NSC697923

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NSC697923  纯度: ≥97.0%

NSC697923 是一种有效的 UBE2N (ubiquitin-conjugating enzyme E2 N, Ubc13) 抑制剂。NSC697923 通过促进 p53 野生型神经母细胞瘤细胞中 p53 的核输入而诱导神经母细胞瘤细胞死亡。NSC697923 通过激活 JNK 介导的凋亡途径诱导 p53 突变神经母细胞瘤细胞死亡。NSC697923 抑制 DNA 损伤和 NF-κB 信号传导。具有抗肿瘤活性。

NSC697923

NSC697923 Chemical Structure

CAS No. : 343351-67-7

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NSC697923 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Metabolism/Protease Compound Library
  • NF-κB Signaling Compound Library
  • Anti-Cancer Compound Library
  • Oxygen Sensing Compound Library
  • Ubiquitination Compound Library
  • Anti-Liver Cancer Compound Library

生物活性

NSC697923 is a potent UBE2N (ubiquitin-conjugating enzyme E2 N, Ubc13) inhibitor. NSC697923 induces neuroblastoma (NB) cell death via promoting nuclear importation of p53 in p53 wild-type NB cells. NSC697923 also induces cell death in p53 mutant NB cells by activation of JNK-mediated apoptotic pathway. NSC697923 inhibits DNA damage and NF-κB signaling. Antitumor activity[1][2].

体外研究
(In Vitro)

NSC697923 (0-5 μM; 24 hours) shows cytotoxic effect on NB cell lines[1].
NSC697923 (3 μM; 2 hours) can also induce apoptosis in p53 mutant NB cells by activation of JNK-mediated apoptotic pathway[1].
NSC697923 induces apoptosis in p53 wild-type NB cell lines by promoting p53 nuclear translocation and activation[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Three MYCN-amplified cell lines: IMR32, NGP, NB19 and three MYCN-non-amplified cell lines: CHLA-255, SK-N-AS, and SH-SY5Y
Concentration: 0-5 μM
Incubation Time: 24 hours
Result: Significantly reduced NB cells viability in a dose-dependent manner. Also induced cell death in the p53 non-functional cell line SK-N-AS and p53 partially functional cell line NB-19.

Western Blot Analysis[1]

Cell Line: p53 wild-type SH-SY5Y and IMR32 cells
Concentration: 3 μM
Incubation Time: 2 hours
Result: Induced expression of p53-targeted gene p21 as well as the cleavage of caspase 3 in two p53 wild-type cell lines SH-SY5Y and IMR32.

体内研究
(In Vivo)

NSC697923 (5 mg/kg; i.p.; daily for 10 days) suppresses NB tumor growth in SH-SY5Y and NGP xenografts[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 5- to 6-week-old female athymic Ncr nude mice (orthotopic mouse model of NB; SH-SY5Y and NGP xenografts)[1]
Dosage: 5 mg/kg
Administration: I.p.; daily for 10 days
Result: Significant tumor regression in both SH-SY5Y and NGP xenografts.

分子量

267.26

Formula

C11H9NO5S
CAS 号

343351-67-7
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 : 100 mg/mL (374.17 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.7417 mL 18.7084 mL 37.4167 mL
5 mM 0.7483 mL 3.7417 mL 7.4833 mL
10 mM 0.3742 mL 1.8708 mL 3.7417 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    90% corn oil

    Solubility: ≥ 2.5 mg/mL (9.35 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.35 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Cheng J, et al. A small-molecule inhibitor of UBE2N induces neuroblastoma cell death via activation of p53 and JNK pathways. Cell Death Dis. 2014;5(2):e1079. Published 2014 Feb 20.

    [2]. Hodge CD, et al. Covalent Inhibition of Ubc13 Affects Ubiquitin Signaling and Reveals Active Site Elements Important for Targeting. ACS Chem Biol. 2015;10(7):1718-1728.

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