NSC 95397
目录号 : KM4578 CAS No. : 93718-83-3 纯度 : 98%

NSC 95397 是一种有效选择性的 Cdc25 双特异性磷酸酶抑制剂 (Cdc25A、Cdc25B 以及 Cdc25C 的 Ki 值分别为 32、96、40 nM,人亚型 Cdc25A、人亚型 Cdc25C 以及 Cdc25B 的 IC50 值分别为 22.3、56.9、125 nM)。NSC 95397 抑制丝裂原活化蛋白激酶磷酸酶-1 (MKP-1),并通过 MKP-1 和 ERK1/2 途径抑制结肠癌细胞的增殖并诱导细胞凋亡。

规格 价格 是否有货 数量
5mg
In-stock
10mg
In-stock
25mg
In-stock
50mg
In-stock
100mg 询价 In-stock

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生物活性

NSC 95397 is a potent, selective Cdc25 dual specificity phosphatase inhibitor (Ki=32 nM (Cdc25A), 96 nM (Cdc25B), 40 nM (Cdc25C); IC50=22.3 nM (human Cdc25A), 56.9 nM (human Cdc25C), 125 nM (Cdc25B)). NSC 95397 inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) and suppresses proliferation and induces apoptosis in colon cancer cells through MKP-1 and ERK1/2 pathway.

体外研究

NSC 95397 (0, 10, and 20 µM; 24 hour) decreases the cell viability of three colon cancer cell lines SW480, SW620, and DLD-1 in a concentration-dependent manner.
NSC 95397(10 μM; 24 hour) upregulates p21 while downregulates CDK4 and CDK6 were d in all three colon cancer cell lines SW480, SW620, and DLD-1 cells.
NSC 95397 (10 μM; 24 hour) reduces the phosphorylation of retinoblastoma protein (Rb) on Ser795 and Ser807/811.
NSC 95397 (20 μM; 24 hours) significantly increases cleaved caspase-9, -3, -7 and PARP levels.
NSC 95397 (10 μM; 6 hours) enhances the phosphorylation of its downstream ERK1/2 at Thr202/Tyr 204.

Cell Viability Assay

Cell Line: Human colon cancer cell lines, SW480, SW620, and DLD-1
Concentration: 0, 10, and 20 µM
Incubation Time: 24 hours
Result: The IC50 values of NSC 95397 for the cell growth of SW480, SW620, and DLD-1 cells were 9.9, 14.1 and 18.6 μM, respectively.

Western Blot Analysis

Cell Line: SW480, SW620, and DLD-1 cells
Concentration: 10 μM
Incubation Time: 24 hours
Result: p21 was upregulated while CDK4 and CDK6 were downregulated.
Rduced the phosphorylation of Rb on Ser795 and Ser807/811
分子式
C14H14O4S2
分子量
310.39
CAS号
93718-83-3
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (322.18 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.2218 mL 16.1088 mL 32.2175 mL
5 mM 0.6444 mL 3.2218 mL 6.4435 mL
10 mM 0.3222 mL 1.6109 mL 3.2218 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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 10 mg/mL (32.22 mM); Clear solution

    此方案可获得 ≥ 10 mg/mL (32.22 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 100.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 10 mg/mL (32.22 mM); Clear solution

    此方案可获得 ≥ 10 mg/mL (32.22 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 100.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

科研文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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