Table 1. Compounds active in patient-derived retinoblastoma cells.
Compounds found to be active (> 70% cell growth inhibition) in HPG-RBT-12L (derived from intraocular tumor) and HPG-CSF1 cells (cells disseminated into the cerebrospinal fluid of a relapsed heavily pretreated patient). Name, supplier catalog number, and mechanism of action are detailed.
| Compound (n = 169) | Selleck code | Mechanism of action |
|---|---|---|
| (−)-Parthenolide | S2341 | NF-κB /HDAC dual inhibitor |
| (+)-JQ1 | S7110 | BET inhibitor |
| Hydroxycamptothecin | S2423 | Topoisomerase I inhibitor |
| 5-Iodotubercidin | S8314 | Adenosine kinase inhibitor |
| Abexinostat | S1090 | HDAC inhibitor |
| ABT-737 | S1002 | BH3 mimetic inhibitor |
| Alvespimycin | S1142 | HSP90 inhibitor |
| AR-42 | S2244 | HDAC inhibitor |
| ARQ 621 | S7355 | KSP inhibitor |
| AT13387 | S1163 | HSP90 inhibitor |
| AT9283 | S1134 | Aurora A,B / JAK2/3 dual inhibitor |
| AUY922 | S1069 | HSP90 inhibitor |
| AZ5104 | S7298 | EGFR inhibitor |
| AZ6102 | S7767 | TNKS inhibitor |
| AZD1480 | S2162 | JAK1/2 inhibitor |
| AZD8055 | S1555 | mTOR inhibitor |
| AZD9291 | S7297 | EGFR inhibitor |
| Bardoxolone methyl | S8078 | Keap1/ Nrf2 activator |
| BAY 11–7082 | S2913 | NF-κBα (IκBα) inhibitor |
| Bay 11–7085 | S7352 | NF-κB α (IκBα) inhibitor |
| Belinostat | S1085 | HDAC inhibitor |
| Benzethonium | S4162 | Antiseptic/ tensioactive |
| BGT226 | S2749 | PI3K/ mTOR dual inhibitor |
| BI 2536 | S1109 | PLK1/ BRD4 inhibitor |
| BIIB021 | S1175 | HSP90 inhibitor |
| BIX 01294 | S8006 | Histone methyltransferase G9a inhibitor |
| BMS-754807 | S1124 | IGF-1R/ IR dual inhibitor |
| Bortezomib | S1013 | Proteasome inhibitor |
| Brefeldin A | S7046 | Antimicrobial (ATPase inhibitor) |
| Buparlisib | S2247 | PI3K inhibitor |
| BV-6 | S7597 | cIAP / XIAP dual inhibitor |
| Caffeic acid phenethyl ester | S7414 | NF-κB inhibitor |
| Camptothecin | S1288 | Topoisomerase I inhibitor |
| Carfilzomib | S2853 | Proteasome inhibitor |
| CB-5083 | S8101 | p97 inhibitor |
| Celastrol | S1290 | Proteasome inhibitor |
| Cepharanthine | S4238 | Anti-inflammatory |
| Ceritinib | S7083 | ALK inhibitor |
| Cetrimonium | S4242 | Antiseptic (quaternary ammonium) |
| Cetylpyridinium | S4172 | Antiseptic (quaternary ammonium) |
| CH5138303 | S7340 | HSP90 inhibitor |
| Ciclopirox | S2528 | Antifungal/ iron chelator |
| Cladribine | S1199 | Adenosine deaminase inhibitor |
| CPI-203 | S7304 | BET inhibitor |
| Crystal Violet | S1917 | Antiseptic (antimitotic) |
| Cucurbitacin B | S8165 | Phytochemical (mitosis inhibitor) |
| CUDC-101 | S1194 | HDAC/ EGFR / HER2 triple inhibitor |
| CUDC-907 | S2759 | PI3K/ HDAC dual inhibitor |
| CX-6258 | S7041 | Pim kinase inhibitor |
| Dacinostat | S1095 | HDAC inhibitor |
| Daunorubicin | S3035 | Anthracycline-topoisomerase II inhibitor |
| Delanzomib | S1157 | Proteasome inhibitor |
| Deltarasin | S7224 | PDEδ/Kras dual inhibitor |
| Digoxin | S4290 | Cardiac glycoside (Na/K ATPase inhibitor) |
| Domiphen | S4186 | Antiseptic (quaternary ammonium) |
| Dovitinib Dilactic Acid | S2769 | RTK inhibitor |
| Dp44Mt | S7909 | Iron chelator |
| Entinostat | S1053 | HDAC inhibitor |
| Epoxomicin | S7038 | Proteasome inhibitor |
| Ethacridine lactate | S4196 | Antiseptic |
| Etoposide | S1225 | Epipodophyllotoxin (topoisomerase II inhibitor) |
| Fedratinib | S2736 | JAK-2 inhibitor |
| Gambogic Acid | S2448 | Apoptosis inducer |
| Ganetespib | S1159 | HSP90 inhibitor |
| GDC-0980 | S2696 | PI3K/ mTOR dual inhibitor |
| Geldanamycin | S2713 | HSP90 inhibitor |
| Gemcitabine | S1714 | Antimetabolite |
| Givinostat | S2170 | HDAC inhibitor |
| GMX1778 | S8117 | NAMPT inhibitor |
| GSK J4 | S7070 | JMJD3/ UTX dual inhibitor |
| GSK1070916 | S2740 | Aurora B/C inhibitor |
| GSK1324726A | S7620 | BET inhibitor |
| GSK2126458 | S2658 | PI3K inhibitor |
| Hesperadin | S1529 | Aurora B kinase inhibitor |
| HSP990 | S7097 | HSP90 inhibitor |
| ICG-001 | S2662 | Wnt pathway inhibitor |
| Idarubicin | S1228 | Anthracycline (topoisomerase II inhibitor) |
| IKK-16 | S2882 | IKK inhibitor |
| Irinotecan | S2217 | Topoisomerase I inhibitor |
| Ispinesib | S1452 | KSP inhibitor |
| Ixazomib | S2180 | Proteasome inhibitor |
| JTC-801 | S2722 | NOP antagonist |
| KPT-185 | S7125 | CRM1 inhibitor |
| KPT-276 | S7251 | CRM1 inhibitor |
| KW-2478 | S2685 | HSP90 inhibitor |
| Linsitinib | S1091 | IGF-1R/ IR dual inhibitor |
| LMK-235 | S7569 | HDAC inhibitor |
| LMTX™ | S7762 | Tau protein aggregation inhibitor |
| LY3023414 | S8322 | PI3K/ mTOR / DNA-PK triple inhibitor |
| M344 | S2779 | HDAC inhibitor |
| MCB-613 | S7913 | SRC stimulator |
| Melphalan | S8266 | Nitrogen mustard (DNA alkylator) |
| Methylene Blue | S4535 | Oxidation-reduction agent |
| MG-101 | S7386 | Cysteine protease inhibitor |
| MG-132 | S2619 | Proteasome inhibitor |
| MI-773 | S7649 | MDM2 inhibitor |
| Milciclib | S2751 | CDK/ TRK dual inhibitor |
| Mitomycin C | S8146 | Antibiotic |
| Mitoxantrone | S1889 | Topoisomerase II inhibitor |
| MK-1775 | S1525 | Wee1 inhibitor |
| MLN9708 | S2181 | Proteasome inhibitor |
| Mocetinostat | S1122 | HDAC inhibitor |
| Navitoclax | S1001 | BCL-2 inhibitor |
| NH125 | S7436 | eEF-2 inhibitor |
| NMS-E973 | S7282 | HSP90 inhibitor |
| NSC 319726 | S7149 | p53 reactivator |
| NVP-ADW742 | S1088 | IGF-1R inhibitor |
| NVP-AEW541 | S1034 | IGF-1R inhibitor |
| Obatoclax | S1057 | BCL-2 inhibitor |
| Oligomycin A | S1478 | Antibiotic (ATPase inhibitor) |
| Omaveloxolone | S7672 | NRF2 activator |
| ONX-0914 | S7172 | Proteasome inhibitor |
| Oprozomib | S7049 | Proteasome inhibitor |
| Oridonin | S2335 | PI3K inhibitor |
| OTX015 | S7360 | BET inhibitor |
| Ouabain | S4016 | Cardiac glycoside (Na/K ATPase inhibitor) |
| Pacritinib | S8057 | JAK2/ FLT3 dual inhibitor |
| Panobinostat | S1030 | HDAC inhibitor |
| PD0166285 | S8148 | Wee1 /Myt1 dual inhibitor |
| PF-04929113 | S2656 | HSP90 inhibitor |
| PF-477736 | S2904 | Chk1 inhibitor |
| Piperlongumine | S7551 | ROS inducer |
| Pirarubicin | S1393 | Antibiotic (anthracycline) |
| Pracinostat | S1515 | HDAC inhibitor |
| PRI-724 | S8262 | Wnt signaling pathway inhibitor in cancer stem cell |
| PU-H71 | S8039 | HSP90 inhibitor |
| Puromycin | S7417 | Antimicrobial/ antibiotic |
| Quisinostat | S1096 | HDAC inhibitor |
| RAF265 | S2161 | RAF/ VEGFR2 dual inhibitor |
| Resminostat | S2693 | HDAC inhibitor |
| Ricolinostat | S8001 | HDAC inhibitor |
| Rigosertib | S1362 | PLK1 inhibitor |
| Romidepsin | S3020 | HDAC inhibitor |
| SB743921 | S2182 | KSP inhibitor |
| SBI-0640756 | S8181 | EIF4G1 inhibitor |
| Scriptaid | S8043 | HDAC inhibitor |
| Selinexor | S7252 | CRM1 inhibitor |
| Sepantronium | S1130 | Survivin inhibitor |
| SGI-1776 | S2198 | Pim kinase inhibitor |
| SGI-7079 | S7847 | Axl inhibitor |
| SN-38 | S4908 | Topoisomerase I inhibitor |
| SNX-2112 | S2639 | HSP90 inhibitor |
| SRT1720 | S1129 | SIRT1 agonist |
| Stattic | S7024 | STAT3 inhibitor |
| Staurosporine | S1421 | Antifungal/ protein kinase C inhibitor |
| STF-118804 | S7316 | NAMPT inhibitor |
| TAE226 | S2820 | FAK/ IGF-1R dual inhibitor |
| Tanespimycin | S1141 | HSP90 inhibitor |
| Teniposide | S1787 | Epipodophyllotoxin (topoisomerase II inhibitor) |
| Tenovin-6 | S4900 | HDAC inhibitor |
| Terfenadine | S4353 | Antihistamine |
| TG101209 | S2692 | JAK-2 inhibitor |
| TIC10 | S7963 | TRAIL inducer |
| Topotecan | S1231 | Topoisomerase I inhibitor |
| Trichostatin A (TSA) | S1045 | HDAC inhibitor |
| Tubercidin | S8095 | Antibiotic (polymerase inhibitor) |
| UM171 | S7608 | HSC self-renewal agonist |
| UNC0631 | S7610 | Histone methyltransferase G9a inhibitor |
| UNC-2025 | S7576 | Mer/ FLT3 inhibitor |
| VER-49009 | S7458 | HSP90 inhibitor |
| VER-50589 | S7459 | HSP90 inhibitor |
| Verdinexor | S7707 | CRM1 inhibitor |
| Vinblastine | S4505 | Vinca alkaloid-mitotic inhibitor |
| Vincristine | S1241 | Vinca alkaloid-mitotic inhibitor |
| Vinflunine | S2209 | Vinca alkaloid-mitotic inhibitor |
| Vinorelbine | S4269 | Vinca alkaloid-mitotic inhibitor |
| Vorinostat | S1047 | HDAC inhibitor |
| VS-5584 | S7016 | PI3K/ mTOR dual inhibitor |
| XL888 | S7122 | HSP90 inhibitor |
ALK, anaplastic lymphoma kinase inhibitor; BCL-2, B-cell lymphoma 2; BET, bromodomain and extraterminal domain; BRD4, bromodomain-containing protein 4; CDK, cyclin-dependent kinase; Chk1, checkpoint kinase 1; cIAP, cellular inhibitor of apoptosis protein-1; CRM1, chromosome region maintenance 1; DNA-PK, DNA-dependent protein kinase; Eef-2, eukaryotic elongation factor 2; EGFR, epidermal growth factor receptor; EIF4G1, eukaryotic translation initiation factor 4 gamma 1; FAK, focal adhesion kinase; FLT3, Fms like tyrosine kinase 3; HDAC, histone deacetylase inhibitors; HER2, human epidermal growth factor receptor type 2; HSC, hematopoietic stem cell; HSP90, heat shock protein 90; IGF-1R, insulin-like growth factor 1 receptor; IKK, inhibitor of nuclear factor kappa-B kinase; IR, insulin receptor; JK2/3, Janus kinase 2,3; JMJD3, Jumanji domain-containing protein D3; Keap1, Kelch-like ECH-associated protein 1; Kras, Kirsten rat sarcoma viral oncogene homolog; KSP, kinesin spindle protein; MDM2, mouse double minute 2 homolog; mTOR, mammalian target of rapamycin; NAMPT, nicotinamide phosphoribosyltransferase; NFR2, nuclear factor erythroid 2-related factor; NF-Κb, nuclear factor kappa-light-chain-enhancer of activated B cells; NOP, nociceptin Receptor; Nrf2, nuclear factor (erythroid-derived 2)-like 2; PDEδ, photoreceptor cGMP phosphodiesterase δ subunit; PI3K, phosphatidylinositol 3-kinase; PLK1, Polo-like kinase 1; RKT, receptor tyrosine kinases; SIRT1, Sirtuin 1; SRC, steroid receptor coactivator; STAT3, signal transducer and activator of transcription 3; TNKS, Tankyrase; TRAIL, TNF-related apoptosis-inducing ligand; TRK, tropomyosin receptor kinase; UTX, ubiquitously transcribed X-chromosome tetratricopeptide repeat protein; VEGFR2, vascular endothelial growth factor receptor 2; XIAP, X-linked inhibitor of apoptosis protein.