2. Apoptosis
  3. Bcl-2 Family Caspase Apoptosis
  4. Mcl-1-IN-16

Mcl-1-IN-16 是一种有效的大环髓细胞白血病基因 1 (Mcl-1) 抑制剂，其 Ki 低于 0.08 nM。Mcl-1-IN-16 与其他抗凋亡 Bcl-2 家族成员 Bcl-2 和 Bcl-xL 相比，对 Mcl-1 具有更高的选择性 (> 50,000 倍)。Mcl-1-IN-16 可激活 caspase-3/7，从而启动细胞凋亡 (apoptosis)。Mcl-1-IN-16 在肺癌来源的肿瘤异种移植小鼠模型中实现了肿瘤消退。Mcl-1-IN-16 可用于实体瘤，如非小细胞肺癌 (NSCLC) 的研究。

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Mcl-1-IN-16

Mcl-1-IN-16 Chemical Structure

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Mcl-1-IN-16 相关抗体

Top Publications Citing Use of Products

查看 Bcl-2 Family 亚型特异性产品:

查看所有亚型
Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3

查看 Caspase 亚型特异性产品:

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Mcl-1-IN-16 is an effective macrocyclic myeloid cell leukemia 1 (Mcl-1) inhibitor with a Ki of below 0.08 nM. Mcl-1-IN-16 maintains high selectivity (>50,000-fold) for Mcl-1 over other antiapoptotic Bcl-2 family members Bcl-2 and Bcl-xL. Mcl-1-IN-16 leads to the activation of caspase-3/7, thereby initiating cell apoptosis. Mcl-1-IN-16 achieves tumor regression in a lung cancer-derived tumor xenograft mice model. Mcl-1-IN-16 can be used in the research of solid tumor such as nonsmall cell lung cancer (NSCLC)[1].

IC50 & Target[1]

Mcl-1

< 0.08 nM (Ki)

Caspase-3

8.8 nM (EC50)

Caspase-7

11 nM (EC50)

体外研究
(In Vitro)

Mcl-1-IN-16 (Compound 13) 抑制细胞增殖，对 H929 和 A427 细胞的 GI50 值分别为 14 和 25 nM，对 K562 细胞无抑制作用[1]。
Mcl-1-IN-16 (4 h) 可激活 H929 和 A427 细胞中的 Caspase 3/7，EC50 分别为 8.8 和 11 nM[1]。

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

Mcl-1-IN-16 相关抗体:
体内研究
(In Vivo)

Mcl-1-IN-16 (Compound 13) (30-60 mg/kg，静脉注射，每 14 天一次，共 28 天) 作为单一试剂在 NSCLC A427 衍生的异种移植小鼠模型中诱导肿瘤消退[1]。

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

Animal Model: A427 cell line-derived NSCLC xenograft model established in Balb/c nude, female mice[1]
Dosage: 30 and 60 mg/kg
Administration: Intravenous injection (i.v.), once every 14 days for 28 days
Result: Achieved complete tumor regression at 60 mg/kg, with the therapeutic effect lasting for 50 days after administration.
No weight loss or clinical signs of toxicity.
分子量

800.73

Formula

C42H43Cl2N5O7
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

Mcl-1-IN-16 相关分类

  • 摩尔计算器

  • 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.

Keywords:

Mcl-1-IN-16Bcl-2 FamilyCaspaseApoptosisH929 cellsA427 cellssolid tumornonsmall cell lung cancermice modelInhibitorinhibitorinhibit

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