Inhibitor SourceBook™ Second Edition

Phosphorylation/Dephosphorylation
Akt (Protein Kinase B) Inhibitors
Product Cat. No. Comments Size Price
Akt Inhibitor 124005 [1L-6-Hydroxymethyl-chiro-inositol 2-(R)-2-O-methyl-3-O-octadecylcarbonate]
A phosphatidylinositol ether analog that potently and selectively inhibits Akt
(IC 50 = 5.0 mM). A weak inhibitor of phosphatidylinositol 3-kinase (IC 50 = 83 mM).
Akt Inhibitor II 124008 (SH-5)
A phosphatidylinositol analog that inhibits the activation of Akt and selected downstream
substrates without affecting the phosphorylation of PDK- and other downstream kinases.
Decreases phosphorylation of Akt without affecting the total Akt level.
Akt Inhibitor III 124009 (SH-6)
A phosphatidylinositol analog that inhibits the activation of Akt and selected downstream
substrates without affecting the phosphorylation of PDK- and other downstream kinases.
Decreases phosphorylation of Akt without affecting the total Akt level.
mg $ 3
mg $247
mg $247
Akt Inhibitor IV 124011 A cell-permeable inhibitor of Akt phosphorylation/activation that targets ATP-binding mg $95
site of a kinase upstream of Akt, but downstream of PI 3-kinase.
5 mg $335
N InSolution Akt
Inhibitor IV
124015 A 0 mM ( mg/ 63 ml) solution of Akt Inhibitor IV (Cat. No. 240 ) in DMSO. mg $95
N Akt Inhibitor V,
Triciribine
Technical Tips for use of Akt inhibitors
Our Akt inhibitors are classified into four groups based on their modes of action.
The first three groups of inhibitors interfere with the cellular activation of Akt and do not affect already activated Akt. These inhibitors should only be used on
cells (with the exception of Cat. No. 240 3, which is not cell-permeable) or in coupled kinase assays, involving non-activated Akt. The fourth group of inhibitors
is suitable for use in cell cultures, as well as in cell-free kinase assays, involving either activated or non-activated Akts.
Group I:
Phosphatidylinositol analogs
(Cat. Nos. 124005/124008/
124009)
These inhibitors compete with PIP 2
thereby preventing the generation
of PIP 3 . They also compete with PIP 3
binding to Akt. The phosphonate
analogs ( 24008/ 24009) display
improved metabolic stability over
the carbonate analog ( 24005).
124012 (Akt/PKB Signaling Inhibitor-2; API-2; NSC 154020; TCN)
Inhibits the cellular phosphorylation/activation of Akt /2/3 by targeting an Akt effector
molecule other than PI 3-K or PDK . Has shown efficacy in vivo.
N Akt Inhibitor VI, Akt-in 124013 (H-AVTDHPDRLWAWEKF-OH; TCL1 10-24 )
A 5-mer peptide that acts as a specific inhibitor of Akt. Shown to bind to Akt-PH
domain (K d ~ 8 mM) and interfere with the Akt-phosphoinositide interaction.
N Akt Inhibitor VII,
TAT-Akt-in
N Akt Inhibitor VIII,
Isozyme-Selective,
Akti- /2
N InSolution Akt
Inhibitor VIII, Isozyme-
Selective, Akti- /2
N Akt Inhibitor IX, API-
59CJ-OMe
Group II:
(Cat. Nos.124011/124012/
124015/124019/124020/
252740/476880)
These inhibitors target yet to be
identified signaling molecules,
other than PDK and PI 3-kinase.
Group III:
(Cat. Nos. 124013/124014)
These inibitors contain a TCL -
derived peptide inhibitor sequence,
which binds to the PH domain of
Akt and interferes with the Aktphosphoinositide
interaction.
124014 (H-YGRKKRRQRRR-AVTDHPDRLWAWEKF-OH; TAT-TCL1 10-24 )
A cell-permeable version of the Akt Inhibitor VI, Akt-in (Cat. No. 240 3) that directly
binds the Akt PH domain, preventing PI binding. Has shown efficacy in vivo.
124018 {Akti-1/2; 1,3-Dihydro-1-(1-((4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)
phenyl)methyl)-4-piperidinyl)-2H-benzimidazol-2-one}
A cell-permeable, potent and selective inhibitor of Akt /Akt2 kinase activity
(IC = 58 nM, 2 0 nM, and 2. 2 mM for Akt , Akt2, and Akt3, respectively. Inhibition is
50
PH (pleckstrin homology) domain-dependent.
124017 A 0 mM ( mg/ 8 ml) solution of Akt Inhibitor VIII, Isozyme-Selective, Akti- /2
(Cat. No. 240 8) in DMSO.
124019 A cell-permeable ellipticine compound that potently and selectively inhibits cell growth
and induces apoptosis in human endometrial cancer cells with elevated Akt levels.
Exhibits minimal effect on cells lacking Akt activity.
Group IV:
(Cat. Nos. 124017/124018)
This inhibition is pleckstrin homology
(PH) domain-dependent. Inhibition
is not seen in Akts lacking the PH
domain or closely related AGC
family kinases. This inhibitor has
the distinct advantage of directly
binding to either non-activated or
activated Akt, thereby inhibiting
both the activation of Akt and the
kinase activity of Akt.
mg $ 47
2 mg $ 42
2 mg $258
mg $ 34
mg $ 34
5 mg $ 85
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