MK2206 4μM R08 exp504

MK2206 4μM R08 exp504

Mechanism of Action

Inhibit Akt1, Akt2, Akt3

Class / Subclass 1: Signal Transduction / Kinase Inhibitor

Technical Notes

Protein References

PubChem Name: MK-2206 dihydrochloride
Synonyms: N/A
CAS #: 1032350-13-2
PubChem CID: 46930998
IUPAC: 8-[4-(1-aminocyclobutyl)phenyl]-9-phenyl-2H-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3-one;dihydrochloride
INCHI Name: InChI=1S/C25H21N5O.2ClH/c26-25(12-4-13-25)18-9-7-17(8-10-18)22-19(16-5-2-1-3-6-16)15-20-21(27-22)11-14-30-23(20)28-29-24(30)31;;/h1-3,5-11,14-15H,4,12-13,26H2,(H,29,31);2*1H
INCHI Key: HWUHTJIKQZZBRA-UHFFFAOYSA-N
Molecular Weight: 480.4
Canonical SMILES: C1CC(C1)(C2=CC=C(C=C2)C3=C(C=C4C(=N3)C=CN5C4=NNC5=O)C6=CC=CC=C6)N.Cl.Cl
Isomeric SMILES: N/A
Molecular Formula: C25H23Cl2N5O

Protein Supplier

Supplier Name: Med Chem Express
Catalog #: HY-10358
Lot #: 18916

Protein Characterization

HRMS (ESI-TOF) m/z: (M+H)+ Calcd for C25H21N5O 408.18189; found 408.18326

Dose Response Curve

Platform ID: MK2206
Min: -6.4318; Max: 99.5790

IC	Concentration (µM)
IC10	0.8020
IC20	1.5180
IC30	2.3200
IC40	3.2850
IC50	4.5190
IC60	6.2180
IC70	8.8030
IC80	13.4500
IC90	25.4700

Screen Summary

Round: 08
Dose: 4µM
Days of incubation: 8
Doublings: 1.4
Numbers of reads: 16015710

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
20/43	Scores	View	View	View	View	View

Gene	CRANKS Score	FDR
SLC5A3	-3.93	<0.01
FLVCR1	-3.74	<0.01
MYB	-3.15	0.05
TCF4	-3.07	<0.01
ARL1	-3.07	<0.01
CREBBP	-3.03	<0.01
MTF1	-3.00	<0.01
MSI2	-2.94	<0.01
CHKA	-2.93	<0.01
ZFY	-2.85	<0.01
NOP2	-2.72	0.15
BRD1	-2.65	0.01
VPS25	-2.65	0.31
ARHGAP5	-2.64	0.01
DERL2	-2.63	0.03
ATP6V0A2	-2.62	0.03
TFAP4	-2.54	0.03
TCF3	-2.53	0.08
XPO6	-2.52	0.03
NCAM2	-2.46	0.03
GPR107	-2.42	0.04
QRICH1	-2.41	0.04
PSTK	-2.34	0.05
YBX1	-2.27	0.07
CAMK2G	-2.24	0.08
IRF2BP2	-2.19	0.10
LMNB1	-2.18	0.10
ZMIZ1	-2.17	0.10
TPR	-2.17	0.15
ZC3HC1	-2.16	0.10
IPO9	2.74	<0.01
CDK8	2.81	<0.01
MEMO1	2.86	<0.01
CBLL1	2.87	<0.01
CMAS	2.95	<0.01
PTPMT1	2.98	0.01
ANKRD17	3.00	<0.01
PGM3	3.03	<0.01
PLEKHA2	3.08	<0.01
ZFC3H1	3.20	0.00
WBP4	3.30	0.00
CNOT2	3.43	0.00
DNAJC2	3.50	0.00
USF2	3.68	0.00
KPTN	3.78	0.00
ATP2B1	4.00	0.00
C12orf66	4.01	0.00
EIF4A1	4.10	0.00
SZT2	4.14	0.00
NANS	4.49	0.00
HSPA14	4.60	0.00
ITFG2	4.80	0.00
FAM122A	5.00	0.00
DEPDC5	6.01	0.00
PTEN	6.76	0.00
NPRL3	7.53	0.00
NPRL2	7.70	0.00
FOXO1	7.85	0.00
TSC1	8.24	0.00
TSC2	8.44	0.00

Screen	Correlation	Plot
WYE-354 6μM R02 exp90	0.07	View
Nicotine 3000μM R08 exp510	0.07	View
Rapamycin 10μM R00 exp30	0.057	View
Rapamycin 2μM plus Cyclosporin-A 3μM R07 exp307	0.054	View
Rapamycin 2μM R07 exp306	0.053	View
Rapamycin 1μM R00 exp29	0.052	View
Rapamycin 0.001μM R08 exp429	0.052	View
NN-Dimethylsphingosine 2.5μM R08 exp508	0.052	View
GSK626616 14μM R08 exp485	0.084	View
Dexamethasone 0.006 to 0.015μM on day4 R07 exp352	0.074	View
Azithromycin 100μM R08 exp452	0.073	View
Cannabidiol 20μM R08 exp466	0.071	View
EPZ-5676 30μM R05 exp233	0.07	View
Hippuristanol 0.12μM R08 exp488	0.068	View
∆-9-Tetrahydrocannabinol 30μM R08 exp445	0.067	View
BS-181 20μM R08 exp461	0.062	View
I-BRD9 4μM R07 exp365	0.059	View
Erlotinib 10μM R05 exp216	0.057	View
Ibrutinib 10μM R08 exp442	0.056	View
FTY720 3μM R08 exp483	0.055	View
All-trans-Retinoic-Acid 40μM R07 exp334	0.052	View
Hippuristanol 0.12μM R08 exp489 no dilution day6	0.051	View

GO Term	Fold Change	Genes
KICSTOR complex	552.30	ITFG2,KPTN
Seh1-associated complex	236.70	NPRL2,NPRL3,DEPDC5
negative regulation of TORC1 signaling	107.77	TSC2,TSC1,NPRL2,NPRL3,DEPDC5,ITFG2,SZT2,KPTN
cellular response to amino acid starvation	69.04	NPRL2,NPRL3,DEPDC5,ITFG2,SZT2,KPTN
negative regulation of TOR signaling	66.95	TSC2,TSC1,NPRL2,NPRL3,DEPDC5,ITFG2,SZT2,KPTN
response to amino acid starvation	64.98	NPRL2,NPRL3,DEPDC5,ITFG2,SZT2,KPTN
regulation of TORC1 signaling	51.38	TSC2,TSC1,NPRL2,NPRL3,DEPDC5,ITFG2,SZT2,KPTN
regulation of TOR signaling	32.73	TSC2,TSC1,NPRL2,NPRL3,DEPDC5,ITFG2,SZT2,KPTN
cellular response to starvation	29.07	TSC2,TSC1,FOXO1,NPRL2,NPRL3,DEPDC5,ITFG2,SZT2,KPTN
cellular response to nutrient levels	23.70	TSC2,TSC1,FOXO1,NPRL2,NPRL3,DEPDC5,ITFG2,SZT2,KPTN,USF2
response to starvation	23.67	TSC2,TSC1,FOXO1,NPRL2,NPRL3,DEPDC5,ITFG2,SZT2,KPTN
cellular response to extracellular stimulus	21.08	TSC2,TSC1,FOXO1,NPRL2,NPRL3,DEPDC5,ITFG2,SZT2,KPTN,USF2
cellular response to external stimulus	16.89	TSC2,TSC1,FOXO1,NPRL2,NPRL3,DEPDC5,ITFG2,SZT2,KPTN,USF2
response to nutrient levels	11.68	TSC2,TSC1,FOXO1,NPRL2,NPRL3,DEPDC5,ITFG2,SZT2,KPTN,USF2
response to extracellular stimulus	11.00	TSC2,TSC1,FOXO1,NPRL2,NPRL3,DEPDC5,ITFG2,SZT2,KPTN,USF2
negative regulation of intracellular signal transduction	10.79	TSC2,TSC1,FOXO1,NPRL2,NPRL3,PTEN,DEPDC5,ITFG2,SZT2,KPTN
lytic vacuole membrane	10.42	TSC2,TSC1,NPRL2,NPRL3,DEPDC5,ITFG2,SZT2,KPTN
lysosomal membrane	10.42	TSC2,TSC1,NPRL2,NPRL3,DEPDC5,ITFG2,SZT2,KPTN
vacuolar membrane	9.48	TSC2,TSC1,NPRL2,NPRL3,DEPDC5,ITFG2,SZT2,KPTN

Table of Contents

MK2206 4μM R08 exp504

Mechanism of Action

Technical Notes

Protein References

Protein Supplier

Protein Characterization

Dose Response Curve

Screen Summary

Screen Results