====== Radicicol 0.16μM R05 exp242 ======
==== Mechanism of Action ====
Inhibits HSP90
* **Class / Subclass 1:** Proteostasis / Chaperone Inhibitor
* **Class / Subclass 2:** Infectious Disease / Antifungal
==== Technical Notes ====
* **PubChem Name:** %%Radicicol%%
* **Synonyms:** N/A
* **CAS #:** 12772-57-5
* **PubChem CID:** [[https://pubchem.ncbi.nlm.nih.gov/compound/6323491|6323491]]
* **IUPAC:** %%(4R,6R,8R,9Z,11E)-16-chloro-17,19-dihydroxy-4-methyl-3,7-dioxatricyclo[13.4.0.06,8]nonadeca-1(15),9,11,16,18-pentaene-2,13-dione%%
* **INCHI Name:** InChI=1S/C18H17ClO6/c1-9-6-15-14(25-15)5-3-2-4-10(20)7-11-16(18(23)24-9)12(21)8-13(22)17(11)19/h2-5,8-9,14-15,21-22H,6-7H2,1H3/b4-2+,5-3-/t9-,14-,15-/m1/s1
* **INCHI Key:** WYZWZEOGROVVHK-GTMNPGAYSA-N
* **Molecular Weight:** 364.8
* **Canonical SMILES:** CC1CC2C(O2)C=CC=CC(=O)CC3=C(C(=CC(=C3Cl)O)O)C(=O)O1
* **Isomeric SMILES:** C[C@@H]1C[C@@H]2[C@H](O2)/C=C\\C=C\\C(=O)CC3=C(C(=CC(=C3Cl)O)O)C(=O)O1
* **Molecular Formula:** C18H17ClO6
{{:chemogenomics:structures:chem-0147.svg?nolink}}
* **Supplier Name:** Cayman Chemical
* **Catalog #:** 13089
* **Lot #:** N/A
* **HRMS (ESI-TOF) m/z:** (M-H)- Calcd for C18H17ClO6 363.06409; found 363.06538
* **Platform ID:** Radicicol
* **Min:** -1.3077; **Max:** 99.5418
{{:chemogenomics:dose_response:dr_272.png?nolink&500 |}}
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^ IC ^ Concentration (µM) ^
| IC10 |N/A |
| IC20 |0.0804 |
| IC30 |0.1576 |
| IC40 |0.2736 |
| IC50 |0.4541 |
| IC60 |N/A |
| IC70 |N/A |
| IC80 |N/A |
| IC90 |N/A |
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==== Screen Summary ====
* **Round**: 05
* **Dose**: 160nM
* **Days of incubation**: 8
* **Doublings**: 4.9
* **Numbers of reads**: 24989585
==== 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^
|19/4|[[https://files.tyerslab.com/files/public/chemogenomics/cranks/Radicicol_0.16uM_Round-5_exp242.txt|Scores]]||||||
{{:chemogenomics:cranks_plots:exp242.png?nolink}}
^Gene^CRANKS Score^FDR^
|[[:human_genes:N:NUDCD1|NUDCD1]]|-3.71|<0.01|
|[[:human_genes:T:TCF4|TCF4]]|-3.33|<0.01|
|[[:human_genes:R:RHOA|RHOA]]|-3.10|<0.01|
|[[:human_genes:S:SLC5A3|SLC5A3]]|-3.00|<0.01|
|[[:human_genes:T:TUBG1|TUBG1]]|-2.99|0.01|
|[[:human_genes:U:UXS1|UXS1]]|-2.96|<0.01|
|[[:human_genes:L:LEF1|LEF1]]|-2.86|<0.01|
|[[:human_genes:A:ANAPC15|ANAPC15]]|-2.77|0.02|
|[[:human_genes:E:ELAVL1|ELAVL1]]|-2.74|<0.01|
|[[:human_genes:L:LMO2|LMO2]]|-2.74|<0.01|
|[[:human_genes:T:TRIM54|TRIM54]]|-2.73|<0.01|
|[[:human_genes:P:PRPS1|PRPS1]]|-2.72|<0.01|
|[[:human_genes:P:PTEN|PTEN]]|-2.71|0.01|
|[[:human_genes:K:KPTN|KPTN]]|-2.57|0.02|
|[[:human_genes:K:KEAP1|KEAP1]]|-2.55|0.04|
|[[:human_genes:H:HSP90AB1|HSP90AB1]]|-2.53|0.05|
|[[:human_genes:F:FBXO38|FBXO38]]|-2.53|0.02|
|[[:human_genes:C:CSK|CSK]]|-2.51|0.09|
|[[:human_genes:S:STK11|STK11]]|-2.41|0.07|
|[[:human_genes:G:GMPPB|GMPPB]]|-2.38|0.16|
|[[:human_genes:S:SZT2|SZT2]]|-2.37|0.05|
|[[:human_genes:I:IRF4|IRF4]]|-2.36|0.05|
|[[:human_genes:L:LDB1|LDB1]]|-2.33|0.05|
|[[:human_genes:S:SEPHS1|SEPHS1]]|-2.30|0.09|
|[[:human_genes:S:SOX4|SOX4]]|-2.26|0.15|
|[[:human_genes:S:SNX32|SNX32]]|-2.23|0.08|
|[[:human_genes:U:UMPS|UMPS]]|-2.22|0.52|
|[[:human_genes:H:HSPA4|HSPA4]]|-2.21|0.12|
|[[:human_genes:P:PRKCE|PRKCE]]|-2.21|0.09|
|[[:human_genes:C:CLTB|CLTB]]|-2.20|0.09|
|[[:human_genes:G:GMEB2|GMEB2]]|2.00|0.32|
|[[:human_genes:E:EIF4G2|EIF4G2]]|2.00|0.32|
|[[:human_genes:U:UBE2H|UBE2H]]|2.00|0.32|
|[[:human_genes:M:MIOS|MIOS]]|2.02|0.32|
|[[:human_genes:H:HDAC5|HDAC5]]|2.04|0.32|
|[[:human_genes:C:COPB1|COPB1]]|2.04|0.50|
|[[:human_genes:F:FA2H|FA2H]]|2.04|0.32|
|[[:human_genes:T:TAZ|TAZ]]|2.08|0.49|
|[[:human_genes:C:CNBP|CNBP]]|2.09|0.28|
|[[:human_genes:T:TIMM8A|TIMM8A]]|2.11|0.32|
|[[:human_genes:D:DHODH|DHODH]]|2.15|0.41|
|[[:human_genes:R:RFC1|RFC1]]|2.17|0.46|
|[[:human_genes:P:PES1|PES1]]|2.19|0.51|
|[[:human_genes:G:GPIHBP1|GPIHBP1]]|2.21|0.28|
|[[:human_genes:P:PPP3CA|PPP3CA]]|2.23|0.18|
|[[:human_genes:P:PHF20|PHF20]]|2.24|0.28|
|[[:human_genes:C:CLN8|CLN8]]|2.27|0.17|
|[[:human_genes:N:NR2C2AP|NR2C2AP]]|2.28|0.32|
|[[:human_genes:T:TCEAL7|TCEAL7]]|2.37|0.13|
|[[:human_genes:C:CMIP|CMIP]]|2.37|0.18|
|[[:human_genes:G:GPR137C|GPR137C]]|2.42|0.17|
|[[:human_genes:C:CDK2|CDK2]]|2.51|0.06|
|[[:human_genes:P:PRPF6|PRPF6]]|2.57|0.41|
|[[:human_genes:H:HK2|HK2]]|2.64|0.24|
|[[:human_genes:E:EIF3A|EIF3A]]|2.74|0.05|
|[[:human_genes:W:WDR5|WDR5]]|2.80|0.28|
|[[:human_genes:D:DGKD|DGKD]]|2.96|<0.01|
|[[:human_genes:S:STRAP|STRAP]]|3.07|<0.01|
|[[:human_genes:E:EIF3G|EIF3G]]|3.19|0.02|
|[[:human_genes:E:EIF4A1|EIF4A1]]|6.11|<0.01|
^Screen^Correlation^Plot^
|[[:results:exp308|Rapamycin 2μM plus FK-506 5μM R07 exp308]]|0.055||
|[[:results:exp307|Rapamycin 2μM plus Cyclosporin-A 3μM R07 exp307]]|0.055||
|[[:results:exp216|Erlotinib 10μM R05 exp216]]|0.079||
|[[:results:exp498|Lead acetate 2000μM R08 exp498 no dilution day6]]|0.075||
|[[:results:exp317|Geldanamycin 0.015 to 0.05μM on day4 R07 exp317]]|0.071||
|[[:results:exp497|Lead acetate 2000μM R08 exp497]]|0.067||
|[[:results:exp500|LY2090314 0.003μM R08 exp500 no dilution day6]]|0.057||
|[[:results:exp499|LY2090314 0.003μM R08 exp499]]|0.054||
|[[:results:exp468|CB-5083 0.4μM R08 exp468]]|0.054||
|[[:results:exp233|EPZ-5676 30μM R05 exp233]]|0.053||
|[[:results:exp514|Phorbol-12-myristate-13-acetate 0.57μM R08 exp514]]|0.051||
{{:chemogenomics:comparison_plots:exp242_vs_exp308.png?nolink |}}
{{:chemogenomics:comparison_plots:exp242_vs_exp307.png?nolink |}}
{{:chemogenomics:comparison_plots:exp216_vs_exp242.png?nolink |}}
{{:chemogenomics:comparison_plots:exp242_vs_exp498.png?nolink |}}
{{:chemogenomics:comparison_plots:exp242_vs_exp317.png?nolink |}}
{{:chemogenomics:comparison_plots:exp242_vs_exp497.png?nolink |}}
{{:chemogenomics:comparison_plots:exp242_vs_exp500.png?nolink |}}
{{:chemogenomics:comparison_plots:exp242_vs_exp499.png?nolink |}}
{{:chemogenomics:comparison_plots:exp242_vs_exp468.png?nolink |}}
{{:chemogenomics:comparison_plots:exp233_vs_exp242.png?nolink |}}
{{:chemogenomics:comparison_plots:exp242_vs_exp514.png?nolink |}}
^GO Term^Fold Change^Genes^
|beta-catenin-TCF complex|147.95|TCF4,LEF1,LDB1|
^GO Term^Fold Change^Genes^
|translation initiation factor activity|47.01|EIF4A1,EIF3G,EIF3A,EIF4G2|
|translational initiation|35.07|EIF4A1,EIF3G,EIF3A,EIF4G2|
|translation regulator activity|20.92|EIF4A1,EIF3G,EIF3A,CNBP,EIF4G2|