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

c-MYC/BCL2 ligand 1 iodide 是一种靶向 c-MYCBcl-2 启动子区域 G-四链体 (G4) 的双靶点配体,其对 c-MYC G4Kd 值为 0.90 μM,对 Bcl-2 G4Kd 值为 0.56 μM。c-MYC/BCL2 ligand 1 iodide 通过与形成 G4 的序列结合来抑制 c-MYCBcl-2 基因的转录,并下调它们的蛋白质表达。c-MYC/BCL2 ligand 1 iodide 可抑制 MCF-7 细胞增殖、迁移,并诱导细胞周期 G1 期阻滞和凋亡 (apoptosis)。c-MYC/BCL2 ligand 1 iodide 在 4T1 同源模型中显著抑制肿瘤生长,且无明显毒性。c-MYC/BCL2 ligand 1 iodide 可以用于乳腺癌的研究。

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c-MYC/BCL2 ligand 1 iodide Chemical Structure

c-MYC/BCL2 ligand 1 iodide Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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 0.56 μM (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].

IC50 & Target[1]

Bcl-2

0.56 μM (Kd)

Caspase 9

 

体外研究
(In Vitro)

c-MYC/BCL2 ligand 1 iodide (Compound Z4) 对 4T1 细胞的 IC50 值为 4.14 μM,对 MCF-7 细胞的 IC50 值为 5.47 μM[1]

c-MYC/BCL2 ligand 1 iodide (2.5-10 μM, 48 h) 显著下调 c-MYCBcl-2 的表达水平,并通过线粒体依赖性凋亡途径诱导 MCF-7 细胞凋亡[1]

c-MYC/BCL2 ligand 1 iodide (2.5-10 μM, 24-48 h) 在 MCF-7 细胞中以剂量依赖的方式抑制细胞迁移,并通过将细胞周期阻滞在 G1 期来抑制细胞增殖[1]

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: 24-48 h
Result: Concentration dependently suppressed cell migration toward the scratch center, indicating its potent anti-migratory activity.
体内研究
(In Vivo)

c-MYC/BCL2 ligand 1 iodide (Compound Z4) (12 mg/kg;腹腔注射;隔天一次,持续21 天) 在 4T1 乳腺癌同源小鼠 (雌性BALB/c;4-5周) 模型中展现出显著的抗肿瘤疗效且安全性良好[1]

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.
分子量

712.72

Formula

C36H45IN2O3S

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    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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c-MYC/BCL2 ligand 1 iodide
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HY-174403
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