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- 文献和实验
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
NSC 697923
- 库存：
999
- 供应商：
北京索莱宝科技有限公司
- CAS号：
343351-67-7
- 规格：
1mg/5mg/10mg/25mg/50mg/100mg
| 规格： | 1mg | 产品价格： | ¥210.00 |
|---|---|---|---|
| 规格： | 5mg | 产品价格： | ¥468.00 |
| 规格： | 10mg | 产品价格： | ¥790.00 |
| 规格： | 25mg | 产品价格： | ¥1376.00 |
| 规格： | 50mg | 产品价格： | ¥2004.00 |
| 规格： | 100mg | 产品价格： | ¥3028.00 |
| CAS | 343351-67-7 |
| 英文名称 | NSC 697923 |
| 分子式 | C11H9NO5S |
| 分子量 | 267.26 |
| 规格 | 1mg ; 5mg ; 10mg ; 25mg ; 50mg ; 100mg |
| 溶解性 | Soluble in DMSO ≥5mg/mL |
| 纯度 | ≥98% |
| 外观(性状) | Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| 运输条件 | 冷藏运输 |
| EC | 803-500-4 |
| MDL | MFCD01925132 |
| SMILES | CC1=CC=C(C=C1)S(=O)(=O)C2=CC=C(O2)[N+](=O)[O-] |
| InChIKey | GAUHIPWCDXOLCZ-UHFFFAOYSA-N |
| InChI | InChI=1S/C11H9NO5S/c1-8-2-4-9(5-3-8)18(15,16)11-7-6-10(17-11)12(13)14/h2-7H,1H3 |
| PubChem CID | 394449 |
| 靶点 | E2 conjugating inhibitor |
| 通路 | Ubiquitin |
| 背景说明 | 是一种细胞选择透过性Ub-conjugating enzyme (E2)复合Ubc13-Uev1A 抑制剂。 |
| 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]. |
| 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. |
| 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. |
| 数据来源文献 | [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. |
| 单位 | 瓶 |
| 表格1 | |*|1mg|5mg|10mg|$$|1mM|3.7417mL|18.7084mL|37.4167mL|$$|5mM|0.7483mL|3.7417mL|7.4833mL|$$|10mM|0.3742mL|1.8708mL|3.7417mL| |
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