1. Apoptosis inducer 62

Apoptosis inducer 62 is an apoptosis inducer that reduces the expression levels of anti-apoptotic proteins Bcl-2 and Bcl-xL. Apoptosis inducer 62 induces ROS accumulation, mitochondrial membrane potential depolarization, DNA damage, cell cycle arrest. Apoptosis inducer 62 exhibits activity in colorectal tumor xenograft models. Apoptosis inducer 62 can be used for research related to colorectal cancer.

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Apoptosis inducer 62

Apoptosis inducer 62 Chemical Structure

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Description

Apoptosis inducer 62 is an apoptosis inducer that reduces the expression levels of anti-apoptotic proteins Bcl-2 and Bcl-xL. Apoptosis inducer 62 induces ROS accumulation, mitochondrial membrane potential depolarization, DNA damage, cell cycle arrest. Apoptosis inducer 62 exhibits activity in colorectal tumor xenograft models. Apoptosis inducer 62 can be used for research related to colorectal cancer[1].

IC50 & Target[1]

Bcl-xL

 

Bcl-2

 

In Vitro

Apoptosis inducer 62 (Compound 28a) (1 μM; 72 h) potently inhibits the proliferation of HCT116, MIA-PaCa-2, HepG-2 and HeLa cancer cells, with IC50 values of 0.34, 0.6, 0.71 and 0.77 μM[1].
Apoptosis inducer 62 (0.5-2 μM; 48 h) significantly increases intracellular ROS levels in HCT116 cells in a concentration-dependent manner in vitro[1].
Apoptosis inducer 62 (0.5-2 μM; 48 h) induces mitochondrial membrane potential depolarization in HCT116 cells in a concentration-dependent manner in vitro[1].
Apoptosis inducer 62 (0.5-2 μM; 48 h) significantly induces apoptosis in HCT116 cells in a concentration-dependent manner in vitro[1].
Apoptosis inducer 62 (0.5-2 μM; 48 h) induces S-phase cell cycle arrest in HCT116 cells in a concentration-dependent manner in vitro[1].
Apoptosis inducer 62 (0.25-1 μM; 24 h) regulates the expression of apoptosis-related proteins and DNA damage-related proteins (Bcl-xL, Bcl-2, Cyt c, γ-H2AX) in HCT116 cells, and promotes cell apoptosis and DNA damage[1].

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

Apoptosis Analysis[1]

Cell Line: HCT116 cells
Concentration: 0.5, 1 and 2 μM
Incubation Time: 48 h
Result: Significantly induced apoptosis in HCT116 cells in a concentration-dependent manner.

Cell Cycle Analysis[1]

Cell Line: HCT116 cells
Concentration: 0.5, 1 and 2 μM
Incubation Time: 48 h
Result: Significantly induced S-phase cell cycle arrest in HCT116 cells in a concentration-dependent manner.

Western Blot Analysis[1]

Cell Line: HCT116 cells
Concentration: 0.25, 0.5 and 1 μM
Incubation Time: 24 h
Result: Decreased Bcl-xL and Bcl-2.
Increased Cyt c and γ-H2AX.
In Vivo

Apoptosis inducer 62 (Compound 28a) (2 mg/kg; i.p.; daily; 14 days) exhibits potent in vivo antitumor efficacy in HCT116 colorectal cancer xenografts, with a 47.9% tumor growth inhibition rate, and no associated body weight loss[1].

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

Animal Model: BALB/c nude (female, 5 weeks old)[1]
Dosage: 2 mg/kg
Administration: i.p.; daily; 14 days
Result: Achieved a tumor growth inhibition rate (TGI) of 47.9%.
Significantly suppressed tumor volume and tumor weight compared to the control group.
Caused no obvious body weight loss during the 14-day treatment period.
Molecular Weight

593.72

Formula

C36H42F3NO3

SMILES

O=C1C=C2[C@]3(C)CC[C@@]4(C)[C@]5([H])C[C@@](C(N)=O)(CC6=CC=C(C(F)(F)F)C=C6)CC[C@]5(C)CC[C@]4(C)C3=CC=C2C(C)=C1O

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Room temperature in continental US; may vary elsewhere.

Storage

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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Apoptosis inducer 62
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HY-184302
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