====== 5-Fluorouracil 20μM R00 exp2 ====== ==== Mechanism of Action ==== Thymidylate synthase inhibitor, blocks DNA replication * **Class / Subclass 1:** Metabolism / Antimetabolite * **Class / Subclass 2:** DNA Damage, Repair and Replication / Replication Inhibitor ==== Technical Notes ==== * **PubChem Name:** %%5-Fluorouracil%% * **Synonyms:** 5-FU * **CAS #:** 51-21-8 * **PubChem CID:** [[https://pubchem.ncbi.nlm.nih.gov/compound/3385|3385]] * **IUPAC:** %%5-fluoro-1H-pyrimidine-2,4-dione%% * **INCHI Name:** InChI=1S/C4H3FN2O2/c5-2-1-6-4(9)7-3(2)8/h1H,(H2,6,7,8,9) * **INCHI Key:** GHASVSINZRGABV-UHFFFAOYSA-N * **Molecular Weight:** 130.08 * **Canonical SMILES:** C1=C(C(=O)NC(=O)N1)F * **Isomeric SMILES:** N/A * **Molecular Formula:** C4H3FN2O2 {{:chemogenomics:structures:chem-0001.svg?nolink}} * **Supplier Name:** Sigma-Aldrich * **Catalog #:** F6627 * **Lot #:** 102K0970 * **LCMS:** Tr 0.14 min, m/z 129- [M-H]- * **Platform ID:** 5-FU * **Min:** -8.9515; **Max:** 61.1847 {{:chemogenomics:dose_response:dr_253.png?nolink&500 |}} \\ \\ \\ \\ |< 300px 100px 200px >| ^ IC ^ Concentration (µM) ^ | IC10 |N/A | | IC20 |12.7820 | | IC30 |22.9250 | | IC40 |37.0071 | | IC50 |57.4305 | | IC60 |N/A | | IC70 |N/A | | IC80 |N/A | | IC90 |N/A | \\ ==== Screen Summary ==== * **Round**: 00 * **Dose**: 20µM * **Days of incubation**: 8 * **Doublings**: 1.5 * **Numbers of reads**: 11051144 ==== Screen Results ==== ^Sensitive/Resistant hits (FDR<0.05)^CRANKS^Score Plot^Top 30 Genes^Screen Similarity^Top 30 Sensitive GO terms^Top 30 Resistant GO terms^ |8/86|[[https://files.tyerslab.com/files/public/chemogenomics/cranks/5-Fluorouracil_20uM_Round-0_exp2.txt|Scores]]|||||| {{:chemogenomics:cranks_plots:exp2.png?nolink}} ^Gene^CRANKS Score^FDR^ |[[:human_genes:P:POLA1|POLA1]]|-3.74|0.11| |[[:human_genes:B:BRD2|BRD2]]|-3.32|<0.01| |[[:human_genes:G:GOLGA6L1|GOLGA6L1]]|-3.06|0.17| |[[:human_genes:A:ATP6V1A|ATP6V1A]]|-3.02|0.02| |[[:human_genes:S:SF3A1|SF3A1]]|-2.93|0.32| |[[:human_genes:S:SEPHS2|SEPHS2]]|-2.75|0.03| |[[:human_genes:V:VPS25|VPS25]]|-2.71|0.18| |[[:human_genes:P:PDS5B|PDS5B]]|-2.68|0.03| |[[:human_genes:B:BCOR|BCOR]]|-2.68|0.05| |[[:human_genes:R:RRM2|RRM2]]|-2.67|0.38| |[[:human_genes:P:PCGF1|PCGF1]]|-2.66|0.03| |[[:human_genes:C:CNOT2|CNOT2]]|-2.64|0.03| |[[:human_genes:P:PAN2|PAN2]]|-2.57|0.07| |[[:human_genes:M:MGA|MGA]]|-2.54|0.05| |[[:human_genes:A:ATXN2L|ATXN2L]]|-2.50|0.08| |[[:human_genes:P:POLR2I|POLR2I]]|-2.46|0.05| |[[:human_genes:S:SPRR2D|SPRR2D]]|-2.43|0.09| |[[:human_genes:D:DDX3X|DDX3X]]|-2.40|0.07| |[[:human_genes:N:NPIPB8|NPIPB8]]|-2.39|0.38| |[[:human_genes:I:INO80E|INO80E]]|-2.37|0.11| |[[:human_genes:P:POLR2A|POLR2A]]|-2.31|0.32| |[[:human_genes:G:GCGR|GCGR]]|-2.29|0.09| |[[:human_genes:P:PRPH|PRPH]]|-2.29|0.09| |[[:human_genes:M:MSI2|MSI2]]|-2.26|0.10| |[[:human_genes:A:ATP6V1B2|ATP6V1B2]]|-2.25|0.16| |[[:human_genes:C:CHMP4B|CHMP4B]]|-2.24|0.11| |[[:human_genes:F:FOXD1|FOXD1]]|-2.24|0.28| |[[:human_genes:N:NPRL3|NPRL3]]|-2.23|0.23| |[[:human_genes:P:POLA2|POLA2]]|-2.22|0.36| |[[:human_genes:S:SAE1|SAE1]]|-2.22|0.24| |[[:human_genes:M:MIOS|MIOS]]|3.28|<0.01| |[[:human_genes:I:ID3|ID3]]|3.28|<0.01| |[[:human_genes:C:CDKN1A|CDKN1A]]|3.28|<0.01| |[[:human_genes:C:CSNK2B|CSNK2B]]|3.32|<0.01| |[[:human_genes:W:WDR5|WDR5]]|3.40|<0.01| |[[:human_genes:A:AURKB|AURKB]]|3.53|<0.01| |[[:human_genes:U:UBE2G1|UBE2G1]]|3.54|<0.01| |[[:human_genes:S:SUV420H1|SUV420H1]]|3.63|<0.01| |[[:human_genes:F:FBXO11|FBXO11]]|3.67|<0.01| |[[:human_genes:M:MEAF6|MEAF6]]|3.67|<0.01| |[[:human_genes:G:GMPPB|GMPPB]]|3.76|<0.01| |[[:human_genes:D:DIABLO|DIABLO]]|3.84|<0.01| |[[:human_genes:F:FAF2|FAF2]]|3.87|<0.01| |[[:human_genes:U:UBE2K|UBE2K]]|4.01|<0.01| |[[:human_genes:T:TLE4|TLE4]]|4.07|<0.01| |[[:human_genes:C:CASP9|CASP9]]|4.44|<0.01| |[[:human_genes:C:CYCS|CYCS]]|4.90|<0.01| |[[:human_genes:R:RPL11|RPL11]]|4.93|<0.01| |[[:human_genes:H:HCCS|HCCS]]|5.04|<0.01| |[[:human_genes:H:HEATR3|HEATR3]]|5.16|<0.01| |[[:human_genes:U:UBQLN1|UBQLN1]]|5.17|<0.01| |[[:human_genes:V:VDAC2|VDAC2]]|5.29|<0.01| |[[:human_genes:P:PLAA|PLAA]]|5.79|<0.01| |[[:human_genes:A:APAF1|APAF1]]|6.23|<0.01| |[[:human_genes:E:ENY2|ENY2]]|6.31|<0.01| |[[:human_genes:X:XPO7|XPO7]]|6.32|<0.01| |[[:human_genes:M:MARCH5|MARCH5]]|6.98|<0.01| |[[:human_genes:B:BAK1|BAK1]]|7.18|<0.01| |[[:human_genes:U:UCK2|UCK2]]|7.25|<0.01| |[[:human_genes:T:TP53|TP53]]|8.50|<0.01| ^Screen^Correlation^Plot^ |[[:results:exp3|Actinomycin-D 0.001μM R00 exp3]]|0.31|| |[[:results:exp28|Pimelic-diphenylamide-106 5μM R00 exp28]]|0.198|| |[[:results:exp34|Rotenone 20μM R00 exp34]]|0.193|| |[[:results:exp19|Etoposide 1μM R00 exp19]]|0.181|| |[[:results:exp199|Etoposide 0.3μM R05 exp199]]|0.164|| |[[:results:exp456|Benzoate 20000μM R08 exp456]]|0.153|| |[[:results:exp503|Mitomycin-C 0.06μM R08 exp503]]|0.139|| |[[:results:exp472|CI-1040 9.5μM R08 exp472]]|0.132|| |[[:results:exp531|THZ1 0.06μM R08 exp531]]|0.128|| |[[:results:exp478|Doxorubicin 0.02μM R08 exp478]]|0.121|| |[[:results:exp459|Bleomycin 5μM R08 exp459]]|0.115|| |[[:results:exp211|AICAR 240μM R05 exp211]]|0.114|| |[[:results:exp22|MLN-4924 2μM R00 exp22]]|0.111|| |[[:results:exp80|RO-3307 4.7μM R02 exp80]]|0.11|| |[[:results:exp440|Aphidicolin 0.4μM R08 exp440]]|0.107|| |[[:results:exp106|UM131593 0.2μM R03 exp106]]|0.106|| |[[:results:exp259|6-Thio-2-deoxyguanosine 2μM R06 exp259]]|0.105|| |[[:results:exp17|DABN 20μM R00 exp17]]|0.098|| |[[:results:exp135|MS023 7μM R03 exp135]]|0.096|| |[[:results:exp443|SNS-032 15μM R08 exp443]]|0.092|| |[[:results:exp7|Bortezomib 0.05μM R00 exp7]]|0.088|| |[[:results:exp485|GSK626616 14μM R08 exp485]]|0.087|| |[[:results:exp451|Atovaquone 15μM R08 exp451]]|0.086|| |[[:results:exp512|Olaparib 4μM R08 exp512]]|0.086|| |[[:results:exp515|PU-H71 1μM R08 exp515]]|0.086|| |[[:results:exp527|Tanespimycin 14μM R08 exp527]]|0.082|| |[[:results:exp435|JQ1 0.8μM R08 exp435]]|0.08|| |[[:results:exp489|Hippuristanol 0.12μM R08 exp489 no dilution day6]]|0.074|| |[[:results:exp116|AICAR 240μM R03 exp116]]|0.072|| |[[:results:exp524|Staurosporine 0.02μM R08 exp524]]|0.071|| |[[:results:exp488|Hippuristanol 0.12μM R08 exp488]]|0.07|| |[[:results:exp350|Deferoxamine 11μM R07 exp350]]|0.068|| |[[:results:exp126|GSK461364A 0.1μM R03 exp126]]|0.068|| |[[:results:exp354|Diepoxybutane 3μM R07 exp354]]|0.067|| |[[:results:exp474|CR131-b 0.005μM R08 exp474]]|0.067|| |[[:results:exp33|Rotenone 2μM R00 exp33]]|0.061|| |[[:results:exp85|UM0129480 7μM R02 exp85]]|0.059|| |[[:results:exp448|Ammonium tetrathiomolybdate 10μM R08 exp448]]|0.059|| |[[:results:exp355|Dinaciclib 0.007μM R07 exp355]]|0.056|| |[[:results:exp500|LY2090314 0.003μM R08 exp500 no dilution day6]]|0.055|| |[[:results:exp20|Etoposide 10μM R00 exp20]]|0.055|| |[[:results:exp343|Centrinone 0.5μM R07 exp343]]|0.055|| |[[:results:exp357|Dorsomorphin 5μM R07 exp357]]|0.054|| |[[:results:exp21|MLN-4924 0.2μM R00 exp21]]|0.053|| |[[:results:exp134|MS023 2μM R03 exp134]]|0.053|| |[[:results:exp450|Artemisinin 50μM R08 exp450]]|0.052|| |[[:results:exp460|BML-284 0.09μM R08 exp460]]|0.051|| |[[:results:exp96|BI-2536 0.02μM R03 exp96]]|0.051|| |[[:results:exp539|42°C R08 exp539]]|0.091|| {{:chemogenomics:comparison_plots:exp2_vs_exp3.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp28.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp34.png?nolink |}} {{:chemogenomics:comparison_plots:exp19_vs_exp2.png?nolink |}} {{:chemogenomics:comparison_plots:exp199_vs_exp2.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp456.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp503.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp472.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp531.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp478.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp459.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp211.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp22.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp80.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp440.png?nolink |}} {{:chemogenomics:comparison_plots:exp106_vs_exp2.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp259.png?nolink |}} {{:chemogenomics:comparison_plots:exp17_vs_exp2.png?nolink |}} {{:chemogenomics:comparison_plots:exp135_vs_exp2.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp443.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp7.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp485.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp451.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp512.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp515.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp527.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp435.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp489.png?nolink |}} {{:chemogenomics:comparison_plots:exp116_vs_exp2.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp488.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp350.png?nolink |}} {{:chemogenomics:comparison_plots:exp126_vs_exp2.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp354.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp474.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp33.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp85.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp448.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp355.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp500.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp20.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp343.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp357.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp21.png?nolink |}} {{:chemogenomics:comparison_plots:exp134_vs_exp2.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp450.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp460.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp96.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp539.png?nolink |}} No GO term hits below threshold. (FDR <0.05) ^GO Term^Fold Change^Genes^ |apoptosome|552.70|APAF1,CASP9| |activation of cysteine-type endopeptidase activity involved in apoptotic process by cytochrome c|442.16|APAF1,CYCS,CASP9,DIABLO| |glial cell apoptotic process|276.35|TP53,CASP9| |positive regulation of mitochondrial membrane permeability|59.22|TP53,BAK1,VDAC2| |cellular response to UV|31.76|TP53,BAK1,CASP9,AURKB,CDKN1A| |intrinsic apoptotic signaling pathway in response to DNA damage|31.14|TP53,BAK1,CASP9,CDKN1A| |cellular response to light stimulus|24.90|TP53,BAK1,CASP9,AURKB,CDKN1A| |intrinsic apoptotic signaling pathway|24.18|TP53,BAK1,APAF1,CYCS,CASP9,DIABLO,CDKN1A| |positive regulation of cysteine-type endopeptidase activity|22.29|BAK1,APAF1,CYCS,CASP9,DIABLO| |positive regulation of endopeptidase activity|19.06|BAK1,APAF1,CYCS,CASP9,DIABLO| |response to UV|18.55|TP53,BAK1,CASP9,AURKB,CDKN1A| |positive regulation of peptidase activity|17.38|BAK1,APAF1,CYCS,CASP9,DIABLO| |cellular response to radiation|16.55|TP53,BAK1,CASP9,AURKB,CDKN1A| |apoptotic signaling pathway|14.36|TP53,BAK1,APAF1,VDAC2,CYCS,CASP9,DIABLO,CDKN1A| |ubiquitin protein ligase binding|11.09|TP53,RPL11,UBE2K,FAF2,UBE2G1,CDKN1A| |ubiquitin-like protein ligase binding|10.46|TP53,RPL11,UBE2K,FAF2,UBE2G1,CDKN1A| |positive regulation of programmed cell death|8.70|TP53,BAK1,APAF1,RPL11,CASP9,DIABLO,CDKN1A,ID3| |regulation of DNA metabolic process|8.69|TP53,ENY2,APAF1,MEAF6,KMT5B,AURKB,CDKN1A,ID3| |regulation of proteolysis|8.43|TP53,BAK1,APAF1,UBQLN1,RPL11,CYCS,CASP9,UBE2K,DIABLO|