====== Wortmannin 5μM R00 exp38 ====== ==== Mechanism of Action ==== Inhibits PI3K and PI3K-related enzymes, non-specific covalent inhibitor * **Class / Subclass 1:** Signal Transduction / Kinase Inhibitor * **Class / Subclass 2:** Proteostasis / Autophagy Inhibitor ==== Technical Notes ==== * **PubChem Name:** %%Wortmannin%% * **Synonyms:** SL-2052; KY-12420 * **CAS #:** 19545-26-7 * **PubChem CID:** [[https://pubchem.ncbi.nlm.nih.gov/compound/312145|312145]] * **IUPAC:** %%[(1R,3R,5S,9R,18S)-18-(methoxymethyl)-1,5-dimethyl-6,11,16-trioxo-13,17-dioxapentacyclo[10.6.1.02,10.05,9.015,19]nonadeca-2(10),12(19),14-trien-3-yl] acetate%% * **INCHI Name:** InChI=1S/C23H24O8/c1-10(24)30-13-7-22(2)12(5-6-14(22)25)16-18(13)23(3)15(9-28-4)31-21(27)11-8-29-20(17(11)23)19(16)26/h8,12-13,15H,5-7,9H2,1-4H3/t12-,13+,15+,22-,23-/m0/s1 * **INCHI Key:** QDLHCMPXEPAAMD-QAIWCSMKSA-N * **Molecular Weight:** 428.4 * **Canonical SMILES:** CC(=O)OC1CC2(C(CCC2=O)C3=C1C4(C(OC(=O)C5=COC(=C54)C3=O)COC)C)C * **Isomeric SMILES:** CC(=O)O[C@@H]1C[C@]2([C@@H](CCC2=O)C3=C1[C@]4([C@H](OC(=O)C5=COC(=C54)C3=O)COC)C)C * **Molecular Formula:** C23H24O8 {{:chemogenomics:structures:chem-0020.svg?nolink}} * **Supplier Name:** LC Laboratories * **Catalog #:** W-2990 * **Lot #:** SS-107 * **HRMS (ESI-TOF) m/z:** (M+Na)+ Calcd for C23H24O8 451.13634; found 451.1358 * **Platform ID:** Wortmannin * **Min:** -10.7381; **Max:** 63.3011 {{:chemogenomics:dose_response:dr_280.png?nolink&500 |}} \\ \\ \\ \\ |< 300px 100px 200px >| ^ IC ^ Concentration (µM) ^ | IC10 |N/A | | IC20 |1.6783 | | IC30 |3.4255 | | IC40 |6.1479 | | IC50 |10.5153 | | IC60 |N/A | | IC70 |N/A | | IC80 |N/A | | IC90 |N/A | \\ ==== Screen Summary ==== * **Round**: 00 * **Dose**: 5µM * **Days of incubation**: 8 * **Doublings**: 3.4 * **Numbers of reads**: 12718276 ==== 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^ |30/18|[[https://files.tyerslab.com/files/public/chemogenomics/cranks/Wortmannin_5uM_Round-0_exp38.txt|Scores]]|||||| {{:chemogenomics:cranks_plots:exp38.png?nolink}} ^Gene^CRANKS Score^FDR^ |[[:human_genes:G:GPR107|GPR107]]|-4.60|<0.01| |[[:human_genes:Q:QRICH1|QRICH1]]|-4.35|<0.01| |[[:human_genes:T:TCF4|TCF4]]|-3.37|<0.01| |[[:human_genes:L:LAMTOR4|LAMTOR4]]|-3.27|<0.01| |[[:human_genes:D:DCAF15|DCAF15]]|-3.20|<0.01| |[[:human_genes:T:TRAF2|TRAF2]]|-3.11|<0.01| |[[:human_genes:R:RSRC2|RSRC2]]|-3.02|0.05| |[[:human_genes:A:ARL1|ARL1]]|-2.94|<0.01| |[[:human_genes:H:HSPA4|HSPA4]]|-2.80|0.01| |[[:human_genes:P:PIK3CA|PIK3CA]]|-2.77|<0.01| |[[:human_genes:Z:ZBTB10|ZBTB10]]|-2.74|0.02| |[[:human_genes:S:SEPHS1|SEPHS1]]|-2.70|0.01| |[[:human_genes:C:C10orf76|C10orf76]]|-2.67|0.01| |[[:human_genes:P:PRKAA1|PRKAA1]]|-2.63|0.01| |[[:human_genes:S:SYK|SYK]]|-2.62|0.01| |[[:human_genes:P:PRKAG1|PRKAG1]]|-2.59|0.02| |[[:human_genes:M:MAPKAP1|MAPKAP1]]|-2.58|0.03| |[[:human_genes:P:PGGT1B|PGGT1B]]|-2.56|0.02| |[[:human_genes:A:ASB3|ASB3]]|-2.50|0.02| |[[:human_genes:R:RIF1|RIF1]]|-2.46|0.05| |[[:human_genes:O:ORC3|ORC3]]|-2.45|0.07| |[[:human_genes:C:CREBBP|CREBBP]]|-2.44|0.07| |[[:human_genes:W:WDR20|WDR20]]|-2.41|0.05| |[[:human_genes:S:SEC23B|SEC23B]]|-2.39|0.05| |[[:human_genes:A:ACOT7|ACOT7]]|-2.38|0.04| |[[:human_genes:P:PIK3C3|PIK3C3]]|-2.37|0.06| |[[:human_genes:F:FURIN|FURIN]]|-2.35|0.06| |[[:human_genes:N:NME1-NME2|NME1-NME2]]|-2.35|0.05| |[[:human_genes:T:TNFAIP3|TNFAIP3]]|-2.34|0.05| |[[:human_genes:H:HDAC1|HDAC1]]|-2.33|0.05| |[[:human_genes:C:CMYA5|CMYA5]]|2.19|0.32| |[[:human_genes:S:SPRED2|SPRED2]]|2.24|0.08| |[[:human_genes:H:HERC4|HERC4]]|2.30|0.06| |[[:human_genes:P:PTEN|PTEN]]|2.32|0.05| |[[:human_genes:U:USP36|USP36]]|2.32|0.05| |[[:human_genes:L:LCMT1|LCMT1]]|2.34|0.05| |[[:human_genes:T:TNFRSF21|TNFRSF21]]|2.34|0.09| |[[:human_genes:P:PMAIP1|PMAIP1]]|2.42|0.04| |[[:human_genes:P:PSMD1|PSMD1]]|2.45|0.39| |[[:human_genes:L:LZTR1|LZTR1]]|2.48|0.03| |[[:human_genes:U:UBQLN1|UBQLN1]]|2.49|0.03| |[[:human_genes:K:KCTD5|KCTD5]]|2.56|0.02| |[[:human_genes:M:MCL1|MCL1]]|2.57|0.07| |[[:human_genes:R:RCSD1|RCSD1]]|2.59|0.03| |[[:human_genes:W:WDR43|WDR43]]|2.63|0.22| |[[:human_genes:V:VDAC2|VDAC2]]|2.63|0.02| |[[:human_genes:M:MPC2|MPC2]]|2.63|0.02| |[[:human_genes:M:MARCH5|MARCH5]]|2.65|0.03| |[[:human_genes:N:NPIPB3|NPIPB3]]|2.66|0.32| |[[:human_genes:N:NKTR|NKTR]]|2.66|0.10| |[[:human_genes:Z:ZDHHC17|ZDHHC17]]|2.72|0.01| |[[:human_genes:U:UBAP1|UBAP1]]|2.80|0.02| |[[:human_genes:D:DUSP6|DUSP6]]|2.81|<0.01| |[[:human_genes:D:DOLPP1|DOLPP1]]|2.83|0.02| |[[:human_genes:H:HMG20B|HMG20B]]|2.86|<0.01| |[[:human_genes:S:SMARCC1|SMARCC1]]|2.99|<0.01| |[[:human_genes:T:TMEM39A|TMEM39A]]|3.11|<0.01| |[[:human_genes:N:NF1|NF1]]|3.24|<0.01| |[[:human_genes:B:BAK1|BAK1]]|3.93|<0.01| |[[:human_genes:T:TXNIP|TXNIP]]|4.16|<0.01| ^Screen^Correlation^Plot^ |[[:results:exp37|Wortmannin 0.5μM R00 exp37]]|0.091|| |[[:results:exp85|UM0129480 7μM R02 exp85]]|0.07|| |[[:results:exp467|CAY10603 0.55μM R08 exp467]]|0.07|| |[[:results:exp351|Dexamethasone 0.006μM R07 exp351]]|0.063|| |[[:results:exp485|GSK626616 14μM R08 exp485]]|0.061|| |[[:results:exp15|Cycloheximide 0.2μM R00 exp15]]|0.056|| |[[:results:exp407|Thapsigargin 0.005μM R07 exp407]]|0.056|| |[[:results:exp497|Lead acetate 2000μM R08 exp497]]|0.056|| |[[:results:exp357|Dorsomorphin 5μM R07 exp357]]|0.056|| |[[:results:exp352|Dexamethasone 0.006 to 0.015μM on day4 R07 exp352]]|0.054|| |[[:results:exp90|WYE-354 6μM R02 exp90]]|0.053|| |[[:results:exp36|TRAIL 50ng/ml R00 exp36]]|0.053|| |[[:results:exp5|Alpha-Amanitin 0.5μM R00 exp5]]|0.051|| |[[:results:exp442|Ibrutinib 10μM R08 exp442]]|0.051|| |[[:results:exp35|TRAIL 5ng/ml R00 exp35]]|0.051|| {{:chemogenomics:comparison_plots:exp37_vs_exp38.png?nolink |}} {{:chemogenomics:comparison_plots:exp38_vs_exp85.png?nolink |}} {{:chemogenomics:comparison_plots:exp38_vs_exp467.png?nolink |}} {{:chemogenomics:comparison_plots:exp351_vs_exp38.png?nolink |}} {{:chemogenomics:comparison_plots:exp38_vs_exp485.png?nolink |}} {{:chemogenomics:comparison_plots:exp15_vs_exp38.png?nolink |}} {{:chemogenomics:comparison_plots:exp38_vs_exp407.png?nolink |}} {{:chemogenomics:comparison_plots:exp38_vs_exp497.png?nolink |}} {{:chemogenomics:comparison_plots:exp357_vs_exp38.png?nolink |}} {{:chemogenomics:comparison_plots:exp352_vs_exp38.png?nolink |}} {{:chemogenomics:comparison_plots:exp38_vs_exp90.png?nolink |}} {{:chemogenomics:comparison_plots:exp36_vs_exp38.png?nolink |}} {{:chemogenomics:comparison_plots:exp38_vs_exp5.png?nolink |}} {{:chemogenomics:comparison_plots:exp38_vs_exp442.png?nolink |}} {{:chemogenomics:comparison_plots:exp35_vs_exp38.png?nolink |}} No GO term hits below threshold. (FDR <0.05) ^GO Term^Fold Change^Genes^ |Bcl-2 family protein complex|184.23|BAK1,MCL1,PMAIP1| |release of cytochrome c from mitochondria|78.96|BAK1,MCL1,PMAIP1| |apoptotic mitochondrial changes|39.48|BAK1,VDAC2,MCL1,PMAIP1| |regulation of apoptotic signaling pathway|10.32|BAK1,NF1,VDAC2,MCL1,UBQLN1,PMAIP1,PTEN|