====== MK2206 4μM R08 exp504 ======
==== Mechanism of Action ====
Inhibit Akt1, Akt2, Akt3
* **Class / Subclass 1:** Signal Transduction / Kinase Inhibitor
==== Technical Notes ====
* **PubChem Name:** %%MK-2206 dihydrochloride%%
* **Synonyms:** N/A
* **CAS #:** 1032350-13-2
* **PubChem CID:** [[https://pubchem.ncbi.nlm.nih.gov/compound/46930998|46930998]]
* **IUPAC:** %%8-[4-(1-aminocyclobutyl)phenyl]-9-phenyl-2H-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3-one;dihydrochloride%%
* **INCHI Name:** 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
* **INCHI Key:** HWUHTJIKQZZBRA-UHFFFAOYSA-N
* **Molecular Weight:** 480.4
* **Canonical SMILES:** C1CC(C1)(C2=CC=C(C=C2)C3=C(C=C4C(=N3)C=CN5C4=NNC5=O)C6=CC=CC=C6)N.Cl.Cl
* **Isomeric SMILES:** N/A
* **Molecular Formula:** C25H23Cl2N5O
{{:chemogenomics:structures:chem-0309.svg?nolink}}
* **Supplier Name:** Med Chem Express
* **Catalog #:** HY-10358
* **Lot #:** 18916
* **HRMS (ESI-TOF) m/z:** (M+H)+ Calcd for C25H21N5O 408.18189; found 408.18326
* **Platform ID:** MK2206
* **Min:** -6.4318; **Max:** 99.5790
{{:chemogenomics:dose_response:dr_556.png?nolink&500 |}}
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^ 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 |
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==== Screen Summary ====
* **Round**: 08
* **Dose**: 4µM
* **Days of incubation**: 8
* **Doublings**: 1.4
* **Numbers of reads**: 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|[[https://files.tyerslab.com/files/public/chemogenomics/cranks/MK2206_4uM_Round-8_exp504.txt|Scores]]||||||
{{:chemogenomics:cranks_plots:exp504.png?nolink}}
^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|
^Screen^Correlation^Plot^
|[[:results:exp90|WYE-354 6μM R02 exp90]]|0.07||
|[[:results:exp510|Nicotine 3000μM R08 exp510]]|0.07||
|[[:results:exp30|Rapamycin 10μM R00 exp30]]|0.057||
|[[:results:exp307|Rapamycin 2μM plus Cyclosporin-A 3μM R07 exp307]]|0.054||
|[[:results:exp306|Rapamycin 2μM R07 exp306]]|0.053||
|[[:results:exp29|Rapamycin 1μM R00 exp29]]|0.052||
|[[:results:exp429|Rapamycin 0.001μM R08 exp429]]|0.052||
|[[:results:exp508|NN-Dimethylsphingosine 2.5μM R08 exp508]]|0.052||
|[[:results:exp485|GSK626616 14μM R08 exp485]]|0.084||
|[[:results:exp352|Dexamethasone 0.006 to 0.015μM on day4 R07 exp352]]|0.074||
|[[:results:exp452|Azithromycin 100μM R08 exp452]]|0.073||
|[[:results:exp466|Cannabidiol 20μM R08 exp466]]|0.071||
|[[:results:exp233|EPZ-5676 30μM R05 exp233]]|0.07||
|[[:results:exp488|Hippuristanol 0.12μM R08 exp488]]|0.068||
|[[:results:exp445|∆-9-Tetrahydrocannabinol 30μM R08 exp445]]|0.067||
|[[:results:exp461|BS-181 20μM R08 exp461]]|0.062||
|[[:results:exp365|I-BRD9 4μM R07 exp365]]|0.059||
|[[:results:exp216|Erlotinib 10μM R05 exp216]]|0.057||
|[[:results:exp442|Ibrutinib 10μM R08 exp442]]|0.056||
|[[:results:exp483|FTY720 3μM R08 exp483]]|0.055||
|[[:results:exp334|All-trans-Retinoic-Acid 40μM R07 exp334]]|0.052||
|[[:results:exp489|Hippuristanol 0.12μM R08 exp489 no dilution day6]]|0.051||
{{:chemogenomics:comparison_plots:exp504_vs_exp90.png?nolink |}}
{{:chemogenomics:comparison_plots:exp504_vs_exp510.png?nolink |}}
{{:chemogenomics:comparison_plots:exp30_vs_exp504.png?nolink |}}
{{:chemogenomics:comparison_plots:exp307_vs_exp504.png?nolink |}}
{{:chemogenomics:comparison_plots:exp306_vs_exp504.png?nolink |}}
{{:chemogenomics:comparison_plots:exp29_vs_exp504.png?nolink |}}
{{:chemogenomics:comparison_plots:exp429_vs_exp504.png?nolink |}}
{{:chemogenomics:comparison_plots:exp504_vs_exp508.png?nolink |}}
{{:chemogenomics:comparison_plots:exp485_vs_exp504.png?nolink |}}
{{:chemogenomics:comparison_plots:exp352_vs_exp504.png?nolink |}}
{{:chemogenomics:comparison_plots:exp452_vs_exp504.png?nolink |}}
{{:chemogenomics:comparison_plots:exp466_vs_exp504.png?nolink |}}
{{:chemogenomics:comparison_plots:exp233_vs_exp504.png?nolink |}}
{{:chemogenomics:comparison_plots:exp488_vs_exp504.png?nolink |}}
{{:chemogenomics:comparison_plots:exp445_vs_exp504.png?nolink |}}
{{:chemogenomics:comparison_plots:exp461_vs_exp504.png?nolink |}}
{{:chemogenomics:comparison_plots:exp365_vs_exp504.png?nolink |}}
{{:chemogenomics:comparison_plots:exp216_vs_exp504.png?nolink |}}
{{:chemogenomics:comparison_plots:exp442_vs_exp504.png?nolink |}}
{{:chemogenomics:comparison_plots:exp483_vs_exp504.png?nolink |}}
{{:chemogenomics:comparison_plots:exp334_vs_exp504.png?nolink |}}
{{:chemogenomics:comparison_plots:exp489_vs_exp504.png?nolink |}}
No GO term hits below threshold. (FDR <0.05)
^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|