiplasmodial activity against drug resistant Plasmodium falciparum Dd2 ring stage cells assessed as reduction parasitemia by Malstat assay, IC50 = 0.71 μM. 22858300
red blood cells Antimalarial assay 72 hrs Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 infected in red blood cells after 72 hrs by SYBR green 1 staining based fluorometric assay, IC50 = 0.75 μM. 27692831
red blood cells Antimalarial assay 48 hrs Antimalarial activity against chloroquine, pyrimethamine, and mefloquine-resistant Plasmodium falciparum Dd2 infected in human O positive red blood cells assessed as inhibition of [3H]-hypoxanthine uptake after 48 hrs, IC50 = 0.98 μM. 21155593
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells expressing CD81 assessed as cell viability after 72 hrs by CellTiter-glo assay, CC50 = 1.6 μM. 25791675
HepG2 Antiplasmodial assay 48 hrs Antiplasmodial activity against liver stage of Plasmodium yoelii 17X NL sporozoites infected in human HepG2 cells expressing CD81 after 48 hrs by DAPI staining-based immunofluorescence analysis, IC50 = 1.65 μM. 25791675
WI38 Antiviral assay 2 hrs Antiviral activity against BKV Gardner ATCC VR837 infected in human WI38 cells assessed as reduction in viral DNA level preincubated for 2 hrs before viral infection measured after 7 days by real time PCR assay, EC50 = 1.7 μM. 17893158
HeLa Growth inhibition assay 48 hrs Growth inhibition of human HeLa cells after 48 hrs by MTT assay in presence of 100 uM ZnCl2, GI50 = 2.1 μM. 19748786
SMB Antiprion assay Antiprion activity against Chandler strain of sheep scrapie prion protein infected in mouse SMB cells assessed as clearance of disease-associated scrapie prion protein, EC50 = 2.3 μM. 21570837
HEK293 Function assay Inhibition of human ERG expressed in HEK293 cells assessed as reduction in tail current at membrane potential of +20 mV, IC50 = 2.5 μM. 25746816
red blood cells Antimalarial assay 24 hrs Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in red blood cells assessed as reduction in mature schizonts formation after 24 hrs by Giemsa-staining based assay, EC50 = 2.97 μM. 29499486
HEK293 Function assay hERG binding assays: Displacement of [3H]-Dofetilide (5 nM final) from hERG membranes obtained from HEK293 cells, Ki = 3.16228 μM. 32353859
1205 Lu Cytotoxicity assay 72 hrs Cytotoxicity against human 1205 Lu cells after 72 hrs by MTT assay, IC50 = 3.6 μM. 25699157
LN229 Cytotoxicity assay 72 hrs Cytotoxicity against human LN229 cells after 72 hrs by MTT assay, IC50 = 3.6 μM. 25699157
C8161 Cytotoxicity assay 72 hrs Cytotoxicity against human C8161 cells after 72 hrs by MTT assay, IC50 = 3.6 μM. 25699157
HT-29 Cytotoxicity assay 72 hrs Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 3.6 μM. 25699157
WI38 Cytotoxicity assay 24 hrs Cytotoxicity against human WI38 cells assessed as inhibition of proliferation after 24 hrs by SRB assay, IC50 = 3.63 μM. 25461309
ScN2a Function assay Half maximal inhibition of Prion protein PrPsc formation was assayed in ScN2a cells, EC50 = 4 μM. 12904059
HepG2 Cytotoxicity assay 24 hrs Cytotoxicity against human HepG2 cells after 24 hrs by neutral red dye uptake assay, TC50 = 4.3 μM. 22783984
HeLa Growth inhibition assay 48 hrs Growth inhibition of human HeLa cells after 48 hrs by MTT assay in presence of 50 uM CuCl2, GI50 = 4.4 μM. 19748786
HeLa Growth inhibition assay 48 hrs Growth inhibition of human HeLa cells after 48 hrs by MTT assay in presence of 10 uM CuCl2, GI50 = 5.3 μM. 19748786
HeLa Growth inhibition assay 48 hrs Growth inhibition of human HeLa cells after 48 hrs by MTT assay in presence of 50 uM ZnCl2, GI50 = 5.6 μM. 19748786
HeLa Growth inhibition assay 48 hrs Growth inhibition of human HeLa cells after 48 hrs by MTT assay in presence of 1 uM CuCl2, GI50 = 6.1 μM. 19748786
SH-SY5Y Function assay 24 hrs Modulation of human wild-type APP695 expressed in SH-SY5Y cells assessed as inhibition of amyloid beta (1 to 40 residues) production measured after 24 hrs, IC50 = 7 μM. 29559198
SH-SY5Y Function assay 24 hrs Inhibition of BACE1 in human SH-SY5Y cells harboring wild type APP695 assessed as reduction in amyloid beta (1 to 40) level after 24 hrs by ELISA method, IC50 = 7 μM. 30268822
CHO Function assay Inhibition of human ERG expressed in CHO cells, Ki = 7.5 μM. 24900603
L6 Cytotoxicity assay Cytotoxicity against L6 cells, IC50 = 7.7 μM. 17280835
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells after 72 hrs by alamar blue assay, IC50 = 8.3 μM. 21155593
WI38 Cytotoxicity assay 2 hrs Cytotoxicity against human WI38 cells assessed as reduction in cellular DNA level preincubated for 2 hrs before viral infection measured after 7 days by real time PCR assay, CC50 = 8.5 μM. 17893158
HepG2 Antimalarial assay Antimalarial activity against sporozoite stage of Plasmodium berghei yoelii infected in human HepG2 cells, IC50 = 9 μM. 26640981
SKHep Growth inhibition assay 48 hrs Growth inhibition of human SKHep cells after 48 hrs by MTT assay in presence of 10% FBS supplemented DMEM medium, GI50 = 9.5 μM. 19748786
HeLa Cytotoxicity assay 7 hrs Cytotoxicity against human HeLa cells assessed as cell survival after 7 hrs by MTT assay, IC50 = 9.665 μM. 17768052
HeLa Cytotoxicity assay 7 days Cytotoxicity against human HeLa cells after 7 days by MTT assay, IC50 = 9.67 μM. 21489789
K562 Cytotoxicity assay 24 hrs Cytotoxicity against human K562 cells assessed as radioactive thymidine incorporation after 24 hrs, CC50 = 9.7 μM. 18680278
Vero Antiviral assay 6 to 7 days Antiviral activity against chikungunya virus Indian ocean strain 899 infected in Vero cells assessed as virus-induced cytopathic effect after 6 to 7 days, EC50 = 10 μM. 25970561
PDAC Function assay Inhibition of cell proliferation of PDAC cells (unknown origin), IC50 = 10 μM. 26135471
Vero Antiviral assay 6 to 7 days Antiviral activity against Chikungunya virus 899 infected in African green monkey Vero cells assessed as inhibition of virus-induced cell death after 6 to 7 days by MTS assay, EC50 = 10 μM. 24926807
HepG2 Cytotoxicity assay 48 hrs Cytotoxicity against human HepG2 cells after 48 hrs by CellTiter-Glo assay, EC50 = 10.1 μM. 29800827
BT-483 Growth inhibition assay 48 hrs Growth inhibition of human BT-483 cells after 48 hrs by MTT assay in presence of 10% FBS supplemented DMEM medium, GI50 = 10.2 μM. 19748786
Vero Antiviral assay 5 days Antiviral activity against Chikungunya virus Indian Ocean 889 infected in African green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTS/PMS method, EC50 = 11 μM. 29336951
Vero A Antiviral assay 6 to 7 days Antiviral activity against Chikungunya virus Indian ocean strain 899 infected in African green monkey Vero A cells assessed as reduction in viral-induced cytopathic effect after 6 to 7 days by MTS/PMS assay, EC50 = 11 μM. 28671832
Vero Antiviral assay 5 days Antiviral activity against Chikungunya virus Indian Ocean strain 899 infected in African green monkey Vero cells assessed as inhibition of viral-induced cytopathic effect measured on day 5 post infection by MTS/PMS assay, EC50 = 11 μM. 29499487
Vero Antiviral assay 7 days Antiviral activity against Chikungunya virus Indian Ocean strain 899 infected in African green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect after 7 days by MTS/PMS method, EC50 = 11 μM. 24800626
Vero Antiviral assay 7 days Antiviral activity against Sindbis virus strain HRsp infected in african green monkey Vero cells assessed as inhibition of virus induced cell death measured after 7 days, EC50 = 11 μM. 25946116
Vero Antiviral assay 7 days Antiviral activity against Chikungunya virus strain 899 infected in african green monkey Vero cells assessed as inhibition of virus induced cell death measured after 7 days, EC50 = 11 μM. 25946116
Vero Antiviral assay 6 to 7 days Antiviral activity against Sindbis virus HRsp infected in African green monkey Vero cells assessed as inhibition of virus-induced cell death after 6 to 7 days by MTS assay, EC50 = 11 μM. 24926807
Vero Antiviral assay 6 to 7 days Antiviral activity against Sindbis virus HRsp infected in african green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect incubated for 6 to 7 days by MTS assay, EC50 = 11 μM. 23215460
Vero Antiviral assay 6 to 7 days Antiviral activity against Chikungunya virus 899 infected in african green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect incubated for 6 to 7 days by MTS assay, EC50 = 11 μM. 23215460
red blood cells Antimalarial assay 48 hrs Antimalarial activity against chloroquine-resistant Plasmodium falciparum K14 infected in human red blood cells after 48 hrs by [3H]hypoxanthine incorporation assay, IC50 = 11 μM. 25282260
red blood cells Antimalarial assay 24 hrs Antimalarial activity against chloroquine-resistant Plasmodium falciparum RKL9 infected in red blood cells assessed as reduction in mature schizonts formation after 24 hrs by Giemsa-staining based assay, EC50 = 11.25 μM. 29499486
MCF7 Cytotoxicity assay Cytotoxicity against human MCF7 cells assessed as [3H]hypoxanthine incorporation, IC50 = 12 μM. 18512987
HEK293 Cytotoxicity assay 72 hrs Cytotoxicity against human HEK293 cells after 72 hrs by alamar blue assay, IC50 = 12 μM. 21155593
Vero Antiviral assay 24 hrs Antiviral activity against Zika virus infected in African green monkey Vero cells assessed as inhibition of viral RNA replication after 24 hrs by RT-PCR method, EC50 = 12 μM. 28068604
Vero Antiviral assay 24 hrs Antiviral activity against Zika virus infected in African green monkey Vero cells assessed as inhibition of viral RNA replication after 24 hrs by RT-PCR method, EC50 = 12 μM. 28092859
HeLa Antiviral assay 48 hrs Antiviral activity against VSV-G pseudotyped HIV1 lentiviral particles infected in human HeLa cells incubated for 48 hrs by spectrofluorometry, IC50 = 12.48 μM. 22858300
SH-SY5Y Function assay 24 hrs Inhibition of BACE1 in human SH-SY5Y cells harboring wild type APP695 assessed as reduction in amyloid beta (1 to 42) level after 24 hrs by ELISA method, IC50 = 12.7 μM. 30268822
SH-SY5Y Function assay 24 hrs Modulation of human wild-type APP695 expressed in SH-SY5Y cells assessed as inhibition of amyloid beta (1 to 42 residues) production measured after 24 hrs by ELISA, IC50 = 12.8 μM. 29559198
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells after 72 hrs by Alamar Blue assay, IC50 = 12.9 μM. 21190857
Vero Antiviral assay 6 to 7 days Antiviral activity against Semliki forest virus Vietnam infected in African green monkey Vero cells assessed as inhibition of virus-induced cell death after 6 to 7 days by MTS assay, EC50 = 13.8 μM. 24926807
Vero Antiviral assay 7 days Antiviral activity against Semliki forest virus strain Vietnam infected in african green monkey Vero cells assessed as inhibition of virus induced cell death measured after 7 days, EC50 = 14 μM. 25946116
Vero Antiviral assay 6 to 7 days Antiviral activity against Semliki forest virus infected in african green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect incubated for 6 to 7 days by MTS assay, EC50 = 14 μM. 23215460
NSO Cytotoxicity assay Cytotoxicity against mouse NSO cells by MTT assay, TC50 = 14.9 μM. 19113955
L1210 Cytotoxicity assay Cytotoxicity against mouse L1210 cells assessed as inhibition of cell proliferation by Coulter counter analysis, IC50 = 15 μM. 26114811
Huh-7 Antiplasmodial assay 48 hrs Antiplasmodial activity against Plasmodium berghei liver stage form transfected in human Huh-7 cells assessed as cell viability after 48 hrs by luciferase reporter gene assay, IC50 = 15.9 μM. 23273038
Daudi Cytotoxicity assay Cytotoxicity against human Daudi cells by MTT assay, TC50 = 16.7 μM. 19113955
HeLa Cytotoxicity assay Cytotoxicity against human HeLa cells assessed as inhibition of cell proliferation by Coulter counter analysis, IC50 = 18 μM. 26114811
J774.1 Cytotoxicity assay 24 hrs Cytotoxicity against mouse J774.1 cells after 24 hrs by AlamarBlue based cytotoxicity assay, IC50 = 18.4 μM. 27316542
HeLa Growth inhibition assay 48 hrs Growth inhibition of human HeLa cells after 48 hrs by MTT assay in presence of 10% FBS supplemented DMEM medium, GI50 = 18.6 μM. 19748786
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, CC50 = 19.4 μM. 20014857
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells after 48 hrs by XTT reduction assay, CC50 = 19.4 μM. 24686013
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells assessed as decrease in cell viability after 48 hrs by XTT assay, CC50 = 19.4 μM. 24594524
MDA-MB-468 Antiproliferative assay 72 hrs Antiproliferative activity against human MDA-MB-468 cells after 72 hrs by SRB assay, IC50 = 19.86 μM. 26602827
KB Cytotoxicity assay 48 hrs Cytotoxicity against human KB cells after 48 hrs by MTT assay, IC50 = 20.4 μM. 11809075
Vero Antiviral assay 5 days Antiviral activity against Chikungunya virus Indian Ocean 889 infected in African green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTS/PMS method, EC90 = 21 μM. 29336951
Vero Antiviral assay Antiviral activity against Chikungunya virus Indian Ocean strain 899 infected in African green monkey Vero cells assessed as inhibition of viral-induced cytopathic effect measured on day 5 post infection by MTS/PMS assay, EC90 = 21 μM. 29499487
Vero Antiviral assay 7 days Antiviral activity against Chikungunya virus Indian Ocean strain 899 infected in African green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect after 7 days by MTS/PMS method, EC90 = 21 μM. 24800626
Vero Cytotoxicity assay 72 hrs Cytotoxicity against african green monkey Vero cells assessed as growth inhibition after 72 hrs by MTS assay, IC50 = 21 μM. 23727538
HepG2 Cytotoxicity assay 48 hrs Cytotoxicity against human HepG2 cells after 48 hrs by lactate dehydrogenase assay, GI50 = 22.16 μM. 21882831
KB Cytotoxicity assay 72 hrs Cytotoxicity against human KB cells after 72 hrs by MTS assay, IC50 = 22.5 μM. 19879150
MDA-MB-231 Cytotoxicity assay 48 hrs Cytotoxicity against human MDA-MB-231 cells after 48 hrs by SRB assay, GI50 = 22.52 μM. 19804979
MDA-MB-231 Antiproliferative assay 48 hrs Antiproliferative activity against human p53, pRB mutant and estrogen receptor deficient MDA-MB-231 cells after 48 hrs by SRB assay, GI50 = 22.52 μM. 20561720
MDA-MB-231 Cytotoxicity assay 48 hrs Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 48 hrs by SRB assay, IC50 = 22.52 μM. 28586716
CEM Cytotoxicity assay Cytotoxicity against human CEM cells assessed as inhibition of cell proliferation by Coulter counter analysis, IC50 = 23 μM. 26114811
CE81T Growth inhibition assay 48 hrs Growth inhibition of human CE81T cells after 48 hrs by MTT assay in presence of 10% FBS supplemented DMEM medium, GI50 = 23.4 μM. 19748786
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells assessed as reduction in cell number incubated for 72 hrs, IC50 = 23.43 μM. 26135471
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells assessed as intracellular ATP level after 72 hrs by Celltiter-Glo luminescent assay, EC50 = 25 μM. 21910466
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells assessed as reduction in cell number incubated for 72 hrs, IC50 = 25 μM. 26135471
BxPC3 Antiproliferative assay 72 hrs Antiproliferative activity against human BxPC3 cells after 72 hrs by SRB method, IC50 = 25 μM. 25699157
MDA-MB-468 Cytotoxicity assay 48 hrs Cytotoxicity against human MDA-MB-468 cells after 48 hrs by SRB assay, GI50 = 28.58 μM. 19804979
MDA-MB-468 Cytotoxicity assay 48 hrs Cytotoxicity against human MDA-MB-468 cells after 48 hrs by SRB assay, GI50 = 28.58 μM. 20106668
MDA-MB-468 Cytotoxicity assay 48 hrs Cytotoxicity against human MDA-MB-468 cells assessed as growth inhibition after 48 hrs by SRB assay, IC50 = 28.58 μM. 28586716
K562 Cytotoxicity assay Cytotoxicity against human K562 cells by MTT assay, IC50 = 29.03 μM. 18562202
HeLa Antiproliferative assay 72 hrs Antiproliferative activity against human HeLa cells after 72 hrs by SRB assay, IC50 = 29.96 μM. 26602827
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, IC50 = 30 μM. 19482476
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, IC50 = 30 μM. 19926173
HepG2 Cytotoxicity assay Cytotoxicity against human HepG2 cells by MTT assay, IC50 = 30 μM. 17981462
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, CC50 = 30 μM. 21741131
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, CC50 = 30 μM. 22889559
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, CC50 = 30 μM. 24946216
SH-SY5Y Cytotoxicity assay 72 hrs Cytotoxicity against human SH-SY5Y cells after 72 hrs by MTT assay, CC50 = 30 μM. 29559198
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, CC50 = 30 μM. 24858543
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells measured after 72 hrs by MTT assay, CC50 = 30 μM. 27155463
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells assessed as cell viability after 72 hrs by MTT assay, CC50 = 30 μM. 25791675
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells incubated for 72 hrs by MTT assay, CC50 = 30 μM. 25282267
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, CC50 = 30 μM. 21852132
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, CC50 = 30 μM. 22608675
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay, CC50 = 30 μM. 27654395
KB Cytotoxicity assay Cytotoxicity against human KB cells by SRB assay, ED50 = 30.8 μM. 16562832
HepG2 Cytotoxicity assay 24 hrs Cytotoxicity against human HepG2 cells assessed as cell viability after 24 hrs by neutral red uptake assay, TC50 = 31 μM. 23145816
K562 Cytotoxicity assay 72 hrs Cytotoxicity against human K562 cells after 72 hrs by flow cytometry, IC50 = 32 μM. 19482476
K562 Cytotoxicity assay 72 hrs Cytotoxicity against human K562 cells after 72 hrs by flow cytometry, IC50 = 32 μM. 19926173
FM3A Antiproliferative assay Antiproliferative activity against Mouse mammary tumor FM3A cells, EC50 = 32 μM. 10966746
FM3A Cytotoxicity assay In vitro cytotoxicity against mouse mammary FM3A cells, EC50 = 32 μM. 12036365
FM3A Cytotoxicity assay Cytotoxicity against mouse mammary tumor FM3A cells representing a model of host, EC50 = 32 μM. 11855978
FM3A Cytotoxicity assay Cytotoxicity against FM3A mouse mammary cells, EC50 = 32 μM. 13678413
FM3A Cytotoxicity assay 48 hrs Cytotoxicity against mouse FM3A cells assessed as inhibition of increase in cell density after 48 hrs, EC50 = 32 μM. 18479926
FM3A Cytotoxicity assay Compound was tested for cytotoxicity against FM3A mouse mammary cells. , EC50 = 32 μM. 10447961
LNCAP Cytotoxicity assay 72 hrs Cytotoxicity against human LNCAP cells assessed as reduction in cell number incubated for 72 hrs, IC50 = 32.87 μM. 26135471
HCT116 Cytotoxicity assay 72 hrs Cytotoxicity against human HCT116 cells after 72 hrs by WST1 assay, IC50 = 33.7 μM. 12398531
KB Cytotoxicity assay 72 hrs Cytotoxicity against human KB cells after 72 hrs by SRB assay, ED50 = 33.7 μM. 9917283
KB Cytotoxicity assay 72 hrs Cytotoxicity against human KB cells after 72 hrs by Alamar blue assay, IC50 = 34 μM. 24900724
CHO Cytotoxicity assay Cytotoxicity against CHO cells by MTT assay, IC50 = 35.8 μM. 26832222
KB Cytotoxicity assay Cytotoxicity against human KB cells assessed as growth inhibition, IC50 = 35.95 μM. 21705220
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 36.1 μM. 19892554
MDA-MB-231 Antiproliferative assay 72 hrs Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay, IC50 = 36.53 μM. 26602827
NFF Cytotoxicity assay 3 days Cytotoxicity against human NFF cells after 3 days by sulforhodamine B assay, IC50 = 37.3 μM. 23117170
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay, GI50 = 38.44 μM. 19804979
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay, GI50 = 38.44 μM. 20106668
p53+/- MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human p53+/- MCF7 cells after 48 hrs by SRB assay, GI50 = 38.44 μM. 20561720
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by SRB assay, IC50 = 38.44 μM. 28586716
Caco2 Antiproliferative assay 2 days Antiproliferative activity against human Caco2 cells after 2 days by sulforhodamine B assay, GI50 = 38.67 μM. 24184076
THP1 Cytotoxicity assay Cytotoxicity against human THP1 cells by MTT assay, IC50 = 40 μM. 17981462
THP1 Cytotoxicity assay 72 hrs Cytotoxicity against human THP1 cells after 72 hrs by propidium iodide staining-based flow cytometry, IC50 = 40 μM. 19748781
THP1 Cytotoxicity assay 72 hrs Cytotoxicity against human THP1 cells assessed as cell viability after 72 hrs by Alamar blue assay, IC50 = 40 μM. 19914747
THP1 Cytotoxicity assay 72 hrs Cytotoxicity against human THP1 cells using propidium iodide staining after 72 hrs by flow cytometry, IC50 = 40 μM. 20638854
HEK293 Cytotoxicity assay 72 hrs Cytotoxicity against HEK293 cells assessed as cell growth inhibition after 72 hrs by Alamar blue assay, IC50 = 40 μM. 28774427
NCH-89 Antiproliferative assay 48 hrs Antiproliferative activity against human carmustine-resistant NCH-89 cells assessed as BrdU incorporation after 48 hrs, IC50 = 41.2 μM. 20329733
HepG2 Cytotoxicity assay 48 hrs Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth after 48 hrs by LDH assay, GI50 = 43.09 μM. 25684422
L6 Toxicity assay Toxicity against rat L6 cells, IC50 = 43.1 μM. 19781948
KB Cytotoxicity assay 72 hrs Cytotoxicity against human KB cells after 72 hrs by alamar blue assay, CC50 = 44 μM. 20014857
MKN28 Antiproliferative assay 2 days Antiproliferative activity against human MKN28 cells after 2 days by sulforhodamine B assay, GI50 = 44.44 μM. 24184076
NFF Cytotoxicity assay Cytotoxicity against human NFF cells, IC50 = 46.608 μM. 30245402
J774 Cytotoxicity assay 72 hrs Cytotoxicity against mouse J774 cells after 72 hrs by CellTiter-96 aqueous one solution cell proliferation assay, EC50 = 47.2 μM. 29215279
HEK293 Cytotoxicity assay 72 hrs Cytotoxicity against HEK293 cells after 72 hrs by Alamar Blue assay, IC50 = 48 μM. 21190857
MRC5 Cytotoxicity assay Cytotoxicity against MRC5 cells 17166718
HeLa Function assay 10 uM 1 hr Stimulation of reactive oxygen species in human HeLa cells at 10 uM in presence of 10 uM CuCl2 after 1 hr by dihydroethidium dye based fluorescence assay 19748786
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 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
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
HEK293 Autophagy assay 10 uM 8 hrs Induction of autophagy in HEK293 cells assessed as increase in p62 level at 10 uM after 8 hrs by immunoblot analysis 28481536
HEK293 Autophagy assay 10 uM 8 hrs Induction of autophagy in HEK293 cells assessed as increase in LC3-2 level at 10 uM after 8 hrs by immunoblot analysis 28481536
LNCAP Function assay Reduction in GFP expression in human LNCAP cells transfected with plasmids co-expressing GFP and shRNAs against REV-ERBbeta followed by compound treatment 24 hrs post-transfection and measured 48 hrs post dose 26135471
SKBR3 Function assay Reduction in GFP expression in human SKBR3 cells transfected with plasmids co-expressing GFP and shRNAs against REV-ERBbeta followed by compound treatment 24 hrs post-transfection and measured 48 hrs post dose 26135471
HepG2 Function assay Reduction in GFP expression in human HepG2 cells transfected with plasmids co-expressing GFP and shRNAs against REV-ERBbeta followed by compound treatment 24 hrs post-transfection and measured 48 hrs post dose 26135471
H460 Apoptosis assay 25 to 75 uM 24 hrs Induction of apoptosis in human H460 cells at 25 to 75 uM after 24 hrs by annexin-V staining-based flow cytometry 25699157
HepG2 Function assay 50 uM 6 hrs Reduction in lysosomal acidification in human HepG2 cells at 50 uM after 6 hrs by DAPI/lyso tracker red-double staining based confocal microscopic analysis relative to control 28197320
Click to View More Cell Line Experimental Data

Biological Activity

Description Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. Chloroquine is also an inhibitor of toll-like receptors (TLRs).
Targets
TLR3 [4] TLR7 [4] TLR8 [4] TLR9 [4] ATM [1]
(Cell-free assay)
In vitro
In vitro

Chloroquine is a chemotherapeutic agent for the clinical treatment of malaria. Chloroquine is able to bind to DNA, and inhibit DNA replication and RNA synthesis which in turn results in cell death. The effect of Chloroquine may also be related to the formation of a toxic heme-Chloroquine complex. Chloroquine inhibits trophozoite hemoglobin degradation through increasing vacuolar pH and inhibiting the activity of vacuolar phospholipase, vacuolar proteases, and heme polymerase[1].

Chloroquine possesses definite antirheumatic properties. Chloroquine has immuno-modulatory effects, suppressing the production/release of tumour necrosis factor and interleukin 6. Moreover, Chloroquine exerts direct antiviral effects, inhibiting pH-dependent steps of the replication of several viruses including members of the flaviviruses, retroviruses, and coronaviruses. Its best-studied effects are those against HIV replication[2].

Chloroquine can accumulate inside the macrophage phagolysosome by ion trapping where it exerts potent antifungal activity against Histoplasma capsulatum and Cryptococcus neoformans by distinct mechanisms. Chloroquine inhibits growth of H. capsulatum by pH-dependent iron deprivation, whereas it is directly toxic to C. neoformans[3].
Cell Research Cell lines Monocytes
Concentrations 20 μM
Incubation Time 1 h
Method

Cells were treated with indicated concentration of drug for 1 h.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p62 / LC3 ZEBRA / p-S824 KAP1 26677873
Immunofluorescence SQSTM1 / MAP1LC3B CD1d-β2m / LAMP1 p-S824 KAP1 / ZEBRA 29872540
Growth inhibition assay Cell viability 25521075
In Vivo
In vivo

Chloroquine has tumor‑inhibitory and tumor‑promoting effects in triple‑negative breast cancer.
Animal Research Animal Models Athymic nude/nu mice
Dosages 80 mg/kg
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05841758 Not yet recruiting
Sarcoidosis Pulmonary
Hospices Civils de Lyon
 April 1 2024 Phase 4
NCT04443270 Unknown status
COVID-19
CMN 20 de Noviembre
 July 27 2020 Phase 1
NCT04462367 Active not recruiting
COVID19|Coronavirus Infection|Pregnancy Disease|Severe Acute Respiratory Syndrome
Instituto Materno Infantil Prof. Fernando Figueira
 July 1 2020 --
NCT04340544 Terminated
COVID-19
University Hospital Tuebingen|Robert Bosch Medical Center|Universitätsklinikum Hamburg-Eppendorf|Bernhard Nocht Institute for Tropical Medicine
 April 22 2020 Phase 2
NCT04334148 Completed
COVID-19
Adrian Hernandez|Patient-Centered Outcomes Research Institute|Duke University
 April 22 2020 Phase 3

Chemical Information & Solubility

Molecular Weight 515.86 Formula

C18H26ClN3.2H3O4P
CAS No. 50-63-5 SDF Download Chloroquine diphosphate SDF
Smiles CCN(CC)CCCC(C)NC1=C2C=CC(=CC2=NC=C1)Cl.OP(=O)(O)O.OP(=O)(O)O
Storage (From the date of receipt)

In vitro
Batch:

Water : 100 mg/mL

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : Insoluble


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In vivo
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Tech Support

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