1. Apoptosis
  2. c-Myc
  3. MYC-IN-4

MYC-IN-4 是一种 MYC 抑制剂。MYC-IN-4 干扰 MYC/MAX 蛋白-蛋白相互作用 (IC50 = 3.06 μM)。MYC-IN-4 抑制 MYC 异常的 PC-3 前列腺癌细胞,其 IC50 为 0.440 μM。MYC-IN-4 在携带 Myc-CaP 前列腺肿瘤同种移植物的 FVB 小鼠中显示出强效的抗肿瘤疗效。MYC-IN-4 可用于前列腺癌研究。

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MYC-IN-4

MYC-IN-4 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MYC-IN-4 is a MYC inhibitor. MYC-IN-4 impairs MYC/MAX protein-protein interaction (IC50 = 3.06 μM). MYC-IN-4 inhibits MYC-aberrant PC-3 prostate cancer cells with an IC50 of 0.440 μM. MYC-IN-4 demonstrates potent antitumor efficacy in FVB mice bearing Myc-CaP prostate tumor allografts. MYC-IN-4 can be used for the study of prostate cancer[1].

体外研究
(In Vitro)

MYC-IN-4 (Compound 15) 对 PC-3 细胞(MYC 异常前列腺癌细胞)显示出强效的抗增殖活性,其 IC50 值为 0.440 μM[1]
MYC-IN-4 (68 h) 对其他 14 种肿瘤细胞系显示出广谱抗增殖活性,包括 MDA-MB-231、HCT-116、Myc-CaP、LN-CaP、NCI-H1581、A549、SK-N-BE、SK-OV-3、HepG-2、A-204、A-431、MG-63、LP-1 和 MV4-11 细胞,其 IC50 值范围为 0.331 μM 至 2.60 μM[1]
MYC-IN-4 (10 μM, 1 h) 通过 Co-IP 实验显著干扰 PC-3 细胞中的 MYC/MAX 蛋白-蛋白相互作用 (PPI)[1]
MYC-IN-4 (0.1-100 μM, 2 h) 在无细胞 AlphaLISA 实验中抑制 MYC/MAX PPI,其 IC50 值为 3.06 μM[1]
MYC-IN-4 (10 μM, 1 h) 降低 PC-3 细胞中内源性 MYC 的热稳定性[1]
MYC-IN-4 (1-10 μM, 24 h) 在 PC-3 细胞中诱导浓度依赖性的 MYC 降解[1]
MYC-IN-4 在转染 E-box 荧光素酶报告质粒的 HEK293T 细胞中抑制 MYC 转录活性,其 IC50 值为 0.739 μM[1]

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

体内研究
(In Vivo)

MYC-IN-4 (Compound 15) (10-50 mg/kg,腹腔注射, 每隔一天, 持续 16 天) 在携带 Myc-CaP 前列腺肿瘤同种移植物的 FVB 小鼠中显示出强效的抗肿瘤疗效[1]

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

Animal Model: Myc-CaP cells (1 × 106 in 100 µL total volume) were subcutaneously implanted into the right flanks of 6-week-old male FVB mice to establish MYC-driven prostate tumor allograft models [1]
Dosage: 10, 30, 50 mg/kg
Administration: i.p., QOD for 16 days
Result: Achieved tumor growth inhibition (TGI) rates of 57% and 70% at doses of 30 mg/kg and 50 mg/kg.
Showed no significant changes in body weight.
Reduced the Ki67 expression.
Combined with INCB086550 (HY-134884) increased the infiltration of CD8⁺ T cells and CD45⁺ leukocytes in the tumor microenvironment.
分子量

396.29

Formula

C19H10F6N2O

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
  • 摩尔计算器

  • 稀释计算器

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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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MYC-IN-4
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HY-178045
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