2. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  3. Microtubule/Tubulin Apoptosis
  4. Antiproliferative agent-23

Antiproliferative agent-23 是一种微管去稳定剂 (MDA)，可有效干扰微管蛋白-微管系统。Antiproliferative agent-23 通过下调 Bcl-2 蛋白、上调 Bax 和 Cyt c 蛋白并激活半胱天冬酶级联反应，以及线粒体依赖性途径诱导细胞凋亡。Antiproliferative agent-23 通过 PERK/ATF4/CHOP 信号通路在 A549/CDDP 细胞 (顺铂耐药癌细胞系) 中启动活性氧 (ROS) 介导的内质网应激。Antiproliferative agent-23 具有抗肿瘤活性。

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Antiproliferative agent-23 Chemical Structure

Antiproliferative agent-23 Chemical Structure

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Antiproliferative agent-23 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Antiproliferative agent-23 is a microtubule-destabilizing agent (MDA) and efficiently disturbes the tubulin-microtubule system. Antiproliferative agent-23 induces apoptosis via a mitochondrion-dependent pathway by downregulating the Bcl-2 protein, upregulating Bax and Cyt c proteins, and activating the caspase cascade. Antiproliferative agent-23 initiates reactive oxygen species (ROS)-mediated endoplasmic reticulum stress in A549/CDDP cells (cisplatin resistant cancer cell line) via the PERK/ATF4/CHOP signaling pathway. Antiproliferative agent-23 has anti-tumor activity[1].

体外研究
(In Vitro)

Antiproliferative agent-23 (72 小时) 对 HepG2 (IC50=0.86)、MDA-MB-231 (IC50=1.53)、MCF-7 (IC50=0.94)、A2780 (IC50=0.88)、A549 (IC50=0.23)、A549/CDDP (IC50=0.35)、HepG2/CDDP (IC50=1.16)、HUEVC (IC50=5.68) 具有抗增殖作用[1]。
Antiproliferative agent-23 (5 μM; 24 小时) 有效诱导 A549/CDDP 细胞凋亡[1]。
Antiproliferative agent-23 (5 μM; 24小时) 可以有效地引起 A549/CDDP 细胞的 DNA 损伤，从而最终引发细胞凋亡。Antiproliferative agent-23 导致 ER 应激相关蛋白表达显着增加[1]。
Antiproliferative agent-23 (10, 20 μM; 24 小时) 导致聚合抑制作用，ic50 为 9.86 μM[1]。
Antiproliferative agent-23 (5 μM; 24小时) 显着增加 A549/CDDP 细胞中的细胞内 ROS[1]。
Antiproliferative agent-23 (1 μM; 24 小时) 在体外试验中有效抑制 A549 细胞迁移[1]。

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

Antiproliferative agent-23 相关抗体:

Apoptosis Analysis[1]

Cell Line: CDDP-resistant non-small cell lung cancer cell line (A549/CDDP)
Concentration: 5 μM
Incubation Time: 24 hours
Result: Effectively induced cell apoptosis in A549/CDDP cells.

Western Blot Analysis[1]

Cell Line: CDDP-resistant non-small cell lung cancer cell line (A549/CDDP)
Concentration: 5 μM
Incubation Time: 24 hours
Result: Induced a high level of γ-H2AX.
Caused a significant increase in the ER stress-related protein (p-PERK, p-eIF2α, ATF 4, and CHOP) expression.
The level of Bcl-2 was downregulated.
体内研究
(In Vivo)

Antiproliferative agent-23 (12.40 mg/kg; 静脉给药; 每 7 天一次; 连续 28 天) 具有抗肿瘤功效并保持高抗肿瘤效率以减弱 CDDP 抗性[1]。

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

Animal Model: Male BALB/c nude mice (20 to 25 g) injected with A549/CDDP[1]
Dosage: 12.40 mg/kg
Administration: IV; every 7 days for 28 consecutive days
Result: The tumor growth inhibition (TGI) values significantly increased to 65.9%.
分子量

743.93

Formula

C23H28Cl3N3O6Pt
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

Antiproliferative agent-23 相关分类

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  • 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:

Antiproliferative agent-23Antiproliferative agent23Antiproliferative agent 23Microtubule/TubulinApoptosismicrotubule-destabilizing agentMDAtubulinmicrotubulemitochondrionBcl-2BaxCyt ccaspase cascadereactive oxygen speciesROSendoplasmic reticulum stressA549/CDDPPERKATF4CHOPanti-tumorInhibitorinhibitorinhibit

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