1. Metabolic Enzyme/Protease Apoptosis
  2. Phosphatase Apoptosis
  3. NSC 95397

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。

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NSC 95397 Chemical Structure

NSC 95397 Chemical Structure

CAS No. : 93718-83-3

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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))[1]. 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[2].

IC50 & Target

Ki: 32 nM (Cdc25A), 96 nM (Cdc25B), 40 nM (Cdc25C)[1]
IC50: 22.3 nM (human Cdc25A) , 56.9 nM (human Cdc25C), 125 nM (Cdc25B)[1]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
1.45 μM
Compound: NCS 95397
Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 28431339]
A549 IC50
13.1 μM
Compound: 4; NSC 95397
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
[PMID: 31563013]
HeLa IC50
10.8 μM
Compound: NSC-95397
Cytotoxicity against human HeLa cells after 6 days by WST1 colorimetric assay
Cytotoxicity against human HeLa cells after 6 days by WST1 colorimetric assay
[PMID: 18789703]
HeLa IC50
8.5 μM
Compound: NSC-95397
Antiproliferative activity against human HeLa cells after 10 days by clonogenic assay
Antiproliferative activity against human HeLa cells after 10 days by clonogenic assay
[PMID: 18789703]
HL-60 IC50
1 μM
Compound: 4; NSC 95397
Cytotoxicity against human HL60 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against human HL60 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
[PMID: 31563013]
Hs 683 IC50
2.8 μM
Compound: NCS 95397
Cytotoxicity against human Hs683 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human Hs683 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 28431339]
Jurkat IC50
3.7 μM
Compound: 4; NSC 95397
Cytotoxicity against human Jurkat cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against human Jurkat cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
[PMID: 31563013]
LS174T IC50
18.1 μM
Compound: 4; NSC 95397
Cytotoxicity against human LS174T cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against human LS174T cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
[PMID: 31563013]
MCF7 IC50
0.96 μM
Compound: NCS 95397
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 28431339]
MCF7 IC50
9.4 μM
Compound: 4; NSC 95397
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
[PMID: 31563013]
MONO-MAC-6 IC50
4.2 μM
Compound: 4; NSC 95397
Cytotoxicity against human MONO-MAC-6 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against human MONO-MAC-6 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
[PMID: 31563013]
PBMC IC50
7.8 μM
Compound: 4; NSC 95397
Cytotoxicity against human PBMC cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against human PBMC cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
[PMID: 31563013]
PC-3 IC50
3.4 μM
Compound: NCS 95397
Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 28431339]
SK-MEL-28 IC50
2.3 μM
Compound: NCS 95397
Cytotoxicity against human SK-MEL-28 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human SK-MEL-28 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 28431339]
SW982 IC50
7.9 μM
Compound: 4; NSC 95397
Cytotoxicity against human SW982 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against human SW982 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
[PMID: 31563013]
THP-1 IC50
1.4 μM
Compound: 4; NSC 95397
Cytotoxicity against human THP1 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against human THP1 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
[PMID: 31563013]
U-937 IC50
3.9 μM
Compound: 4; NSC 95397
Cytotoxicity against human U937 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against human U937 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
[PMID: 31563013]
体外研究
(In Vitro)

NSC 95397 (0, 10, and 20 μM; 24 hour) 以浓度依赖性方式降低三种结肠癌细胞系 SW480、SW620 和 DLD-1 的细胞活力[2]
NSC 95397(10 μM; 24 h) 在所有三种结肠癌细胞系 SW480、SW620 和 DLD-1 细胞中上调 p21,同时下调 CDK4CDK6[2]
NSC 95397 (10 μM;24 h) 降低 Ser795 和 Ser807/811 上视网膜母细胞瘤蛋白 (Rb) 的磷酸化[2]
NSC 95397 (20 μM;24 h) 显著增加裂解的 caspase-9、-3、-7 和 PARP 水平[2]
NSC 95397 (10 μM;6 h) 增强其下游 ERK1/2 在 Thr202/Tyr 204 处的磷酸化[2]

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

Cell Viability Assay[2]

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[2]

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
分子量

310.39

Formula

C14H14O4S2

CAS 号
性状

固体

颜色

Light yellow to orange

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
细胞实验: 

DMSO 中的溶解度 : ≥ 100 mg/mL (322.18 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" 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
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

动物实验:

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

  • 方案 一

    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); 澄清溶液

    此方案可获得 ≥ 10 mg/mL(饱和度未知)的澄清溶液。

    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;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    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); 澄清溶液

    此方案可获得 ≥ 10 mg/mL(饱和度未知)的澄清溶液。

    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。

    2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
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

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: ≥99.0%

参考文献

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 3.2218 mL 16.1088 mL 32.2175 mL 80.5438 mL
5 mM 0.6444 mL 3.2218 mL 6.4435 mL 16.1088 mL
10 mM 0.3222 mL 1.6109 mL 3.2218 mL 8.0544 mL
15 mM 0.2148 mL 1.0739 mL 2.1478 mL 5.3696 mL
20 mM 0.1611 mL 0.8054 mL 1.6109 mL 4.0272 mL
25 mM 0.1289 mL 0.6444 mL 1.2887 mL 3.2218 mL
30 mM 0.1074 mL 0.5370 mL 1.0739 mL 2.6848 mL
40 mM 0.0805 mL 0.4027 mL 0.8054 mL 2.0136 mL
50 mM 0.0644 mL 0.3222 mL 0.6444 mL 1.6109 mL
60 mM 0.0537 mL 0.2685 mL 0.5370 mL 1.3424 mL
80 mM 0.0403 mL 0.2014 mL 0.4027 mL 1.0068 mL
100 mM 0.0322 mL 0.1611 mL 0.3222 mL 0.8054 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.

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产品名称:
NSC 95397
目录号:
HY-108543
需求量: