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

ClpP activator-2 (Compound GU18) 是一种 ClpP 激活剂，对 HsClpP 的 Kd 为 5.01 μM。ClpP activator-2 可增强 HsClpP 的蛋白水解活性，促进 HsClpP 对 α-casein 的降解，其 EC50 为 1.09 μM。ClpP activator-2 可诱导线粒体活性氧 (ROS) 的积累，引发线粒体结构与功能损伤。ClpP activator-2 具有显著的体内抗多发性骨髓瘤活性。

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ClpP activator-2

ClpP activator-2 Chemical Structure

CAS No. : 3036751-71-7

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ClpP 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

ClpP activator-2 (Compound GU18) is a ClpP activator with a Kd of 5.01 μM for HsClpP. ClpP activator-2 enhances the proteolytic activity of HsClpP and promotes the degradation of α-casein by HsClpP, with an EC50 of 1.09 μM. ClpP activator-2 induces the accumulation of mitochondrial reactive oxygen species (ROS), leading to damage to mitochondrial structure and function. ClpP activator-2 exhibits significant in vivo anti-multiple myeloma activity[1].

体外研究
(In Vitro)

ClpP activator-2 强效激活纯化的 HsClpP，其 EC50 为 0.54 ± 0.12 μM[1]。
ClpP activator-2 (2 h) 可促进 HsClpP 对 α-casein 的降解，其 EC50 为 1.09 ± 0.08 μM[1]。
ClpP activator-2 可与纯化的 HsClpP 结合，通过 ITC 测得其解离常数 Kd 为 5.01 ± 1.05 μM[1]。
ClpP activator-2 (0.45 μM; 24 h) 可在 0.45 μM 处理 24 h 后对 AMO.1 MM 细胞造成显著的线粒体超微结构损伤[1]。
ClpP activator-2 (0.15-0.6 μM; 48 h) 可在处理 48 h 后，以浓度依赖的方式促进 AMO.1 和 ARP1 多发性骨髓瘤 (MM) 细胞中线粒体活性氧 (ROS) 的积累[1]。

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

ClpP activator-2 相关抗体:

Cell Viability Assay[1]

Cell Line: Human multiple myeloma cell lines AMO.1, ARP1
Concentration: Gradient concentrations
Incubation Time: 24 h, 48 h, 72 h
Result: Reduced cell viability in a time- and concentration-dependent manner.
For AMO.1 cells, reached IC50 values of 1.30 ± 0.08 μM (24 h), 0.68 ± 0.03 μM (48 h), and 0.08 ± 0.01 μM (72 h).
For ARP1 cells, reached IC50 values of 1.81 ± 0.14 μM (24 h), 0.86 ± 0.08 μM (48 h), and 0.21 ± 0.02 μM (72 h).

Cell Cycle Analysis[1]

Cell Line: Human multiple myeloma cell lines AMO.1, ARP1
Concentration: 0.15-0.6 μM
Incubation Time: 24 h
Result: Induced dose-dependent G1 phase.

Apoptosis Analysis[1]

Cell Line: Human multiple myeloma cell lines AMO.1, ARP1
Concentration: 0.15-0.6 μM (apoptosis assay); 0.45 μM (Western blotting)
Incubation Time: 24 h, 48 h, 72 h (apoptosis assay); 48 h (Western blotting)
Result: Induced time- and concentration-dependent apoptosis, with 95% of AMO.1 cells and 73.8% of ARP1 cells apoptotic after 72 h of 0.6 μM treatment.
Upregulated cleaved caspase-3.
药代动力学
(Parmacokinetics)
Species Dose Route Cmax T1/2 Bioavailability
Rat[1] 5 mg/kg i.v. 16733.33 ng/mL 3.854 h 38.9 %
Rat[1] 10 mg/kg p.o. 6050 ng/mL 3.198 h /
体内研究
(In Vivo)

ClpP activator-2 (5-30 mg/kg；腹腔注射；隔日一次；14 天) 可剂量依赖性地抑制 NOD/SCID 小鼠体内多发性骨髓瘤的肿瘤生长[1]。

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

Animal Model: NOD/SCID (female, 6-8 weeks old, subcutaneous xenograft model)[1]
Dosage: 5 mg/kg; 15 mg/kg; 30 mg/kg
Administration: i.p.; every other day; 14 days
Result: Achieved 56.7% tumor volume inhibition at 5 mg/kg.
Achieved 83.4% tumor volume inhibition at 15 mg/kg.
Achieved 91.4% tumor volume inhibition at 30 mg/kg.
Showed no treatment-related damage to major organs in the 30 mg/kg group compared to controls.
分子量

483.31

Formula

C22H19Cl2F3N4O
CAS 号
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

ClpP 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:

ClpP activator-23036751-71-7ClpP activator2ClpP activator 2ClpPReactive Oxygen Species (ROS)Mitochondrial MetabolismCaseinolytic protease Pcaspase-3mitochondrial respiratory chain complexes I-Vmultiple myelomaAMO.1Homo sapiens caseinolytic protease PARP1apoptosisNOD/SCID miceHsClpPmitochondrial dysfunctionInhibitorinhibitorinhibit

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