Akti-1/2

Catalog No.S7776 Batch:S777602

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Technical Data

Formula

C34H29N7O
Molecular Weight 551.64 CAS No. 612847-09-3
Solubility (25°C)* In vitro DMSO 22 mg/mL (39.88 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Akti-1/2 (Akt Inhibitor VIII) is a highly selective Akt1/Akt2 inhibitor with IC50 of 58 nM/210 nM, respectively, about 36-fold selectivity for Akt1 over Akt3. Akti-1/2 induces apoptosis.
Targets
Akt1 [1]
(Cell-free assay)		 Akt2 [1]
(Cell-free assay)		 Akt3 [1]
(Cell-free assay)
58 nM 210 nM 2119 nM
In vitro

In a cell-based IPKA (C33A) assay, Akti-1/2 inhibits Akt1 and Akt2 with IC50 of 305 nM and 2086 nM, respectively. In HT29, MCF7, and A2780 cells, Akti-1/2 induces cell apoptosis by dramatically increasing caspase-3 activity. [1]

In liver cells, Akti-1/2 blocks regulation of PEPCK, G6Pase expression, and FOXO1 activity. [2]

Akti-1/2 also strongly potentiates PAR-1-mediated platelet aggregation by blocking PKB. [3]

In HCC827, NCI-H522, NCI-1651, and PC-9 cells, Akti-1/2 inhibits cell growth with IC50 of 4.7 μM, 7.25 μM, and 9.5 μM, when in combination, Akti-1/2 causes enhanced inhibition of cell growth and apoptosis. [4]
In vivo

In mice, Akti-1/2 (50 mg/kg, i.p.) inhibits basal and IGF-stimulated Akt1 and Akt2 phosphorylation in lung. [1]

Protocol (from reference)

Kinase Assay:

[2]
  • Kinase screen

    Briefly, all assays (25.5 μl at 21°C for 30 min) are performed using a Biomek 2000 Laboratory Automation Workstation in a 96-well format. Reactions contains 5–20 mU purified kinase along with substrate peptide or protein and are initiated by the addition of 10 mM MgAcetate and 5, 20, or 50 μM ATP ([γ-33P]-ATP, 800 cpm/pmol).
Cell Assay:

[4 ]
  • Cell lines

    HCC827, NCI-H522, NCI-1651, and PC-9 cells

  • Concentrations

    ~10 μM

  • Incubation Time

    96 h

  • Method

    The cell growth inhibitory effect of AKTi-1/2 is studied using the 96 h sulforhodamine B assay (SRB). Drug concentrations that inhibited 50% of cell growth (IC50) are calculated for each compound in GraphPad Prism 6.0 using non-linear regression analysis and sigmoidal dose–response (variable slope) equation.
Animal Study:

[5]
  • Animal Models

    C57BL/6 J mice

  • Dosages

    50 mg/kg

  • Administration

    i.p.

Customer Product Validation

Data from [Data independently produced by , , Biochem Biophys Res Commun, 2016, 480(3):334-340]

Data from [Data independently produced by , , Biochem Biophys Res Commun, 2016, 480(3):334-340.]

Selleck's Akti-1/2 has been cited by 25 publications

Combined inhibition of HER2 and VEGFR synergistically improves therapeutic efficacy via PI3K-AKT pathway in advanced ovarian cancer [ J Exp Clin Cancer Res, 2024, 43(1):56] PubMed: 38403634
Necrosulfonamide causes oxidation of PCM1 and impairs ciliogenesis and autophagy [ iScience, 2024, 27(4):109580] PubMed: 38600973
Jnk1 and downstream signalling hubs regulate anxiety-like behaviours in a zebrafish larvae phenotypic screen [ Sci Rep, 2024, 14(1):11174] PubMed: 38750129
P. gingivalis Infection Upregulates PD-L1 Expression on Dendritic Cells, Suppresses CD8+ T-cell Responses, and Aggravates Oral Cancer [ Cancer Immunol Res, 2023, 11(3):290-305] PubMed: 36633576
P. gingivalis Infection Upregulates PD-L1 Expression on Dendritic Cells, Suppresses CD8+ T-cell Responses, and Aggravates Oral Cancer [ Cancer Immunol Res, 2023, 11(3):290-305] PubMed: 36633576
AKT regulates IL-1β-induced proliferation and activation of hepatic stellate cells [ BIOCELL, 2023, 47(3): 669-676] PubMed: none
Colorectal Cancer Patient-Derived 2D and 3D Models Efficiently Recapitulate Inter- and Intratumoral Heterogeneity [ Adv Sci (Weinh), 2022, e2201539] PubMed: 35652270
PSMG2-controlled proteasome-autophagy balance mediates the tolerance for MEK-targeted therapy in triple-negative breast cancer [ Cell Rep Med, 2022, 3(9):100741] PubMed: 36099919
A hotspot mutation targeting the R-RAS2 GTPase acts as a potent oncogenic driver in a wide spectrum of tumors [ Cell Rep, 2022, 38(11):110522] PubMed: 35294890
Selective inhibition reveals the regulatory function of DYRK2 in protein synthesis and calcium entry [ Elife, 2022, 11e77696] PubMed: 35439114

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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