1. Metabolic Enzyme/Protease NF-κB
  2. Quinone Reductase NF-κB
  3. ES 936

ES 936 是一种强效且特异性的 NQO1 抑制剂。ES 936 抑制 MIA PaCa-2 和 BxPC-3 细胞的生长,IC50 值分别为 108 nM 和 365 nM。ES936 显著抑制小鼠中 MIA PaCa-2 异种移植瘤的生长速率。ES 936 可用于胰腺癌研究。

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ES 936

ES 936 Chemical Structure

CAS No. : 192820-78-3

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查看 NF-κB 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ES 936 is a potent and specific NQO1 inhibitor. ES 936 inhibits the growth of MIA PaCa-2 and BxPC-3 cells, with IC50 values of 108 nM and 365 nM, respectively. ES936 significantly inhitbits the growth rate of MIA PaCa-2 xenograft tumors in mice. ES 936 can be used for the study of pancreatic cancer[1][2][3].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
MIA PaCa-2 IC50
508 nM
Compound: 1, ES936
Cytotoxicity against human MIA PaCa2 cells after 72 hrs by MTT assay
Cytotoxicity against human MIA PaCa2 cells after 72 hrs by MTT assay
[PMID: 17944451]
MIA PaCa-2 IC50
629 nM
Compound: 1, ES936
Cytotoxicity against human MIA PaCa2 cells after 4 hrs by MTT assay
Cytotoxicity against human MIA PaCa2 cells after 4 hrs by MTT assay
[PMID: 17944451]
体外研究
(In Vitro)

ES 936 (0-250 nM,30-120 分钟) 在 HCT116、HT-29、MDA468 NQ16、MIA PaCa-2 和 BxPC-3 细胞中抑制超过 95% 的 NQO1 活性[1][2]
ES 936 (100 nM,预处理 30 分钟) 在 MDA468 NQ16 细胞中使链霉色素的 IC50 增加约 6 倍,在 HCT116 细胞中增加约 2 倍,消除其毒性[1]
ES 936 (0-500 nM,2 小时) 在大鼠肝微粒体中诱导剂量依赖的 DNA 链断裂,并刺激低水平的 NAD(P)H 氧化[1]
ES 936 (100 nM,预处理 2 小时) 显著抑制转化的人骨髓内皮细胞 (TrHBMECs) 中 TNF 诱导的 E-selectin 表达,并降低 TNF 诱导的 VCAM-1 和 ICAM-1 蛋白水平[3]
ES 936 (100 nM,预处理 2 小时) 在平行板流动室实验中显著减少 TNF 诱导的 CD34+ KG1a 细胞与 TrHBMECs 的粘附[3]

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

Cell Viability Assay[3]

Cell Line: Transformed human bone marrow endothelial cells (TrHBMECs)
Concentration: 100 nM
Incubation Time: 2 h pretreatment
Result: Decreased TNF-stimulated E-selectin protein levels.
Reduced TNF-induced VCAM-1 and ICAM-1 protein levels.
Resulted in lower nuclear levels of phospho-p65, phospho-c-Jun, and phospho-ATF2 in TrHBMECs.
体内研究
(In Vivo)

ES936 (5 mg/kg,腹腔注射,每日一次,持续 10 天) 显著抑制雌性无胸腺裸鼠中 MIA PaCa-2 异种移植瘤的生长速率[2]

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

Animal Model: MIA PaCa-2 cells in log-phase growth (2×106 in 100 µL of 75:25 unsupplemented medium/Matrigel) were subcutaneously injected into the right flanks of 5- to 6-week-old female athymic nude mice (Ncr nu/nu)[2]
Dosage: 5 mg/kg
Administration: i.p. daily for 10 days
Result: Achieved a maximal T/C value of 47% based on tumor volume analysis in MIA PaCa-2 xenograft tumors.
Showed no obvious toxicities and no difference in body weight between ES936-treated and control (DMSO) animals.
Significantly slowed the growth rate of MIA PaCa-2 xenograft tumors, with the inhibitory effect more significant during treatment (days 1-10) than after cessation of therapy (days 11-20).
分子量

356.33

Formula

C18H16N2O6

CAS 号
性状

固体

颜色

Orange to red

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
细胞实验: 

DMSO 中的溶解度 : 2 mg/mL (5.61 mM; 超声加热助溶; 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 2.8064 mL 14.0319 mL 28.0639 mL
5 mM 0.5613 mL 2.8064 mL 5.6128 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

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

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 2.8064 mL 14.0319 mL 28.0639 mL 70.1597 mL
5 mM 0.5613 mL 2.8064 mL 5.6128 mL 14.0319 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:
ES 936
目录号:
HY-100367
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