1. PI3K/Akt/mTOR
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  3. Anticancer agent 308

Anticancer agent 308 (compound 3s) is an AKT inhibitor with antitumor activity. Anticancer agent 308 reduces total AKT protein levels, thereby inhibiting the pro-survival PI3K/AKT signaling pathway. Anticancer agent 308 induces apoptosis, disrupts mitochondrial membrane potential, promotes reactive oxygen species (ROS) accumulation in mitochondria, and induces cell cycle arrest. Anticancer agent 308 inhibits cancer cell migration. Anticancer agent 308 is applicable to research related to breast cancer, lung adenocarcinoma, cervical cancer, prostate cancer, and hepatocellular carcinoma.

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Anticancer agent 308

Anticancer agent 308 Chemical Structure

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Description

Anticancer agent 308 (compound 3s) is an AKT inhibitor with antitumor activity. Anticancer agent 308 reduces total AKT protein levels, thereby inhibiting the pro-survival PI3K/AKT signaling pathway. Anticancer agent 308 induces apoptosis, disrupts mitochondrial membrane potential, promotes reactive oxygen species (ROS) accumulation in mitochondria, and induces cell cycle arrest. Anticancer agent 308 inhibits cancer cell migration. Anticancer agent 308 is applicable to research related to breast cancer, lung adenocarcinoma, cervical cancer, prostate cancer, and hepatocellular carcinoma[1].

In Vitro

Anticancer agent 308 (compound 3s) (IC50 1.16-4.23 μM) potently inhibits viability of MCF-7, MDA-MB-231, MDA-MB-468, A549, HepG2, HeLa, and PC-3 cancer cells at low micromolar concentrations while sparing normal NKE cells (IC50 84.15 μM), resulting in high selectivity indices[1].
Anticancer agent 308 (compound 3s) induces dose-dependent cell death and reduces colony formation in MDA-MB-231 cells, while having minimal toxicity to NKE cells[1].
Anticancer agent 308 (compound 3s) (0.5-2 μM; 24 h) induces concentration-dependent caspase-3-mediated apoptosis in MDA-MB-231 cells, with 66.8% apoptosis observed at 2 μM for 24 h[1].
Anticancer agent 308 (compound 3s) (0.5-2 μM; 24 h) induces concentration-dependent activation of caspase-3/7 in MDA-MB-231 cells, reaching 4.16-fold activity at 2 μM for 24 h[1].
Anticancer agent 308 (compound 3s) (0.5-2 μM; 24 h) induces concentration-dependent G2/M phase cell cycle arrest and increases subG0 apoptotic cell accumulation in MDA-MB-231 cells, with 50.43% of cells in G2/M phase at 2 μM for 24 h[1].
Anticancer agent 308 (compound 3s) modulates expression and activation of apoptosis-related proteins (Bax, caspase-3, PARP) and suppresses AKT in MDA-MB-231 cells[1].
Anticancer agent 308 (compound 3s) (0.5-2 μM; 24 h) induces concentration-dependent accumulation of intracellular and mitochondrial ROS in MDA-MB-231 cells, with 3.78-fold intracellular ROS and 2.89-fold mitochondrial ROS at 2 μM for 24 h, and this effect is suppressed by NAC pre-treatment[1].
Anticancer agent 308 (compound 3s) (0.5-2 μM; 24 h) induces concentration-dependent cleavage of PARP in MDA-MB-231 cells, reaching 4.25-fold fluorescence intensity at 2 μM for 24 h[1].
Anticancer agent 308 (compound 3s) (0.5-2 μM; 24 h) induces concentration-dependent mitochondrial depolarization in MDA-MB-231 cells, with only 20.81% of cells retaining polarized mitochondria at 2 μM for 24 h[1].
Anticancer agent 308 (compound 3s) (0.5-2 μM; 24 h) inhibits MDA-MB-231 cell migration in a concentration-dependent manner, reducing wound closure to 41.2% and Transwell migration to 27.8% at 2 μM for 24 h[1].

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

Apoptosis Analysis[1]

Cell Line: MDA-MB-231
Concentration: 0.5 μM, 1 μM, 2 μM; 2 μM (co-treated with caspase-3 inhibitor)
Incubation Time: 24 h
Result: Induced overall apoptosis rates of 58.19% (0.5 μM), 58.35% (1 μM), and 66.8% (2 μM).
Reduced apoptosis to 13.12% when co-treated with 2 μM target reagent and a caspase-3 inhibitor.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231
Concentration: 0.5 μM, 1 μM, 2 μM
Incubation Time: 24 h
Result: Increased the proportion of cells in G2/M phase from 12.86% (control) to 19.39% (0.5 μM), 34.51 % (1 μM), and 50.43% (2 μM).
Decreased G1/S population from 70.66% (control) to 40.23% (0.5 μM), 30.11% (1 μM), and 20.19% (2 μM).
Increased subG0 apoptotic cell population from 1.23% (control) to 10.16 % (0.5 μM), 11.16% (1 μM), and 9.26% (2 μM).

Immunofluorescence[1]

Cell Line: MDA-MB-231
Concentration: 0.5 μM, 1 μM, 2 μM
Incubation Time: 24 h
Result: Increased cleaved PARP fluorescence intensity to 2.65-fold (0.5 μM), 3.44-fold (1 μM), and 4.25-fold (2 μM) relative to control (1.00).

Cell Migration Assay[1]

Cell Line: MDA-MB-231
Concentration: 0.5 μM, 1 μM, 2 μM
Incubation Time: 24 h
Result: Reduced wound closure to 92.3% (0.5 μM), 67.8 % (1 μM), and 41.2% (2 μM) relative to control.
Reduced Transwell migration to 72.7% (0.5 μM), 45.7% (1 μM), and 27.8% (2 μM) relative to control.
Molecular Weight

265.27

Formula

C15H11N3O2

SMILES

NC(C1=C(C2=CC=CC=C2)N=C3C=CC=CN3C1=O)=O

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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

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    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.

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Product Name:
Anticancer agent 308
Cat. No.:
HY-182003
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