====== Senexin-A 25μM R07 exp400 ====== ==== Mechanism of Action ==== Inhibits CDK8, suppresses induction of gene expression * **Class / Subclass 1:** Signal Transduction / Kinase Inhibitor * **Class / Subclass 2:** Gene Regulation / Transcription Inhibitor ==== Technical Notes ==== * **PubChem Name:** %%4-(2-Phenylethylamino)quinazoline-6-carbonitrile;hydrochloride%% * **Synonyms:** N/A * **CAS #:** 1780390-76-2 * **PubChem CID:** [[https://pubchem.ncbi.nlm.nih.gov/compound/90488980|90488980]] * **IUPAC:** %%4-(2-phenylethylamino)quinazoline-6-carbonitrile;hydrochloride%% * **INCHI Name:** InChI=1S/C17H14N4.ClH/c18-11-14-6-7-16-15(10-14)17(21-12-20-16)19-9-8-13-4-2-1-3-5-13;/h1-7,10,12H,8-9H2,(H,19,20,21);1H * **INCHI Key:** POENYXHGUHRXFR-UHFFFAOYSA-N * **Molecular Weight:** 310.8 * **Canonical SMILES:** C1=CC=C(C=C1)CCNC2=NC=NC3=C2C=C(C=C3)C#N.Cl * **Isomeric SMILES:** N/A * **Molecular Formula:** C17H15ClN4 {{:chemogenomics:structures:chem-0238.svg?nolink}} * **Supplier Name:** Tocris Bioscience * **Catalog #:** 4875 * **Lot #:** N/A * **HRMS (ESI-TOF) m/z:** (M+H)+ Calcd for C17H14N4 275.12912; found 275.12926 * **Platform ID:** Senexin_A * **Min:** -11.6276; **Max:** 42.3607 {{:chemogenomics:dose_response:dr_401.png?nolink&500 |}} \\ \\ \\ \\ |< 300px 100px 200px >| ^ IC ^ Concentration (µM) ^ | IC10 |N/A | | IC20 |16.7423 | | IC30 |N/A | | IC40 |N/A | | IC50 |N/A | | IC60 |N/A | | IC70 |N/A | | IC80 |N/A | | IC90 |N/A | \\ ==== Screen Summary ==== * **Round**: 07 * **Dose**: 25µM * **Days of incubation**: 8 * **Doublings**: 3.2 * **Numbers of reads**: 22291136 ==== 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^ |13/4|[[https://files.tyerslab.com/files/public/chemogenomics/cranks/Senexin_A_25uM_Round-7_exp400.txt|Scores]]|||||| {{:chemogenomics:cranks_plots:exp400.png?nolink}} ^Gene^CRANKS Score^FDR^ |[[:human_genes:S:SNX27|SNX27]]|-4.81|<0.01| |[[:human_genes:P:PRKAA1|PRKAA1]]|-3.83|<0.01| |[[:human_genes:G:GOT1|GOT1]]|-3.70|<0.01| |[[:human_genes:R:RAB10|RAB10]]|-3.30|<0.01| |[[:human_genes:D:DENND4A|DENND4A]]|-3.15|<0.01| |[[:human_genes:L:LMAN1L|LMAN1L]]|-2.83|0.03| |[[:human_genes:B:BCL2|BCL2]]|-2.76|0.01| |[[:human_genes:C:CCDC22|CCDC22]]|-2.74|0.01| |[[:human_genes:L:L3MBTL2|L3MBTL2]]|-2.71|0.02| |[[:human_genes:M:MYSM1|MYSM1]]|-2.69|0.01| |[[:human_genes:C:CMTM6|CMTM6]]|-2.65|0.02| |[[:human_genes:M:MGA|MGA]]|-2.58|0.02| |[[:human_genes:C:COMMD5|COMMD5]]|-2.55|0.02| |[[:human_genes:Q:QRICH1|QRICH1]]|-2.52|0.11| |[[:human_genes:S:SLC2A1|SLC2A1]]|-2.40|0.10| |[[:human_genes:R:RAB7A|RAB7A]]|-2.35|0.07| |[[:human_genes:A:ARPC4|ARPC4]]|-2.26|0.10| |[[:human_genes:N:NKX2-5|NKX2-5]]|-2.21|0.19| |[[:human_genes:P:PBRM1|PBRM1]]|-2.21|0.12| |[[:human_genes:V:VPS29|VPS29]]|-2.17|0.23| |[[:human_genes:T:TSC22D1|TSC22D1]]|-2.16|0.15| |[[:human_genes:C:CDC25A|CDC25A]]|-2.14|0.25| |[[:human_genes:T:TAZ|TAZ]]|-2.13|0.34| |[[:human_genes:P:PSTPIP2|PSTPIP2]]|-2.12|0.17| |[[:human_genes:P:PRKAG1|PRKAG1]]|-2.11|0.18| |[[:human_genes:I:INTS3|INTS3]]|-2.10|0.37| |[[:human_genes:K:KIF13A|KIF13A]]|-2.09|0.28| |[[:human_genes:G:GPAA1|GPAA1]]|-2.08|0.19| |[[:human_genes:A:ARID1A|ARID1A]]|-2.04|0.34| |[[:human_genes:P:PRKAR2B|PRKAR2B]]|-2.01|0.26| |[[:human_genes:S:SLC25A32|SLC25A32]]|2.15|0.22| |[[:human_genes:S:SHMT2|SHMT2]]|2.17|0.22| |[[:human_genes:B:BTAF1|BTAF1]]|2.17|0.22| |[[:human_genes:G:GANAB|GANAB]]|2.17|0.23| |[[:human_genes:C:CDC45|CDC45]]|2.18|0.37| |[[:human_genes:S:SSR3|SSR3]]|2.19|0.15| |[[:human_genes:M:MSI2|MSI2]]|2.20|0.22| |[[:human_genes:M:MLEC|MLEC]]|2.20|0.22| |[[:human_genes:A:ATP5B|ATP5B]]|2.21|0.14| |[[:human_genes:F:FH|FH]]|2.23|0.22| |[[:human_genes:M:MBD1|MBD1]]|2.24|0.22| |[[:human_genes:P:PPP6C|PPP6C]]|2.27|0.18| |[[:human_genes:S:SRD5A3|SRD5A3]]|2.29|0.11| |[[:human_genes:T:TMEM206|TMEM206]]|2.30|0.11| |[[:human_genes:I:ISY1|ISY1]]|2.32|0.32| |[[:human_genes:A:ALG5|ALG5]]|2.33|0.11| |[[:human_genes:H:HIST1H2AJ|HIST1H2AJ]]|2.36|0.14| |[[:human_genes:N:NDUFB6|NDUFB6]]|2.36|0.14| |[[:human_genes:S:SIRT1|SIRT1]]|2.38|0.10| |[[:human_genes:U:UGP2|UGP2]]|2.38|0.10| |[[:human_genes:P:PMVK|PMVK]]|2.39|0.10| |[[:human_genes:G:GPR33|GPR33]]|2.43|0.11| |[[:human_genes:A:ARGLU1|ARGLU1]]|2.44|0.18| |[[:human_genes:I:ISY1-RAB43|ISY1-RAB43]]|2.52|0.23| |[[:human_genes:D:DDX3X|DDX3X]]|2.55|0.06| |[[:human_genes:E:ECD|ECD]]|2.77|0.24| |[[:human_genes:A:AP1S1|AP1S1]]|3.02|0.01| |[[:human_genes:V:VHL|VHL]]|3.06|<0.01| |[[:human_genes:S:SPI1|SPI1]]|4.05|<0.01| |[[:human_genes:T:TXNIP|TXNIP]]|4.53|<0.01| ^Screen^Correlation^Plot^ |[[:results:exp492|iCRT14 30μM R08 exp492]]|0.091|| {{:chemogenomics:comparison_plots:exp400_vs_exp492.png?nolink |}} ^GO Term^Fold Change^Genes^ |endocytic recycling|42.64|SNX27,CCDC22,CMTM6,RAB7A,VPS29| |vesicle-mediated transport to the plasma membrane|34.95|SNX27,RAB10,CCDC22,CMTM6,RAB7A,VPS29,KIF13A| |endosomal transport|15.88|SNX27,RAB10,CCDC22,CMTM6,RAB7A,VPS29| No GO term hits below threshold. (FDR <0.05)