PI3K/AKT-IN-7
PI3K/AKT-IN-7 is a PI3K/Akt signaling pathway inhibitor with selective antiproliferative activity against hepatocellular carcinoma cells. PI3K/AKT-IN-7 downregulates the phosphorylation of PI3K and Akt and binds to NCF2 (Kd = 1.40 μM). PI3K/AKT-IN-7 induces apoptosis, S-phase cell cycle arrest, loss of mitochondrial membrane potential, and ROS accumulation, while inhibiting proliferation, migration, invasion, and DNA synthesis. PI3K/AKT-IN-7 inhibits tumor growth in a Hep3B xenograft BALB/c mouse model and reduces the expression of Ki67, PCNA, and MMP9. PI3K/AKT-IN-7 can be used for research on hepatocellular carcinoma.
For research use only. We do not sell to patients.
- Formula: C28H26O7
- Molecular Weight:474.50
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
PI3K |
Akt |
MMP-9 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
2.5 μM
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Cytotoxicity against human HeLa cells assessed as viability reduction incubated 48 hrs by CCK-8 assay.
Cytotoxicity against human HeLa cells assessed as viability reduction incubated 48 hrs by CCK-8 assay.
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42679701 |
| HepG2 | IC50 |
0.8 μM
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Antiproliferative activity against human Hep G2 cells assessed as viability reduction incubated 48 hrs by CCK-8 assay.
Antiproliferative activity against human Hep G2 cells assessed as viability reduction incubated 48 hrs by CCK-8 assay.
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42679701 |
| MDA-MB-231 | IC50 |
5.3 μM
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Antiproliferative activity against human MDA-MB-231 cells assessed as viability reduction incubated 48 hrs by CCK-8 assay.
Antiproliferative activity against human MDA-MB-231 cells assessed as viability reduction incubated 48 hrs by CCK-8 assay.
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42679701 |
| Hep 3B2 | IC50 |
3.6 μM
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Antiproliferative activity against human Hep 3B cells assessed as viability reduction incubated 48 hrs by CCK-8 assay.
Antiproliferative activity against human Hep 3B cells assessed as viability reduction incubated 48 hrs by CCK-8 assay.
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42679701 |
| AML12 | IC50 |
11.52 μM
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Cytotoxicity against mouse AML-12 cells assessed as viability reduction incubated 48 hrs by CCK-8 assay.
Cytotoxicity against mouse AML-12 cells assessed as viability reduction incubated 48 hrs by CCK-8 assay.
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42679701 |
In Vitro
PI3K/AKT-IN-7 (1.0-2.0 μM; 14 days) inhibits clonogenic survival of Hep G2 cells in a dose-dependent manner[1].
PI3K/AKT-IN-7 (1.0-2.0 μM; 48 h) inhibits Hep G2 cell migration[1].
PI3K/AKT-IN-7 (0.5-2.0 μM) modulates Bax/Bcl-2 expression in Hep G2 cells, shifting the balance toward apoptosis; it inhibits PI3K/Akt signaling in Hep G2 cells, reducing p-PI3K and p-Akt without altering total PI3K or Akt[1].
PI3K/AKT-IN-7 (48 h) alters the Hep G2 transcriptome, including NCF2 and PI3K/Akt-related pathways[1].
PI3K/AKT-IN-7 binds NCF2 in ITC with a reported Kd of 1.40 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Hep G2 cells
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Concentration:1.0 and 2.0 μM
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Incubation Time:14 days
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Result:Significantly inhibited colony formation in Hep G2 cells in a dose-dependent manner.
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Cell Line:Hep G2 cells
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Concentration:1.0 and 2.0 μM
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Incubation Time:48 h
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Result:Induced significant S-phase arrest after 48 h.
The S-phase proportion increased from 27.21% in the control to 57.97% at 2.0 μM.
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Cell Line:Hep G2 cells
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Concentration:1.0, and 2.0 μM
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Incubation Time:48 h
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Result:Increased the proportion of apoptotic cells from 6.12% at 0 μM to 29.65% at 1.0 μM and 52.95% at 2.0 μM.
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Cell Line:Hep G2 cells
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Concentration:1.0 and 2.0 μM
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Incubation Time:48 h
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Result:Inhibited Hep G2 cell migration in the wound-healing assay.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (female, 4-6 weeks old, a 100 μL suspension of Hep 3B cells containing 1 × 107 cells)[1]
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Dosage:15 mg/kg; 30 mg/kg
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Administration:i.p.; every 48 h; 14 days
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Result:Inhibited tumor growth in a dose-dependent manner and had no effect on mouse body weight.
Compared with control and Sorafenib (HY-10201), 30 mg/kg PI3K/AKT-IN-7 reduced tumor weight.
Immunohistochemical analysis showed reduced expression of Ki67, PCNA, and MMP9.
No organ damage or morphological abnormalities in major tissues.
- RNA extraction experimental
- Cell migration
- Liver Cancer Modeling
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Fluorescent plasma-membrane potential dye assay
- Mitochondrial membrane-potential and mitochondrial mass staining
- Apoptosis Solutions
- Cell invasion
- Western Blot
- Mitochondrial membrane-potential fluorescent assay
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- ROS/oxidative-stress fluorescent staining
- Patient-Derived Orthotopic Xenograft (PDOX)
- Protocol for Cell Cycle
- Cell Viability Determination by MTT Colorimetric Assay
- How to Choose the Right Model Animal
- Kinase activity and phosphorylation assays
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- PCNA Immunodetection Proliferation Assay
- Patient-Derived Xenograft (PDX)
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Protocol for Kinase activity and phosphorylation assays
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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Molecular Weight 474.50
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Formula C28H26O7
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SMILES
C/C=C/C1=CC([C@@H]([C@H]1OC(/C=C/C2=CC=C(C=C2)OC)=O)OC(/C=C/C3=CC=C(C=C3)OC)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PI3K/AKT-IN-7 Related Classifications
HY-189668 Related Classifications
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