====== Golgicide-A 4μM R03 exp122 ======
==== Mechanism of Action ====
Inhibits cis-Golgi ArfGEF, blocks secretion at ER-Golgi
* **Class / Subclass 1:** Organelle Function / Vesicule Trafficking Inhibitor
==== Technical Notes ====
* **PubChem Name:** %%6,8-Difluoro-4-pyridin-3-yl-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline%%
* **Synonyms:** N/A
* **CAS #:** 1005036-73-6
* **PubChem CID:** [[https://pubchem.ncbi.nlm.nih.gov/compound/3154410|3154410]]
* **IUPAC:** %%6,8-difluoro-4-pyridin-3-yl-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline%%
* **INCHI Name:** InChI=1S/C17H14F2N2/c18-11-7-14-12-4-1-5-13(12)16(10-3-2-6-20-9-10)21-17(14)15(19)8-11/h1-4,6-9,12-13,16,21H,5H2
* **INCHI Key:** NJZHEQOUHLZCOX-UHFFFAOYSA-N
* **Molecular Weight:** 284.3
* **Canonical SMILES:** C1C=CC2C1C(NC3=C2C=C(C=C3F)F)C4=CN=CC=C4
* **Isomeric SMILES:** N/A
* **Molecular Formula:** C17H14F2N2
{{:chemogenomics:structures:chem-0075.svg?nolink}}
* **Supplier Name:** Sigma-Aldrich
* **Catalog #:** G0923
* **Lot #:** 105M4619V
* **HRMS (ESI-TOF) m/z:** (M+H)+ Calcd for C17H14F2N2 285.11978; found 285.11995
Dose response curve not available.
==== Screen Summary ====
* **Round**: 03
* **Dose**: 4µM
* **Days of incubation**: 8
* **Doublings**: 7.0
* **Numbers of reads**: 15252670
==== 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^
|66/23|[[https://files.tyerslab.com/files/public/chemogenomics/cranks/Golgicide_A_4uM_Round-3_exp122.txt|Scores]]||||||
{{:chemogenomics:cranks_plots:exp122.png?nolink}}
^Gene^CRANKS Score^FDR^
|[[:human_genes:A:ARF1|ARF1]]|-4.82|<0.01|
|[[:human_genes:S:SLC35E1|SLC35E1]]|-4.26|<0.01|
|[[:human_genes:R:RAB3GAP2|RAB3GAP2]]|-4.12|<0.01|
|[[:human_genes:P:PDIA6|PDIA6]]|-3.97|<0.01|
|[[:human_genes:D:DRG2|DRG2]]|-3.77|<0.01|
|[[:human_genes:Y:YIPF5|YIPF5]]|-3.75|<0.01|
|[[:human_genes:N:NPRL3|NPRL3]]|-3.71|<0.01|
|[[:human_genes:D:DNAJC3|DNAJC3]]|-3.64|<0.01|
|[[:human_genes:S:SZT2|SZT2]]|-3.39|<0.01|
|[[:human_genes:A:ATP2B1|ATP2B1]]|-3.33|<0.01|
|[[:human_genes:C:CSK|CSK]]|-3.21|<0.01|
|[[:human_genes:R:RBM26|RBM26]]|-3.15|<0.01|
|[[:human_genes:A:ATG9A|ATG9A]]|-3.08|<0.01|
|[[:human_genes:D:DERL2|DERL2]]|-3.08|<0.01|
|[[:human_genes:T:TMED10|TMED10]]|-3.00|<0.01|
|[[:human_genes:K:KIAA0922|KIAA0922]]|-2.97|<0.01|
|[[:human_genes:C:C1orf27|C1orf27]]|-2.97|<0.01|
|[[:human_genes:P:PRKAA1|PRKAA1]]|-2.87|<0.01|
|[[:human_genes:U:UBA6|UBA6]]|-2.87|<0.01|
|[[:human_genes:M:MANF|MANF]]|-2.84|<0.01|
|[[:human_genes:R:RBM14|RBM14]]|-2.83|0.01|
|[[:human_genes:I:ITFG2|ITFG2]]|-2.78|<0.01|
|[[:human_genes:P:PLAA|PLAA]]|-2.76|<0.01|
|[[:human_genes:V:VKORC1L1|VKORC1L1]]|-2.75|<0.01|
|[[:human_genes:R:RBM14-RBM4|RBM14-RBM4]]|-2.74|0.02|
|[[:human_genes:P:PTPN6|PTPN6]]|-2.71|<0.01|
|[[:human_genes:U:UFC1|UFC1]]|-2.70|<0.01|
|[[:human_genes:X:XPOT|XPOT]]|-2.66|<0.01|
|[[:human_genes:S:SMPD4|SMPD4]]|-2.65|<0.01|
|[[:human_genes:D:DNAJB11|DNAJB11]]|-2.64|0.01|
|[[:human_genes:D:DNAJB2|DNAJB2]]|2.27|0.36|
|[[:human_genes:M:MTMR9|MTMR9]]|2.27|0.11|
|[[:human_genes:R:RELB|RELB]]|2.31|0.10|
|[[:human_genes:I:ITSN1|ITSN1]]|2.32|0.05|
|[[:human_genes:X:XBP1|XBP1]]|2.35|0.04|
|[[:human_genes:R:RBBP5|RBBP5]]|2.41|0.03|
|[[:human_genes:S:SLC30A7|SLC30A7]]|2.42|0.06|
|[[:human_genes:G:GAGE2A|GAGE2A]]|2.44|0.52|
|[[:human_genes:S:SF3B3|SF3B3]]|2.45|0.19|
|[[:human_genes:U:UBE3D|UBE3D]]|2.46|0.03|
|[[:human_genes:S:SLC30A5|SLC30A5]]|2.53|0.02|
|[[:human_genes:H:HNRNPU|HNRNPU]]|2.53|0.02|
|[[:human_genes:E:EIF2AK3|EIF2AK3]]|2.57|0.02|
|[[:human_genes:A:ANKHD1-EIF4EBP3|ANKHD1-EIF4EBP3]]|2.60|0.03|
|[[:human_genes:R:RAB2A|RAB2A]]|2.61|0.03|
|[[:human_genes:A:ANKRD17|ANKRD17]]|2.63|0.03|
|[[:human_genes:P:PRPF18|PRPF18]]|2.66|0.19|
|[[:human_genes:M:MTMR6|MTMR6]]|2.79|0.03|
|[[:human_genes:A:AHCYL1|AHCYL1]]|2.80|0.02|
|[[:human_genes:K:KDELR2|KDELR2]]|3.19|<0.01|
|[[:human_genes:G:GALNT2|GALNT2]]|3.84|<0.01|
|[[:human_genes:E:ERP44|ERP44]]|3.87|<0.01|
|[[:human_genes:E:ERGIC1|ERGIC1]]|4.03|<0.01|
|[[:human_genes:S:SEC31A|SEC31A]]|4.24|<0.01|
|[[:human_genes:S:SAR1A|SAR1A]]|4.26|<0.01|
|[[:human_genes:A:ARFGAP1|ARFGAP1]]|4.34|<0.01|
|[[:human_genes:A:ARF5|ARF5]]|4.48|<0.01|
|[[:human_genes:S:SEC23B|SEC23B]]|4.55|<0.01|
|[[:human_genes:S:SLC30A6|SLC30A6]]|4.66|<0.01|
|[[:human_genes:A:ARF4|ARF4]]|5.33|<0.01|
^Screen^Correlation^Plot^
|[[:results:exp6|Bortezomib 0.005μM R00 exp6]]|0.058||
|[[:results:exp180|Dynasore 10μM R04 exp180]]|0.057||
{{:chemogenomics:comparison_plots:exp122_vs_exp6.png?nolink |}}
{{:chemogenomics:comparison_plots:exp122_vs_exp180.png?nolink |}}
^GO Term^Fold Change^Genes^
|negative regulation of TORC1 signaling|59.91|NPRL3,SZT2,PRKAA1,ITFG2|
|negative regulation of TOR signaling|37.21|NPRL3,SZT2,PRKAA1,ITFG2|
^GO Term^Fold Change^Genes^
|zinc ion import into Golgi lumen|552.63|SLC30A5,SLC30A7|
|cytosol to Golgi apparatus transport|368.42|SLC30A5,SLC30A7|
|zinc ion import into organelle|207.24|SLC30A6,SLC30A5,SLC30A7|
|COPII-coated vesicle cargo loading|118.42|SEC23B,SAR1A,SEC31A|
|zinc ion transmembrane transporter activity|72.08|SLC30A6,SLC30A5,SLC30A7|
|zinc ion transmembrane transport|63.77|SLC30A6,SLC30A5,SLC30A7|
|zinc ion transport|61.40|SLC30A6,SLC30A5,SLC30A7|
|vesicle cargo loading|53.48|SEC23B,SAR1A,SEC31A|
|endoplasmic reticulum exit site|53.48|SEC23B,SAR1A,SEC31A|
|retrograde vesicle-mediated transport, Golgi to endoplasmic reticulum|46.05|ARF4,ARF5,ERGIC1,KDELR2|
|ER to Golgi transport vesicle membrane|37.47|SEC23B,SAR1A,SEC31A,SLC30A5|
|COPII-coated ER to Golgi transport vesicle|37.26|SEC23B,SAR1A,SEC31A,ERGIC1,SLC30A5,CNIH4|
|endoplasmic reticulum to Golgi vesicle-mediated transport|35.37|ARF4,SEC23B,SAR1A,SEC31A,ERGIC1,KDELR2,RAB2A,CNIH4|
|endoplasmic reticulum-Golgi intermediate compartment|21.59|ERGIC1,ERP44,MTMR6,RAB2A,CNIH4|
|Golgi vesicle transport|18.09|ARF4,SEC23B,ARF5,SAR1A,SEC31A,ERGIC1,KDELR2,RAB2A,CNIH4|
|coated vesicle membrane|14.32|SEC23B,SAR1A,SEC31A,KDELR2,SLC30A5|
|coated vesicle|12.77|SEC23B,SAR1A,SEC31A,ERGIC1,KDELR2,SLC30A5,CNIH4|
|Golgi membrane|6.74|ARF4,ARFGAP1,ERGIC1,GALNT2,KDELR2,RAB2A,SLC30A5,SLC30A7|
|perinuclear region of cytoplasm|6.17|SEC23B,ARF5,SEC31A,GALNT2,MTMR6,EIF2AK3,SLC30A7,MTMR9|