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IC50 (uM) Clonogenic Assay** PubMed cancer PubMed HCC 23 predicit drugs (fromCMAP) 148 drugs (fromVendor) Mahlavu

PLC5 Huh 7 HepG2 Huh7 Mahlavu PLC5 HepG2


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

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