QNZ 0.01μM R05 exp241

Inhibits NF-κB activation, TNF-α production

Class / Subclass 1: Gene Regulation / Transcription Inhibitor
Class / Subclass 2: Signal Transduction / Apoptosis Inhibitor

Compound References

PubChem Name: 6-Amino-4-(4-phenoxyphenylethylamino)quinazoline
Synonyms: EVP4593
CAS #: 545380-34-5
PubChem CID: 509554
IUPAC: 4-N-[2-(4-phenoxyphenyl)ethyl]quinazoline-4,6-diamine
INCHI Name: InChI=1S/C22H20N4O/c23-17-8-11-21-20(14-17)22(26-15-25-21)24-13-12-16-6-9-19(10-7-16)27-18-4-2-1-3-5-18/h1-11,14-15H,12-13,23H2,(H,24,25,26)
INCHI Key: IBAKVEUZKHOWNG-UHFFFAOYSA-N
Molecular Weight: 356.4
Canonical SMILES: C1=CC=C(C=C1)OC2=CC=C(C=C2)CCNC3=NC=NC4=C3C=C(C=C4)N
Isomeric SMILES: N/A
Molecular Formula: C22H20N4O

Compound Supplier

Supplier Name: Toronto Research Chemicals
Catalog #: A621350
Lot #: N/A

Compound Characterization

HRMS (ESI-TOF) m/z: (M+H)+ Calcd for C22H20N4O 357.17099; found 357.17163

Dose Response Curve

Platform ID: QNZ
Min: 5.7879; Max: 89.7941

IC	Concentration (µM)
IC10	N/A
IC20	N/A
IC30	0.0006
IC40	0.0166
IC50	0.3525
IC60	N/A
IC70	N/A
IC80	N/A
IC90	N/A

Screen Summary

Round: 05
Dose: 10nM
Days of incubation: 8
Doublings: 4.4
Numbers of reads: 14834962

Sensitive/Resistant hits (FDR<0.05)	CRANKS	Score Plot	Top 30 Genes	Screen Similarity	Top 30 Sensitive GO terms	Top 30 Resistant GO terms
5/9	Scores	View	View	View	View	View

Gene	CRANKS Score	FDR
GOT1	-5.26	<0.01
RSRC2	-3.41	0.05
PDXK	-3.21	<0.01
SUCLG1	-3.20	<0.01
WSB1	-2.83	0.04
NNT	-2.83	0.06
ALDOA	-2.77	0.29
LIAS	-2.60	0.04
HPRT1	-2.59	0.07
GSR	-2.45	0.10
GCLC	-2.44	0.10
SLC16A1	-2.39	0.12
BSG	-2.38	0.17
LIPT2	-2.36	0.12
ELAVL1	-2.35	0.10
GCLM	-2.34	0.10
TRIM54	-2.27	0.11
BIRC2	-2.24	0.17
ECHS1	-2.23	0.12
RPE	-2.23	0.17
PNPO	-2.17	0.19
CADPS	-2.17	0.19
IDH2	-2.13	0.17
GCDH	-2.12	0.21
CNOT8	-2.12	0.17
MECR	-2.11	0.17
ALG1L	-2.11	0.21
SEPHS2	-2.11	0.17
TBL1XR1	-2.09	0.22
VPS39	-2.06	0.19
TMSB15B	2.20	0.46
MINOS1	2.24	0.12
SLC25A32	2.24	0.12
UBAP2L	2.26	0.09
LARS2	2.26	0.12
MOAP1	2.27	0.09
TADA2A	2.28	0.09
FXYD5	2.28	0.11
XPNPEP3	2.28	0.09
ATP5D	2.29	0.11
G3BP2	2.29	0.09
SLC7A1	2.29	0.24
TFDP1	2.30	0.16
ACSL3	2.33	0.10
ZNF626	2.37	0.08
CTU2	2.37	0.09
OR1L8	2.39	0.09
ATP5A1	2.45	0.09
SCAP	2.46	0.09
IPMK	2.47	0.05
ANO5	2.48	0.05
OTUD4	2.50	0.05
ATP5C1	2.56	0.07
ITPK1	2.71	0.02
ATP5E	2.71	0.10
PRPS1	2.91	<0.01
ATP5B	2.96	<0.01
ATP5O	2.99	<0.01
GPT2	3.16	<0.01
SLC25A51	4.48	<0.01

Screen	Correlation	Plot
Rotenone 0.07μM R08 exp431	0.108	View
QNZ 0.01μM R08 exp439	0.099	View
UM0131023 0.05μM R05 exp248	0.062	View
iCRT14 30μM R08 exp492	0.057	View
NMS-873 0.07μM R07 exp380	0.107	View
Phenformin 20μM R05 exp212	0.103	View
Mubritinib 0.2μM R01 exp48	0.094	View
Mubritinib 0.2μM R02 exp65	0.093	View
Chloramphenicol 20μM R00 exp13	0.084	View
Phenformin 20μM R03 exp143	0.079	View
Citral 50μM R06 exp274	0.06	View
Calcium Ionophore 0.4μM R07 exp342	0.055	View

GO Term	Fold Change	Genes
response to human chorionic gonadotropin	306.85	GCLC,GCLM
glutamate metabolic process	65.75	GOT1,GCLC,GCLM
tricarboxylic acid cycle	57.53	SUCLG1,NNT,IDH2
pyridine-containing compound metabolic process	40.91	PDXK,NNT,RPE,PNPO,IDH2
dicarboxylic acid metabolic process	27.90	GOT1,GCLC,GCLM,IDH2
alpha-amino acid metabolic process	15.74	GOT1,GCLC,GCLM,GCDH,SEPHS2
amino acid metabolic process	13.39	GOT1,GCLC,GCLM,ECHS1,GCDH,SEPHS2
purine nucleotide metabolic process	10.77	SUCLG1,NNT,ALDOA,HPRT1,RPE,IDH2,GCDH
mitochondrial matrix	10.36	SUCLG1,LIAS,GSR,LIPT2,ECHS1,IDH2,GCDH,MECR
purine-containing compound metabolic process	10.06	SUCLG1,NNT,ALDOA,HPRT1,RPE,IDH2,GCDH
small molecule biosynthetic process	9.59	GOT1,PDXK,LIAS,HPRT1,PNPO,MECR,SEPHS2
nucleotide metabolic process	9.38	SUCLG1,NNT,ALDOA,HPRT1,RPE,IDH2,GCDH
nucleoside phosphate metabolic process	9.20	SUCLG1,NNT,ALDOA,HPRT1,RPE,IDH2,GCDH
carboxylic acid metabolic process	9.13	GOT1,ALDOA,LIAS,GCLC,SLC16A1,LIPT2,GCLM,ECHS1,IDH2,GCDH,MECR,SEPHS2
oxoacid metabolic process	8.88	GOT1,ALDOA,LIAS,GCLC,SLC16A1,LIPT2,GCLM,ECHS1,IDH2,GCDH,MECR,SEPHS2
organic acid metabolic process	8.81	GOT1,ALDOA,LIAS,GCLC,SLC16A1,LIPT2,GCLM,ECHS1,IDH2,GCDH,MECR,SEPHS2
monocarboxylic acid metabolic process	8.54	ALDOA,LIAS,SLC16A1,ECHS1,IDH2,GCDH,MECR
nucleobase-containing small molecule metabolic process	8.01	SUCLG1,NNT,ALDOA,HPRT1,RPE,IDH2,GCDH
organophosphate metabolic process	6.39	PDXK,SUCLG1,NNT,ALDOA,HPRT1,RPE,PNPO,IDH2,GCDH

GO Term	Fold Change	Genes
mitochondrial proton-transporting ATP synthase complex, catalytic sector F(1)	552.33	ATP5F1B,ATP5F1E,ATP5F1C,ATP5F1A
proton-transporting ATP synthase complex, catalytic core F(1)	552.33	ATP5PO,ATP5F1B,ATP5F1E,ATP5F1C,ATP5F1A
proton-transporting ATP synthase activity, rotational mechanism	236.71	ATP5PO,ATP5F1B,ATP5F1E,ATP5F1C,ATP5F1A,ATP5F1D
mitochondrial proton-transporting ATP synthase complex	220.93	ATP5PO,ATP5F1B,ATP5F1E,ATP5F1C,ATP5F1A,ATP5F1D
proton-transporting two-sector ATPase complex, catalytic domain	194.94	ATP5PO,ATP5F1B,ATP5F1E,ATP5F1C,ATP5F1A,ATP5F1D
proton-transporting ATP synthase complex	172.60	ATP5F1B,ATP5F1E,ATP5F1C,ATP5F1A,ATP5F1D
proton channel activity	125.53	ATP5F1B,ATP5F1E,ATP5F1C,ATP5F1A,ATP5F1D
proton-transporting two-sector ATPase complex	73.64	ATP5PO,ATP5F1B,ATP5F1E,ATP5F1C,ATP5F1A,ATP5F1D
proton motive force-driven mitochondrial ATP synthesis	62.53	ATP5PO,ATP5F1B,ATP5F1E,ATP5F1C,ATP5F1A,ATP5F1D
proton motive force-driven ATP synthesis	55.23	ATP5PO,ATP5F1B,ATP5F1E,ATP5F1C,ATP5F1A,ATP5F1D
ATP biosynthetic process	47.34	ATP5PO,ATP5F1B,ATP5F1E,ATP5F1C,ATP5F1A,ATP5F1D
oxidative phosphorylation	39.05	SLC25A51,ATP5PO,ATP5F1B,ATP5F1E,ATP5F1C,ATP5F1A,ATP5F1D
aerobic respiration	31.34	SLC25A51,ATP5PO,ATP5F1B,ATP5F1E,ATP5F1C,ATP5F1A,ATP5F1D,MDH1
inner mitochondrial membrane protein complex	29.29	ATP5PO,ATP5F1B,ATP5F1E,ATP5F1C,ATP5F1A,ATP5F1D,MICOS10
ligase activity	27.79	ATP5PO,ATP5F1B,ATP5F1E,ATP5F1C,ATP5F1A,ACSL3,ATP5F1D,LARS2
cellular respiration	26.15	SLC25A51,ATP5PO,ATP5F1B,ATP5F1E,ATP5F1C,ATP5F1A,ATP5F1D,MDH1
ribose phosphate biosynthetic process	22.43	ATP5PO,ATP5F1B,PRPS1,ATP5F1E,ATP5F1C,ATP5F1A,ACSL3,ATP5F1D
purine nucleotide biosynthetic process	20.84	ATP5PO,ATP5F1B,PRPS1,ATP5F1E,ATP5F1C,ATP5F1A,ACSL3,ATP5F1D
purine-containing compound biosynthetic process	19.99	ATP5PO,ATP5F1B,PRPS1,ATP5F1E,ATP5F1C,ATP5F1A,ACSL3,ATP5F1D

QNZ 0.01μM R05 exp241

Mechanism of Action

Technical Notes

Compound References

Compound Supplier

Compound Characterization

Dose Response Curve

Screen Summary

Screen Results