2. PI3K/Akt/mTOR Apoptosis
  3. PI3K Akt Apoptosis
  4. PI3K/AKT-IN-1

PI3K/AKT-IN-1 is an effective PI3K/AKT dual inhibitor (IC50 of 6.99, 4.01 and 3.36 μM for PI3Kγ, PI3Kδ and AKT, respectively). PI3K/AKT-IN-1 has anticancer activity and acts by inhibiting PI3K/AKT axis and inducing caspase 3 dependent apoptosis.

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CAS No. : 3033069-84-7

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Based on 15 publication(s) in Google Scholar

PI3K/AKT-IN-1 Related Antibodies

Top Publications Citing Use of Products

    PI3K/AKT-IN-1 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 May 22;16(1):4779.  [Abstract]

    We treated primary hepatocytes with the PI3K/AKT specific inhibitor PI3K/AKT-IN-1 (10 μM) and found that the inhibitory effect of NNMT/1-MNA on FOXO1 and ANGPT2 was partially reduced.

    PI3K/AKT-IN-1 purchased from MedChemExpress. Usage Cited in: Gut Microbes. 2025 Dec;17(1):2449095.  [Abstract]

    Amino acid shortage model (AAS) for placental BeWo cells was established by mixing basic and amino acid-free DMEM/F12 medium (7:1), and supplemented with/without SCFAs cocktail and/or PI3K/AKT-IN-1 for 24 h. Relative gene expressions of inflammatory cytokines.

    PI3K/AKT-IN-1 purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Nov 7;11(1):511.  [Abstract]

    We performed Pxr overexpression in these cells by using the plasmid containing the full-length coding sequence of Mus musculus Nr1i2 (PNr1i2) or empty vector as negative control (PNC), and used PI3K/AKT-IN-1 (5 μM), a specific inhibitor of the PI3K/Akt pathway, to assess the pathway’s role in mediating Pxr function in BMSCs.

    PI3K/AKT-IN-1 purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Nov 7;11(1):511.  [Abstract]

    Pxr overexpression significantly enhanced PI3K/Akt pathway activity in aged BMSCs, while treatment with the inhibitor PI3K/AKT-IN-1 (5 μM) suppressed this Pxr overexpression-induced activation of the PI3K/Akt pathway.

    PI3K/AKT-IN-1 purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Nov 7;11(1):511.  [Abstract]

    The promotional effect of Pxr overexpression on osteogenesis in aged BMSCs was significantly weakened by the addition of PI3K/AKT-IN-1 (5 μM).

    PI3K/AKT-IN-1 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Apr;45(4):844-856.  [Abstract]

    Wound healing assay were used to evaluate cell motility, respectively, in PANC-1 cell lines treated with TGF-β1 (5 ng/ml, 24 h) and a MAPK1/ERK2-MAPK3/ERK1 inhibitor (U0126), MAPK/p38 inhibitor (SB203580), MAPK/JNK inhibitor (SP600125), PI3K/AKT-IN-1 (HY-144806), RAC1 inhibitor and CDC42 inhibitor.

    PI3K/AKT-IN-1 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Apr;45(4):844-856.  [Abstract]

    Transwell invasion were used to evaluate cell invasion, respectively, in PANC-1 cell lines treated with TGF-β1 (5 ng/ml, 24 h) and a MAPK1/ERK2-MAPK3/ERK1 inhibitor (U0126), MAPK/p38 inhibitor (SB203580), MAPK/JNK inhibitor (SP600125), PI3K/AKT-IN-1 (HY-144806), RAC1 inhibitor and CDC42 inhibitor.

    View All PI3K Isoform Specific Products:

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    PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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    Akt Akt1 Akt2 Akt3

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    Description

    PI3K/AKT-IN-1 is an effective PI3K/AKT dual inhibitor (IC50 of 6.99, 4.01 and 3.36 μM for PI3Kγ, PI3Kδ and AKT, respectively). PI3K/AKT-IN-1 has anticancer activity and acts by inhibiting PI3K/AKT axis and inducing caspase 3 dependent apoptosis[1].

    IC50 & Target[1]

    PI3Kγ

    6.99 μM (IC50)

    PI3Kδ

    4.01 μM (IC50)

    In Vitro

    PI3K/AKT-IN-1 (compound 7f) (0.04-100 µM; 48 hours) has high cytotoxic activity on both cell lines with better activity on leukaemia cell line (K562 IC50=2.62 µM) than on the breast cancer cell line (MCF-7 IC50=3.22 µM)[1].
    PI3K/AKT-IN-1 (2.62 µM) can promote S-phase cell cycle arrest and apoptosis induction in K562 cells[1].
    PI3K/AKT-IN-1 (2.62 µM; 48 hours) causes an increase in the percentage of Annexin-V positive apoptotic cells both in the early and late stage[1].
    PI3K/AKT-IN-1 (2.62 µM; 48 hours) markedly reduces the expression of PI3K, AKT, Cyclin D1 and NF-κB[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    PI3K/AKT-IN-1 Related Antibodies

    Cell Cytotoxicity Assay

    Cell Line: MCF-7 and K562 cells[1]
    Concentration: 0.04-100 µM
    Incubation Time: 48 hours
    Result: Demonstrated high cytotoxic activity on both cell lines with better activity on leukaemia cell line (K562 IC50=2.62 µM) than on the breast cancer cell line (MCF-7 IC50=3.22 µM).

    Cell Cycle Analysis

    Cell Line: K562 cells[1]
    Concentration: 2.62 µM
    Incubation Time:
    Result: Promoted S-phase cell cycle arrest and apoptosis induction.

    Apoptosis Analysis

    Cell Line: K562 cells[1]
    Concentration: 2.62 µM
    Incubation Time: 48 hours
    Result: Caused an increase in the percentage of Annexin-V positive apoptotic cells both in the early and late stage.

    Western Blot Analysis

    Cell Line: K562 cells[1]
    Concentration: 2.62 µM
    Incubation Time: 48 hours
    Result: Markedly reduced the expression of PI3K, p-PI3K, AKT, p-AKT, Cyclin D1 and NF-κB.
    In Vivo

    PI3K/AKT-IN-1 (2000 mg/kg; p.o.; single) is non-toxic and is well tolerated by experimental animals[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Female rats (180-200g)[1]
    Dosage: 2000 mg/kg
    Administration: p.o.; single
    Result: The median lethal dose (LD50) was greater than the test dose (2000 mg/kg).
    Molecular Weight

    465.52

    Formula

    C23H23N5O4S
    CAS No.
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

    N#CC1=C(N/N=C/C2=CC(OC)=C(OC)C(OC)=C2)N=C(SC)N=C1C3=CC=C(OC)C=C3
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (107.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1481 mL 10.7407 mL 21.4814 mL
    5 mM 0.4296 mL 2.1481 mL 4.2963 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    Working solution concentration: mg/mL
    Purity & Documentation
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.1481 mL 10.7407 mL 21.4814 mL 53.7034 mL
    5 mM 0.4296 mL 2.1481 mL 4.2963 mL 10.7407 mL
    10 mM 0.2148 mL 1.0741 mL 2.1481 mL 5.3703 mL
    15 mM 0.1432 mL 0.7160 mL 1.4321 mL 3.5802 mL
    20 mM 0.1074 mL 0.5370 mL 1.0741 mL 2.6852 mL
    25 mM 0.0859 mL 0.4296 mL 0.8593 mL 2.1481 mL
    30 mM 0.0716 mL 0.3580 mL 0.7160 mL 1.7901 mL
    40 mM 0.0537 mL 0.2685 mL 0.5370 mL 1.3426 mL
    50 mM 0.0430 mL 0.2148 mL 0.4296 mL 1.0741 mL
    60 mM 0.0358 mL 0.1790 mL 0.3580 mL 0.8951 mL
    80 mM 0.0269 mL 0.1343 mL 0.2685 mL 0.6713 mL
    100 mM 0.0215 mL 0.1074 mL 0.2148 mL 0.5370 mL
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    PI3K/AKT-IN-1 Related Classifications

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    PI3K/AKT-IN-13033069-84-7PI3KAktApoptosisPhosphoinositide 3-kinasePKBProtein kinase BPyrimidine-5-carbonitrileleukaemiaBreast cancerLeukaemia K562MCF-7PI3K/AKT pathwayDual inhibitorInhibitorinhibitorinhibit

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