====== Monensin 0.3μM R08 exp507 ====== ==== Mechanism of Action ==== Polyether antibiotic, binds monovalent cations, Na+/H+ antiporter, blocks Golgi transport * **Class / Subclass 1:** Infectious Disease / Antibiotic * **Class / Subclass 2:** Organelle Function / Membrane Ionophore ==== Technical Notes ==== * **PubChem Name:** %%Monensin sodium%% * **Synonyms:** Monensin A sodium salt * **CAS #:** 22373-78-0 * **PubChem CID:** [[https://pubchem.ncbi.nlm.nih.gov/compound/23667299|23667299]] * **IUPAC:** %%sodium;(2S,3R,4S)-4-[(2S,5R,7S,8R,9S)-2-[(2R,5S)-5-ethyl-5-[(2R,3S,5R)-5-[(2S,3S,5R,6R)-6-hydroxy-6-(hydroxymethyl)-3,5-dimethyloxan-2-yl]-3-methyloxolan-2-yl]oxolan-2-yl]-7-hydroxy-2,8-dimethyl-1,10-dioxaspiro[4.5]decan-9-yl]-3-methoxy-2-methylpentanoate%% * **INCHI Name:** InChI=1S/C36H62O11.Na/c1-10-34(31-20(3)16-26(43-31)28-19(2)15-21(4)36(41,18-37)46-28)12-11-27(44-34)33(8)13-14-35(47-33)17-25(38)22(5)30(45-35)23(6)29(42-9)24(7)32(39)40;/h19-31,37-38,41H,10-18H2,1-9H3,(H,39,40);/q;+1/p-1/t19-,20-,21+,22+,23-,24-,25-,26+,27+,28-,29+,30-,31+,33-,34-,35+,36-;/m0./s1 * **INCHI Key:** XOIQMTLWECTKJL-FBZUZRIGSA-M * **Molecular Weight:** 692.9 * **Canonical SMILES:** CCC1(CCC(O1)C2(CCC3(O2)CC(C(C(O3)C(C)C(C(C)C(=O)[O-])OC)C)O)C)C4C(CC(O4)C5C(CC(C(O5)(CO)O)C)C)C.[Na+] * **Isomeric SMILES:** CC[C@]1(CC[C@@H](O1)[C@@]2(CC[C@@]3(O2)C[C@@H]([C@H]([C@H](O3)[C@@H](C)[C@H]([C@H](C)C(=O)[O-])OC)C)O)C)[C@H]4[C@H](C[C@@H](O4)[C@@H]5[C@H](C[C@H]([C@@](O5)(CO)O)C)C)C.[Na+] * **Molecular Formula:** C36H61NaO11 {{:chemogenomics:structures:chem-0312.svg?nolink}} * **Supplier Name:** Med Chem Express * **Catalog #:** HY-N0150 * **Lot #:** 28765 * **HRMS (ESI-TOF) m/z:** (M+Na)+ Calcd for C36H62O11 693.41843; found 693.41958 * **Platform ID:** Monensin * **Min:** -4.4012; **Max:** 96.4158 {{:chemogenomics:dose_response:dr_467.png?nolink&500 |}} \\ \\ \\ \\ |< 300px 100px 200px >| ^ IC ^ Concentration (µM) ^ | IC10 |N/A | | IC20 |0.0433 | | IC30 |0.0965 | | IC40 |0.1929 | | IC50 |0.3731 | | IC60 |N/A | | IC70 |N/A | | IC80 |N/A | | IC90 |N/A | \\ ==== Screen Summary ==== * **Round**: 08 * **Dose**: 300nM * **Days of incubation**: 8 * **Doublings**: 0.9 * **Numbers of reads**: 16398044 ==== 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^ |19/5|[[https://files.tyerslab.com/files/public/chemogenomics/cranks/Monensin_0.3uM_Round-8_exp507.txt|Scores]]|||||| {{:chemogenomics:cranks_plots:exp507.png?nolink}} ^Gene^CRANKS Score^FDR^ |[[:human_genes:T:TMEM189|TMEM189]]|-3.49|<0.01| |[[:human_genes:A:ARL1|ARL1]]|-3.39|<0.01| |[[:human_genes:C:C10orf76|C10orf76]]|-3.35|<0.01| |[[:human_genes:U:UGCG|UGCG]]|-3.31|<0.01| |[[:human_genes:A:AVL9|AVL9]]|-3.29|<0.01| |[[:human_genes:A:ARFRP1|ARFRP1]]|-3.29|<0.01| |[[:human_genes:A:APBA3|APBA3]]|-3.14|<0.01| |[[:human_genes:C:COPB2|COPB2]]|-3.10|0.06| |[[:human_genes:R:RAB14|RAB14]]|-3.00|<0.01| |[[:human_genes:G:GPR107|GPR107]]|-2.97|<0.01| |[[:human_genes:S:SYS1|SYS1]]|-2.93|0.02| |[[:human_genes:D:DDX23|DDX23]]|-2.84|0.22| |[[:human_genes:S:SPTLC2|SPTLC2]]|-2.82|<0.01| |[[:human_genes:R:RAB1B|RAB1B]]|-2.78|0.02| |[[:human_genes:P:PI4KB|PI4KB]]|-2.68|0.03| |[[:human_genes:U:UXS1|UXS1]]|-2.68|0.01| |[[:human_genes:K:KIAA1432|KIAA1432]]|-2.63|0.03| |[[:human_genes:P:PCYT1A|PCYT1A]]|-2.46|0.03| |[[:human_genes:T:TMEM189-UBE2V1|TMEM189-UBE2V1]]|-2.45|0.03| |[[:human_genes:T:TBC1D23|TBC1D23]]|-2.45|0.03| |[[:human_genes:A:AP5B1|AP5B1]]|-2.44|0.03| |[[:human_genes:P:POLE|POLE]]|-2.38|0.25| |[[:human_genes:C:COPZ1|COPZ1]]|-2.29|0.06| |[[:human_genes:U:UFD1L|UFD1L]]|-2.28|0.17| |[[:human_genes:C:CDIPT|CDIPT]]|-2.28|0.23| |[[:human_genes:E:EFCAB2|EFCAB2]]|-2.27|0.07| |[[:human_genes:P:PSMA7|PSMA7]]|-2.23|0.25| |[[:human_genes:T:TREML1|TREML1]]|-2.22|0.14| |[[:human_genes:C:COPB1|COPB1]]|-2.22|0.33| |[[:human_genes:S:SCN9A|SCN9A]]|-2.20|0.10| |[[:human_genes:N:NRAP|NRAP]]|2.11|0.21| |[[:human_genes:T:TAZ|TAZ]]|2.12|0.42| |[[:human_genes:S:SCUBE2|SCUBE2]]|2.12|0.16| |[[:human_genes:C:COMP|COMP]]|2.13|0.16| |[[:human_genes:C:CRYAB|CRYAB]]|2.13|0.25| |[[:human_genes:S:SCO2|SCO2]]|2.15|0.24| |[[:human_genes:M:MLLT10|MLLT10]]|2.16|0.15| |[[:human_genes:I:ID3|ID3]]|2.19|0.14| |[[:human_genes:D:DCAF15|DCAF15]]|2.20|0.16| |[[:human_genes:Y:YARS2|YARS2]]|2.21|0.16| |[[:human_genes:T:TRIAP1|TRIAP1]]|2.22|0.21| |[[:human_genes:K:KLHL23|KLHL23]]|2.22|0.13| |[[:human_genes:V:VDAC2|VDAC2]]|2.27|0.11| |[[:human_genes:M:MRPS18A|MRPS18A]]|2.27|0.11| |[[:human_genes:D:DDX39A|DDX39A]]|2.29|0.11| |[[:human_genes:S:SPG21|SPG21]]|2.32|0.11| |[[:human_genes:T:TPK1|TPK1]]|2.37|0.12| |[[:human_genes:V:VARS2|VARS2]]|2.37|0.21| |[[:human_genes:M:MRPS33|MRPS33]]|2.41|0.16| |[[:human_genes:U:URM1|URM1]]|2.42|0.08| |[[:human_genes:F:FAM58A|FAM58A]]|2.42|0.08| |[[:human_genes:T:TMEM126B|TMEM126B]]|2.44|0.11| |[[:human_genes:T:TRMT10A|TRMT10A]]|2.59|0.04| |[[:human_genes:R:RTCB|RTCB]]|2.60|0.16| |[[:human_genes:D:DDX1|DDX1]]|2.66|0.04| |[[:human_genes:R:RPTOR|RPTOR]]|2.68|0.06| |[[:human_genes:T:TMED10|TMED10]]|2.69|0.04| |[[:human_genes:S:STT3A|STT3A]]|2.76|0.11| |[[:human_genes:N:NDUFA2|NDUFA2]]|3.06|0.02| |[[:human_genes:E:ENY2|ENY2]]|3.15|0.02| ^Screen^Correlation^Plot^ |[[:results:exp434|Vemurafenib 6.6μM R08 exp434]]|0.077|| |[[:results:exp515|PU-H71 1μM R08 exp515]]|0.06|| |[[:results:exp90|WYE-354 6μM R02 exp90]]|0.057|| |[[:results:exp527|Tanespimycin 14μM R08 exp527]]|0.057|| |[[:results:exp89|Vemurafenib 6.6μM R02 exp89]]|0.055|| |[[:results:exp164|Q15 1 to 2μM on day4 R04 exp164]]|0.052|| |[[:results:exp510|Nicotine 3000μM R08 exp510]]|0.051|| |[[:results:exp448|Ammonium tetrathiomolybdate 10μM R08 exp448]]|0.07|| |[[:results:exp435|JQ1 0.8μM R08 exp435]]|0.062|| |[[:results:exp461|BS-181 20μM R08 exp461]]|0.061|| |[[:results:exp68|Clomiphene 4.4μM R02 exp68]]|0.059|| |[[:results:exp469|CFI-400945 25μM R08 exp469]]|0.057|| |[[:results:exp169|BH1 1μM R04 exp169]]|0.056|| {{:chemogenomics:comparison_plots:exp434_vs_exp507.png?nolink |}} {{:chemogenomics:comparison_plots:exp507_vs_exp515.png?nolink |}} {{:chemogenomics:comparison_plots:exp507_vs_exp90.png?nolink |}} {{:chemogenomics:comparison_plots:exp507_vs_exp527.png?nolink |}} {{:chemogenomics:comparison_plots:exp507_vs_exp89.png?nolink |}} {{:chemogenomics:comparison_plots:exp164_vs_exp507.png?nolink |}} {{:chemogenomics:comparison_plots:exp507_vs_exp510.png?nolink |}} {{:chemogenomics:comparison_plots:exp448_vs_exp507.png?nolink |}} {{:chemogenomics:comparison_plots:exp435_vs_exp507.png?nolink |}} {{:chemogenomics:comparison_plots:exp461_vs_exp507.png?nolink |}} {{:chemogenomics:comparison_plots:exp507_vs_exp68.png?nolink |}} {{:chemogenomics:comparison_plots:exp469_vs_exp507.png?nolink |}} {{:chemogenomics:comparison_plots:exp169_vs_exp507.png?nolink |}} ^GO Term^Fold Change^Genes^ |COPI vesicle coat|212.42|COPB2,COPZ1,COPB1| |COPI-coated vesicle membrane|136.56|COPB2,COPZ1,COPB1| |COPI-coated vesicle|91.04|COPB2,COPZ1,COPB1| |protein localization to Golgi apparatus|65.92|ARL1,ARFRP1,SYS1| |intra-Golgi vesicle-mediated transport|61.67|COPB2,COPZ1,COPB1| |Golgi-associated vesicle|28.97|COPB2,RAB14,COPZ1,COPB1| |coated membrane|28.64|COPB2,AP5B1,COPZ1,COPB1| |membrane coat|28.64|COPB2,AP5B1,COPZ1,COPB1| |retrograde transport, endosome to Golgi|28.32|ARL1,ARFRP1,RIC1,TBC1D23| |cytosolic transport|25.32|ARL1,ARFRP1,RAB14,SYS1,RIC1,TBC1D23| |trans-Golgi network membrane|24.99|ARL1,ARFRP1,SYS1,RIC1| |endosomal transport|16.48|ARL1,ARFRP1,RAB14,RIC1,TBC1D23,AP5B1| |Golgi vesicle transport|16.22|ARFRP1,COPB2,RAB14,SYS1,RAB1B,COPZ1,COPB1| |trans-Golgi network|15.29|ARL1,ARFRP1,RAB14,SYS1,RIC1,TBC1D23| |Golgi apparatus subcompartment|12.26|ARL1,ARFRP1,RAB14,SYS1,UXS1,RIC1,TBC1D23| |Golgi membrane|9.71|ARL1,UGCG,COPB2,RAB14,SYS1,RAB1B,PI4KB,RIC1,COPZ1,COPB1| |intracellular protein transport|8.46|ARL1,ARFRP1,COPB2,RAB14,RAB1B,RIC1,COPZ1,UFD1,COPB1| ^GO Term^Fold Change^Genes^ |tRNA metabolic process|17.82|DDX1,RTCB,TRMT10A,URM1,VARS2,YARS2|