P. Thr308. P. Ser473. PIP3. PIP2. PI3K. Growth Factors p85 p110. PIP3. AKT ... Description. SC 79. Activator of Akt. 740
PATHWAYS & KEY MOLECULAR TARGETS
PI3K-AKT Signaling Mechanism of Activation and Major Phosphorylation Sites of AKT1 Agonists
Cytokine Cytokine Receptor
Integrin
Growth Factor
GPCR
FAK
PI3K
PI3K
IRS-1
JAK1
ILK
Gab1 Gab2
α/β
PI3K
TO
SYK
Glut4
DEPTOR PRR5
Rictor
Sin1
PDK1
GBL GβL
Membrane Recruitment & Activation
PDK1
Glucose Import
PHLPP eNOS
PDK1 ACLY
Synthesis of Fatty Acids
GYS1
Glycogen Synthesis
S6
Translational Initiation
RPS6
mT OR
C1
PI3K
Raptor AKT
mTOR TSC2
DEPTOR
4EBP1
RAC, BTK, PDK1-SGK3 mTORC2-NFkB, mTORC2-cMyc
Glycolysis
PFKFB2
G βL
PDCD4
TSC1
PRAS40 MEK 1/2
DNA-PK FOXO1
Apoptosis
BCL2
Cell Survival
BIM Glycogen Synthase
Bax
Gene Transcription
AR
Wnt-β-catenin signaling
Caspase 9
BAD
Girdin
p21
GSK3B
14-3-3
Migration CREB
MDM2
Survival Genes
Cyclin D1
PP1
Wee
p27
MYT1
IKKa
IKB NFKB
IKB Degradation Cell Proliferation
NFAT
p53 Degradation
Cell Proliferation
CREB FKH2 p53
MDM2
NFKB
NFAT GATA4
Pathway Key Direct Activation
s cleu
Nu
m
las
op Cyt
Direct Inhibition
PI3K Independent AKT Activity Ack I, IKK epsilon, TBK1, Scr kinase, PTK6
Tumor Growth
X
AKT
AKT
Tumor Growth
X
PI3K
Small Molecule Inhibitors of AKT*
Cell proliferation
Survival signaling
Target Protein (s)
Inhibitor (s)
Cyclin D1 p21/Cip p27/Kip Myt1 Wee1
Bad MDM2/p53 FOXO1 Bcl-2 Bax
Akt (PKB)
Akti-1/2, API-1, API-2, 10-DEBC hydrochloride, FPA 124, GSK 690693, Perifosine, SC 66
Akt and PDK1
PHT 427
mTOR
Rapamycin, Torin 1, AZD 3147, eCF 309
Metabolism
Translational Control
GSK-3 PFKFB2 PIP5K AS160 TBC1D4 PDE3B Neuronal Function
S6 kinase RPS6 TSC1 mTOR PDCD4
PDK1
GSK 2334470, BX 795, OSU 03012
PIP3
PIT 1
PI3K
LY 294002, Wortmannin, PI 828
PI3K p110α
A66
PI3Kβ
AZD 6482
PI3K p110δ
PI 3065
Huntingtin Ataxin-1 GABAA receptor NFkB
TSC-mTORC1 FOXO1 GSK3β ACLY
PI3K γ
AS 605240
Immunity
Invasion/Migration
Others
Palladin Girdin Rac/GTP
WNK1 eNOS LMNA
Other molecules for AKT Signaling*
Multistep Activation Multistep Inhibition
Plasma Membrane
Ser473
Thr308
Thr308
PI3K-AKT Signaling: Processes & Targets*
Ras
Autophagy
XIAP
P
Organization of Nuclear Protein
LMNA
RAF1
ATG13
Regulatory domain
P
AKT Independent PI3K Activity
Cardiovascular Homeostasis
Huntingtin
P70S6K
AKT
Kinase domain
Linker
Glucose Transport
PIP5K AS160
14-3-3
PH domain
P
PIP3
PP2A
Neuroprotection
p110
LYN
P
PIP3 PIP3
PIP2
AKT1
Ser473
DNA-PK
SGK3
C2
mTOR
Membrane Recruitment & Activation
p85
PI3K
BCAP
PIP2
m
α/β
g
PI3K
R
PTEN
ATAXIN
PTEN
BCR
ml
PTEN
PIP3
AKT
GBP Gα-GTP PI3K
Paxillin
PIP2
Aggregation & Neurodegeneration
Growth Factors
mlg Gβγ
Synaptic Signaling
CD19 Ag
RTK GABAAR
mTORC2
Translocation Independant Activation
Small molecule
Description
SC 79
Activator of Akt
740 YP
Cell permeable activator of PI3K
Akt/SKG Substrate Peptide
Synthetic substrate of Akt/PKB
AKTide-2T
Peptide substrate for Akt/PKB
PI3K-AKT Signaling in Diseases Overgrowth syndromes, cancer (growth, angiogenesis and metastasis), cardiovascular diseases, glucose metabolism related disorders (insulin resistance and diabetes), autoimmune diseases and inflammation, and neurodegeneration related disorders. *Visit www.novusbio.com, www.rndsystems.com and www.tocris.com to learn more.
www.novusbio.com
PS-PM_AKT_23311