====== Dinaciclib 0.007μM R07 exp355 ======
==== Mechanism of Action ====
Inhibits CDK2, CDK5, CDK1, CDK9
* **Class / Subclass 1:** Cell Cycle / Cell Cycle Inhibitor
* **Class / Subclass 2:** Signal Transduction / Kinase Inhibitor
* **Class / Subclass 3:** Gene Regulation / Transcription Inhibitor
==== Technical Notes ====
* **PubChem Name:** %%Dinaciclib%%
* **Synonyms:** SCH 727965
* **CAS #:** 779353-01-4
* **PubChem CID:** [[https://pubchem.ncbi.nlm.nih.gov/compound/46926350|46926350]]
* **IUPAC:** %%2-[(2S)-1-[3-ethyl-7-[(1-oxidopyridin-1-ium-3-yl)methylamino]pyrazolo[1,5-a]pyrimidin-5-yl]piperidin-2-yl]ethanol%%
* **INCHI Name:** InChI=1S/C21H28N6O2/c1-2-17-14-23-27-19(22-13-16-6-5-9-25(29)15-16)12-20(24-21(17)27)26-10-4-3-7-18(26)8-11-28/h5-6,9,12,14-15,18,22,28H,2-4,7-8,10-11,13H2,1H3/t18-/m0/s1
* **INCHI Key:** PIMQWRZWLQKKBJ-SFHVURJKSA-N
* **Molecular Weight:** 396.5
* **Canonical SMILES:** CCC1=C2N=C(C=C(N2N=C1)NCC3=C[N+](=CC=C3)[O-])N4CCCCC4CCO
* **Isomeric SMILES:** CCC1=C2N=C(C=C(N2N=C1)NCC3=C[N+](=CC=C3)[O-])N4CCCC[C@H]4CCO
* **Molecular Formula:** C21H28N6O2
{{:chemogenomics:structures:chem-0210.svg?nolink}}
* **Supplier Name:** Toronto Research Chemicals
* **Catalog #:** D479725
* **Lot #:** 2-MJS-149-1
* **HRMS (ESI-TOF) m/z:** (M+H)+ Calcd for C21H28N6O2 397.23465; found 397.23573
* **Platform ID:** Dinaclib
* **Min:** -9.1162; **Max:** 88.5880
{{:chemogenomics:dose_response:dr_383.png?nolink&500 |}}
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^ IC ^ Concentration (µM) ^
| IC10 |N/A |
| IC20 |0.0052 |
| IC30 |0.0064 |
| IC40 |0.0077 |
| IC50 |0.0093 |
| IC60 |N/A |
| IC70 |N/A |
| IC80 |N/A |
| IC90 |N/A |
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==== Screen Summary ====
* **Round**: 07
* **Dose**: 7nM
* **Days of incubation**: 8
* **Doublings**: 0.5
* **Numbers of reads**: 18702654
==== 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^
|0/24|[[https://files.tyerslab.com/files/public/chemogenomics/cranks/Dinaciclib_0.007uM_Round-7_exp355.txt|Scores]]||||||
{{:chemogenomics:cranks_plots:exp355.png?nolink}}
^Gene^CRANKS Score^FDR^
|[[:human_genes:Z:ZBTB1|ZBTB1]]|-2.51|0.22|
|[[:human_genes:P:PTPN23|PTPN23]]|-2.49|0.24|
|[[:human_genes:S:SMG5|SMG5]]|-2.49|0.53|
|[[:human_genes:P:PRMT7|PRMT7]]|-2.43|0.22|
|[[:human_genes:P:POLR1B|POLR1B]]|-2.43|0.54|
|[[:human_genes:Z:ZFAND5|ZFAND5]]|-2.41|0.22|
|[[:human_genes:S:SMG7|SMG7]]|-2.41|0.36|
|[[:human_genes:C:CADPS|CADPS]]|-2.28|0.42|
|[[:human_genes:N:NDRG4|NDRG4]]|-2.27|0.30|
|[[:human_genes:N:NBAS|NBAS]]|-2.21|0.33|
|[[:human_genes:U:UBE4A|UBE4A]]|-2.19|0.33|
|[[:human_genes:R:RNF103-CHMP3|RNF103-CHMP3]]|-2.19|0.46|
|[[:human_genes:H:HEXIM1|HEXIM1]]|-2.17|0.33|
|[[:human_genes:N:NR1D2|NR1D2]]|-2.16|0.36|
|[[:human_genes:S:SYNCRIP|SYNCRIP]]|-2.14|0.42|
|[[:human_genes:M:MKLN1|MKLN1]]|-2.13|0.35|
|[[:human_genes:Y:YPEL5|YPEL5]]|-2.12|0.35|
|[[:human_genes:F:FOXK1|FOXK1]]|-2.11|0.36|
|[[:human_genes:K:KPNA2|KPNA2]]|-2.10|0.35|
|[[:human_genes:K:KCTD10|KCTD10]]|-2.09|0.35|
|[[:human_genes:N:NCAPH|NCAPH]]|-2.07|0.53|
|[[:human_genes:C:C12orf66|C12orf66]]|-2.06|0.36|
|[[:human_genes:M:MUL1|MUL1]]|-2.05|0.42|
|[[:human_genes:A:ACP1|ACP1]]|-2.04|0.36|
|[[:human_genes:I:IPO13|IPO13]]|-2.04|0.46|
|[[:human_genes:P:PTPDC1|PTPDC1]]|-2.04|0.42|
|[[:human_genes:M:MTFR1|MTFR1]]|-2.03|0.36|
|[[:human_genes:T:TOMM70A|TOMM70A]]|-2.02|0.36|
|[[:human_genes:K:KIF11|KIF11]]|-2.01|0.77|
|[[:human_genes:A:ADK|ADK]]|-2.00|0.36|
|[[:human_genes:F:FAU|FAU]]|2.22|0.24|
|[[:human_genes:S:SRM|SRM]]|2.22|0.07|
|[[:human_genes:P:PLAA|PLAA]]|2.22|0.07|
|[[:human_genes:X:XPR1|XPR1]]|2.27|0.06|
|[[:human_genes:H:HDAC7|HDAC7]]|2.31|0.05|
|[[:human_genes:C:CDK5|CDK5]]|2.33|0.04|
|[[:human_genes:M:MARCH5|MARCH5]]|2.36|0.04|
|[[:human_genes:N:NRBP1|NRBP1]]|2.40|0.06|
|[[:human_genes:E:EBF1|EBF1]]|2.53|0.04|
|[[:human_genes:L:LSG1|LSG1]]|2.56|0.04|
|[[:human_genes:A:ARID4B|ARID4B]]|2.59|0.03|
|[[:human_genes:P:PHF2|PHF2]]|2.65|0.04|
|[[:human_genes:A:ATIC|ATIC]]|2.68|<0.01|
|[[:human_genes:F:FAF2|FAF2]]|2.71|0.02|
|[[:human_genes:U:UBQLN1|UBQLN1]]|2.72|<0.01|
|[[:human_genes:K:KLF16|KLF16]]|2.81|0.03|
|[[:human_genes:S:SSU72|SSU72]]|2.84|<0.01|
|[[:human_genes:K:KIAA0195|KIAA0195]]|2.89|<0.01|
|[[:human_genes:M:MDH1|MDH1]]|2.91|<0.01|
|[[:human_genes:V:VDAC2|VDAC2]]|2.93|<0.01|
|[[:human_genes:E:EIF3G|EIF3G]]|3.19|<0.01|
|[[:human_genes:E:EIF4A1|EIF4A1]]|3.20|<0.01|
|[[:human_genes:I:INTS8|INTS8]]|3.25|<0.01|
|[[:human_genes:B:BAK1|BAK1]]|3.36|<0.01|
|[[:human_genes:U:UMPS|UMPS]]|3.37|0.06|
|[[:human_genes:I:INTS1|INTS1]]|3.37|<0.01|
|[[:human_genes:I:INTS6|INTS6]]|3.87|0.01|
|[[:human_genes:C:C2CD5|C2CD5]]|4.46|<0.01|
|[[:human_genes:F:FIBP|FIBP]]|5.11|<0.01|
|[[:human_genes:I:IMPDH2|IMPDH2]]|5.25|<0.01|
^Screen^Correlation^Plot^
|[[:results:exp80|RO-3307 4.7μM R02 exp80]]|0.085||
|[[:results:exp199|Etoposide 0.3μM R05 exp199]]|0.077||
|[[:results:exp512|Olaparib 4μM R08 exp512]]|0.076||
|[[:results:exp524|Staurosporine 0.02μM R08 exp524]]|0.074||
|[[:results:exp503|Mitomycin-C 0.06μM R08 exp503]]|0.072||
|[[:results:exp485|GSK626616 14μM R08 exp485]]|0.067||
|[[:results:exp28|Pimelic-diphenylamide-106 5μM R00 exp28]]|0.064||
|[[:results:exp489|Hippuristanol 0.12μM R08 exp489 no dilution day6]]|0.061||
|[[:results:exp478|Doxorubicin 0.02μM R08 exp478]]|0.06||
|[[:results:exp488|Hippuristanol 0.12μM R08 exp488]]|0.06||
|[[:results:exp234|Ethanol 0.01 R05 exp234]]|0.059||
|[[:results:exp357|Dorsomorphin 5μM R07 exp357]]|0.056||
|[[:results:exp19|Etoposide 1μM R00 exp19]]|0.055||
|[[:results:exp85|UM0129480 7μM R02 exp85]]|0.053||
|[[:results:exp435|JQ1 0.8μM R08 exp435]]|0.052||
|[[:results:exp456|Benzoate 20000μM R08 exp456]]|0.103||
|[[:results:exp459|Bleomycin 5μM R08 exp459]]|0.063||
|[[:results:exp259|6-Thio-2-deoxyguanosine 2μM R06 exp259]]|0.062||
|[[:results:exp440|Aphidicolin 0.4μM R08 exp440]]|0.062||
|[[:results:exp3|Actinomycin-D 0.001μM R00 exp3]]|0.062||
|[[:results:exp116|AICAR 240μM R03 exp116]]|0.061||
|[[:results:exp211|AICAR 240μM R05 exp211]]|0.057||
|[[:results:exp2|5-Fluorouracil 20μM R00 exp2]]|0.056||
|[[:results:exp343|Centrinone 0.5μM R07 exp343]]|0.051||
{{:chemogenomics:comparison_plots:exp355_vs_exp80.png?nolink |}}
{{:chemogenomics:comparison_plots:exp199_vs_exp355.png?nolink |}}
{{:chemogenomics:comparison_plots:exp355_vs_exp512.png?nolink |}}
{{:chemogenomics:comparison_plots:exp355_vs_exp524.png?nolink |}}
{{:chemogenomics:comparison_plots:exp355_vs_exp503.png?nolink |}}
{{:chemogenomics:comparison_plots:exp355_vs_exp485.png?nolink |}}
{{:chemogenomics:comparison_plots:exp28_vs_exp355.png?nolink |}}
{{:chemogenomics:comparison_plots:exp355_vs_exp489.png?nolink |}}
{{:chemogenomics:comparison_plots:exp355_vs_exp478.png?nolink |}}
{{:chemogenomics:comparison_plots:exp355_vs_exp488.png?nolink |}}
{{:chemogenomics:comparison_plots:exp234_vs_exp355.png?nolink |}}
{{:chemogenomics:comparison_plots:exp355_vs_exp357.png?nolink |}}
{{:chemogenomics:comparison_plots:exp19_vs_exp355.png?nolink |}}
{{:chemogenomics:comparison_plots:exp355_vs_exp85.png?nolink |}}
{{:chemogenomics:comparison_plots:exp355_vs_exp435.png?nolink |}}
{{:chemogenomics:comparison_plots:exp355_vs_exp456.png?nolink |}}
{{:chemogenomics:comparison_plots:exp355_vs_exp459.png?nolink |}}
{{:chemogenomics:comparison_plots:exp259_vs_exp355.png?nolink |}}
{{:chemogenomics:comparison_plots:exp355_vs_exp440.png?nolink |}}
{{:chemogenomics:comparison_plots:exp3_vs_exp355.png?nolink |}}
{{:chemogenomics:comparison_plots:exp116_vs_exp355.png?nolink |}}
{{:chemogenomics:comparison_plots:exp211_vs_exp355.png?nolink |}}
{{:chemogenomics:comparison_plots:exp2_vs_exp355.png?nolink |}}
{{:chemogenomics:comparison_plots:exp343_vs_exp355.png?nolink |}}
No GO term hits below threshold. (FDR <0.05)
^GO Term^Fold Change^Genes^
|integrator complex|103.62|INTS6,INTS1,INTS8|
|snRNA 3-end processing|78.95|INTS6,INTS1,INTS8|
|RNA 3-end processing|31.40|INTS6,INTS1,INTS8,SSU72,AHCYL1|