Skp2 inhibitor 1
目录号 : GC69911Skp2 inhibitor 1(compound 14i) 是一种 Skp2 抑制剂，干扰 Skp2-Cks1 相互作用，IC50为 2.8 μM。Skp2 inhibitor 1 也具有抗癌活性。
Cas No.:2760612-63-1
Sample solution is provided at 25 µL, 10mM.
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Skp2 inhibitor 1 (compound 14i) is a potent and selective Skp2 inhibitor against the Skp2-Cks1 interaction with an IC50 of 2.8 μM. Skp inhibitor 1 exhibits anticancer activity[1].
Skp2 inhibitor 1 (2.8 μM，72 小时) 干扰 Skp2-Cks1 相互作用，对 PC-3 和 MGC-803 细胞的 IC50 值分别为 4.8 μM和 7.0 μM[1]。
Skp2 inhibitor 1 (10 μM，48 小时) 抑制 PC-3 和 MGC-803 细胞的增殖和迁移，诱导细胞在 S 期阻滞并促进细胞凋亡[1]。
Cell Viability Assay[1]
| Cell Line: | PC-3 , MGC-803 |
| Concentration: | 0-10 μM |
| Incubation Time: | 72 h |
| Result: | Against the Skp2-Cks1 interaction with an IC50 value of 2.8 μM, and against PC-3 and MGC-803 cells with IC50 values of 4.8 and 7.0 μM, respectively. |
Apoptosis Analysis[1]
| Cell Line: | PC-3 , MGC-803 |
| Concentration: | 2.5 μM , 5 μM , 10 μM |
| Incubation Time: | 0-48 h |
| Result: | Leaded to cell cycle S-phase arrest in a dose-dependent manner, and induced apoptosis in a dose-dependent manner, such as nuclear fragmentation, condensation, and cell shrinkage. |
Cell Proliferation Assay[1]
| Cell Line: | PC-3 , MGC-803 |
| Concentration: | 0.5 μM , 1 μM , 2 μM |
| Incubation Time: | 10 days |
| Result: | Inhibited colony-forming abilities in a dose-dependent manner. |
Cell Migration Assay [1]
| Cell Line: | PC-3 , MGC-803 |
| Concentration: | 2.5 μM , 5 μM , 10 μM |
| Incubation Time: | 48 h |
| Result: | Inhibited migration in a dose-dependent manner. |
Cell Invasion Assay[1]
| Cell Line: | PC-3 , MGC-803 |
| Concentration: | 0.5 μM , 1 μM , 2 μM |
| Incubation Time: | 48 h |
| Result: | Inhibited invasion in a dose-dependent manner. |
Western Blot Analysis[1]
| Cell Line: | PC-3 , MGC-803 |
| Concentration: | 2.5 μM , 5 μM , 10 μM |
| Incubation Time: | 0-48 h |
| Result: | Inhibited the protein levels of Skp2 in a dose-dependent manner, restored the expression of p21 and p27 in a time-dependent manner. |
Skp2 inhibitor 1 (10 mg/kg; 25 mg/kg, 50 mg/kg；腹腔注射/2天，21天) 在 NOD-SCID 小鼠异种移植模型中显著抑制肿瘤生长且没有明显毒性。此外，Skp2 inhibitor 1 (50mg/Kg/2天) 处理完全抑制肿瘤生长[1]。
Skp2 inhibitor 1通过抑制 Skp2 信号通路降低肿瘤恶性程度，并上调肿瘤组织中细胞凋亡的比例[1]。
| Animal Model: | The xenograft models of PC-3 and MGC-803 cells in NOD-SCID mice[1]. |
| Dosage: | 10 mg/kg; 25 mg/kg, 50 mg/kg |
| Administration: | Intraperitoneal injection (i.p.) |
| Result: | Inhibited tumor growth without obvious toxicity, the tumor growth inhibition ratio was 55.68, 71.86, and 90.42% with 10, 25, and 50 mg/Kg/2 day, respectively. |
[1]. Zhang K, et al. Discovery of Novel 1,3-Diphenylpyrazine Derivatives as Potent S-Phase Kinase-Associated Protein 2 (Skp2) Inhibitors for the Treatment of Cancer. J Med Chem. 2023 Jun 8;66(11):7221-7242.
| Cas No. | 2760612-63-1 | SDF | Download SDF |
| 分子式 | C23H23ClN4O | 分子量 | 406.91 |
| 溶解度 | DMSO : 50 mg/mL (122.88 mM; Need ultrasonic) | 储存条件 | 4°C, away from moisture and light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4575 mL | 12.2877 mL | 24.5755 mL |
| 5 mM | 0.4915 mL | 2.4575 mL | 4.9151 mL |
| 10 mM | 0.2458 mL | 1.2288 mL | 2.4575 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet