1. Apoptosis
  2. Bcl-2 Family c-Myc Apoptosis
  3. c-MYC/BCL2 ligand 1 iodide

c-MYC/BCL2 ligand 1 (iodide) is a dual-targeting c-MYC/Bcl-2 G4 ligand with Kd values of 0.90 μM (c-MYC G4) and 0.56μM (Bcl-2 G4). c-MYC/BCL2 ligand 1 (iodide) inhibits c-MYC and Bcl-2 gene transcription by binding to G4-forming sequences and downregulates their protein expression. c-MYC/BCL2 ligand 1 (iodide) inhibits suppresses migration, induces caspase-dependent apoptosis, and triggers cell cycle G1 arrest in MCF-7 cells. c-MYC/BCL2 ligand 1 (iodide) significantly suppresses tumor growth in a 4T1 syngeneic model with no observable toxicity. c-MYC/BCL2 ligand 1 (iodide) can be used for the research of breast Cancer[1].

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c-MYC/BCL2 ligand 1 iodide Chemical Structure

c-MYC/BCL2 ligand 1 iodide Chemical Structure

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Description

c-MYC/BCL2 ligand 1 (iodide) is a dual-targeting c-MYC/Bcl-2 G4 ligand with Kd values of 0.90 μM (c-MYC G4) and 0.56μM (Bcl-2 G4). c-MYC/BCL2 ligand 1 (iodide) inhibits c-MYC and Bcl-2 gene transcription by binding to G4-forming sequences and downregulates their protein expression. c-MYC/BCL2 ligand 1 (iodide) inhibits suppresses migration, induces caspase-dependent apoptosis, and triggers cell cycle G1 arrest in MCF-7 cells. c-MYC/BCL2 ligand 1 (iodide) significantly suppresses tumor growth in a 4T1 syngeneic model with no observable toxicity. c-MYC/BCL2 ligand 1 (iodide) can be used for the research of breast Cancer[1].

In Vitro

c-MYC/BCL2 ligand 1 (iodide) (Compound Z4) displays high potency with IC50 values of 4.14 μM (4T1 cells) and 5.47 μM (MCF-7 cells)[1].

c-MYC/BCL2 ligand 1 (iodide) (2.5-10 μM, 48 h) significantly downregulates the expression levels of c-MYC and Bcl-2, and induces cell death through the mitochondrial-dependent apoptotic pathway in MCF-7 cells[1].

c-MYC/BCL2 ligand 1 (iodide) (2.5-10 μM, 24 h) dependently impeds migration and inhibits proliferation by arresting the cell cycle at the G1 phase in MCF-7 cells[1].

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

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 2.5, 5, 10 μM
Incubation Time: 48 h
Result: Significantly downregulated c-MYC and Bcl-2 protein expression in a concentration-dependent manner.
Dose dependently elevated the expression of cleaved caspase-9.

Cell Migration Assay [1]

Cell Line: MCF-7 cells
Concentration: 2.5, 5, 10 μM
Incubation Time: 24 h
Result: Concentration dependently suppressed cell migration toward the scratch center, indicating its potent anti-migratory activity.
In Vivo

c-MYC/BCL2 ligand 1 (iodide) (Compound Z4) (12 mg/kg, i.p., every other day for 21 days) exerts considerable antitumor efficacy with a favorable safety in 4T1 breast cancer syngeneic mice (female, BALB/c, 4–5 weeks) models[1].

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

Animal Model: 4T1 breast cancer syngeneic mice (female BALB/c, 4-5 weeks) models[1]
Dosage: 12 mg/kg
Administration: Intraperitoneal injections, every other day for 21 days.
Result: Reduced tumor volume by 49.97 % compared to the PBS group.
Markedly reduced terminal tumor weights with a tumor growth inhibition (TGI) rate of 47.81%.
Exhibited marked cellular shrinkage and nuclear fragmentation (H&E staining), suggesting the possible presence of apoptosis.
Remained body weight stable and showed no remarkable histopathological abnormalities of major organs (heart, liver, spleen, lungs, and kidneys) via H&E staining.
Molecular Weight

712.72

Formula

C36H45IN2O3S

SMILES

CC[N+]1=C(/C=C/C2=CC=C(OCCNS(C3=C(C(C)C)C=C(C(C)C)C=C3C(C)C)(=O)=O)C=C2)C=CC4=CC=CC=C41.[I-]

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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:
c-MYC/BCL2 ligand 1 iodide
Cat. No.:
HY-174403
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