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Ask your administrator if you think this is wrong. ====== Pyridostatin 4μM R05 exp240 ====== ==== Mechanism of Action ==== Binds and stabilizes telomeric and interstitial G-quadruplexes * **<color #00a2e8>Class / Subclass 1:</color>** DNA Damage, Repair and Replication / G-Quadruplex Stabilizer ==== Technical Notes ==== <accordion collapsed='true'> <panel title='Compound References' collapsed='true'> * **<color #00a2e8>PubChem Name:</color>** %%Pyridostatin%% * **<color #00a2e8>Synonyms:</color>** N/A * **<color #00a2e8>CAS #:</color>** 1085412-37-8 * **<color #00a2e8>PubChem CID:</color>** [[https://pubchem.ncbi.nlm.nih.gov/compound/25227847|25227847]] * **<color #00a2e8>IUPAC:</color>** %%4-(2-aminoethoxy)-2-N,6-N-bis[4-(2-aminoethoxy)quinolin-2-yl]pyridine-2,6-dicarboxamide%% * **<color #00a2e8>INCHI Name:</color>** InChI=1S/C31H32N8O5/c32-9-12-42-19-15-24(30(40)38-28-17-26(43-13-10-33)20-5-1-3-7-22(20)36-28)35-25(16-19)31(41)39-29-18-27(44-14-11-34)21-6-2-4-8-23(21)37-29/h1-8,15-18H,9-14,32-34H2,(H,36,38,40)(H,37,39,41) * **<color #00a2e8>INCHI Key:</color>** VGHSATQVJCTKEF-UHFFFAOYSA-N * **<color #00a2e8>Molecular Weight:</color>** 596.6 * **<color #00a2e8>Canonical SMILES:</color>** C1=CC=C2C(=C1)C(=CC(=N2)NC(=O)C3=CC(=CC(=N3)C(=O)NC4=NC5=CC=CC=C5C(=C4)OCCN)OCCN)OCCN * **<color #00a2e8>Isomeric SMILES:</color>** N/A * **<color #00a2e8>Molecular Formula:</color>** C31H32N8O5 {{:chemogenomics:structures:chem-0145.svg?nolink}} </panel> <panel title='Compound Supplier' collapsed='true'> * **<color #00a2e8>Supplier Name:</color>** Chemietek * **<color #00a2e8>Catalog #:</color>** CT-PYRI * **<color #00a2e8>Lot #:</color>** N/A </panel> <panel title='Compound Characterization' collapsed='true'> * **<color #00a2e8>HRMS (ESI-TOF) m/z:</color>** [M+H]+ Calcd for C31H33N8O5 597.2569; found 597.2543 </panel> <panel title='Dose Response Curve' collapsed='true'> * **<color #00a2e8>Platform ID:</color>** Pyridostatin * **<color #00a2e8>Min:</color>** -4.5804; **<color #00a2e8>Max:</color>** 98.7377 {{:chemogenomics:dose_response:dr_234.png?nolink&500 |}} \\ \\ \\ \\ |< 300px 100px 200px >| ^ IC ^ Concentration (µM) ^ | IC10 |N/A | | IC20 |3.3625 | | IC30 |4.0583 | | IC40 |4.7348 | | IC50 |5.4543 | | IC60 |N/A | | IC70 |N/A | | IC80 |N/A | | IC90 |N/A | \\ </panel> </accordion> ==== Screen Summary ==== * **<color #00a2e8>Round</color>**: 05 * **<color #00a2e8>Dose</color>**: 4µM * **<color #00a2e8>Days of incubation</color>**: 8 * **<color #00a2e8>Doublings</color>**: 1.6 * **<color #00a2e8>Numbers of reads</color>**: 14359977 ==== 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^ |11/38|<color #e85500>[[https://files.tyerslab.com/files/public/chemogenomics/cranks/Pyridostatin_4uM_Round-5_exp240.txt|Scores]]</color>|<button type="primary" size="sm" modal="ScorePlot">View</button>|<button type="primary" size="sm" modal="modal_hits">View</button>|<button type="primary" size="sm" modal="modal_screen_similarity">View</button>|<button type="primary" size="sm" modal="modal_go_sensitive">View</button>|<button type="primary" size="sm" modal="modal_go_resistant">View</button>| <modal id='ScorePlot' size='lg' title='Pyridostatin 4μM R05 exp240'> {{:chemogenomics:cranks_plots:exp240.png?nolink}} </modal> <modal id="modal_hits" size="sm" title="Top 30 S/R Genes"> ^Gene^CRANKS Score^FDR^ |[[:human_genes:A:ATP8B2|ATP8B2]]|-5.08|<0.01| |[[:human_genes:D:DHX36|DHX36]]|-3.70|<0.01| |[[:human_genes:T:TMEM30A|TMEM30A]]|-3.62|<0.01| |[[:human_genes:M:MCM9|MCM9]]|-3.10|<0.01| |[[:human_genes:L:LEF1|LEF1]]|-3.09|<0.01| |[[:human_genes:R:RHOA|RHOA]]|-3.03|<0.01| |[[:human_genes:N:NHEJ1|NHEJ1]]|-3.03|<0.01| |[[:human_genes:R:RAD54L2|RAD54L2]]|-2.86|<0.01| |[[:human_genes:Z:ZSWIM7|ZSWIM7]]|-2.67|0.01| |[[:human_genes:Z:ZNF451|ZNF451]]|-2.57|0.05| |[[:human_genes:S:SWI5|SWI5]]|-2.54|0.05| |[[:human_genes:T:TNPO1|TNPO1]]|-2.53|0.03| |[[:human_genes:A:ATP6AP1|ATP6AP1]]|-2.52|0.19| |[[:human_genes:K:KPNB1|KPNB1]]|-2.51|0.40| |[[:human_genes:K:KANK4|KANK4]]|-2.50|0.06| |[[:human_genes:C:C7orf49|C7orf49]]|-2.50|0.03| |[[:human_genes:L:LIG4|LIG4]]|-2.49|0.06| |[[:human_genes:H:HIST1H1B|HIST1H1B]]|-2.41|0.05| |[[:human_genes:B:BRE|BRE]]|-2.25|0.10| |[[:human_genes:T:TDP2|TDP2]]|-2.25|0.18| |[[:human_genes:D:DERL2|DERL2]]|-2.23|0.18| |[[:human_genes:R:RAD54L|RAD54L]]|-2.19|0.13| |[[:human_genes:V:VRK1|VRK1]]|-2.14|0.23| |[[:human_genes:A:ARL1|ARL1]]|-2.12|0.18| |[[:human_genes:A:AP2A1|AP2A1]]|-2.11|0.18| |[[:human_genes:U:UBE2N|UBE2N]]|-2.10|0.25| |[[:human_genes:S:SLC25A25|SLC25A25]]|-2.09|0.18| |[[:human_genes:X:XRCC4|XRCC4]]|-2.09|0.18| |[[:human_genes:S:SNRPD3|SNRPD3]]|-2.08|0.61| |[[:human_genes:F:FZR1|FZR1]]|-2.06|0.36| |[[:human_genes:C:CHST15|CHST15]]|2.41|0.04| |[[:human_genes:U:UBXN7|UBXN7]]|2.42|0.02| |[[:human_genes:S:SNRNP70|SNRNP70]]|2.43|0.20| |[[:human_genes:E:EIF4G1|EIF4G1]]|2.48|0.03| |[[:human_genes:U:UBQLN1|UBQLN1]]|2.51|0.01| |[[:human_genes:D:DEGS1|DEGS1]]|2.52|0.01| |[[:human_genes:P:PCBP2|PCBP2]]|2.52|0.01| |[[:human_genes:C:CYCS|CYCS]]|2.59|0.01| |[[:human_genes:P:PACSIN2|PACSIN2]]|2.59|0.01| |[[:human_genes:C:CCDC58|CCDC58]]|2.60|0.02| |[[:human_genes:C:CHSY1|CHSY1]]|2.60|0.01| |[[:human_genes:N:NANS|NANS]]|2.66|<0.01| |[[:human_genes:H:HEATR3|HEATR3]]|2.72|<0.01| |[[:human_genes:B:B3GAT3|B3GAT3]]|2.75|0.01| |[[:human_genes:C:CCNL1|CCNL1]]|2.82|<0.01| |[[:human_genes:A:ARID4B|ARID4B]]|2.85|<0.01| |[[:human_genes:P:PAPSS1|PAPSS1]]|2.94|<0.01| |[[:human_genes:A:APAF1|APAF1]]|2.98|<0.01| |[[:human_genes:S:SNN|SNN]]|3.00|<0.01| |[[:human_genes:B:B3GALT6|B3GALT6]]|3.08|<0.01| |[[:human_genes:N:NAA15|NAA15]]|3.12|<0.01| |[[:human_genes:B:BAK1|BAK1]]|3.18|<0.01| |[[:human_genes:K:KAT7|KAT7]]|3.22|<0.01| |[[:human_genes:E:EIF3A|EIF3A]]|3.23|<0.01| |[[:human_genes:B:BRD1|BRD1]]|3.59|<0.01| |[[:human_genes:R:RABIF|RABIF]]|3.78|<0.01| |[[:human_genes:T:TOP2A|TOP2A]]|4.11|<0.01| |[[:human_genes:E:EIF4A1|EIF4A1]]|4.50|<0.01| |[[:human_genes:T:TOP2B|TOP2B]]|4.79|<0.01| |[[:human_genes:C:COPS7B|COPS7B]]|5.28|<0.01| </modal> <modal id="modal_screen_similarity" size="lg" title="Correlated Screens"> ^Screen^Correlation^Plot^ |[[:results:exp190|Vincristine 0.0005μM R04 exp190]]|0.053|<button type="primary" size="small" modal="1">View</button>| |[[:results:exp444|THZ531 0.225μM R08 exp444]]|0.051|<button type="primary" size="small" modal="2">View</button>| |[[:results:exp198|Etoposide 0.1μM R05 exp198]]|0.123|<button type="primary" size="small" modal="3">View</button>| |[[:results:exp478|Doxorubicin 0.02μM R08 exp478]]|0.108|<button type="primary" size="small" modal="4">View</button>| |[[:results:exp360|Genistein 15μM R07 exp360]]|0.098|<button type="primary" size="small" modal="5">View</button>| |[[:results:exp357|Dorsomorphin 5μM R07 exp357]]|0.083|<button type="primary" size="small" modal="6">View</button>| |[[:results:exp199|Etoposide 0.3μM R05 exp199]]|0.081|<button type="primary" size="small" modal="7">View</button>| |[[:results:exp210|LB-100 2μM R05 exp210]]|0.078|<button type="primary" size="small" modal="8">View</button>| |[[:results:exp72|LB-100 4.1μM R02 exp72]]|0.073|<button type="primary" size="small" modal="9">View</button>| |[[:results:exp488|Hippuristanol 0.12μM R08 exp488]]|0.063|<button type="primary" size="small" modal="10">View</button>| |[[:results:exp3|Actinomycin-D 0.001μM R00 exp3]]|0.062|<button type="primary" size="small" modal="11">View</button>| |[[:results:exp512|Olaparib 4μM R08 exp512]]|0.057|<button type="primary" size="small" modal="12">View</button>| |[[:results:exp374|Latrunculin-B 10μM R07 exp374]]|0.054|<button type="primary" size="small" modal="13">View</button>| |[[:results:exp497|Lead acetate 2000μM R08 exp497]]|0.052|<button type="primary" size="small" modal="14">View</button>| |[[:results:exp234|Ethanol 0.01 R05 exp234]]|0.052|<button type="primary" size="small" modal="15">View</button>| </modal> <modal id="1" size="lg" title="Pyridostatin 4μM R05 exp240 vs Vincristine 0.0005μM R04 exp190"> {{:chemogenomics:comparison_plots:exp190_vs_exp240.png?nolink |}} </modal> <modal id="2" size="lg" title="Pyridostatin 4μM R05 exp240 vs THZ531 0.225μM R08 exp444"> {{:chemogenomics:comparison_plots:exp240_vs_exp444.png?nolink |}} </modal> <modal id="3" size="lg" title="Etoposide 0.1μM R05 exp198 vs Pyridostatin 4μM R05 exp240"> {{:chemogenomics:comparison_plots:exp198_vs_exp240.png?nolink |}} </modal> <modal id="4" size="lg" title="Doxorubicin 0.02μM R08 exp478 vs Pyridostatin 4μM R05 exp240"> {{:chemogenomics:comparison_plots:exp240_vs_exp478.png?nolink |}} </modal> <modal id="5" size="lg" title="Genistein 15μM R07 exp360 vs Pyridostatin 4μM R05 exp240"> {{:chemogenomics:comparison_plots:exp240_vs_exp360.png?nolink |}} </modal> <modal id="6" size="lg" title="Dorsomorphin 5μM R07 exp357 vs Pyridostatin 4μM R05 exp240"> {{:chemogenomics:comparison_plots:exp240_vs_exp357.png?nolink |}} </modal> <modal id="7" size="lg" title="Etoposide 0.3μM R05 exp199 vs Pyridostatin 4μM R05 exp240"> {{:chemogenomics:comparison_plots:exp199_vs_exp240.png?nolink |}} </modal> <modal id="8" size="lg" title="LB-100 2μM R05 exp210 vs Pyridostatin 4μM R05 exp240"> {{:chemogenomics:comparison_plots:exp210_vs_exp240.png?nolink |}} </modal> <modal id="9" size="lg" title="LB-100 4.1μM R02 exp72 vs Pyridostatin 4μM R05 exp240"> {{:chemogenomics:comparison_plots:exp240_vs_exp72.png?nolink |}} </modal> <modal id="10" size="lg" title="Hippuristanol 0.12μM R08 exp488 vs Pyridostatin 4μM R05 exp240"> {{:chemogenomics:comparison_plots:exp240_vs_exp488.png?nolink |}} </modal> <modal id="11" size="lg" title="Actinomycin-D 0.001μM R00 exp3 vs Pyridostatin 4μM R05 exp240"> {{:chemogenomics:comparison_plots:exp240_vs_exp3.png?nolink |}} </modal> <modal id="12" size="lg" title="Olaparib 4μM R08 exp512 vs Pyridostatin 4μM R05 exp240"> {{:chemogenomics:comparison_plots:exp240_vs_exp512.png?nolink |}} </modal> <modal id="13" size="lg" title="Latrunculin-B 10μM R07 exp374 vs Pyridostatin 4μM R05 exp240"> {{:chemogenomics:comparison_plots:exp240_vs_exp374.png?nolink |}} </modal> <modal id="14" size="lg" title="Lead acetate 2000μM R08 exp497 vs Pyridostatin 4μM R05 exp240"> {{:chemogenomics:comparison_plots:exp240_vs_exp497.png?nolink |}} </modal> <modal id="15" size="lg" title="Ethanol 0.01 R05 exp234 vs Pyridostatin 4μM R05 exp240"> {{:chemogenomics:comparison_plots:exp234_vs_exp240.png?nolink |}} </modal> <modal id="modal_go_sensitive" size="lg" title="Top 30 sensitive GO terms"> ^GO Term^Fold Change^Genes^ |DNA ligase IV complex|591.79|LIG4,XRCC4| |DNA ligation involved in DNA repair|443.84|NHEJ1,LIG4,XRCC4| |immunoglobulin V(D)J recombination|295.89|NHEJ1,LIG4,XRCC4| |DNA ligation|197.26|NHEJ1,LIG4,XRCC4| |V(D)J recombination|139.24|LEF1,NHEJ1,LIG4,XRCC4| |DNA repair complex|88.77|NHEJ1,LIG4,XRCC4| |somatic cell DNA recombination|57.74|LEF1,NHEJ1,LIG4,XRCC4| |somatic diversification of immune receptors via germline recombination within a single locus|57.74|LEF1,NHEJ1,LIG4,XRCC4| |somatic diversification of immune receptors|48.31|LEF1,NHEJ1,LIG4,XRCC4| |double-strand break repair|29.44|MCM9,NHEJ1,ZSWIM7,SWI5,LIG4,BABAM2,TDP2,RAD54L,UBE2N,XRCC4| |response to ionizing radiation|26.70|NHEJ1,SWI5,LIG4,BABAM2,RAD54L,XRCC4| |double-strand break repair via homologous recombination|25.51|MCM9,ZSWIM7,SWI5,RAD54L,UBE2N| |recombinational repair|24.86|MCM9,ZSWIM7,SWI5,RAD54L,UBE2N| |DNA recombination|23.78|MCM9,LEF1,NHEJ1,ZSWIM7,SWI5,LIG4,RAD54L,UBE2N,XRCC4| |catalytic activity, acting on DNA|14.98|DHX36,MCM9,RAD54L2,LIG4,TDP2,RAD54L| |DNA repair|12.56|MCM9,NHEJ1,ZSWIM7,SWI5,LIG4,BABAM2,TDP2,RAD54L,UBE2N,XRCC4| |response to radiation|10.10|DHX36,NHEJ1,SWI5,LIG4,BABAM2,RAD54L,XRCC4| |DNA damage response|9.10|MCM9,NHEJ1,ZSWIM7,SWI5,LIG4,BABAM2,TDP2,RAD54L,VRK1,UBE2N,XRCC4| |DNA metabolic process|9.09|MCM9,LEF1,NHEJ1,ZSWIM7,SWI5,LIG4,BABAM2,TDP2,RAD54L,UBE2N,XRCC4| </modal> <modal id="modal_go_resistant" size="lg" title="Top 30 resistant GO terms"> ^GO Term^Fold Change^Genes^ |DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) activity|552.33|TOP2B,TOP2A| |viral translational termination-reinitiation|276.17|EIF3A,EIF3G| |activation of cysteine-type endopeptidase activity involved in apoptotic process by cytochrome c|220.93|APAF1,CYCS| |viral translation|103.56|EIF3A,PCBP2,EIF3G| |chondroitin sulfate proteoglycan biosynthetic process|96.06|B3GALT6,B3GAT3,CHSY1,CHST15| |chondroitin sulfate biosynthetic process|92.06|B3GALT6,CHSY1,CHST15| |cytoplasmic translational initiation|76.18|EIF4A1,EIF3A,EIF4G1,EIF3G| |chondroitin sulfate proteoglycan metabolic process|71.27|B3GALT6,B3GAT3,CHSY1,CHST15| |chondroitin sulfate metabolic process|63.73|B3GALT6,CHSY1,CHST15| |translation initiation factor activity|47.01|EIF4A1,EIF3A,EIF4G1,EIF3G| |proteoglycan biosynthetic process|37.45|B3GALT6,B3GAT3,CHSY1,CHST15| |translational initiation|35.07|EIF4A1,EIF3A,EIF4G1,EIF3G| |glycosaminoglycan biosynthetic process|34.52|B3GALT6,B3GAT3,CHSY1,CHST15| |aminoglycan biosynthetic process|33.47|B3GALT6,B3GAT3,CHSY1,CHST15| |translation factor activity, RNA binding|27.62|EIF4A1,EIF3A,EIF4G1,EIF3G| |proteoglycan metabolic process|26.30|B3GALT6,B3GAT3,CHSY1,CHST15| |translation regulator activity, nucleic acid binding|21.24|EIF4A1,EIF3A,EIF4G1,EIF3G| |glycosaminoglycan metabolic process|21.04|B3GALT6,B3GAT3,CHSY1,CHST15| |sulfur compound biosynthetic process|19.31|B3GALT6,PAPSS1,B3GAT3,CHSY1,CHST15| </modal> Last modified: 2026/01/15 21:36by 127.0.0.1