====== Staurosporine 0.02μM R08 exp524 ====== ==== Mechanism of Action ==== Inhibits many protein kinases including PKC, PKA, tyrosine kinases, CDKs, others * **Class / Subclass 1:** Signal Transduction / Kinase Inhibitor ==== Technical Notes ==== * **PubChem Name:** %%Staurosporine%% * **Synonyms:** Antibiotic AM-2282; STS; AM-2282 * **CAS #:** 62996-74-1 * **PubChem CID:** [[https://pubchem.ncbi.nlm.nih.gov/compound/44259|44259]] * **IUPAC:** %%(2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-16-one%% * **INCHI Name:** InChI=1S/C28H26N4O3/c1-28-26(34-3)17(29-2)12-20(35-28)31-18-10-6-4-8-14(18)22-23-16(13-30-27(23)33)21-15-9-5-7-11-19(15)32(28)25(21)24(22)31/h4-11,17,20,26,29H,12-13H2,1-3H3,(H,30,33)/t17-,20-,26-,28+/m1/s1 * **INCHI Key:** HKSZLNNOFSGOKW-FYTWVXJKSA-N * **Molecular Weight:** 466.5 * **Canonical SMILES:** CC12C(C(CC(O1)N3C4=CC=CC=C4C5=C6C(=C7C8=CC=CC=C8N2C7=C53)CNC6=O)NC)OC * **Isomeric SMILES:** C[C@@]12[C@@H]([C@@H](C[C@@H](O1)N3C4=CC=CC=C4C5=C6C(=C7C8=CC=CC=C8N2C7=C53)CNC6=O)NC)OC * **Molecular Formula:** C28H26N4O3 {{:chemogenomics:structures:chem-0329.svg?nolink}} * **Supplier Name:** Med Chem Express * **Catalog #:** HY-15141 * **Lot #:** 32940 * **HRMS (ESI-TOF) m/z:** (M+H)+ Calcd for C28H26N4O3 467.20777; found 467.20856 * **Platform ID:** Staurosporin * **Min:** -7.4960; **Max:** 99.8510 {{:chemogenomics:dose_response:dr_581.png?nolink&500 |}} \\ \\ \\ \\ |< 300px 100px 200px >| ^ IC ^ Concentration (µM) ^ | IC10 |0.0059 | | IC20 |0.0122 | | IC30 |0.0197 | | IC40 |0.0292 | | IC50 |0.0419 | | IC60 |0.0602 | | IC70 |0.0892 | | IC80 |0.1443 | | IC90 |0.2973 | \\ ==== Screen Summary ==== * **Round**: 08 * **Dose**: 20nM * **Days of incubation**: 8 * **Doublings**: 0.5 * **Numbers of reads**: 17250856 ==== 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^ |2/66|[[https://files.tyerslab.com/files/public/chemogenomics/cranks/Staurosporin_0.02uM_Round-8_exp524.txt|Scores]]|||||| {{:chemogenomics:cranks_plots:exp524.png?nolink}} ^Gene^CRANKS Score^FDR^ |[[:human_genes:O:OTUB1|OTUB1]]|-3.45|<0.01| |[[:human_genes:E:EP300|EP300]]|-2.85|0.12| |[[:human_genes:M:MBTD1|MBTD1]]|-2.81|0.03| |[[:human_genes:K:KCTD10|KCTD10]]|-2.56|0.09| |[[:human_genes:A:ATP6V0A2|ATP6V0A2]]|-2.54|0.11| |[[:human_genes:C:CWC27|CWC27]]|-2.51|0.09| |[[:human_genes:C:CMYA5|CMYA5]]|-2.48|0.23| |[[:human_genes:I:IPO11|IPO11]]|-2.46|0.09| |[[:human_genes:P:PSMC5|PSMC5]]|-2.44|0.38| |[[:human_genes:C:CDK19|CDK19]]|-2.42|0.11| |[[:human_genes:C:CENPE|CENPE]]|-2.38|0.18| |[[:human_genes:C:CHMP7|CHMP7]]|-2.37|0.11| |[[:human_genes:I:INCENP|INCENP]]|-2.33|0.37| |[[:human_genes:S:SOX4|SOX4]]|-2.30|0.30| |[[:human_genes:R:RAD21|RAD21]]|-2.22|0.36| |[[:human_genes:D:DRD3|DRD3]]|-2.15|0.30| |[[:human_genes:M:MORF4L1|MORF4L1]]|-2.14|0.27| |[[:human_genes:F:FAM217A|FAM217A]]|-2.11|0.33| |[[:human_genes:G:GPX4|GPX4]]|-2.11|0.29| |[[:human_genes:H:HNRNPD|HNRNPD]]|-2.09|0.29| |[[:human_genes:C:CSE1L|CSE1L]]|-2.09|0.49| |[[:human_genes:U:UBE2N|UBE2N]]|-2.09|0.29| |[[:human_genes:M:MED12|MED12]]|-2.08|0.49| |[[:human_genes:D:DUSP23|DUSP23]]|-2.06|0.30| |[[:human_genes:M:MLLT10|MLLT10]]|-2.05|0.30| |[[:human_genes:E:EPAS1|EPAS1]]|-2.05|0.37| |[[:human_genes:Z:ZBTB7A|ZBTB7A]]|-2.04|0.30| |[[:human_genes:E:EIF3L|EIF3L]]|-2.04|0.40| |[[:human_genes:P:PSMB1|PSMB1]]|-2.03|0.41| |[[:human_genes:G:GPR101|GPR101]]|-2.02|0.30| |[[:human_genes:N:NSD1|NSD1]]|2.83|<0.01| |[[:human_genes:F:FAM204A|FAM204A]]|2.86|<0.01| |[[:human_genes:H:HDAC5|HDAC5]]|2.87|<0.01| |[[:human_genes:F:FBXO11|FBXO11]]|2.87|<0.01| |[[:human_genes:R:ROMO1|ROMO1]]|2.89|<0.01| |[[:human_genes:T:TSR2|TSR2]]|2.92|0.09| |[[:human_genes:M:MAP2K5|MAP2K5]]|3.04|<0.01| |[[:human_genes:T:TAZ|TAZ]]|3.04|0.02| |[[:human_genes:S:SRM|SRM]]|3.17|0.00| |[[:human_genes:A:ARID4B|ARID4B]]|3.21|0.00| |[[:human_genes:N:NCOR1|NCOR1]]|3.24|0.00| |[[:human_genes:L:LPAR5|LPAR5]]|3.25|0.00| |[[:human_genes:C:CASP9|CASP9]]|3.26|0.00| |[[:human_genes:K:KMT2D|KMT2D]]|3.36|0.00| |[[:human_genes:R:RBM12|RBM12]]|3.37|0.00| |[[:human_genes:Y:YLPM1|YLPM1]]|3.49|<0.01| |[[:human_genes:M:MAPK7|MAPK7]]|3.77|0.00| |[[:human_genes:V:VDAC2|VDAC2]]|3.94|0.00| |[[:human_genes:F:FAF2|FAF2]]|3.99|0.00| |[[:human_genes:B:BUB3|BUB3]]|4.04|0.00| |[[:human_genes:P:PRKACA|PRKACA]]|4.08|0.00| |[[:human_genes:M:MIDN|MIDN]]|4.12|0.00| |[[:human_genes:P:PLAA|PLAA]]|4.13|0.00| |[[:human_genes:A:ATMIN|ATMIN]]|4.32|0.00| |[[:human_genes:C:CXorf56|CXorf56]]|4.32|0.00| |[[:human_genes:G:GNAS|GNAS]]|4.75|0.00| |[[:human_genes:U:UBQLN1|UBQLN1]]|4.94|0.00| |[[:human_genes:A:APAF1|APAF1]]|5.05|0.00| |[[:human_genes:M:MARCH5|MARCH5]]|5.12|0.00| |[[:human_genes:B:BAK1|BAK1]]|7.39|0.00| ^Screen^Correlation^Plot^ |[[:results:exp527|Tanespimycin 14μM R08 exp527]]|0.077|| |[[:results:exp531|THZ1 0.06μM R08 exp531]]|0.077|| |[[:results:exp529|Thimerosal 0.85μM R08 exp529]]|0.065|| |[[:results:exp85|UM0129480 7μM R02 exp85]]|0.061|| |[[:results:exp456|Benzoate 20000μM R08 exp456]]|0.132|| |[[:results:exp489|Hippuristanol 0.12μM R08 exp489 no dilution day6]]|0.12|| |[[:results:exp488|Hippuristanol 0.12μM R08 exp488]]|0.118|| |[[:results:exp503|Mitomycin-C 0.06μM R08 exp503]]|0.116|| |[[:results:exp459|Bleomycin 5μM R08 exp459]]|0.115|| |[[:results:exp135|MS023 7μM R03 exp135]]|0.105|| |[[:results:exp502|Milciclib 2μM R08 exp502]]|0.101|| |[[:results:exp485|GSK626616 14μM R08 exp485]]|0.101|| |[[:results:exp440|Aphidicolin 0.4μM R08 exp440]]|0.1|| |[[:results:exp3|Actinomycin-D 0.001μM R00 exp3]]|0.096|| |[[:results:exp134|MS023 2μM R03 exp134]]|0.094|| |[[:results:exp478|Doxorubicin 0.02μM R08 exp478]]|0.093|| |[[:results:exp515|PU-H71 1μM R08 exp515]]|0.091|| |[[:results:exp80|RO-3307 4.7μM R02 exp80]]|0.09|| |[[:results:exp474|CR131-b 0.005μM R08 exp474]]|0.089|| |[[:results:exp199|Etoposide 0.3μM R05 exp199]]|0.088|| |[[:results:exp435|JQ1 0.8μM R08 exp435]]|0.084|| |[[:results:exp357|Dorsomorphin 5μM R07 exp357]]|0.079|| |[[:results:exp28|Pimelic-diphenylamide-106 5μM R00 exp28]]|0.079|| |[[:results:exp374|Latrunculin-B 10μM R07 exp374]]|0.078|| |[[:results:exp211|AICAR 240μM R05 exp211]]|0.075|| |[[:results:exp443|SNS-032 15μM R08 exp443]]|0.075|| |[[:results:exp355|Dinaciclib 0.007μM R07 exp355]]|0.074|| |[[:results:exp234|Ethanol 0.01 R05 exp234]]|0.073|| |[[:results:exp512|Olaparib 4μM R08 exp512]]|0.072|| |[[:results:exp505|ML-792 0.2μM R08 exp505]]|0.071|| |[[:results:exp2|5-Fluorouracil 20μM R00 exp2]]|0.071|| |[[:results:exp34|Rotenone 20μM R00 exp34]]|0.07|| |[[:results:exp19|Etoposide 1μM R00 exp19]]|0.07|| |[[:results:exp468|CB-5083 0.4μM R08 exp468]]|0.066|| |[[:results:exp216|Erlotinib 10μM R05 exp216]]|0.061|| |[[:results:exp472|CI-1040 9.5μM R08 exp472]]|0.061|| |[[:results:exp259|6-Thio-2-deoxyguanosine 2μM R06 exp259]]|0.06|| |[[:results:exp451|Atovaquone 15μM R08 exp451]]|0.052|| |[[:results:exp349|Cytochalasin-B 5μM R07 exp349]]|0.052|| |[[:results:exp450|Artemisinin 50μM R08 exp450]]|0.051|| |[[:results:exp116|AICAR 240μM R03 exp116]]|0.051|| {{:chemogenomics:comparison_plots:exp524_vs_exp527.png?nolink |}} {{:chemogenomics:comparison_plots:exp524_vs_exp531.png?nolink |}} {{:chemogenomics:comparison_plots:exp524_vs_exp529.png?nolink |}} {{:chemogenomics:comparison_plots:exp524_vs_exp85.png?nolink |}} {{:chemogenomics:comparison_plots:exp456_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp489_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp488_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp503_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp459_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp135_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp502_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp485_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp440_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp3_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp134_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp478_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp515_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp524_vs_exp80.png?nolink |}} {{:chemogenomics:comparison_plots:exp474_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp199_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp435_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp357_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp28_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp374_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp211_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp443_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp355_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp234_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp512_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp505_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp2_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp34_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp19_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp468_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp216_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp472_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp259_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp451_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp349_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp450_vs_exp524.png?nolink |}} {{:chemogenomics:comparison_plots:exp116_vs_exp524.png?nolink |}} No GO term hits below threshold. (FDR <0.05) No GO term hits below threshold. (FDR <0.05)