NSC697923
目录号 : GC11932
A selective inhibitor of Ubc13
Cas No.:343351-67-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
Human NB cell lines with MYCN amplification (IMR-32, NGP and NB-19) and without (CHLA-255, SK-N-AS and SH-SY5Y) |
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Preparation method |
The solubility of this compound in DMSO is >10mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
5μM ;24hours |
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Applications |
Treatment with NSC697923 significantly reduced NB cells viability in a dose-dependent manner and inhibited both anchorage-dependent and -independent colony formation of NB cells. NSC697923 induced apoptosis in all NB cell lines tested. In addition, NSC697923 also induced apoptosis in p53 mutant NB cells by activation of JNK-mediated apoptotic pathway. NSC697923 exhibited its effect primarily through inducing p53 nuclear translocation but not increasing its total amount. NSC697923 treatment also induced more phosphorylation of JNK, p38, and ERK in SK-N-AS. |
| Animal experiment [2]: | |
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Animal models |
5- to 6-week-old female athymic Ncr nude mice (SH-SY5Y and NGP xenografts) |
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Dosage form |
5 mg/kg , intraperitoneal injection everyday for 10 days |
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Application |
These results showed significant tumor regression in NSC697923 treatment group of both SH-SY5Y and NGP xenografts. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Cheng J, Fan YH, Xu X., 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. |
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NSC697923 is a selective and permeable inhibitor of the ubiquitin-conjugating enzyme Ubc13-Uev1A which blocks the formation of ubiquitin thioester conjugate. And the small-molecule inhibitor inhibits proliferation and survival of diffuse large B-cell lymphoma cells (DLBCL) [1].
Diffuse large cell lymphoma is the most common lymphoma that has a rapid growth rate and causes masses infiltrating tissues or obstructing organs. Unless treated in time, it will kill people quickly.
NSC697923 is an potent inhibitor of the formation of the Ubc13 and NF-κB activation in DLBCL. There are constitutive NF-kB pathway activities in DLBCL. So, impeding NF-kB activation in DLBCL would be a good solution to inhibit the proliferation and survival of diffuse of DLBCL. Also, NSC697923 blocks the formation of the Ubc13-Uev1A by inhibiting the formation of the Ubc13_Ub conjugate while it is a key component for DLBCL grown. In the long term, the cell cannot survive without Ubc13 expression. In conclusion, compound NSC697923 is an efficient inhibitor of DLBAL survival [1,2].
In a xenograft mouse model, NSC697923 has significantly reduced the proliferation and survival of diffuse large B-cell lymphoma (DLBCL) cells and induces NB cell death [1,3].
References:
[1]. Pulvino M, Liang Y, Oleksyn D, et al. Inhibition of proliferation and survival of diffuse large B-cell lymphoma cells by a small-moleculeinhibitor of the ubiquitin-conjugating enzyme Ubc13-Uev1A. Blood, 2012, 120: 1668–1677.
[2]. Zhaojia Wu, Siqi Shen, Zhiling Zhang, et al. Ubiquitin-conjugating enzyme complex Uev1A-Ubc13 promotes breast cancer metastasis through nuclear factor-кB mediated matrix metalloproteinase-1 gene regulation. Breast Cancer Research, 2014, 16:75-90.
[3]. J Cheng, Y-H Fan, X Xu, et al. A small-molecule inhibitor of UBE2N induces neuroblastoma cell death via activation of p53 and JNK pathways. Cell Death and Disease, 2014, 54: 1079.
| Cas No. | 343351-67-7 | SDF | |
| 化学名 | 2-(4-methylphenyl)sulfonyl-5-nitrofuran | ||
| Canonical SMILES | CC1=CC=C(C=C1)S(=O)(=O)C2=CC=C(O2)[N+](=O)[O-] | ||
| 分子式 | C11H9NO5S | 分子量 | 267.26 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20° C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。