Show pageOld revisionsBacklinksFold/unfold allBack to top This page is read only. You can view the source, but not change it. Ask your administrator if you think this is wrong. ====== MK2206 4μM R08 exp504 ====== ==== Mechanism of Action ==== Inhibit Akt1, Akt2, Akt3 * **<color #00a2e8>Class / Subclass 1:</color>** Signal Transduction / Kinase Inhibitor ==== Technical Notes ==== <accordion collapsed='true'> <panel title='Compound References' collapsed='true'> * **<color #00a2e8>PubChem Name:</color>** %%MK-2206 dihydrochloride%% * **<color #00a2e8>Synonyms:</color>** N/A * **<color #00a2e8>CAS #:</color>** 1032350-13-2 * **<color #00a2e8>PubChem CID:</color>** [[https://pubchem.ncbi.nlm.nih.gov/compound/46930998|46930998]] * **<color #00a2e8>IUPAC:</color>** %%8-[4-(1-aminocyclobutyl)phenyl]-9-phenyl-2H-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3-one;dihydrochloride%% * **<color #00a2e8>INCHI Name:</color>** InChI=1S/C25H21N5O.2ClH/c26-25(12-4-13-25)18-9-7-17(8-10-18)22-19(16-5-2-1-3-6-16)15-20-21(27-22)11-14-30-23(20)28-29-24(30)31;;/h1-3,5-11,14-15H,4,12-13,26H2,(H,29,31);2*1H * **<color #00a2e8>INCHI Key:</color>** HWUHTJIKQZZBRA-UHFFFAOYSA-N * **<color #00a2e8>Molecular Weight:</color>** 480.4 * **<color #00a2e8>Canonical SMILES:</color>** C1CC(C1)(C2=CC=C(C=C2)C3=C(C=C4C(=N3)C=CN5C4=NNC5=O)C6=CC=CC=C6)N.Cl.Cl * **<color #00a2e8>Isomeric SMILES:</color>** N/A * **<color #00a2e8>Molecular Formula:</color>** C25H23Cl2N5O {{:chemogenomics:structures:chem-0309.svg?nolink}} </panel> <panel title='Compound Supplier' collapsed='true'> * **<color #00a2e8>Supplier Name:</color>** Med Chem Express * **<color #00a2e8>Catalog #:</color>** HY-10358 * **<color #00a2e8>Lot #:</color>** 18916 </panel> <panel title='Compound Characterization' collapsed='true'> * **<color #00a2e8>HRMS (ESI-TOF) m/z:</color>** (M+H)+ Calcd for C25H21N5O 408.18189; found 408.18326 </panel> <panel title='Dose Response Curve' collapsed='true'> * **<color #00a2e8>Platform ID:</color>** MK2206 * **<color #00a2e8>Min:</color>** -6.4318; **<color #00a2e8>Max:</color>** 99.5790 {{:chemogenomics:dose_response:dr_556.png?nolink&500 |}} \\ \\ \\ \\ |< 300px 100px 200px >| ^ IC ^ Concentration (µM) ^ | IC10 |0.8020 | | IC20 |1.5180 | | IC30 |2.3200 | | IC40 |3.2850 | | IC50 |4.5190 | | IC60 |6.2180 | | IC70 |8.8030 | | IC80 |13.4500 | | IC90 |25.4700 | \\ </panel> </accordion> ==== Screen Summary ==== * **<color #00a2e8>Round</color>**: 08 * **<color #00a2e8>Dose</color>**: 4µM * **<color #00a2e8>Days of incubation</color>**: 8 * **<color #00a2e8>Doublings</color>**: 1.4 * **<color #00a2e8>Numbers of reads</color>**: 16015710 ==== 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^ |20/43|<color #e85500>[[https://files.tyerslab.com/files/public/chemogenomics/cranks/MK2206_4uM_Round-8_exp504.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="default" 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='MK2206 4μM R08 exp504'> {{:chemogenomics:cranks_plots:exp504.png?nolink}} </modal> <modal id="modal_hits" size="sm" title="Top 30 S/R Genes"> ^Gene^CRANKS Score^FDR^ |[[:human_genes:S:SLC5A3|SLC5A3]]|-3.93|<0.01| |[[:human_genes:F:FLVCR1|FLVCR1]]|-3.74|<0.01| |[[:human_genes:M:MYB|MYB]]|-3.15|0.05| |[[:human_genes:T:TCF4|TCF4]]|-3.07|<0.01| |[[:human_genes:A:ARL1|ARL1]]|-3.07|<0.01| |[[:human_genes:C:CREBBP|CREBBP]]|-3.03|<0.01| |[[:human_genes:M:MTF1|MTF1]]|-3.00|<0.01| |[[:human_genes:M:MSI2|MSI2]]|-2.94|<0.01| |[[:human_genes:C:CHKA|CHKA]]|-2.93|<0.01| |[[:human_genes:Z:ZFY|ZFY]]|-2.85|<0.01| |[[:human_genes:N:NOP2|NOP2]]|-2.72|0.15| |[[:human_genes:B:BRD1|BRD1]]|-2.65|0.01| |[[:human_genes:V:VPS25|VPS25]]|-2.65|0.31| |[[:human_genes:A:ARHGAP5|ARHGAP5]]|-2.64|0.01| |[[:human_genes:D:DERL2|DERL2]]|-2.63|0.03| |[[:human_genes:A:ATP6V0A2|ATP6V0A2]]|-2.62|0.03| |[[:human_genes:T:TFAP4|TFAP4]]|-2.54|0.03| |[[:human_genes:T:TCF3|TCF3]]|-2.53|0.08| |[[:human_genes:X:XPO6|XPO6]]|-2.52|0.03| |[[:human_genes:N:NCAM2|NCAM2]]|-2.46|0.03| |[[:human_genes:G:GPR107|GPR107]]|-2.42|0.04| |[[:human_genes:Q:QRICH1|QRICH1]]|-2.41|0.04| |[[:human_genes:P:PSTK|PSTK]]|-2.34|0.05| |[[:human_genes:Y:YBX1|YBX1]]|-2.27|0.07| |[[:human_genes:C:CAMK2G|CAMK2G]]|-2.24|0.08| |[[:human_genes:I:IRF2BP2|IRF2BP2]]|-2.19|0.10| |[[:human_genes:L:LMNB1|LMNB1]]|-2.18|0.10| |[[:human_genes:Z:ZMIZ1|ZMIZ1]]|-2.17|0.10| |[[:human_genes:T:TPR|TPR]]|-2.17|0.15| |[[:human_genes:Z:ZC3HC1|ZC3HC1]]|-2.16|0.10| |[[:human_genes:I:IPO9|IPO9]]|2.74|<0.01| |[[:human_genes:C:CDK8|CDK8]]|2.81|<0.01| |[[:human_genes:M:MEMO1|MEMO1]]|2.86|<0.01| |[[:human_genes:C:CBLL1|CBLL1]]|2.87|<0.01| |[[:human_genes:C:CMAS|CMAS]]|2.95|<0.01| |[[:human_genes:P:PTPMT1|PTPMT1]]|2.98|0.01| |[[:human_genes:A:ANKRD17|ANKRD17]]|3.00|<0.01| |[[:human_genes:P:PGM3|PGM3]]|3.03|<0.01| |[[:human_genes:P:PLEKHA2|PLEKHA2]]|3.08|<0.01| |[[:human_genes:Z:ZFC3H1|ZFC3H1]]|3.20|0.00| |[[:human_genes:W:WBP4|WBP4]]|3.30|0.00| |[[:human_genes:C:CNOT2|CNOT2]]|3.43|0.00| |[[:human_genes:D:DNAJC2|DNAJC2]]|3.50|0.00| |[[:human_genes:U:USF2|USF2]]|3.68|0.00| |[[:human_genes:K:KPTN|KPTN]]|3.78|0.00| |[[:human_genes:A:ATP2B1|ATP2B1]]|4.00|0.00| |[[:human_genes:C:C12orf66|C12orf66]]|4.01|0.00| |[[:human_genes:E:EIF4A1|EIF4A1]]|4.10|0.00| |[[:human_genes:S:SZT2|SZT2]]|4.14|0.00| |[[:human_genes:N:NANS|NANS]]|4.49|0.00| |[[:human_genes:H:HSPA14|HSPA14]]|4.60|0.00| |[[:human_genes:I:ITFG2|ITFG2]]|4.80|0.00| |[[:human_genes:F:FAM122A|FAM122A]]|5.00|0.00| |[[:human_genes:D:DEPDC5|DEPDC5]]|6.01|0.00| |[[:human_genes:P:PTEN|PTEN]]|6.76|0.00| |[[:human_genes:N:NPRL3|NPRL3]]|7.53|0.00| |[[:human_genes:N:NPRL2|NPRL2]]|7.70|0.00| |[[:human_genes:F:FOXO1|FOXO1]]|7.85|0.00| |[[:human_genes:T:TSC1|TSC1]]|8.24|0.00| |[[:human_genes:T:TSC2|TSC2]]|8.44|0.00| </modal> <modal id="modal_screen_similarity" size="lg" title="Correlated Screens"> ^Screen^Correlation^Plot^ |[[:results:exp90|WYE-354 6μM R02 exp90]]|0.07|<button type="primary" size="small" modal="1">View</button>| |[[:results:exp510|Nicotine 3000μM R08 exp510]]|0.07|<button type="primary" size="small" modal="2">View</button>| |[[:results:exp30|Rapamycin 10μM R00 exp30]]|0.057|<button type="primary" size="small" modal="3">View</button>| |[[:results:exp307|Rapamycin 2μM plus Cyclosporin-A 3μM R07 exp307]]|0.054|<button type="primary" size="small" modal="4">View</button>| |[[:results:exp306|Rapamycin 2μM R07 exp306]]|0.053|<button type="primary" size="small" modal="5">View</button>| |[[:results:exp29|Rapamycin 1μM R00 exp29]]|0.052|<button type="primary" size="small" modal="6">View</button>| |[[:results:exp429|Rapamycin 0.001μM R08 exp429]]|0.052|<button type="primary" size="small" modal="7">View</button>| |[[:results:exp508|NN-Dimethylsphingosine 2.5μM R08 exp508]]|0.052|<button type="primary" size="small" modal="8">View</button>| |[[:results:exp485|GSK626616 14μM R08 exp485]]|0.084|<button type="primary" size="small" modal="9">View</button>| |[[:results:exp352|Dexamethasone 0.006 to 0.015μM on day4 R07 exp352]]|0.074|<button type="primary" size="small" modal="10">View</button>| |[[:results:exp452|Azithromycin 100μM R08 exp452]]|0.073|<button type="primary" size="small" modal="11">View</button>| |[[:results:exp466|Cannabidiol 20μM R08 exp466]]|0.071|<button type="primary" size="small" modal="12">View</button>| |[[:results:exp233|EPZ-5676 30μM R05 exp233]]|0.07|<button type="primary" size="small" modal="13">View</button>| |[[:results:exp488|Hippuristanol 0.12μM R08 exp488]]|0.068|<button type="primary" size="small" modal="14">View</button>| |[[:results:exp445|∆-9-Tetrahydrocannabinol 30μM R08 exp445]]|0.067|<button type="primary" size="small" modal="15">View</button>| |[[:results:exp461|BS-181 20μM R08 exp461]]|0.062|<button type="primary" size="small" modal="16">View</button>| |[[:results:exp365|I-BRD9 4μM R07 exp365]]|0.059|<button type="primary" size="small" modal="17">View</button>| |[[:results:exp216|Erlotinib 10μM R05 exp216]]|0.057|<button type="primary" size="small" modal="18">View</button>| |[[:results:exp442|Ibrutinib 10μM R08 exp442]]|0.056|<button type="primary" size="small" modal="19">View</button>| |[[:results:exp483|FTY720 3μM R08 exp483]]|0.055|<button type="primary" size="small" modal="20">View</button>| |[[:results:exp334|All-trans-Retinoic-Acid 40μM R07 exp334]]|0.052|<button type="primary" size="small" modal="21">View</button>| |[[:results:exp489|Hippuristanol 0.12μM R08 exp489 no dilution day6]]|0.051|<button type="primary" size="small" modal="22">View</button>| </modal> <modal id="1" size="lg" title="MK2206 4μM R08 exp504 vs WYE-354 6μM R02 exp90"> {{:chemogenomics:comparison_plots:exp504_vs_exp90.png?nolink |}} </modal> <modal id="2" size="lg" title="MK2206 4μM R08 exp504 vs Nicotine 3000μM R08 exp510"> {{:chemogenomics:comparison_plots:exp504_vs_exp510.png?nolink |}} </modal> <modal id="3" size="lg" title="MK2206 4μM R08 exp504 vs Rapamycin 10μM R00 exp30"> {{:chemogenomics:comparison_plots:exp30_vs_exp504.png?nolink |}} </modal> <modal id="4" size="lg" title="MK2206 4μM R08 exp504 vs Rapamycin 2μM plus Cyclosporin-A 3μM R07 exp307"> {{:chemogenomics:comparison_plots:exp307_vs_exp504.png?nolink |}} </modal> <modal id="5" size="lg" title="MK2206 4μM R08 exp504 vs Rapamycin 2μM R07 exp306"> {{:chemogenomics:comparison_plots:exp306_vs_exp504.png?nolink |}} </modal> <modal id="6" size="lg" title="MK2206 4μM R08 exp504 vs Rapamycin 1μM R00 exp29"> {{:chemogenomics:comparison_plots:exp29_vs_exp504.png?nolink |}} </modal> <modal id="7" size="lg" title="MK2206 4μM R08 exp504 vs Rapamycin 0.001μM R08 exp429"> {{:chemogenomics:comparison_plots:exp429_vs_exp504.png?nolink |}} </modal> <modal id="8" size="lg" title="MK2206 4μM R08 exp504 vs NN-Dimethylsphingosine 2.5μM R08 exp508"> {{:chemogenomics:comparison_plots:exp504_vs_exp508.png?nolink |}} </modal> <modal id="9" size="lg" title="GSK626616 14μM R08 exp485 vs MK2206 4μM R08 exp504"> {{:chemogenomics:comparison_plots:exp485_vs_exp504.png?nolink |}} </modal> <modal id="10" size="lg" title="Dexamethasone 0.006 to 0.015μM on day4 R07 exp352 vs MK2206 4μM R08 exp504"> {{:chemogenomics:comparison_plots:exp352_vs_exp504.png?nolink |}} </modal> <modal id="11" size="lg" title="Azithromycin 100μM R08 exp452 vs MK2206 4μM R08 exp504"> {{:chemogenomics:comparison_plots:exp452_vs_exp504.png?nolink |}} </modal> <modal id="12" size="lg" title="Cannabidiol 20μM R08 exp466 vs MK2206 4μM R08 exp504"> {{:chemogenomics:comparison_plots:exp466_vs_exp504.png?nolink |}} </modal> <modal id="13" size="lg" title="EPZ-5676 30μM R05 exp233 vs MK2206 4μM R08 exp504"> {{:chemogenomics:comparison_plots:exp233_vs_exp504.png?nolink |}} </modal> <modal id="14" size="lg" title="Hippuristanol 0.12μM R08 exp488 vs MK2206 4μM R08 exp504"> {{:chemogenomics:comparison_plots:exp488_vs_exp504.png?nolink |}} </modal> <modal id="15" size="lg" title="∆-9-Tetrahydrocannabinol 30μM R08 exp445 vs MK2206 4μM R08 exp504"> {{:chemogenomics:comparison_plots:exp445_vs_exp504.png?nolink |}} </modal> <modal id="16" size="lg" title="BS-181 20μM R08 exp461 vs MK2206 4μM R08 exp504"> {{:chemogenomics:comparison_plots:exp461_vs_exp504.png?nolink |}} </modal> <modal id="17" size="lg" title="I-BRD9 4μM R07 exp365 vs MK2206 4μM R08 exp504"> {{:chemogenomics:comparison_plots:exp365_vs_exp504.png?nolink |}} </modal> <modal id="18" size="lg" title="Erlotinib 10μM R05 exp216 vs MK2206 4μM R08 exp504"> {{:chemogenomics:comparison_plots:exp216_vs_exp504.png?nolink |}} </modal> <modal id="19" size="lg" title="Ibrutinib 10μM R08 exp442 vs MK2206 4μM R08 exp504"> {{:chemogenomics:comparison_plots:exp442_vs_exp504.png?nolink |}} </modal> <modal id="20" size="lg" title="FTY720 3μM R08 exp483 vs MK2206 4μM R08 exp504"> {{:chemogenomics:comparison_plots:exp483_vs_exp504.png?nolink |}} </modal> <modal id="21" size="lg" title="All-trans-Retinoic-Acid 40μM R07 exp334 vs MK2206 4μM R08 exp504"> {{:chemogenomics:comparison_plots:exp334_vs_exp504.png?nolink |}} </modal> <modal id="22" size="lg" title="Hippuristanol 0.12μM R08 exp489 no dilution day6 vs MK2206 4μM R08 exp504"> {{:chemogenomics:comparison_plots:exp489_vs_exp504.png?nolink |}} </modal> <modal id="modal_go_sensitive" size="lg" title="Top 30 sensitive GO terms">No GO term hits below threshold. (FDR <0.05)</modal> <modal id="modal_go_resistant" size="lg" title="Top 30 resistant GO terms"> ^GO Term^Fold Change^Genes^ |KICSTOR complex|552.30|ITFG2,KPTN| |Seh1-associated complex|236.70|NPRL2,NPRL3,DEPDC5| |negative regulation of TORC1 signaling|107.77|TSC2,TSC1,NPRL2,NPRL3,DEPDC5,ITFG2,SZT2,KPTN| |cellular response to amino acid starvation|69.04|NPRL2,NPRL3,DEPDC5,ITFG2,SZT2,KPTN| |negative regulation of TOR signaling|66.95|TSC2,TSC1,NPRL2,NPRL3,DEPDC5,ITFG2,SZT2,KPTN| |response to amino acid starvation|64.98|NPRL2,NPRL3,DEPDC5,ITFG2,SZT2,KPTN| |regulation of TORC1 signaling|51.38|TSC2,TSC1,NPRL2,NPRL3,DEPDC5,ITFG2,SZT2,KPTN| |regulation of TOR signaling|32.73|TSC2,TSC1,NPRL2,NPRL3,DEPDC5,ITFG2,SZT2,KPTN| |cellular response to starvation|29.07|TSC2,TSC1,FOXO1,NPRL2,NPRL3,DEPDC5,ITFG2,SZT2,KPTN| |cellular response to nutrient levels|23.70|TSC2,TSC1,FOXO1,NPRL2,NPRL3,DEPDC5,ITFG2,SZT2,KPTN,USF2| |response to starvation|23.67|TSC2,TSC1,FOXO1,NPRL2,NPRL3,DEPDC5,ITFG2,SZT2,KPTN| |cellular response to extracellular stimulus|21.08|TSC2,TSC1,FOXO1,NPRL2,NPRL3,DEPDC5,ITFG2,SZT2,KPTN,USF2| |cellular response to external stimulus|16.89|TSC2,TSC1,FOXO1,NPRL2,NPRL3,DEPDC5,ITFG2,SZT2,KPTN,USF2| |response to nutrient levels|11.68|TSC2,TSC1,FOXO1,NPRL2,NPRL3,DEPDC5,ITFG2,SZT2,KPTN,USF2| |response to extracellular stimulus|11.00|TSC2,TSC1,FOXO1,NPRL2,NPRL3,DEPDC5,ITFG2,SZT2,KPTN,USF2| |negative regulation of intracellular signal transduction|10.79|TSC2,TSC1,FOXO1,NPRL2,NPRL3,PTEN,DEPDC5,ITFG2,SZT2,KPTN| |lytic vacuole membrane|10.42|TSC2,TSC1,NPRL2,NPRL3,DEPDC5,ITFG2,SZT2,KPTN| |lysosomal membrane|10.42|TSC2,TSC1,NPRL2,NPRL3,DEPDC5,ITFG2,SZT2,KPTN| |vacuolar membrane|9.48|TSC2,TSC1,NPRL2,NPRL3,DEPDC5,ITFG2,SZT2,KPTN| </modal> Last modified: 2026/01/15 21:36by 127.0.0.1