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c-MYC/BCL2 ligand 1 iodide

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Catalog No. T211076

c-MYC/BCL2 ligand 1 iodide is a dual-target ligand that specifically interacts with the G-quadruplex (G4) regions of the c-MYC and Bcl-2 promoters, exhibiting Kd values of 0.90 μM for c-MYCG4 and 0.56 μM for Bcl-2G4. It works by binding to these G4-forming sequences to inhibit transcription of the c-MYC and Bcl-2 genes, leading to reduced protein expression. This compound effectively suppresses MCF-7 cell proliferation and migration, induces G1 phase cell cycle arrest, and triggers apoptosis. Additionally, it significantly hampers tumor growth in the 4T1 homogenous model with negligible toxicity. c-MYC/BCL2 ligand 1 iodide is applicable in breast cancer research.

c-MYC/BCL2 ligand 1 iodide

c-MYC/BCL2 ligand 1 iodide

😃Good
Catalog No. T211076
c-MYC/BCL2 ligand 1 iodide is a dual-target ligand that specifically interacts with the G-quadruplex (G4) regions of the c-MYC and Bcl-2 promoters, exhibiting Kd values of 0.90 μM for c-MYCG4 and 0.56 μM for Bcl-2G4. It works by binding to these G4-forming sequences to inhibit transcription of the c-MYC and Bcl-2 genes, leading to reduced protein expression. This compound effectively suppresses MCF-7 cell proliferation and migration, induces G1 phase cell cycle arrest, and triggers apoptosis. Additionally, it significantly hampers tumor growth in the 4T1 homogenous model with negligible toxicity. c-MYC/BCL2 ligand 1 iodide is applicable in breast cancer research.
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Product Introduction

Bioactivity
Description
c-MYC/BCL2 ligand 1 iodide is a dual-target ligand that specifically interacts with the G-quadruplex (G4) regions of the c-MYC and Bcl-2 promoters, exhibiting Kd values of 0.90 μM for c-MYCG4 and 0.56 μM for Bcl-2G4. It works by binding to these G4-forming sequences to inhibit transcription of the c-MYC and Bcl-2 genes, leading to reduced protein expression. This compound effectively suppresses MCF-7 cell proliferation and migration, induces G1 phase cell cycle arrest, and triggers apoptosis. Additionally, it significantly hampers tumor growth in the 4T1 homogenous model with negligible toxicity. c-MYC/BCL2 ligand 1 iodide is applicable in breast cancer research.
Targets&IC50
Bcl-2:0.56 μM (Kd)
In vitro
c-MYC/BCL2 ligand 1 iodide (Compound Z4) demonstrates an IC50 of 4.14 μM against 4T1 cells and 5.47 μM against MCF-7 cells. Treatment with c-MYC/BCL2 ligand 1 iodide (2.5-10 μM, 48 h) significantly reduces the expression levels of c-MYC and Bcl-2, inducing apoptosis in MCF-7 cells via a mitochondrial-dependent pathway. Additionally, c-MYC/BCL2 ligand 1 iodide (2.5-10 μM, 24-48 h) hinders cell migration in a dose-dependent manner and inhibits cell proliferation in MCF-7 cells by arresting the cell cycle at the G1 phase.
In vivo
c-MYC/BCL2 ligand 1 iodide (Compound Z4) (12 mg/kg; intraperitoneal injection; administered every other day for 21 days) demonstrated significant antitumor efficacy and good safety in a 4T1 breast cancer syngeneic mouse model (female BALB/c; 4-5 weeks old).
Chemical Properties
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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