AICAR 240μM R05 exp211

AICAR 240μM R05 exp211

Mechanism of Action

Metabolic intermediate in purine biosynthesis, activates AMPK, has other putative targets

Class / Subclass 1: Metabolism / Metabolite
Class / Subclass 2: Signal Transduction / Kinase Activator

Technical Notes

Protein References

PubChem Name: Acadesine
Synonyms: Acadesine; AICA Riboside
CAS #: 2627-69-2
PubChem CID: 17513
IUPAC: 5-amino-1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]imidazole-4-carboxamide
INCHI Name: InChI=1S/C9H14N4O5/c10-7-4(8(11)17)12-2-13(7)9-6(16)5(15)3(1-14)18-9/h2-3,5-6,9,14-16H,1,10H2,(H2,11,17)/t3-,5-,6-,9-/m1/s1
INCHI Key: RTRQQBHATOEIAF-UUOKFMHZSA-N
Molecular Weight: 258.23
Canonical SMILES: C1=NC(=C(N1C2C(C(C(O2)CO)O)O)N)C(=O)N
Isomeric SMILES: C1=NC(=C(N1[C@H]2[C@@H]([C@@H]([C@H](O2)CO)O)O)N)C(=O)N
Molecular Formula: C9H14N4O5

Protein Supplier

Supplier Name: AK scientific
Catalog #: AMTNS043
Lot #: DM-079-143-2

Protein Characterization

LCMS: Tr 0.15 min, m/z 259+ [M+H]+, 257- [M-H]-

Dose Response Curve

Platform ID: AICAR
Min: -11.2747; Max: 24.1473

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

Screen Summary

Round: 05
Dose: 240µM
Days of incubation: 8
Doublings: 1.5
Numbers of reads: 17899422

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
1/115	Scores	View	View	View	View	View

Gene	CRANKS Score	FDR
UCK2	-4.28	<0.01
RPL30	-2.80	0.37
SKIV2L2	-2.70	0.39
UGDH	-2.68	0.06
NPRL2	-2.64	0.06
USP5	-2.63	0.10
CREBBP	-2.60	0.10
PPP1R18	-2.48	0.26
GNL3	-2.47	0.20
NUP133	-2.43	0.26
DNAH3	-2.41	0.19
SUPT3H	-2.40	0.10
TK1	-2.40	0.10
RPS13	-2.27	0.44
NIPBL	-2.27	0.26
TRIM44	-2.27	0.20
ZNF259	-2.26	0.20
HMGCS1	-2.21	0.28
YBX3	-2.21	0.25
DTYMK	-2.20	0.25
SRSF10	-2.19	0.29
UBE2D3	-2.19	0.20
TRIM66	-2.19	0.20
KRTAP4-8	-2.18	0.35
MIER3	-2.16	0.20
CHMP6	-2.16	0.26
F7	-2.15	0.20
COX7A2	-2.15	0.20
CMPK1	-2.15	0.20
LSM6	-2.14	0.30
LIAS	3.38	<0.01
ATIC	3.38	<0.01
MAPKAP1	3.38	<0.01
GUK1	3.41	<0.01
FDX1	3.42	<0.01
MARCH5	3.44	<0.01
MLX	3.49	<0.01
MLST8	3.53	<0.01
APAF1	3.61	<0.01
HEATR3	3.65	<0.01
TP53	3.95	<0.01
BAK1	3.97	<0.01
SLC25A51	4.28	<0.01
MTRR	4.37	<0.01
PRUNE	4.55	<0.01
MTHFD1L	4.89	<0.01
MTR	4.96	<0.01
DLD	4.99	<0.01
YLPM1	5.03	<0.01
SLC29A1	5.11	<0.01
SLC19A1	5.15	<0.01
ADSS	5.35	<0.01
MMACHC	5.43	<0.01
MTHFD2	5.45	<0.01
SHMT2	5.57	<0.01
SLC25A32	6.31	<0.01
IMPDH2	7.40	<0.01
AK2	8.09	<0.01
NUDT2	8.48	<0.01
ADK	8.50	<0.01

Screen	Correlation	Plot
Benzoate 20000μM R08 exp456	0.128	View
Aphidicolin 0.4μM R08 exp440	0.115	View
Actinomycin-D 0.001μM R00 exp3	0.111	View
MS023 7μM R03 exp135	0.109	View
Olaparib 4μM R08 exp512	0.104	View
Etoposide 0.3μM R05 exp199	0.101	View
Mitomycin-C 0.06μM R08 exp503	0.098	View
Atovaquone 15μM R08 exp451	0.097	View
MS023 2μM R03 exp134	0.094	View
RO-3307 4.7μM R02 exp80	0.091	View
THZ1 0.06μM R08 exp531	0.09	View
Doxorubicin 0.02μM R08 exp478	0.087	View
GSK626616 14μM R08 exp485	0.087	View
CI-1040 9.5μM R08 exp472	0.081	View
CR131-b 0.005μM R08 exp474	0.08	View
Bleomycin 5μM R08 exp459	0.079	View
Rotenone 20μM R00 exp34	0.078	View
UM131593 0.2μM R03 exp106	0.077	View
Artemisinin 50μM R08 exp450	0.076	View
Staurosporine 0.02μM R08 exp524	0.075	View
Nutlin-3A 1.6μM R06 exp294	0.074	View
Hippuristanol 0.12μM R08 exp488	0.073	View
Etoposide 1μM R00 exp19	0.071	View
PU-H71 1μM R08 exp515	0.071	View
Tanespimycin 14μM R08 exp527	0.07	View
ML-792 0.2μM R08 exp505	0.07	View
Hippuristanol 0.12μM R08 exp489 no dilution day6	0.068	View
Thimerosal 0.85μM R08 exp529	0.068	View
MLN-4924 0.2μM R00 exp21	0.066	View
JQ1 0.8μM R08 exp435	0.066	View
Ammonium tetrathiomolybdate 10μM R08 exp448	0.065	View
Deferoxamine 11μM R07 exp350	0.064	View
GSK-J4 1.5μM R08 exp441	0.063	View
SNS-032 15μM R08 exp443	0.062	View
Pimelic-diphenylamide-106 5μM R00 exp28	0.061	View
Diepoxybutane 3μM R07 exp354	0.061	View
Latrunculin-B 10μM R07 exp374	0.061	View
TRAIL 5ng/ml R00 exp35	0.06	View
Ethanol 0.01 R05 exp234	0.058	View
Dinaciclib 0.007μM R07 exp355	0.057	View
Hydroxyurea 100μM R07 exp329	0.057	View
LY2090314 0.003μM R08 exp500 no dilution day6	0.057	View
TRAIL 50ng/ml R00 exp36	0.054	View
UM0129480 7μM R02 exp85	0.053	View
LY2090314 0.003μM R08 exp499	0.052	View
Arsenate 40μM R06 exp264	0.052	View
CB-5083 0.4μM R08 exp468	0.051	View
Tozasertib 0.1μM R07 exp414	0.051	View
Rotenone 0.07μM R08 exp431	0.051	View
AICAR 240μM R03 exp116	0.209	View
5-Fluorouracil 20μM R00 exp2	0.114	View
6-Thio-2-deoxyguanosine 2μM R06 exp259	0.076	View
2-Deoxy-D-glucose 800μM R05 exp214	0.051	View

GO Term	Fold Change	Genes
thymidine metabolic process	285.69	TK1,DTYMK
nucleoside kinase activity	214.27	UCK2,TK1,CMPK1
pyrimidine nucleotide biosynthetic process	57.14	UCK2,DTYMK,CMPK1
pyrimidine-containing compound biosynthetic process	57.14	UCK2,TK1,DTYMK,CMPK1
nucleobase-containing compound kinase activity	55.74	UCK2,TK1,DTYMK,CMPK1

GO Term	Fold Change	Genes
tetrahydrofolate metabolic process	197.26	SHMT2,MTHFD2,MTR,MTHFD1L,ATIC
AMP biosynthetic process	184.11	ADK,NUDT2,ADSS2,ATIC
folic acid-containing compound metabolic process	154.65	SHMT2,MTHFD2,SLC19A1,MTR,MTHFD1L,MTRR,ATIC
purine ribonucleoside monophosphate biosynthetic process	153.43	ADK,NUDT2,IMPDH2,ADSS2,ATIC
pteridine-containing compound metabolic process	142.54	SLC25A32,SHMT2,MTHFD2,SLC19A1,MTR,MTHFD1L,MTRR,ATIC
purine nucleoside monophosphate biosynthetic process	138.08	ADK,NUDT2,IMPDH2,ADSS2,ATIC
purine ribonucleoside monophosphate metabolic process	96.66	ADK,NUDT2,AK2,IMPDH2,ADSS2,GUK1,ATIC
purine nucleoside monophosphate metabolic process	92.06	ADK,NUDT2,AK2,IMPDH2,ADSS2,GUK1,ATIC
ribonucleoside monophosphate biosynthetic process	81.23	ADK,NUDT2,IMPDH2,ADSS2,ATIC
water-soluble vitamin metabolic process	66.66	SLC25A32,SHMT2,MTHFD2,MMACHC,SLC19A1,MTR,MTRR
ribonucleoside monophosphate metabolic process	65.53	ADK,NUDT2,AK2,IMPDH2,ADSS2,GUK1,ATIC
nucleoside monophosphate metabolic process	50.87	ADK,NUDT2,AK2,IMPDH2,ADSS2,GUK1,ATIC
dicarboxylic acid metabolic process	50.21	SLC25A32,SHMT2,MTHFD2,ADSS2,SLC19A1,MTHFD1L,MTRR,ATIC
vitamin metabolic process	39.86	SLC25A32,SHMT2,MTHFD2,MMACHC,SLC19A1,MTR,MTRR
cellular modified amino acid metabolic process	38.76	SLC25A32,SHMT2,MTHFD2,SLC19A1,MTR,MTHFD1L,MTRR,ATIC
purine-containing compound biosynthetic process	22.49	ADK,NUDT2,AK2,IMPDH2,SHMT2,ADSS2,DLD,GUK1,ATIC
purine nucleotide biosynthetic process	20.84	ADK,NUDT2,AK2,IMPDH2,ADSS2,DLD,GUK1,ATIC
carboxylic acid metabolic process	8.21	SLC25A32,SHMT2,MTHFD2,ADSS2,SLC19A1,DLD,MTR,MTHFD1L,MTRR,TP53,ATIC,LIAS
oxoacid metabolic process	8.00	SLC25A32,SHMT2,MTHFD2,ADSS2,SLC19A1,DLD,MTR,MTHFD1L,MTRR,TP53,ATIC,LIAS

Table of Contents

AICAR 240μM R05 exp211

Mechanism of Action

Technical Notes

Protein References

Protein Supplier

Protein Characterization

Dose Response Curve

Screen Summary

Screen Results