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。
| 生物活性 | NSC697923 is a potentUBE2N(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 andNF-κBsignaling. 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].
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. |
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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].
| 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. |
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| 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 |
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| 溶解性数据 | In Vitro: DMSO : 200 mg/mL(748.33 mM;Need ultrasonic) 配制储备液 | 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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: ≥ 5 mg/mL (18.71 mM); Clear solution
此方案可获得 ≥ 5 mg/mL (18.71 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 50.0 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%corn oil Solubility: ≥ 5 mg/mL (18.71 mM); Clear solution
此方案可获得 ≥ 5 mg/mL (18.71 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 50.0 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本网站选购。
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