5-Fluorouracil 20μM R00 exp2

5-Fluorouracil 20μM R00 exp2

Mechanism of Action

Thymidylate synthase inhibitor, blocks DNA replication

Class / Subclass 1: Metabolism / Antimetabolite
Class / Subclass 2: DNA Damage, Repair and Replication / Replication Inhibitor

Technical Notes

Protein References

PubChem Name: 5-Fluorouracil
Synonyms: 5-FU
CAS #: 51-21-8
PubChem CID: 3385
IUPAC: 5-fluoro-1H-pyrimidine-2,4-dione
INCHI Name: InChI=1S/C4H3FN2O2/c5-2-1-6-4(9)7-3(2)8/h1H,(H2,6,7,8,9)
INCHI Key: GHASVSINZRGABV-UHFFFAOYSA-N
Molecular Weight: 130.08
Canonical SMILES: C1=C(C(=O)NC(=O)N1)F
Isomeric SMILES: N/A
Molecular Formula: C4H3FN2O2

Protein Supplier

Supplier Name: Sigma-Aldrich
Catalog #: F6627
Lot #: 102K0970

Protein Characterization

LCMS: Tr 0.14 min, m/z 129- [M-H]-

Dose Response Curve

Platform ID: 5-FU
Min: -8.9515; Max: 61.1847

IC	Concentration (µM)
IC10	N/A
IC20	12.7820
IC30	22.9250
IC40	37.0071
IC50	57.4305
IC60	N/A
IC70	N/A
IC80	N/A
IC90	N/A

Screen Summary

Round: 00
Dose: 20µM
Days of incubation: 8
Doublings: 1.5
Numbers of reads: 11051144

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
8/86	Scores	View	View	View	View	View

Gene	CRANKS Score	FDR
POLA1	-3.74	0.11
BRD2	-3.32	<0.01
GOLGA6L1	-3.06	0.17
ATP6V1A	-3.02	0.02
SF3A1	-2.93	0.32
SEPHS2	-2.75	0.03
VPS25	-2.71	0.18
PDS5B	-2.68	0.03
BCOR	-2.68	0.05
RRM2	-2.67	0.38
PCGF1	-2.66	0.03
CNOT2	-2.64	0.03
PAN2	-2.57	0.07
MGA	-2.54	0.05
ATXN2L	-2.50	0.08
POLR2I	-2.46	0.05
SPRR2D	-2.43	0.09
DDX3X	-2.40	0.07
NPIPB8	-2.39	0.38
INO80E	-2.37	0.11
POLR2A	-2.31	0.32
GCGR	-2.29	0.09
PRPH	-2.29	0.09
MSI2	-2.26	0.10
ATP6V1B2	-2.25	0.16
CHMP4B	-2.24	0.11
FOXD1	-2.24	0.28
NPRL3	-2.23	0.23
POLA2	-2.22	0.36
SAE1	-2.22	0.24
MIOS	3.28	<0.01
ID3	3.28	<0.01
CDKN1A	3.28	<0.01
CSNK2B	3.32	<0.01
WDR5	3.40	<0.01
AURKB	3.53	<0.01
UBE2G1	3.54	<0.01
SUV420H1	3.63	<0.01
FBXO11	3.67	<0.01
MEAF6	3.67	<0.01
GMPPB	3.76	<0.01
DIABLO	3.84	<0.01
FAF2	3.87	<0.01
UBE2K	4.01	<0.01
TLE4	4.07	<0.01
CASP9	4.44	<0.01
CYCS	4.90	<0.01
RPL11	4.93	<0.01
HCCS	5.04	<0.01
HEATR3	5.16	<0.01
UBQLN1	5.17	<0.01
VDAC2	5.29	<0.01
PLAA	5.79	<0.01
APAF1	6.23	<0.01
ENY2	6.31	<0.01
XPO7	6.32	<0.01
MARCH5	6.98	<0.01
BAK1	7.18	<0.01
UCK2	7.25	<0.01
TP53	8.50	<0.01

Screen	Correlation	Plot
Actinomycin-D 0.001μM R00 exp3	0.31	View
Pimelic-diphenylamide-106 5μM R00 exp28	0.198	View
Rotenone 20μM R00 exp34	0.193	View
Etoposide 1μM R00 exp19	0.181	View
Etoposide 0.3μM R05 exp199	0.164	View
Benzoate 20000μM R08 exp456	0.153	View
Mitomycin-C 0.06μM R08 exp503	0.139	View
CI-1040 9.5μM R08 exp472	0.132	View
THZ1 0.06μM R08 exp531	0.128	View
Doxorubicin 0.02μM R08 exp478	0.121	View
Bleomycin 5μM R08 exp459	0.115	View
AICAR 240μM R05 exp211	0.114	View
MLN-4924 2μM R00 exp22	0.111	View
RO-3307 4.7μM R02 exp80	0.11	View
Aphidicolin 0.4μM R08 exp440	0.107	View
UM131593 0.2μM R03 exp106	0.106	View
6-Thio-2-deoxyguanosine 2μM R06 exp259	0.105	View
DABN 20μM R00 exp17	0.098	View
MS023 7μM R03 exp135	0.096	View
SNS-032 15μM R08 exp443	0.092	View
Bortezomib 0.05μM R00 exp7	0.088	View
GSK626616 14μM R08 exp485	0.087	View
Atovaquone 15μM R08 exp451	0.086	View
Olaparib 4μM R08 exp512	0.086	View
PU-H71 1μM R08 exp515	0.086	View
Tanespimycin 14μM R08 exp527	0.082	View
JQ1 0.8μM R08 exp435	0.08	View
Hippuristanol 0.12μM R08 exp489 no dilution day6	0.074	View
AICAR 240μM R03 exp116	0.072	View
Staurosporine 0.02μM R08 exp524	0.071	View
Hippuristanol 0.12μM R08 exp488	0.07	View
Deferoxamine 11μM R07 exp350	0.068	View
GSK461364A 0.1μM R03 exp126	0.068	View
Diepoxybutane 3μM R07 exp354	0.067	View
CR131-b 0.005μM R08 exp474	0.067	View
Rotenone 2μM R00 exp33	0.061	View
UM0129480 7μM R02 exp85	0.059	View
Ammonium tetrathiomolybdate 10μM R08 exp448	0.059	View
Dinaciclib 0.007μM R07 exp355	0.056	View
LY2090314 0.003μM R08 exp500 no dilution day6	0.055	View
Etoposide 10μM R00 exp20	0.055	View
Centrinone 0.5μM R07 exp343	0.055	View
Dorsomorphin 5μM R07 exp357	0.054	View
MLN-4924 0.2μM R00 exp21	0.053	View
MS023 2μM R03 exp134	0.053	View
Artemisinin 50μM R08 exp450	0.052	View
BML-284 0.09μM R08 exp460	0.051	View
BI-2536 0.02μM R03 exp96	0.051	View
42°C R08 exp539	0.091	View

GO Term	Fold Change	Genes
apoptosome	552.70	APAF1,CASP9
activation of cysteine-type endopeptidase activity involved in apoptotic process by cytochrome c	442.16	APAF1,CYCS,CASP9,DIABLO
glial cell apoptotic process	276.35	TP53,CASP9
positive regulation of mitochondrial membrane permeability	59.22	TP53,BAK1,VDAC2
cellular response to UV	31.76	TP53,BAK1,CASP9,AURKB,CDKN1A
intrinsic apoptotic signaling pathway in response to DNA damage	31.14	TP53,BAK1,CASP9,CDKN1A
cellular response to light stimulus	24.90	TP53,BAK1,CASP9,AURKB,CDKN1A
intrinsic apoptotic signaling pathway	24.18	TP53,BAK1,APAF1,CYCS,CASP9,DIABLO,CDKN1A
positive regulation of cysteine-type endopeptidase activity	22.29	BAK1,APAF1,CYCS,CASP9,DIABLO
positive regulation of endopeptidase activity	19.06	BAK1,APAF1,CYCS,CASP9,DIABLO
response to UV	18.55	TP53,BAK1,CASP9,AURKB,CDKN1A
positive regulation of peptidase activity	17.38	BAK1,APAF1,CYCS,CASP9,DIABLO
cellular response to radiation	16.55	TP53,BAK1,CASP9,AURKB,CDKN1A
apoptotic signaling pathway	14.36	TP53,BAK1,APAF1,VDAC2,CYCS,CASP9,DIABLO,CDKN1A
ubiquitin protein ligase binding	11.09	TP53,RPL11,UBE2K,FAF2,UBE2G1,CDKN1A
ubiquitin-like protein ligase binding	10.46	TP53,RPL11,UBE2K,FAF2,UBE2G1,CDKN1A
positive regulation of programmed cell death	8.70	TP53,BAK1,APAF1,RPL11,CASP9,DIABLO,CDKN1A,ID3
regulation of DNA metabolic process	8.69	TP53,ENY2,APAF1,MEAF6,KMT5B,AURKB,CDKN1A,ID3
regulation of proteolysis	8.43	TP53,BAK1,APAF1,UBQLN1,RPL11,CYCS,CASP9,UBE2K,DIABLO

Table of Contents

5-Fluorouracil 20μM R00 exp2

Mechanism of Action

Technical Notes

Protein References

Protein Supplier

Protein Characterization

Dose Response Curve

Screen Summary

Screen Results