Table 1.
The correlation between STAT3 expression and drug response (Top 10).
| Primary Site | Compound | Correlation r | p-Value | Status | Gene Symbol of Protein Target | Target or Activity of Compound |
|---|---|---|---|---|---|---|
| Breast | ||||||
| abiraterone | −0.969 | 0.031 | FDA | CYP17A1 | inhibitor of 17 alpha-hydroxylase and C17, 20 lyase | |
| bafilomycin A1 | 0.762 | 0.046 | probe | ATP6V0A1 | inhibitor of the vacuolar-type H+-ATPase | |
| BRD-K84807411 | −0.717 | 0.006 | GE-active | product of diversity-oriented synthesis | ||
| BEC | −0.705 | 0.007 | probe | ARG1; ARG2 | inhibitor of arginase I and II | |
| BRD-K30019337 | −0.595 | 0.032 | GE-active | product of diversity-oriented synthesis | ||
| fulvestrant | 0.590 | 0.043 | FDA | ESR1; GPER1 | antagonist of the estrogen receptor | |
| MLN2238 | −0.524 | 0.001 | clinical | PSMB5 | inhibitor of 20S proteasome at the chymotrypsin-like proteolytic (β−5) site | |
| BRD-K42260513 | −0.524 | 0.026 | probe | EZH2 | inhibitor of enhancer of zeste polycomb repressive complex 2 subunit | |
| SB-525334 | 0.523 | 0.001 | probe | TGFBR1 | inhibitor of the transforming growth factor beta type 1 receptor | |
| sildenafil | 0.474 | 0.003 | FDA | PDE5 | inhibitor of phosphodiesterase type 5 | |
| Central nervous system | ||||||
| docetaxel | 0.654 | 0.006 | FDA | inhibitor of microtubule depolymerization | ||
| myriocin | −0.612 | 0.012 | probe | SPTLC1; SPTLC2; SPTLC3 | inhibitor of serine-palmitoyl-transferase | |
| GSK461364 | 0.604 | 0.000 | clinical | PLK1 | inhibitor of polo-like kinase 1 (PLK1) | |
| sitagliptin | 0.591 | 0.016 | FDA | DPP4 | inhibitor of dipetidyl peptidase 4 | |
| AT13387 | 0.564 | 0.006 | clinical | HSP90 | inhibitor of HSP90 | |
| vincristine | 0.549 | 0.000 | FDA | inhibitor of microtubule assembly | ||
| rigosertib | 0.538 | 0.000 | clinical | PIK3; PLK1 | inhibitor of polo-like kinase 1; inhibitor of PI3K catalytic subunits α and β | |
| triazolothiadiazine | 0.529 | 0.000 | probe | PDE4A; PDE4B; PDE4D | inhibitor of phosphdiesterase 4A/B/D | |
| BRD-K70511574 | 0.522 | 0.000 | probe | PLK1 | inhibitor of polo-like kinase 1 (PLK1) | |
| CHM-1 | 0.522 | 0.000 | probe | inhibitor of tubulin polymerization | ||
| Hematopoietic and lymphoid tissue | ||||||
| VX-680 | 0.618 | 0.024 | clinical | AURKA; AURKB; AURKC | inhibitor of aurora kinases | |
| staurosporine | 0.505 | 0.002 | probe | inhibitor of multiple kinases | ||
| YM-155 | 0.430 | 0.000 | clinical | BIRC5 | inhibitor of survivin expression | |
| BRD-K79669418 | 0.399 | 0.000 | probe | MDM2; MDM4 | inhibitor of MDM4-p53 interaction | |
| ruxolitinib | −0.389 | 0.000 | FDA | JAK1; JAK2 | inhibitor of Janus kinases 1 and 2 | |
| ML239 | −0.360 | 0.000 | probe | inhibitor of breast cancer stem cell proliferation | ||
| MK-2206 | 0.356 | 0.000 | clinical | AKT1 | inhibitor of AKT1 | |
| AZD6482 | 0.351 | 0.000 | clinical | PIK3CB; PIK3CD | inhibitor of PI3K catalytic subunits beta and delta | |
| sitagliptin | 0.349 | 0.043 | FDA | DPP4 | inhibitor of dipetidyl peptidase-4 | |
| AZD1480 | −0.348 | 0.011 | clinical | JAK1; JAK2 | inhibitor of Janus kinases 1 and 2 | |
| Large intestine | ||||||
| JW-55 | −0.655 | 0.006 | probe | TNKS | inhibitor of tankyrase | |
| O-6-benzylguanine | −0.569 | 0.017 | clinical | MGMT | inhibitor of O(6)-alkylguanine DNA alkyltransferases | |
| ML210 | −0.488 | 0.001 | probe | selectively kills engineered cells expressing mutant HRAS | ||
| ML162 | −0.446 | 0.002 | probe | selectively kills engineered cells expressing mutant HRAS | ||
| PRL-3 inhibitor I | −0.437 | 0.003 | probe | PTP4A3 | inhibitor of phosphatase of regenerating liver-3 (PRL3) | |
| imatinib | −0.432 | 0.003 | FDA | ABL1; BCR; KIT | inhibitor of BCR-ABL1 and c-KIT | |
| 1S,3R-RSL-3 | −0.421 | 0.003 | probe | GPX4 | synthetic lethal with HRAS in engineered cells; inhibitor of GPX4 | |
| betulinic acid | −0.396 | 0.008 | probe | natural product; inhibitor of specificity protein 1 transcription factor in cells | ||
| KH-CB19 | −0.391 | 0.024 | probe | CLK1; CLK4 | inhibitor of CDC2-like kinases 1 and 4 | |
| palmostatin B | −0.386 | 0.026 | probe | LYPLA1 | inhibitor of acyl-protein thioesterase 1 | |
| Lung | ||||||
| GSK-J4 | 0.608 | 0.047 | probe | KDM6A; KDM6B | inhibitor of lysine-specific demethylases | |
| BRD-K49290616 | −0.376 | 0.011 | GE-active | product of diversity-oriented synthesis | ||
| TGX-221 | −0.325 | 0.000 | probe | PIK3CB | inhibitor of PI3K catalytic subunit beta | |
| BRD-K96431673 | −0.302 | 0.046 | GE-active | product of diversity-oriented synthesis | ||
| Ovary | ||||||
| istradefylline | 0.586 | 0.028 | clinical | ADORA2A | antagonist of the adenosine A2A receptor | |
| BRD-K03536150 | 0.507 | 0.001 | probe | BAX | activator of BAX | |
| LY-2183240 | 0.448 | 0.005 | probe | FAAH | inhibitor of fatty acid amide hydrolase; inhibitor of anandamide uptake | |
| fumonisin B1 | −0.447 | 0.004 | probe | CERS1; CERS2; CERS3; CERS4; CERS5 | inhibitor of ceramide synthase | |
| manumycin A | 0.437 | 0.006 | probe | FNTA; FNTB | inhibitor of RAS farnesyltransferase | |
| ML311 | 0.431 | 0.006 | probe | MCL1; Bim | inhibitor of the Mcl-1/Bim interaction | |
| methotrexate | 0.421 | 0.010 | FDA | DHFR | inhibitor of dihydrofolate reductase | |
| SCH-79797 | 0.411 | 0.009 | FDA | DHFR | inhibitor of dihydrofolate reductase | |
| BRD-K94991378 | 0.378 | 0.019 | probe | F2R | antagonist of proteinase-activated receptor 1 (PAR1) | |
| ibrutinib | −0.373 | 0.047 | clinical | BTK | inhibitor of Bruton’s tyrosine kinase | |
| Pancreas | ||||||
| CIL70 | −0.500 | 0.034 | probe | screening hit | ||
| RITA | 0.401 | 0.011 | probe | MDM2; TP53 | inhibitor of p53-MDM2 interaction | |
| sotrastaurin | 0.400 | 0.028 | clinical | PKC | inhibitor of protein kinase C | |
| NVP-BEZ235 | 0.386 | 0.032 | clinical | MTOR;PIK3CA; PIK3CB; PIK3CD | inhibitor of PI3K and mTOR kinase activity | |
| purmorphamine | 0.384 | 0.016 | probe | SMO | activator of smoothened receptor | |
| dexamethasone | 0.365 | 0.022 | FDA | NR3C1 | agonist of glucocorticoid receptor | |
| doxorubicin | −0.363 | 0.023 | FDA | TOP2A | inhibitor of topoisomerase II | |
| BRD8899 | 0.358 | 0.0275 | probe | STK33 | inhibitor of serine/threonine kinasase STK33 | |
| cabozantinib | −0.355 | 0.0290 | FDA | FLT3; KDR; MET; RET | inhibitor of c-MET, VEGFR2/3, and RET | |
| PF-750 | 0.354 | 0.0271 | probe | FAAH | inhibitor of fatty acid amide hydrolase | |
| Skin | ||||||
| bafilomycin A1 | −0.999 | 0.023 | probe | ATP6V0A1 | inhibitor of the vacuolar-type H+-ATPase | |
| BRD-K09344309 | 0.662 | 0.01 | probe | screening hit | ||
| tigecycline | −0.515 | 0.029 | FDA | analog of tetracycline | ||
| sotrastaurin | 0.475 | 0.001 | clinical | PKC | inhibitor of protein kinase C | |
| HBX-41108 | −0.432 | 0.003 | probe | USP7 | inhibitor of the deubiquitinase activity of USP7 | |
| itraconazole | −0.414 | 0.003 | FDA | anti-fungal agent; inhibitor of hedgehog signaling pathway | ||
| 1S,3R-RSL-3 | −0.409 | 0.002 | probe | GPX4 | synthetic lethal with HRAS in engineered cells; inhibitor of GPX4 | |
| bleomycin A2 | −0.406 | 0.005 | FDA | inducer of DNA damage | ||
| indisulam | −0.376 | 0.008 | clinical | CA9 | inhibitor of carbonic anhydrase isoform IX | |
| ML162 | −0.371 | 0.007 | probe | selectively kills engineered cells expressing mutant HRAS | ||
| Stomach | ||||||
| KH-CB19 | 0.567 | 0.014 | probe | CLK1; CLK4 | inhibitor of CDC2-like kinases 1 and 4 | |
| cerulenin | 0.555 | 0.001 | probe | FASN; HMGCS1 | inhibitor of fatty acid synthase; inhibitor of HMG-CoA synthase | |
| obatoclax | 0.554 | 0.001 | clinical | BCL2; BCL2L1; MCL1 | inhibitor of MCL1, BCL2, and BCL-xL | |
| fingolimod | 0.551 | 0.001 | FDA | S1PR1 | inhibitor of sphingosine 1-phosphate receptor | |
| quizartinib | 0.539 | 0.002 | clinical | FLT3 | inhibtor of VEGFR3 | |
| ouabain | 0.538 | 0.001 | probe | ATP1A1; ATP1A2; ATP1A3; ATP1B1 | cardiac glycoside; inhibitor of the Na+/K+-ATPase | |
| B02 | 0.511 | 0.003 | probe | RAD51 | inhibitor of RAD51 | |
| darinaparsin | −0.500 | 0.029 | clinical | inducer of ROS; inhibitor of microtubule assembly | ||
| vorapaxar | 0.492 | 0.004 | clinical | F2R | antagonist of proteinase-activated receptor 1 (PAR1) | |
| cyclophosphamide | 0.473 | 0.047 | FDA | DNA alkylator | ||
| Upper aerodigestive tract | ||||||
| JW-55 | 0.998 | 0.007 | probe | TNKS | inhibitor of tankyrase | |
| BRD-K29086754 | −0.735 | 0.043 | GE-active | product of diversity-oriented synthesis | ||
| nutlin-3 | 0.712 | 0.015 | clinical | MDM2 | inhibitor of p53-MDM2 interaction | |
| BRD-K49290616 | −0.699 | 0.000 | GE-active | product of diversity-oriented synthesis | ||
| BRD-K48334597 | −0.682 | 0.017 | GE-active | product of diversity-oriented synthesis | ||
| CIL55A | 0.678 | 0.021 | probe | screening hit | ||
| BRD-K34485477 | −0.618 | 0.008 | GE-active | product of diversity-oriented synthesis | ||
| NSC48300 | 0.591 | 0.043 | probe | TASP1 | inhibitor of threonine endopeptidase taspase 1 | |
| linifanib | 0.589 | 0.001 | clinical | FLT1; FLT3; KDR | inhibitor of VEGFRs | |
| tubastatin A | −0.548 | 0.001 | probe | HDAC6 | inhibitor of tubulin deacetylase activity of HDAC6 |