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CAS No.: 343351-67-7

NSC697923 Catalog No. CSN17303

Synonyms: N/A

NSC 697923 is a cell-permeable and selective inhibitor of the Ub-conjugating enzyme (E2) complex Ubc13-Uev1A.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述NSC697923 is a novel Ubc13-Uev1A inhibitor exhibiting potent cytotoxicity in a panel of neuroblastoma cell lines, including IMR32, SH-SY5Y, NGP, NB-19 and CHLA-255, through induction of apoptosis at concentration<5μM post 24h. NSC697923 induced nuclear accumulation of p53, which led to its increased transcriptional activity and tumor suppressor function, in p53 wild-type neuroblastoma cells at 3μM, but induced cell death by activating JNK pathway in p53 mutant neuroblastoma cells at 10μM. NSC697923 impeded cell growth of chemoresistant LA-N-6 NB cell line in a manner greater than conventional chemotherapy drugs doxorubicin and etoposide. Administration of NSC697923 at 5mg/kg by intraperitoneal injection daily for 10 days exhibited in vivo antitumor efficacy in NB orthotopic xenografts. NSC697923 suppressed constitutive NF-κB activity in ABC-DLBCL cells at 1μM post 3.5h, as well as inhibited the proliferation and survival of ABC-DLBCL cells and GCB-DLBCL cells at 2μM.
作用机制NSC697923 impedes the formation of the Ubc13 and ubiquitin thioester conjugate.^[2]
动物研究
剂量
Mice: 5 mg/kg^[1] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 5 mg/kg^[1] (i.p.)
给药途径	i.p.

[1] Cheng J, Fan YH, et al. A small-molecule inhibitor of UBE2N induces neuroblastoma cell death via activation of p53 and JNK pathways. Cell Death Dis. 2014 Feb 20;5:e1079.
[2] Pulvino M, Liang Y, et al. Inhibition of proliferation and survival of diffuse large B-cell lymphoma cells by a small-molecule inhibitor of the ubiquitin-conjugating enzyme Ubc13-Uev1A. Blood. 2012 Aug 23;120(8):1668-77.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.7417 mL
- 18.7085 mL
- 37.4170 mL
- 5 mM
- 0.7483 mL
- 3.7417 mL
- 7.4834 mL
- 10 mM
- 0.3742 mL
- 1.8709 mL
- 3.7417 mL

技术信息

CAS号

343351-67-7

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C11H9NO5S

运输

蓝冰

分子量

267.26

别名

N/A

溶解度

DMSO	53.0 mg/mL (198.3 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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