====== 6-Thio-2-deoxyguanosine 2μM R06 exp259 ====== ==== Mechanism of Action ==== Nucleoside analog, incorporated into telomeric DNA by telomerase, impairs proliferation of telomerase-positive cells * **Class / Subclass 1:** Metabolism / Antimetabolite * **Class / Subclass 2:** DNA Damage, Repair and Replication / Helix-Distorting Adduct ==== Technical Notes ==== * **PubChem Name:** %%2'-Deoxythioguanosine%% * **Synonyms:** 6-thio-dG; β-TGdR; 6-thio-dG;β-TGdR * **CAS #:** 789-61-7 * **PubChem CID:** [[https://pubchem.ncbi.nlm.nih.gov/compound/3000603|3000603]] * **IUPAC:** %%2-amino-9-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-3H-purine-6-thione%% * **INCHI Name:** InChI=1S/C10H13N5O3S/c11-10-13-8-7(9(19)14-10)12-3-15(8)6-1-4(17)5(2-16)18-6/h3-6,16-17H,1-2H2,(H3,11,13,14,19)/t4-,5+,6+/m0/s1 * **INCHI Key:** SCVJRXQHFJXZFZ-KVQBGUIXSA-N * **Molecular Weight:** 283.31 * **Canonical SMILES:** C1C(C(OC1N2C=NC3=C2NC(=NC3=S)N)CO)O * **Isomeric SMILES:** C1[C@@H]([C@H](O[C@H]1N2C=NC3=C2NC(=NC3=S)N)CO)O * **Molecular Formula:** C10H13N5O3S {{:chemogenomics:structures:chem-0154.svg?nolink}} * **Supplier Name:** Selleck Chemicals * **Catalog #:** S7757 * **Lot #:** N/A * **HRMS (ESI-TOF) m/z:** (M+H)+ Calcd for C10H13N5O3S 284.08119; found 284.07903 Dose response curve not available. ==== Screen Summary ==== * **Round**: 06 * **Dose**: 2µM * **Days of incubation**: 8 * **Doublings**: 0.6 * **Numbers of reads**: 8752501 ==== 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^ |0/28|[[https://files.tyerslab.com/files/public/chemogenomics/cranks/6-Thio-2-deoxyguanosine_2uM_Round-6_exp259.txt|Scores]]|||||| {{:chemogenomics:cranks_plots:exp259.png?nolink}} ^Gene^CRANKS Score^FDR^ |[[:human_genes:C:CKAP5|CKAP5]]|-2.81|0.56| |[[:human_genes:M:MAU2|MAU2]]|-2.63|0.56| |[[:human_genes:P:PPP2CA|PPP2CA]]|-2.59|0.20| |[[:human_genes:T:TMEM132A|TMEM132A]]|-2.56|0.20| |[[:human_genes:R:RAPSN|RAPSN]]|-2.48|0.20| |[[:human_genes:I:IL1RL2|IL1RL2]]|-2.43|0.20| |[[:human_genes:M:MGA|MGA]]|-2.36|0.20| |[[:human_genes:I:INTS6|INTS6]]|-2.34|0.56| |[[:human_genes:C:CCNA2|CCNA2]]|-2.29|0.53| |[[:human_genes:O:ORC1|ORC1]]|-2.28|0.53| |[[:human_genes:S:SV2A|SV2A]]|-2.27|0.22| |[[:human_genes:C:C12orf66|C12orf66]]|-2.27|0.22| |[[:human_genes:C:CDT1|CDT1]]|-2.24|0.56| |[[:human_genes:Z:ZFAND2B|ZFAND2B]]|-2.21|0.53| |[[:human_genes:P:PRC1|PRC1]]|-2.21|0.56| |[[:human_genes:L:LANCL2|LANCL2]]|-2.18|0.56| |[[:human_genes:P:PPP2R1A|PPP2R1A]]|-2.15|0.53| |[[:human_genes:S:SKIV2L2|SKIV2L2]]|-2.15|0.57| |[[:human_genes:F:FGF10|FGF10]]|-2.08|0.56| |[[:human_genes:W:WEE1|WEE1]]|-2.07|0.61| |[[:human_genes:T:TICRR|TICRR]]|-2.05|0.56| |[[:human_genes:I:INCENP|INCENP]]|-2.04|0.63| |[[:human_genes:D:DNAJB8|DNAJB8]]|-2.04|0.53| |[[:human_genes:P:POLA1|POLA1]]|-2.03|0.75| |[[:human_genes:P:PSMC6|PSMC6]]|-2.02|0.56| |[[:human_genes:Z:ZFAND5|ZFAND5]]|-2.01|0.53| |[[:human_genes:Z:ZNF821|ZNF821]]|-1.98|0.56| |[[:human_genes:V:VPREB1|VPREB1]]|-1.97|0.56| |[[:human_genes:C:CACNA1F|CACNA1F]]|-1.97|0.56| |[[:human_genes:M:MEIG1|MEIG1]]|-1.96|0.69| |[[:human_genes:H:H2AFZ|H2AFZ]]|2.32|0.04| |[[:human_genes:R:RPS25|RPS25]]|2.32|0.04| |[[:human_genes:U:UBQLN1|UBQLN1]]|2.33|0.04| |[[:human_genes:P:PIK3CD|PIK3CD]]|2.37|0.04| |[[:human_genes:G:GTF3C5|GTF3C5]]|2.37|0.09| |[[:human_genes:P:PPP6C|PPP6C]]|2.39|0.05| |[[:human_genes:T:TUT1|TUT1]]|2.40|0.05| |[[:human_genes:T:THG1L|THG1L]]|2.40|0.05| |[[:human_genes:M:MOCS3|MOCS3]]|2.41|0.05| |[[:human_genes:Q:QARS|QARS]]|2.41|0.33| |[[:human_genes:P:PLAA|PLAA]]|2.42|0.03| |[[:human_genes:F:FBXO11|FBXO11]]|2.61|0.03| |[[:human_genes:T:TMED10|TMED10]]|2.66|0.02| |[[:human_genes:V:VDAC2|VDAC2]]|2.71|<0.01| |[[:human_genes:I:INO80C|INO80C]]|2.72|<0.01| |[[:human_genes:C:CTU1|CTU1]]|2.76|<0.01| |[[:human_genes:I:IKZF1|IKZF1]]|2.88|<0.01| |[[:human_genes:I:IRF2|IRF2]]|3.09|<0.01| |[[:human_genes:E:ENY2|ENY2]]|3.11|<0.01| |[[:human_genes:E:ELP3|ELP3]]|3.14|<0.01| |[[:human_genes:R:RPTOR|RPTOR]]|3.16|<0.01| |[[:human_genes:K:KCTD5|KCTD5]]|3.23|<0.01| |[[:human_genes:E:EIF4A1|EIF4A1]]|3.37|<0.01| |[[:human_genes:F:FAF2|FAF2]]|3.53|<0.01| |[[:human_genes:G:GOLGA8H|GOLGA8H]]|3.55|0.03| |[[:human_genes:G:GUK1|GUK1]]|4.00|<0.01| |[[:human_genes:B:BAK1|BAK1]]|4.51|<0.01| |[[:human_genes:S:SLC43A3|SLC43A3]]|4.89|<0.01| |[[:human_genes:N:NUDT5|NUDT5]]|8.08|<0.01| |[[:human_genes:H:HPRT1|HPRT1]]|8.50|<0.01| ^Screen^Correlation^Plot^ |[[:results:exp456|Benzoate 20000μM R08 exp456]]|0.16|| |[[:results:exp135|MS023 7μM R03 exp135]]|0.118|| |[[:results:exp459|Bleomycin 5μM R08 exp459]]|0.109|| |[[:results:exp199|Etoposide 0.3μM R05 exp199]]|0.109|| |[[:results:exp472|CI-1040 9.5μM R08 exp472]]|0.101|| |[[:results:exp80|RO-3307 4.7μM R02 exp80]]|0.099|| |[[:results:exp85|UM0129480 7μM R02 exp85]]|0.097|| |[[:results:exp478|Doxorubicin 0.02μM R08 exp478]]|0.096|| |[[:results:exp531|THZ1 0.06μM R08 exp531]]|0.096|| |[[:results:exp503|Mitomycin-C 0.06μM R08 exp503]]|0.086|| |[[:results:exp527|Tanespimycin 14μM R08 exp527]]|0.084|| |[[:results:exp3|Actinomycin-D 0.001μM R00 exp3]]|0.083|| |[[:results:exp443|SNS-032 15μM R08 exp443]]|0.081|| |[[:results:exp488|Hippuristanol 0.12μM R08 exp488]]|0.077|| |[[:results:exp211|AICAR 240μM R05 exp211]]|0.076|| |[[:results:exp28|Pimelic-diphenylamide-106 5μM R00 exp28]]|0.076|| |[[:results:exp357|Dorsomorphin 5μM R07 exp357]]|0.076|| |[[:results:exp489|Hippuristanol 0.12μM R08 exp489 no dilution day6]]|0.074|| |[[:results:exp512|Olaparib 4μM R08 exp512]]|0.073|| |[[:results:exp34|Rotenone 20μM R00 exp34]]|0.071|| |[[:results:exp515|PU-H71 1μM R08 exp515]]|0.07|| |[[:results:exp450|Artemisinin 50μM R08 exp450]]|0.069|| |[[:results:exp21|MLN-4924 0.2μM R00 exp21]]|0.069|| |[[:results:exp440|Aphidicolin 0.4μM R08 exp440]]|0.068|| |[[:results:exp134|MS023 2μM R03 exp134]]|0.067|| |[[:results:exp116|AICAR 240μM R03 exp116]]|0.063|| |[[:results:exp355|Dinaciclib 0.007μM R07 exp355]]|0.062|| |[[:results:exp19|Etoposide 1μM R00 exp19]]|0.062|| |[[:results:exp451|Atovaquone 15μM R08 exp451]]|0.062|| |[[:results:exp108|Vinblastine 0.2μM R03 exp108]]|0.062|| |[[:results:exp524|Staurosporine 0.02μM R08 exp524]]|0.06|| |[[:results:exp234|Ethanol 0.01 R05 exp234]]|0.057|| |[[:results:exp485|GSK626616 14μM R08 exp485]]|0.056|| |[[:results:exp435|JQ1 0.8μM R08 exp435]]|0.054|| |[[:results:exp468|CB-5083 0.4μM R08 exp468]]|0.053|| |[[:results:exp502|Milciclib 2μM R08 exp502]]|0.052|| |[[:results:exp96|BI-2536 0.02μM R03 exp96]]|0.051|| |[[:results:exp2|5-Fluorouracil 20μM R00 exp2]]|0.105|| |[[:results:exp214|2-Deoxy-D-glucose 800μM R05 exp214]]|0.058|| {{:chemogenomics:comparison_plots:exp259_vs_exp456.png?nolink |}} {{:chemogenomics:comparison_plots:exp135_vs_exp259.png?nolink |}} {{:chemogenomics:comparison_plots:exp259_vs_exp459.png?nolink |}} {{:chemogenomics:comparison_plots:exp199_vs_exp259.png?nolink |}} {{:chemogenomics:comparison_plots:exp259_vs_exp472.png?nolink |}} {{:chemogenomics:comparison_plots:exp259_vs_exp80.png?nolink |}} {{:chemogenomics:comparison_plots:exp259_vs_exp85.png?nolink |}} {{:chemogenomics:comparison_plots:exp259_vs_exp478.png?nolink |}} {{:chemogenomics:comparison_plots:exp259_vs_exp531.png?nolink |}} {{:chemogenomics:comparison_plots:exp259_vs_exp503.png?nolink |}} {{:chemogenomics:comparison_plots:exp259_vs_exp527.png?nolink |}} {{:chemogenomics:comparison_plots:exp259_vs_exp3.png?nolink |}} {{:chemogenomics:comparison_plots:exp259_vs_exp443.png?nolink |}} {{:chemogenomics:comparison_plots:exp259_vs_exp488.png?nolink |}} {{:chemogenomics:comparison_plots:exp211_vs_exp259.png?nolink |}} {{:chemogenomics:comparison_plots:exp259_vs_exp28.png?nolink |}} {{:chemogenomics:comparison_plots:exp259_vs_exp357.png?nolink |}} {{:chemogenomics:comparison_plots:exp259_vs_exp489.png?nolink |}} {{:chemogenomics:comparison_plots:exp259_vs_exp512.png?nolink |}} {{:chemogenomics:comparison_plots:exp259_vs_exp34.png?nolink |}} {{:chemogenomics:comparison_plots:exp259_vs_exp515.png?nolink |}} {{:chemogenomics:comparison_plots:exp259_vs_exp450.png?nolink |}} {{:chemogenomics:comparison_plots:exp21_vs_exp259.png?nolink |}} {{:chemogenomics:comparison_plots:exp259_vs_exp440.png?nolink |}} {{:chemogenomics:comparison_plots:exp134_vs_exp259.png?nolink |}} {{:chemogenomics:comparison_plots:exp116_vs_exp259.png?nolink |}} {{:chemogenomics:comparison_plots:exp259_vs_exp355.png?nolink |}} {{:chemogenomics:comparison_plots:exp19_vs_exp259.png?nolink |}} {{:chemogenomics:comparison_plots:exp259_vs_exp451.png?nolink |}} {{:chemogenomics:comparison_plots:exp108_vs_exp259.png?nolink |}} {{:chemogenomics:comparison_plots:exp259_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp234_vs_exp259.png?nolink |}} {{:chemogenomics:comparison_plots:exp259_vs_exp485.png?nolink |}} {{:chemogenomics:comparison_plots:exp259_vs_exp435.png?nolink |}} {{:chemogenomics:comparison_plots:exp259_vs_exp468.png?nolink |}} {{:chemogenomics:comparison_plots:exp259_vs_exp502.png?nolink |}} {{:chemogenomics:comparison_plots:exp259_vs_exp96.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp259.png?nolink |}} {{:chemogenomics:comparison_plots:exp214_vs_exp259.png?nolink |}} ^GO Term^Fold Change^Genes^ |DNA replication checkpoint signaling|108.31|ORC1,CDT1,TICRR| |regulation of DNA replication|25.15|PPP2CA,CCNA2,CDT1,PPP2R1A,TICRR| |mitotic cell cycle process|13.03|CKAP5,CCNA2,ORC1,CDT1,PRC1,PPP2R1A,FGF10,WEE1,TICRR,INCENP,POLA1| |mitotic cell cycle|12.23|CKAP5,PPP2CA,CCNA2,ORC1,CDT1,PRC1,PPP2R1A,FGF10,WEE1,TICRR,INCENP,POLA1| |regulation of mitotic cell cycle phase transition|11.40|PPP2CA,ORC1,FGF10,WEE1,TICRR,INCENP| |regulation of cell cycle phase transition|10.33|PPP2CA,ORC1,CDT1,FGF10,WEE1,TICRR,INCENP| |chromosomal region|9.90|CKAP5,PPP2CA,ORC1,CDT1,PPP2R1A,INCENP| |cell division|8.47|CKAP5,MAU2,CCNA2,CDT1,PRC1,WEE1,INCENP| |cell cycle process|8.43|CKAP5,MAU2,CCNA2,ORC1,CDT1,PRC1,PPP2R1A,FGF10,WEE1,TICRR,INCENP,POLA1| |regulation of cell cycle process|7.97|PPP2CA,ORC1,CDT1,PRC1,PPP2R1A,FGF10,WEE1,TICRR,INCENP| ^GO Term^Fold Change^Genes^ |protein urmylation|368.27|CTU1,MOCS3| |tRNA thio-modification|276.20|CTU1,MOCS3| |tRNA wobble uridine modification|103.58|ELP3,CTU1,MOCS3| |tRNA wobble base modification|87.22|ELP3,CTU1,MOCS3| |tRNA modification|25.11|ELP3,CTU1,MOCS3,THG1L| |nucleotidyltransferase activity|20.31|NUDT5,CTU1,MOCS3,THG1L,TUT1| |tRNA metabolic process|17.92|ELP3,CTU1,QARS1,MOCS3,THG1L,GTF3C5| |ncRNA metabolic process|8.79|ELP3,CTU1,QARS1,MOCS3,THG1L,TUT1,GTF3C5,RPS25| |intracellular protein-containing complex|5.68|EIF4A1,KCTD5,RPTOR,ELP3,ENY2,CTU1,FBXO11,QARS1,UBQLN1|