1. PI3K/Akt/mTOR
  2. Akt


Cat. No.: HY-10425 Purity: 99.90%
Handling Instructions

A-443654 is a potent small-molecule inhibitor of all three Akt serine/threonine kinases, with Ki of 160 pM for Akt1.

For research use only. We do not sell to patients.
A-443654 Chemical Structure

A-443654 Chemical Structure

CAS No. : 552325-16-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 367 In-stock
1 mg USD 132 In-stock
5 mg USD 420 In-stock
10 mg USD 780 In-stock
50 mg   Get quote  
100 mg   Get quote  

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    A-443654 purchased from MCE. Usage Cited in: CNS Neurosci Ther. 2018 Jan 19.

    The MPP/PHTPP-and G15-induced decreases in p-AKT, AKT, and rictor expression are differently affected by mTORC2 activation with A-443654 in the adult female hippocampus.

    View All Akt Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References


    A-443654 is a potent small-molecule inhibitor of all three Akt serine/threonine kinases, with Ki of 160 pM for Akt1.

    IC50 & Target[1]


    160 pM (Ki)


    160 pM (Ki)


    160 pM (Ki)


    6.3 nM (Ki)


    11 nM (Ki)


    24 nM (Ki)


    24 nM (Ki)


    33 nM (Ki)


    41 nM (Ki)


    340 nM (Ki)


    1.2 μM (Ki)


    2.3 μM (Ki)


    2.4 μM (Ki)


    2.6 μM (Ki)


    3.1 μM (Ki)


    3.3 μM (Ki)


    3.6 μM (Ki)

    In Vitro

    A-443654 exhibits a Ki of 160 pM, a 30,000-fold improvement in potency versus the initial lead molecule. A-443654 is 40-fold selective for Akt over PKA. A-443654 inhibits Akt1, Akt2, or Akt3 equally within cells. A-443654 reduces the P-GSK3 in a dose-responsive manner in all three cell lines. A-443654 inhibits the proliferation of tumor cells with EC50 of 0.1 μM[1]. A-443654-induced morphological changes occur very rapidly (within 2 to 4 h) in both 10A and 10CA1a cells, with 10CA1a cells more sensitive to A-443654 than the 10A cells. A-443654 alone at 2 μM causes the 10CA1a cells, but not the 10A cells, to detach from the plate after 12 h, whereas 1 μM of A-443654 causes 10CA1a cells to detach from the plate after 12 h. FACScan Analysis of rapamycin and A-443654 effects on DNA content in 10A and 10CA1a cells. In contrast, A-443654 at 2 and 5 μM decreases Bcl-2 levels by 30 to 40% in the 10CA1a cells at 8h. The combination of rapamycin with 2 or 5 μM A-443654, however, markedly decreases Bcl-2 protein levels by appr 40 to 50% in the 10A cells and by appr 70% in the 10CA1a cells, respectively[2]. A-443654 demonstrates the greatest selective effect on the mutant cells compared to the WT cells with greater than 3.5 fold relative growth inhibition of the mutant cells[3].

    In Vivo

    A-443654 (7.5 mg/kg/d, s.c.) inhibits tumor growth in the 3T3-Akt1 flank tumor model. A-443654 (50 mg/kg, s.c.) induces apoptosis in 3T3-Akt1 flank tumors. A-443654 (30 mg/kg, s.c.) leads to increased levels of phosphorylated Akt1 in MiaPaCa-2 tumors[1].

    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 2.5159 mL 12.5796 mL 25.1591 mL
    5 mM 0.5032 mL 2.5159 mL 5.0318 mL
    10 mM 0.2516 mL 1.2580 mL 2.5159 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay

    The cells on 96-well plates are gently washed with 200 μL of PBS. Alamar Blue reagent is diluted 1:10 in normal growth media. The diluted Alamar Blue reagent (100 μL) is added to each well on the 96-well plates and incubated until the reaction is complete as per manufacturer's instructions. Analysis is done using an fmaxFluorescence Microplate Reader, set at the excitation wavelength of 544 nm and emission wavelength of 595 nm. Data are analyzed using SOFTmax PRO software provided by the manufacturer. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration

    A-443654 is given s.c. in a vehicle of 0.2% HPMC.

    Immunocompromised male scid mice are 6 to 8 weeks of age. The 3T3-Akt1 cell line is developed and characterized in our laboratory. The 1×106 3T3-Akt1 or 2×106 MiaPaCa-2 and PC-3 cells in 50% Matrigel are inoculated s.c. into the flank. For early treatment studies, mice are randomLy assigned to treatment groups and therapy is initiated the day after inoculation. Ten animals are assigned to each group, including controls. For established tumor studies, tumors are allowed to reach a designated size and mice are assigned to treatment groups of equal tumor size (n=10 mice per group). Tumor size is evaluated by twice weekly measurements with digital calipers. Tumor volume is estimated using the formula: V=L×W2/2. A-443654 is given s.c. in a vehicle of 0.2% HPMC. A-674563 is given orally in a vehicle of 5% dextrose. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Molecular Weight




    CAS No.



    N[[email protected]](COC1=CN=CC(C2=CC3=C(NN=C3C)C=C2)=C1)CC4=CNC5=CC=CC=C54

    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    A-443654 (A443654) is dissolved in DMSO and diluted with sterile saline solution before injection (40% DMSO+60% sterile saline solution)[4].

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.


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