2. Cell Cycle/DNA Damage Apoptosis Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  3. ClpP Apoptosis Reactive Oxygen Species (ROS)
  4. HsClpP activator-2

HsClpP activator-2 是一种口服活性的 HsClpP 激动剂，KD 为 40 nM。HsClpP activator-2 对小细胞肺癌 (SCLC) 细胞具有显著的抑制作用，包括 H69 (IC50 = 0.17 μM) 和 H82 (IC50 = 0.19 μM)。HsClpP activator-2 可破坏线粒体膜电位 (MMP)，并在 H82 细胞中诱导凋亡 (apoptosis) 和 ROS 产生。HsClpP activator-2 在 non-SMC 细胞异种移植瘤模型中显著抑制肿瘤生长。HsClpP activator-2 可用于小细胞肺癌 (SCLC) 的研究。

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HsClpP activator-2

HsClpP activator-2 Chemical Structure

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HsClpP activator-2 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HsClpP activator-2 is an orally active HsClpP agonist with a KD of 40 nM. HsClpP activator-2 potently inhibits SCLC cells including H69 (IC50 = 0.17 μM) and H82 (IC50 = 0.19 μM). HsClpP activator-2 disrupts mitochondrial membrane potential (MMP), as well as induces apoptosis and ROS in H82 cells. HsClpP activator-2 significantly inhibits tumor growth in non-SMC xenograft models with a tumor growth inhibition. HsClpP activator-2 can be used for the study of small cell lung carcinoma (SCLC)[1].

IC50 & Target[1]

HsClpP

40 nM (Kd)

体外研究
(In Vitro)

HsClpP activator-2 (Compound 8o) (0.02-10 μM, 72 h) 对 H69、H82 和非 SMC 细胞表现出显著的抗增殖活性，IC50 值分别为 0.17 μM、0.19 μM 和 0.1 μM[1].
HsClpP activator-2 (100-400 nM, 72 h) 在 H82 细胞中以剂量依赖方式诱导线粒体 OXPHOS 复合物蛋白 (NDUFB8、SDHB、UQCRC2、MTCO1、ATP5A) 的降解[1].
HsClpP activator-2 (100-400 nM, 72 h) 在 H82 细胞中以剂量依赖方式显著降低细胞内 ATP 水平并升高 ROS 水平[1].
HsClpP activator-2 (100-400 nM, 48-72 h) 在 H82 细胞中破坏线粒体膜电位 (MMP) 并诱导凋亡[1].
HsClpP activator-2 (100-400 nM, 24-48 h) 抑制非 SMC 细胞的克隆形成和迁移[1].

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

HsClpP activator-2 相关抗体:

Western Blot Analysis[1]

Cell Line: H82 cells
Concentration: 100, 200, 400 nM
Incubation Time: 72 h
Result: Induced dose-dependent degradation of mitochondrial OXPHOS complex proteins (NDUFB8, SDHB, UQCRC2, MTCO1, ATP5A) in H82 cells.
体内研究
(In Vivo)

HsClpP activator-2 (Compound 8o) (1.3-5 mg/kg，腹腔注射，每周两次，连续 20 天) 在携带 non-SMC 细胞异种移植瘤的雄性 BALB/c 裸鼠中表现出显著的抗肿瘤功效[1]。

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

Animal Model: Non-SMC cells (1×106 cells) were subcutaneously implanted into the flanks of 6-8-week-old male BALB/c nude mice (18-22 g)[1]
Dosage: 1.3, 2.5, 5 mg/kg
Administration: i.p., twice weekly, 20 days
Result: Achieved tumor growth inhibition (TGI) rates of 37.03%, 49.12%, and 60.44% for tumor weight, as well as 41.93%, 50.08%, and 63.01% for tumor volume at doses of 1.3, 2.5, and 5 mg/kg, respectively.
Showed no significant changes in body weight and no pathological damage in major organs (heart, liver, spleen, lung, kidney).
Reduced the Ki67 expression.
Increased the Caspase 3 expression in tumor.
分子量

505.53

Formula

C29H26F3N3O2
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

HsClpP activator-2 相关分类

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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:

HsClpP activator-2HsClpP activator2HsClpP activator 2ClpPApoptosisReactive Oxygen Species (ROS)Caseinolytic protease Psmall cell lung carcinoma (SCLC)H69H82HsClpPInhibitorinhibitorinhibit

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