====== Phorbol-12-myristate-13-acetate 0.57μM R08 exp514 ======
==== Mechanism of Action ====
Activates PKC isoforms, potent tumour promoter
* **Class / Subclass 1:** Signal Transduction / Kinase Activator
==== Technical Notes ====
* **PubChem Name:** %%Phorbol 12-myristate 13-acetate%%
* **Synonyms:** PMA
* **CAS #:** 16561-29-8
* **PubChem CID:** [[https://pubchem.ncbi.nlm.nih.gov/compound/27924|27924]]
* **IUPAC:** %%[(1S,2S,6R,10S,11R,13S,14R,15R)-13-acetyloxy-1,6-dihydroxy-8-(hydroxymethyl)-4,12,12,15-tetramethyl-5-oxo-14-tetracyclo[8.5.0.02,6.011,13]pentadeca-3,8-dienyl] tetradecanoate%%
* **INCHI Name:** InChI=1S/C36H56O8/c1-7-8-9-10-11-12-13-14-15-16-17-18-29(39)43-32-24(3)35(42)27(30-33(5,6)36(30,32)44-25(4)38)20-26(22-37)21-34(41)28(35)19-23(2)31(34)40/h19-20,24,27-28,30,32,37,41-42H,7-18,21-22H2,1-6H3/t24-,27+,28-,30-,32-,34-,35-,36-/m1/s1
* **INCHI Key:** PHEDXBVPIONUQT-RGYGYFBISA-N
* **Molecular Weight:** 616.8
* **Canonical SMILES:** CCCCCCCCCCCCCC(=O)OC1C(C2(C(C=C(CC3(C2C=C(C3=O)C)O)CO)C4C1(C4(C)C)OC(=O)C)O)C
* **Isomeric SMILES:** CCCCCCCCCCCCCC(=O)O[C@@H]1[C@H]([C@]2([C@@H](C=C(C[C@]3([C@H]2C=C(C3=O)C)O)CO)[C@H]4[C@@]1(C4(C)C)OC(=O)C)O)C
* **Molecular Formula:** C8H8HgO2
{{:chemogenomics:structures:chem-0319.svg?nolink}}
* **Supplier Name:** Med Chem Express
* **Catalog #:** HY-18739
* **Lot #:** 24554
* **HRMS (ESI-TOF) m/z:** (M+Na)+ Calcd for C36 H56 O8 639.38674; found 639.38537
* **Platform ID:** TPA
* **Min:** 11.8198; **Max:** 99.9039
{{:chemogenomics:dose_response:dr_453.png?nolink&500 |}}
\\
\\
\\
\\
|< 300px 100px 200px >|
^ IC ^ Concentration (µM) ^
| IC10 |N/A |
| IC20 |7.0489 |
| IC30 |8.4531 |
| IC40 |9.4877 |
| IC50 |10.4307 |
| IC60 |N/A |
| IC70 |N/A |
| IC80 |N/A |
| IC90 |N/A |
\\
==== Screen Summary ====
* **Round**: 08
* **Dose**: 570nM
* **Days of incubation**: 8
* **Doublings**: 6.2
* **Numbers of reads**: 16332845
==== 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^
|33/33|[[https://files.tyerslab.com/files/public/chemogenomics/cranks/Phorbol_12-myristate_13-acetate_0.57uM_Round-8_exp514.txt|Scores]]||||||
{{:chemogenomics:cranks_plots:exp514.png?nolink}}
^Gene^CRANKS Score^FDR^
|[[:human_genes:T:TM2D2|TM2D2]]|-4.86|<0.01|
|[[:human_genes:S:SOX4|SOX4]]|-3.64|<0.01|
|[[:human_genes:R:RALGAPB|RALGAPB]]|-3.62|<0.01|
|[[:human_genes:M:MARK2|MARK2]]|-3.52|<0.01|
|[[:human_genes:A:ATP2B1|ATP2B1]]|-3.52|<0.01|
|[[:human_genes:R:RHOA|RHOA]]|-3.44|<0.01|
|[[:human_genes:B:BACH2|BACH2]]|-3.18|<0.01|
|[[:human_genes:P:PRKACA|PRKACA]]|-3.15|<0.01|
|[[:human_genes:R:RASA2|RASA2]]|-3.15|<0.01|
|[[:human_genes:T:TMEM203|TMEM203]]|-2.97|<0.01|
|[[:human_genes:C:CNOT8|CNOT8]]|-2.91|<0.01|
|[[:human_genes:T:TCF4|TCF4]]|-2.90|<0.01|
|[[:human_genes:G:GNAS|GNAS]]|-2.90|<0.01|
|[[:human_genes:T:TM2D3|TM2D3]]|-2.83|<0.01|
|[[:human_genes:D:DUSP6|DUSP6]]|-2.73|<0.01|
|[[:human_genes:S:STRAP|STRAP]]|-2.72|<0.01|
|[[:human_genes:L:LZTR1|LZTR1]]|-2.65|<0.01|
|[[:human_genes:Z:ZNF292|ZNF292]]|-2.58|0.01|
|[[:human_genes:S:SNRK|SNRK]]|-2.58|0.01|
|[[:human_genes:U:UBE3A|UBE3A]]|-2.56|0.01|
|[[:human_genes:Z:ZDHHC6|ZDHHC6]]|-2.55|0.01|
|[[:human_genes:C:CSK|CSK]]|-2.54|0.01|
|[[:human_genes:P:PRRC2C|PRRC2C]]|-2.52|0.03|
|[[:human_genes:S:STUB1|STUB1]]|-2.50|0.01|
|[[:human_genes:U:UBA3|UBA3]]|-2.49|0.06|
|[[:human_genes:M:MBTPS2|MBTPS2]]|-2.45|0.02|
|[[:human_genes:R:RTCB|RTCB]]|-2.44|0.12|
|[[:human_genes:U:UBE2D3|UBE2D3]]|-2.44|0.02|
|[[:human_genes:K:KCTD5|KCTD5]]|-2.40|0.03|
|[[:human_genes:T:TM2D1|TM2D1]]|-2.38|0.05|
|[[:human_genes:R:RIC8A|RIC8A]]|2.44|0.02|
|[[:human_genes:G:GABRB1|GABRB1]]|2.44|0.02|
|[[:human_genes:P:PRR21|PRR21]]|2.51|0.01|
|[[:human_genes:G:GNA15|GNA15]]|2.57|0.01|
|[[:human_genes:M:MYCBP2|MYCBP2]]|2.57|0.05|
|[[:human_genes:W:WDR20|WDR20]]|2.65|0.02|
|[[:human_genes:K:KDM5C|KDM5C]]|2.73|0.01|
|[[:human_genes:L:LPAR5|LPAR5]]|2.73|<0.01|
|[[:human_genes:S:SARS|SARS]]|2.81|0.29|
|[[:human_genes:S:SETD1B|SETD1B]]|2.83|0.02|
|[[:human_genes:A:API5|API5]]|2.89|<0.01|
|[[:human_genes:M:MAP2K1|MAP2K1]]|2.90|<0.01|
|[[:human_genes:D:DIEXF|DIEXF]]|2.99|0.02|
|[[:human_genes:G:GNG5|GNG5]]|3.08|0.00|
|[[:human_genes:B:BCL6|BCL6]]|3.10|0.00|
|[[:human_genes:N:NPRL3|NPRL3]]|3.28|<0.01|
|[[:human_genes:P:PRKCE|PRKCE]]|3.42|0.00|
|[[:human_genes:I:ICMT|ICMT]]|3.48|0.00|
|[[:human_genes:N:NSD1|NSD1]]|3.53|0.00|
|[[:human_genes:G:GNB1|GNB1]]|3.57|0.00|
|[[:human_genes:T:TSC2|TSC2]]|3.70|0.00|
|[[:human_genes:S:STIM2|STIM2]]|3.75|0.00|
|[[:human_genes:P:PRKCD|PRKCD]]|4.13|0.00|
|[[:human_genes:P:PPP3R1|PPP3R1]]|4.31|0.00|
|[[:human_genes:M:MAPK1|MAPK1]]|4.42|0.00|
|[[:human_genes:S:SCRIB|SCRIB]]|4.74|0.00|
|[[:human_genes:R:RCE1|RCE1]]|4.85|0.00|
|[[:human_genes:S:SHOC2|SHOC2]]|4.88|0.00|
|[[:human_genes:R:RAF1|RAF1]]|5.73|0.00|
|[[:human_genes:N:NRAS|NRAS]]|6.55|0.00|
^Screen^Correlation^Plot^
|[[:results:exp242|Radicicol 0.16μM R05 exp242]]|0.051||
|[[:results:exp488|Hippuristanol 0.12μM R08 exp488]]|0.054||
{{:chemogenomics:comparison_plots:exp242_vs_exp514.png?nolink |}}
{{:chemogenomics:comparison_plots:exp488_vs_exp514.png?nolink |}}
No GO term hits below threshold. (FDR <0.05)
^GO Term^Fold Change^Genes^
|MAPK cascade|16.09|NRAS,RAF1,RCE1,MAPK1,PRKCE,MAP2K1|