2. Metabolic Enzyme/Protease
  3. E1/E2/E3 Enzyme
  4. SCFSkp2-IN-2

SCFSkp2-IN-2 (Compound AAA-237) 是一种 Skp2 抑制剂，其 KD 为 28.77 μM。AAA-237 诱导 NSCLC 细胞凋亡 (apoptosis)，显示出抗肿瘤活性。

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SCFSkp2-IN-2 Chemical Structure

SCFSkp2-IN-2 Chemical Structure

CAS No. : 1375060-02-8

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10 mM * 1 mL in DMSO ￥550
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Customer Review

SCFSkp2-IN-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

SCFSkp2-IN-2 (Compound AAA-237) is a Skp2 inhibitor with a KD of 28.77 μM. AAA-237 induces apoptosis of NSCLC cells and shows antitumor activities[1].

IC50 & Target

KD: 28.77 μM (Skp2)[1]
体外研究
(In Vitro)

SCFSkp2-IN-2 (Compound AAA-237) (0.3-3 μM; 24-72 h) 可直接与 Skp2 结合，导致 Skp2 被蛋白酶体降解。AAA-237 对 Skp2 mRNA 表达无显著影响，但对 NSCLC 细胞中 Skp2 蛋白表达有时间依赖性的抑制作用[1]。
SCFSkp2-IN-2 (0.3-3 μM; 24-72 h) 以剂量和时间依赖的方式抑制 A549 和 H1299 细胞的增殖[1]。
SCFSkp2-IN-2 (0.3-3 μM; 24-72 h) 通过调节 Skp2-Cip/Kip 和 PI3K/Akt-FOXO1 信号通路，在 G0/G1 检查点阻止细胞周期[1]。
SCFSkp2-IN-2 (0.3-3 μM; 24-72 h) 以剂量和时间依赖的方式诱导 A549 和 H1299 细胞凋亡[1]。
SCFSkp2-IN-2 (0.3 μM; 1-7 days) 诱导 NSCLC 细胞衰老[1]。

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

SCFSkp2-IN-2 相关抗体:

Western Blot Analysis[1]

Cell Line: A549 and H1299 cells
Concentration: 0.3, 1 and 3 μM
Incubation Time: 24, 48 and 72 h
Result: Increased the expression levels of p21Cip1 and p27Kip1. Decreased the level of Skp2.
Reduced the expression levels of CDK2, p-CDK2, cyclin E1, CDK4, p-CDK4 and cyclin D.
Increased the levels of cleaved PARP, cleaved caspase 3, cleaved caspase 9 and Bax. Decreased the expression of PARP and Bcl-2.

Cell Proliferation Assay[1]

Cell Line: A549 and H1299 cells
Concentration: 0.3, 1 and 3 μM
Incubation Time: 24, 48 and 72 h
Result: Inhibited the proliferation of A549 and H1299 cells in a dose- and time-dependent manner. The IC50 for A549 was 3 μM at 24 h, 2.5 μM at 48 h and 0.7 μM at 72 h. The IC50 for H1299 was 3.9 μM at 24 h, 1.8 μM at 48 h and 1.1 μM at 72 h.

Cell Cycle Analysis[1]

Cell Line: A549 and H1299 cells
Concentration: 0.3, 1 and 3 μM
Incubation Time: 24, 48 and 72 h
Result: Arrested the cell cycle at G0/G1 in a dose- and time-dependent manner.

Apoptosis Analysis[1]

Cell Line: A549 and H1299 cells
Concentration: 0.3, 1 and 3 μM
Incubation Time: 24, 48 and 72 h
Result: The ratio of JC-1 monomer/JC-1 polymer was increased in A549 and H1299 cells as the concentration was increased.
体内研究
(In Vivo)

SCFSkp2-IN-2 (Compound AAA-237) (15 or 45 mg/kg; i.p.; daily for 14 days) 在肺癌 A549 异种移植小鼠模型中显示出抗肿瘤活性[1]。

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

Animal Model: A549 xenograft model[1]
Dosage: 15 or 45 mg/kg
Administration: Intraperitoneal administration, daily for 14 days
Result: Significantly reduced tumor volume and weight. The tumor growth inhibition of the low dose and high dose was 55% and 64%, respectively. No obvious weight loss or abnormal behavior was observed. Reduced the expression of Ki67 in tumor tissue. Reduced the expression of Skp2 and Bcl-2 and increased the expression of p27, the cleaving of caspase 3, caspase 9, PARP and Bax.
分子量

312.37

Formula

C17H20N4O2
CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 125 mg/mL (400.17 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.2013 mL 16.0067 mL 32.0133 mL
5 mM 0.6403 mL 3.2013 mL 6.4027 mL
查看完整储备液配制表

* 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, 6 months; -20°C, 1 month。-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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

SCFSkp2-IN-2 相关分类

完整储备液配制表

* 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, 6 months; -20°C, 1 month。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2013 mL 16.0067 mL 32.0133 mL 80.0333 mL
5 mM 0.6403 mL 3.2013 mL 6.4027 mL 16.0067 mL
10 mM 0.3201 mL 1.6007 mL 3.2013 mL 8.0033 mL
15 mM 0.2134 mL 1.0671 mL 2.1342 mL 5.3356 mL
20 mM 0.1601 mL 0.8003 mL 1.6007 mL 4.0017 mL
25 mM 0.1281 mL 0.6403 mL 1.2805 mL 3.2013 mL
30 mM 0.1067 mL 0.5336 mL 1.0671 mL 2.6678 mL
40 mM 0.0800 mL 0.4002 mL 0.8003 mL 2.0008 mL
50 mM 0.0640 mL 0.3201 mL 0.6403 mL 1.6007 mL
60 mM 0.0534 mL 0.2668 mL 0.5336 mL 1.3339 mL
80 mM 0.0400 mL 0.2001 mL 0.4002 mL 1.0004 mL
100 mM 0.0320 mL 0.1601 mL 0.3201 mL 0.8003 mL
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:

SCFSkp2-IN-21375060-02-8E1/E2/E3 EnzymeE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseA549H1299NSCLCSkp2-Cip/KipPI3K/Akt-FOXO1CDK2CDK4Inhibitorinhibitorinhibit

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