Phenformin 20μM R05 exp212

Inhibits mitochondrial respiratory chain complex I, indirectly activates AMPK

Class / Subclass 1: Organelle Function / Mitochondrial Inhibitor
Class / Subclass 2: Metabolism / Metabolic Enzyme Activator

Compound References

PubChem Name: Phenformin hydrochloride
Synonyms: Phenethylbiguanide hydrochloride
CAS #: 834-28-6
PubChem CID: 13266
IUPAC: 1-(diaminomethylidene)-2-(2-phenylethyl)guanidine;hydrochloride
INCHI Name: InChI=1S/C10H15N5.ClH/c11-9(12)15-10(13)14-7-6-8-4-2-1-3-5-8;/h1-5H,6-7H2,(H6,11,12,13,14,15);1H
INCHI Key: YSUCWSWKRIOILX-UHFFFAOYSA-N
Molecular Weight: 241.72
Canonical SMILES: C1=CC=C(C=C1)CCN=C(N)N=C(N)N.Cl
Isomeric SMILES: N/A
Molecular Formula: C10H16ClN5

Compound Supplier

Supplier Name: Sigma-Aldrich (Supelco)
Catalog #: P7045
Lot #: MKBV9127V

Compound Characterization

HRMS (ESI-TOF) m/z: (M+H)+ Calcd for C10H15N5 208.14493; found 208.14677

Dose Response Curve

Platform ID: PHENFORMINE
Min: -0.7796; Max: 41.1406

IC	Concentration (µM)
IC10	N/A
IC20	4.1494
IC30	21.8108
IC40	85.0051
IC50	N/A
IC60	N/A
IC70	N/A
IC80	N/A
IC90	N/A

Screen Summary

Round: 05
Dose: 20µM
Days of incubation: 8
Doublings: 3.5
Numbers of reads: 20548414

Sensitive/Resistant hits (FDR<0.05)	CRANKS	Score Plot	Top 30 Genes	Screen Similarity	Top 30 Sensitive GO terms	Top 30 Resistant GO terms
3/6	Scores	View	View	View	View	View

Gene	CRANKS Score	FDR
GOT1	-4.75	<0.01
SUCLG1	-3.13	<0.01
ENO1	-2.91	<0.01
LOC391322	-2.46	0.64
NUDT5	-2.41	0.30
CIC	-2.28	0.30
TBC1D3L	-2.27	0.56
TBC1D3K	-2.24	0.56
TBC1D3E	-2.22	0.56
TBC1D3I	-2.20	0.56
SMIM6	-2.17	0.40
UBE2N	-2.17	0.44
TAS2R60	-2.16	0.40
CCL16	-2.13	0.44
ZNF229	-2.10	0.44
SOD1	-2.07	0.54
NME6	-2.07	0.44
CD5L	-2.05	0.44
RAPH1	-2.03	0.46
PTEN	-2.02	0.44
NAGK	-2.01	0.46
ADK	-2.01	0.44
CMC2	-2.00	0.64
PDXK	-2.00	0.44
TMEM60	-2.00	0.46
GCDH	-2.00	0.46
RGCC	-2.00	0.44
SERPINA6	-1.99	0.44
KEAP1	-1.98	0.49
B4GALT5	-1.98	0.44
DNAJC24	2.19	0.10
IPMK	2.19	0.10
COX7B	2.20	0.10
C6orf203	2.21	0.10
ATP5F1	2.22	0.13
ZNF91	2.23	0.10
ITPK1	2.24	0.10
SCAP	2.24	0.13
RXFP2	2.25	0.10
COA6	2.26	0.10
NRBP1	2.26	0.15
NBPF12	2.27	0.52
ATP5C1	2.27	0.12
LARS2	2.32	0.10
PDS5B	2.33	0.10
MRPS25	2.34	0.19
MRPL33	2.36	0.18
DHX35	2.37	0.10
CAPRIN1	2.39	0.08
SERP2	2.43	0.08
ATP5A1	2.48	0.10
ATP5L	2.54	0.10
VARS2	2.56	0.08
TRMT61A	2.57	0.10
PMVK	2.58	0.05
G3BP1	2.62	0.05
ATP5B	2.69	0.04
ACSL3	2.72	0.05
SLC25A51	3.39	<0.01
PTPMT1	3.48	<0.01

Screen	Correlation	Plot
QNZ 0.01μM R08 exp439	0.105	View
QNZ 0.01μM R05 exp241	0.103	View
Rotenone 0.07μM R08 exp431	0.102	View
UM0131023 0.05μM R05 exp248	0.072	View
iCRT14 30μM R08 exp492	0.06	View
NMS-873 0.07μM R07 exp380	0.091	View
Chloramphenicol 20μM R00 exp13	0.09	View
Mubritinib 0.2μM R02 exp65	0.079	View
Amiloride 100μM R08 exp447	0.063	View
Phenformin 20μM R03 exp143	0.061	View
Mubritinib 0.2μM R01 exp48	0.059	View
Hypoxia 5%O2 R04 exp191	0.057	View
LLY-283 2.6μM R06 exp290	0.051	View

GO Term	Fold Change	Genes
proton-transporting ATP synthase activity, rotational mechanism	197.26	ATP5F1B,ATP5MG,ATP5F1A,ATP5F1C,ATP5PB
mitochondrial proton-transporting ATP synthase complex	184.11	ATP5F1B,ATP5MG,ATP5F1A,ATP5F1C,ATP5PB
proton-transporting ATP synthase complex	172.60	ATP5F1B,ATP5MG,ATP5F1A,ATP5F1C,ATP5PB
proton channel activity	125.53	ATP5F1B,ATP5MG,ATP5F1A,ATP5F1C,ATP5PB
oxidative phosphorylation	44.63	SLC25A51,ATP5F1B,ATP5MG,ATP5F1A,ATP5F1C,COA6,ATP5PB,COX7B
ligase activity	34.74	ACSL3,ATP5F1B,VARS2,ATP5MG,ATP5F1A,LARS2,ATP5F1C,ATP5PB,MTHFD1,ACSL4
aerobic respiration	31.34	SLC25A51,ATP5F1B,ATP5MG,ATP5F1A,ATP5F1C,COA6,ATP5PB,COX7B
cellular respiration	26.15	SLC25A51,ATP5F1B,ATP5MG,ATP5F1A,ATP5F1C,COA6,ATP5PB,COX7B
purine ribonucleotide biosynthetic process	25.25	ACSL3,ATP5F1B,ATP5MG,ATP5F1A,ATP5F1C,ATP5PB,MTHFD1,ACSL4
ribonucleotide biosynthetic process	23.26	ACSL3,ATP5F1B,ATP5MG,ATP5F1A,ATP5F1C,ATP5PB,MTHFD1,ACSL4
ribose phosphate biosynthetic process	22.43	ACSL3,ATP5F1B,ATP5MG,ATP5F1A,ATP5F1C,ATP5PB,MTHFD1,ACSL4
purine nucleotide biosynthetic process	20.84	ACSL3,ATP5F1B,ATP5MG,ATP5F1A,ATP5F1C,ATP5PB,MTHFD1,ACSL4
purine-containing compound biosynthetic process	19.99	ACSL3,ATP5F1B,ATP5MG,ATP5F1A,ATP5F1C,ATP5PB,MTHFD1,ACSL4
purine ribonucleotide metabolic process	15.53	ACSL3,ATP5F1B,PMVK,ATP5MG,ATP5F1A,ATP5F1C,ATP5PB,MTHFD1,ACSL4
ribonucleotide metabolic process	14.62	ACSL3,ATP5F1B,PMVK,ATP5MG,ATP5F1A,ATP5F1C,ATP5PB,MTHFD1,ACSL4
mitochondrial inner membrane	12.06	PTPMT1,SLC25A51,ATP5F1B,ATP5MG,ATP5F1A,MRPL33,MRPS25,ATP5F1C,ATP5PB,COX7B
organophosphate biosynthetic process	11.71	PTPMT1,ACSL3,ATP5F1B,PMVK,ATP5MG,ATP5F1A,ATP5F1C,ATP5PB,MTHFD1,ACSL4,IPMK
mitochondrial envelope	9.56	PTPMT1,SLC25A51,ACSL3,ATP5F1B,ATP5MG,ATP5F1A,MRPL33,MRPS25,ATP5F1C,COA6,ATP5PB,COX7B,ACSL4
mitochondrial membrane	9.40	PTPMT1,SLC25A51,ACSL3,ATP5F1B,ATP5MG,ATP5F1A,MRPL33,MRPS25,ATP5F1C,ATP5PB,COX7B,ACSL4

Phenformin 20μM R05 exp212

Mechanism of Action

Technical Notes

Compound References

Compound Supplier

Compound Characterization

Dose Response Curve

Screen Summary

Screen Results