Camptothecin v 10 (> 10 M) 10 M > 10 M > 10 M DMSO Daunorubicin v < 0.33 M 1 M 0.33 M 1 M V 5.26 2.72 >10 >10 DMSO Doxorubicin V Ellipticine v V 10 M > 10 M 10 M > 10 M V 1.72 1.00 2.90 4.30 DMSO Etoposide v DMSO Irinotecan v V > 10 M > 10 M > 10 M > 10 M DMSO Mitoxantrone v < 0.33 M 3.3M 0.33 M 10 M V 6.91 7.94 6.55 >10 DMSO Piperlongumine v V V 8.12 8.05 >10 >10 DMSO Puromycin V Azacitidine v > 10 M > 10 M > 10 M > 10 M DMSO Alvespimycin V Anisomycin v V > 10 M 0.33 M 1 M > 10 M H2O Tanespimycin v V (HSP90 inhibitor) < 0.1 N/A Yes[24] Yes[24] > 1 M > 1 M < 0.033 M > 1 M DMSO Cephaeline V Ouabain v V DMSO Staurosporine Digoxin V Proscillaridin v V DMSO Strophanthidin v V DMSO Digitoxigenin v V DMSO Digoxigenin v V DMSO Chlorpromazine v V (Antipsychotic drugs) > 10 Effective Yes[36],[38] No V > 10 M > 10 M > 10 M > 10 M V >10 10 >10 >10 DMSO Niclosamide v DMSO Paroxetine Parthenolide v V V 10 6.79 >10 7.17 DMSO Resveratrol v DMSO Sulconazole v V (Antifungal agents) > 10 Effective No No V > 10 M > 10 M > 10 M > 10 M DMSO PA file cell lines : Mahlavu, PLC5, HepG2, and Huh7 Glycoside () Solvent Antineoplastic agent () Antibiotic () Alkaloid () Cardiotonic agent () Category Drug name MTT PLOSE ONE(15 drugs) Roger paper Lab IC50 (M) Drug Name Description Frequency* IC50 (uM) Clonogenic Assay** Tanespimycin HSP90 inhibitor 3 < 0.1 N/A Trichostatin A HDAC inhibitor 9 0.1~1 N/A Thioguanosine Purine analog 9 5~10 N/A Thioridazine Antipsychotic drugs 4 5~10 N/A Phenoxybenzamine Antihypertensive drugs 6 > 10 Effective Trifluoperazine Antipsychotic drugs 2 > 10 Effective Dipyridamole Platelet aggregation inhibitor 5 > 10 Effective Sulconazole Antifungal agents 7 > 10 Effective Apigenin Flavone 8 > 10 Effective Chlorpromazine Antipsychotic drugs 4 > 10 Effective Luteolin Flavonoid 9 > 10 Effective Medrysone Steroid 9 > 10 Ineffective 8-azaguanine Purine analog 7 > 10 Ineffective Repaglinide Antidiabetic Agents 7 > 10 Ineffective Alpha-estradiol Hormone 7 > 10 Ineffective PubMed cancer PubMed HCC Yes[24] Yes[24] Yes[25],[26] Yes[32] Yes[27] Yes[27] Yes[37] No No No Yes[37] No Yes[37] No No No Yes[37] Yes[37] Yes[36],[38] No Yes[39] Yes[39] No No Yes[40] No No No No No Drug Name Anisomycin Alexidine Dihydrochloride Chlorpromazine Mitoxantrone Dihydrochloride Ellipticine Sanguinarine Irinotecan Daunorubicin Hydrochloride Parthenolide Mefloquine Hydrochloride Piperlongumine Emetine Dihydrochloride Sulconazole Pyrvinium Pamoate Withaferin A Piperlongumine Astemizole Radicicol Monensin GBR 12909 Dihydrochloride Ellipticine Thiostrepton Camptothecine (S,+) Trichostatin A Ciclopirox Ethanolamine Thioridazine Hydrochloride Lasalocid Sodium Salt Nortriptyline Hydrochloride Cloperastine Hydrochloride Rotenone Anisomycin Antimycin A Parthenolide Thapsigargin Tanespimycin (17-AAG)-1 Mm Chlorpromazine Norcyclobenzaprine Podophyllotoxin Fluphenazine Tyloxapol VE-465 Mebendazole Luteolin Sulindac MS-275 Mometasone Furoate Verteporfin Thioguanosine Perphenazine Bepridil Hydrochloride Suberoylanilide Hydroxamic Acid Amiodarone Hydrochloride Prochlorperazine Dimaleate Miconazole Sulconazole Nitrarine Dihydrochloride Irinotecan Hexestrol Clioquinol Norgestrel-(-)-d Securinine Azacytidine-5 Trifluoperazine Propafenone Hydrochloride Prenylamine Lactate Berberine (-)-Eseroline Fumarate Salt Acepromazine rapamycin Cetirizine Promazine Triflupromazine Biperiden (Signature Positive) Diphenylpyraline Zimelidine Dihydrochloride Monohydrate Nitrofurantoin Methylergometrine Maleate Roxithromycin Ethacrynic Acid Morantel Tartrate Triprolidine 8-methyl-n-vanillylnonanamide Sulfameter Bezafibrate Leucomisine Ticlopidine S(-)eticlopride Hydrochloride Promethazine Levamisol Phenoxybenzamine (Prestwick-944) Antazoline D-cycloserine Procaine Hydrochloride Eucatropine Hydrochloride Trioxsalen 8-azaguanine Fenoprofen Calcium Salt Dihydrate Bacitracin Cinnarizine Gliclazide Dexverapamil Chrysin Trazodone Diltiazem Hydrochloride Streptozocin Triflusal Repaglinide Epicatechin-(-) Fulvestrant Phthalylsulfathiazole Fillalbin Skimmianine 2-aminobenzenesulfonamide Naringenine Thiamine Apigenin Aconitine Spiperone 15-delta prostaglandin J2 Meticrane Alpha-estradiol Felodipine Ifenprodil Tartrate Spironolactone Fludrocortisone Bufexamac Dipyridamole Ginkgolide A Flutamide Lomustine Ronidazole Medrysone Milrinone Exemestane Semustine Isoniazid Evoxine GW-8510 Buspirone Iressa (Genftinib) Tacrolimus (FK-506) Erythromycin Thiorphan Etodolac Bumetanide Piroxicam Pargyline Hydrochloride Depudecin Valdecoxib Betamethasone Nimesulide Benzbromarone Celecoxib DO 897/99 Ondansetron Cmap name Frequency Description Cephaeline 3 Alkaloids Alvespimycin 2 Heat shock protein 90 inhibitor Calmidazolium 2 Inhibitor of calmodulin-regulated enzymes Digoxin 2 Cardiac glycoside Geldanamycin 2 Heat shock protein 90 inhibitor Lanatoside C 2 Cardiac glycoside Mg-262 2 Proteasome inhibitor Proscillaridin 2 Cardiac glycoside Suloctidil 2 Vasodilator 0175029-0000 1 Alsterpaullone 1 Cyclin-dependent kinase inhibitor Digitoxigenin 1 Cardiac glycoside Digoxigenin 1 Cardiac glycoside Disulfiram 1 Proteasome inhibitor Doxorubicin 1 Anti-cancer drugs H-7 1 Helveticoside 1 Intermediate-acting hypnotic drug Ouabain 1 Cardiac glycoside Perhexiline 1 Anti-aging drugs Puromycin 1 Antibiotics Scriptaid 1 Histone deacetylase inhibitor Strophanthidin 1 Cardiac glycoside Terfenadine 1 Anti-histamine drugs Alvespimycin Cephaeline Digitoxigenin Digoxigenin Digoxin Doxorubicin Ouabain Proscillaridin Puromycin Strophanthidin
Monensin DMSO 10 mM 50 ul - Radicicol DMSO 10 mM 50 ul - ThioridazineDMSO 10 mM 50 ul O 8-aza DMSO 10 mM 50 ul X Chlorpromazine DMSO 10 mM 50 ul O TSA DMSO 10 mM 20 ul O Trifluoperazine DMSO 10 mM 50 ul O Withaferin AEtOH 1 mM 100 ul X Antimycin A DMSO 10 mM 50 ul O Pyrvinium Prestwick-1040 1040 DMSO 10 mM 50 ul X Perphenazine Prestwick-125 125 DMSO 10 mM 20 ul - Mefloquine Prestwick-126 126 DMSO 10 mM 50 ul - Astemizole Prestwick-136 136 DMSO 10 mM 50 ul X Dipyridamole Prestwick-142 142 DMSO 10 mM 30 ul - Nortriptyline Prestwick-254 254 H2O 10 mM 20 ul O Mitoxantrone Prestwick-385 385 DMSO 10 mM 50 ul - vanoxerine Prestwick-386 386 H2O 10 mM 50 ul X Daunorubicin Prestwick-487 487 DMSO 10 mM 50 ul O Thiostrepton Prestwick-522 522 DMSO 10 mM 50 ul X Ciclopirox Prestwick-541 541 DMSO 10 mM 50 ul O Parthenolide Prestwick-550 550 DMSO 10 mM 50 ul X prenylamine Prestwick-560 560 DMSO 10 mM 50 ul - Emetine Prestwick-570 570 DMSO 10 mM 50 ul - mometasone Prestwick-572 572 DMSO 10 mM 50 ul - Piperlongumine Prestwick-604 604 DMSO 10 mM 50 ul X Ellipticine Prestwick-614 614 DMSO 10 mM 50 ul X Alexidine Prestwick-777 777 DMSO 10 mM 50 ul - Lasalocid Prestwick-828 828 DMSO 10 mM 50 ul O Sanguinarine Prestwick-987 987 DMSO 10 mM 50 ul O promazine DMSO 10 mM 50 ul O Triflupromazine DMSO 10 mM 50 ul O Trifluoperazine Withaferin A Antimycin A Promazine Triflupromazine stock conc. Monensin Radicicol Thioridazine volume side population Trichostatin A Chlorpromazine drug name labeled as solvent 8-azaguanine normal cell (lung) HUVEC Huh7 Mahlavu PLC5 HepG2 Lung cancer >10 -- 8.44 >10 2.32 2.78 <1 Chlorpromazine <10 -- 0.33 0.33 6.22 >10 <0.1 Daunorubicin >10 5.3 >10 7.18 >10 10.00 >5 Ellipticine >10 36.5 3.2 >10 >10 >10 >10 >5 Mitoxantrone >10 14.7 >10 10.00 >10 >10 >5 Parthenolide <10 -- >10 3.30 2.33 >10 <1 Piperlongumine >10 15.2 >10 >10 >10 >10 >10 <10 5.7 0.54 0.41 0.54 1.00 <1 >10 20.4 0.2 0.33 10.00 >10 10.00 <1 <10 -- 0.60 <0.33 6.55 2.27 <0.1 <10 -- 8.14 5.85 7.40 5.80 >5 <10 -- 8.30 5.66 10.00 >10 >5 >10 151.4 5.3 >10 >10 >10 >10 >10 >10 -- 8.91 8.42 >10 >10 >10 <10 5.2 0.33 <0.33 3.93 2.72 <1 ok -- 6.91 7.94 6.55 >10 >5 <10 -- <0.33 <0.33 0.87 0.33 <1 <10 5.6 5.26 2.72 >10 >10 <5 >10 -- 7.04 1.99 >10 >10 <1 <10 8.0 >10 2.74 >10 >10 <5 >10 -- 10.00 6.79 >10 7.17 >10 >10 -- <0.33 <0.33 1.02 1.88 <0.1 >10 -- 6.53 >10 >10 >10 >10 <10 -- 6.48 0.39 7.25 >10 <1 >10 16.9 0.9 8.12 8.05 >10 >10 <1 <10 -- 1.72 1.00 2.90 4.30 <1 <10 -- 10.00 6.76 >10 >10 >5 <10 7.5 0.78 1.00 2.88 2.53 <1 >10 -- >10 >10 >10 >10 >10 >10 -- >10 >10 >10 >10 >10 >10 -- >10 >10 >10 >10 >10 IC50 (M) Chlorpromazine Daunorubicin Mitoxantrone Parthenolide Piperlongumine Pubmed HCC cell cycle PMID: 21272161 V X PMID: 23744428 X (Jurkat T cell) V (arrest at G1/G0) PMID: 12218360 X (prostate cancer) V Tanespimycin (17-AAG) PMID: 19082595 V V PMID: 20460749 V V (arrest at S) PMID: 18088458 X ( leukemia cells) V PMID: 12218360 X (prostate cancer) V PMID: 10696143 X ( spinal cord astrocytes) V (arrest at S) PMID: 24995076 X (HUVECs ) V Proscillaridin X Strophanthidin X Digitoxigenin X Digoxigenin X PMID: 22087264 V X PMID: 20368687 X (C6 glioma cells) V PMID: 7872960 X (doxorubicin-resistant murine leukemic P388/R-84 cells) V (arrest at S)-->Doxorubicin (DOX) and daunorubicin (DNR) coincubation with chlorpromazine (CPZ) enhanced accumulation more in S-phase than in G1- and G2/M-phase cells. PMID: 6744425 X (P388 murine leukemic cells) V PMID: 21413021 V X (tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) PMID: 19821157 V X (as NF-kappaB inhibitor) PMID: 21040711 X (glioblastomas) V PMID: 20878078 X (leukemia cells) V PMID: 19956905 X (lung adenocarcinoma cells) V PMID: 19397439 X (TP53 null prostate cancer cells) only small alterations in G1 and G2/M cells PMID: 18088190 X (CGL1 cells) V Sulconazole X Parthenolide Reference G2 drugs Anisomycin Ouabain Chlorpromazine G2/M arrest X X X V X V X (Cardiac glycosides exhibited amazing ability to reverse the G2/M arrest) X V (37%) X V X V X X V V V X V Reference Paper HCC Oncogene (2005) 24, 512519 V PMID: 24797310 V PMID: 15519653 V Oncogene (2005) 24, 512519 V PMID: 21468663 V PMID: 20025574 V PMID: 19003983 V PMID: 18520067 V PMID: 16170360 X (colon cancer) PMID: 12711013 X (breast cancer) PMID: 8603450 X (L1210 cells) PMID: 15790488 X (HeLa and A549 cells) PMID: 14504478 X (leukemic HL-60 cells) chemodrugs Reference Doxorubicin Etoposide Irinotecan (CPT-11) Mitoxantrone cell cycle G2/M arrest V V V V V V V V X X X X X X V (arrest at S) X V (arrest at G1 in p53(wt) cell lines) V (p53-deficient cell lines) V V V G2 arrest V V V (arrest at S) X Reference G2 drugs PA file Anisomycin Tanespimycin (17-AAG) Ouabain Alkaloid () Proscillaridin Strophanthidin Digitoxigenin Digoxigenin Chlorpromazine Parthenolide Sulconazole Chemodrugs PA file Doxorubicin Etoposide Irinotecan (CPT-11) Mitoxantrone Etoposide-->IC50 = 59.2 M Antineoplastic agent () Antibiotic () Cardiotonic agent() Glycoside() Function Protein synthesis inhibitor (blocks translation) Inhibitor of heat shock protein 90 (Hsp90) chaperone activity Selective Na+, K+-ATPase inhibitor treatment of congestive heart failure and cardiac arrhythmia Selective Na+, K+-ATPase inhibitor is cardenolide is a hapten, a small molecule with high Antigenicity is a dopamine antagonist of the typical anti-psychotic class of medications Antisecretory, anti-inflammatory and spasmolytic; inhibits the release of 5-HT from blood platelets antifungal medication Function Antitumor antibiotic agent that inhibits DNA topoisomerase II Topoisomerase II inhibitor Inhibitor of DNA topoisomerase I Topoisomerase II inhibitor; immunosuppressive and antineoplastic agent