SCFSkp2-IN-2|cas:1375060-02-8|西域试剂

SCFSkp2-IN-2,99.44%

产品编号：Bellancom-148900| CAS NO：1375060-02-8| 分子式：C₁₇H₂₀N₄O₂| 分子量：312.37

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货号	价格	库存与货期
Bellancom-148900	￥500.00	杭州北京（现货）
Bellancom-148900	￥800.00	杭州北京（现货）
Bellancom-148900	￥1600.00	杭州北京（现货）
Bellancom-148900	￥2600.00	杭州北京（现货）
Bellancom-148900	￥4500.00	杭州北京（现货）

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SCFSkp2-IN-2

产品介绍

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

生物活性

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

体外研究

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。
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。
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。
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。
SCFSkp2-IN-2 (0.3 μM; 1-7 days) 诱导 NSCLC 细胞衰老。

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

Western Blot Analysis

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

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

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

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。

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

Animal Model:	A549 xenograft model
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.

体内研究

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。

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

Animal Model:	A549 xenograft model
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.

体内研究

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。

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

Animal Model:	A549 xenograft model
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (400.17 mM; ultrasonic and warming and heat to 60°C)

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
10 mM	0.3201 mL	1.6007 mL	3.2013 mL

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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式