Skip to Content
Merck

124018

Sigma-Aldrich

Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2

Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2, CAS 612847-09-3, is a cell-permeable, reversible inhibitor of Akt1/Akt2 (IC50 = 58 nM, 210 nM, & 2.12 µM for Akt1, Akt2, and Akt3, respectively).

Synonym(s):

Akt Inhibitor VIII, Isozyme-Selective, 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, Akti-1/2

Sign Into View Organizational & Contract Pricing

Select a Size

About This Item

Empirical Formula (Hill Notation):
C34H29N7O
CAS Number:
612847-09-3
Molecular Weight:
551.64
MDL number:
MFCD09026909
UNSPSC Code:
12352200
NACRES:
NA.28

Key Documents

View All Documentation
Technical Service
Need help? Our team of experienced scientists is here for you.
Let Us Assist
Technical Service
Need help? Our team of experienced scientists is here for you.
Let Us Assist

Quality Level

200

Assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

yellow

solubility

DMSO: 5 mg/mL

shipped in

ambient

storage temp.

2-8°C

SMILES string

N6(CCC(CC6)[n]7c8c(nc7O)cccc8)Cc1ccc(cc1)c2nc3c(nc2c5ccccc5)cc4[nH]cnc4c3

InChI

1S/C34H29N7O/c42-34-39-26-8-4-5-9-31(26)41(34)25-14-16-40(17-15-25)20-22-10-12-24(13-11-22)33-32(23-6-2-1-3-7-23)37-29-18-27-28(36-21-35-27)19-30(29)38-33/h1-13,18-19,21,25H,14-17,20H2,(H,35,36)(H,39,42)

InChI key

BIWGYFZAEWGBAL-UHFFFAOYSA-N

General description

A cell-permeable and reversible quinoxaline compound that potently and selectively inhibits Akt1/Akt2 activity (IC50 = 58 nM, 210 nM, and 2.12 µM for Akt1, Akt2, and Akt3, respectively, in in vitro kinase assays). The inhibition appears to be pleckstrin homology (PH) domain-dependent. It does not exhibit any inhibitory effect against PH domain-lacking Akts, or other closely related AGC family kinases, PKA, PKC, and SGK, even at concentrations as high as 50 µM. Overcomes Akt1/Akt2-mediated resistance to chemotherapeutics in tumor cells and is shown to block basal and stimulated phosphorylation/activation of Akt1/Akt2 both in cultured cells in vitro and in mice in vivo. A 10 mM (1 mg/181 µl) solution of Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 (Cat. No. 124017 ) in DMSO is also available.
A cell-permeable, reversible, potent, and selective inhibitor of Akt1/Akt2 activity (IC50 = 58 nM, 210 nM, and 2.12 µM for Akt1, Akt2, and Akt3, respectively, in in vitro kinase assays). The inhibition is reported to be pleckstrin homology (PH) domain-dependent. It does not exhibit any inhibitory effect against PH domain-lacking Akts, or other closely related AGC family kinases, PKA, PKC, and SGK, even at concentrations as high as 50 µM. Overcomes Akt1/Akt2-mediated resistance to chemotherapeutics in tumor cells and is shown to block basal and stimulated phosphorylation/activation of Akt1/Akt2 both in cultured cells in vitro and in mice in vivo.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Akt1, Akt2, Akt3
Product does not compete with ATP.
Reversible: yes
Target IC50: 58 nM, 210 nM, 2.12 µM against Akt1, Akt2, and Akt3, respectively, in in vitro kinase assays

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.

Other Notes

Calleja, V., et al. 2009. PLoS Biol.7, e17.
Logie, L., et al. 2007. Diabetes56, 228.
Barnett, S.F., et al. 2005. Biochem. J.385, 399.
DeFeo-Jones, D., et al. 2005. Mol. Cancer Ther.4, 271.
Zhao, Z., et al. 2005. Bioorg. Med. Chem. Lett.15, 905.
Lindsley, C.W., et al. 2005. Bioorg. Med. Chem. Lett.15, 761.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

Already Own This Product?

Find documentation for the products that you have recently purchased in the Document Library.

Visit the Document Library

Giacomo Della Verde et al.
Life science alliance, 5(3) (2021-12-15)
Fms-like tyrosine kinase 3 (Flt3) is a regulator of hematopoietic progenitor cells and a target of tyrosine kinase inhibitors. Flt3-targeting tyrosine kinase inhibitors can have cardiovascular side effects. Flt3 and its ligand (Flt3L) are expressed in the heart, but little
Chasity E Trammell et al.
PLoS pathogens, 18(4), e1010411-e1010411 (2022-04-05)
The recent global Zika epidemics have revealed the significant threat that mosquito-borne viruses pose. There are currently no effective vaccines or prophylactics to prevent Zika virus (ZIKV) infection. Limiting exposure to infected mosquitoes is the best way to reduce disease
Oh-Hoon Kwon et al.
Membranes, 11(12) (2021-12-24)
Like protein phosphorylation, O-GlcNAcylation is a common post-translational protein modification. We already reported that O-GlcNAcylation of amyloid precursor protein (APP) in response to insulin signaling reduces neurotoxic amyloid-β (Aβ) production via inhibition of APP endocytosis. Internalized APP is delivered to
Kiyomi Tsuji-Tamura et al.
Journal of cell science, 134(15) (2021-08-03)
Elongation of vascular endothelial cells (ECs) is an important process in angiogenesis; however, the molecular mechanisms remain unknown. The actin-crosslinking protein TAGLN (transgelin, also known as SM22 or SM22α) is abundantly expressed in smooth muscle cells (SMCs) and is widely
Danica Sims et al.
Cancers, 12(2) (2020-02-27)
Rhabdomyosarcoma is a highly aggressive malignant cancer that arises from skeletal muscle progenitor cells and is the third most common solid tumour in children. Despite significant advances, rhabdomyosarcoma still presents a therapeutic challenge, and while targeted therapy has shown promise
View All Related Papers

Related Content

Human Kinome & InhibitorSelect™ Libraries

Human Kinome Poster: The InhibitorSelect™ Protein Kinase Inhibitor Libraries provide broad coverage of the human kinome as shown here. The depicted human kinome dendrogram of 518 kinases are classified into five broad groups, 90 families, and 145 subfamilies. Inhibitor coverage was assigned based upon published data related to potency (IC50, EC50, Kd, etc.) for individual kinases harvested from the literature. Colored dots denote which library contains an inhibitor with demonstrated potent activity against the designated kinase and do not necessarily reflect known specificity of the inhibitor. Coverage of lipid and atypical kinases are depicted as a separate dendrogram. As shown, Calbiochem® Protein Kinase Inhibitor Libraries cover all major kinase families including TK, CMGC, CAMK, AGC, CK1, STE, TKL, as well as Lipid or Atypical kinase families.

Akt

Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.

Contact Technical Service