NSC697923是一种有效的、细胞可渗透的UBE2N（泛素结合酶E2 N，Ubc13）抑制剂。
Cas No.:343351-67-7
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
NSC697923 is a potent, cell-permeable UBE2N (ubiquitin-conjugating enzyme E2 N, Ubc13) inhibitor. NSC697923 induces cell death by promoting nuclear import of p53 or activating the JNK-mediated apoptotic pathway. NSC697923 can be used in studies related to neuroblastoma and diffuse large B-cell lymphoma (DLBCL)[1-4].
In vitro, NSC697923 (0.5-2μM) was used to treat ABC-DLBCL cells, GCB-DLBCL cells, and primary DLBCL cells for 24 hours. NSC697923 significantly inhibited cell proliferation and survival, while inducing apoptosis[5]. NSC697923 (0.1-0.5μM) was used to treat neuroblastoma cell lines (including SH-SY5Y, IMR32, SK-N-AS, LA-N-6, etc.) for 24 hours. NSC697923 significantly induced apoptosis, while inhibiting cell proliferation and colony formation[6].
In vivo, NSC697923 (5mg/kg) was intraperitoneally injected every other day into NSG SCID mice bearing A375 xenograft tumors for 18 days. NSC697923 significantly reduced subcutaneous tumor growth[7]. NSC697923 (3mg/kg; three times per week) combined with Ramipril (2mg/kg; three times per week) was intraperitoneally injected into STZ-induced diabetic DBA/2J mice for 6 weeks. NSC697923 significantly reduced the accumulation of K63-ubiquitinated proteins, renal fibrosis, and glomerulosclerosis[8].
References:
[1] Gombodorj N, Yokobori T, Yoshiyama S, et al. Inhibition of Ubiquitin-conjugating Enzyme E2 May Activate the Degradation of Hypoxia-inducible Factors and, thus, Overcome Cellular Resistance to Radiation in Colorectal Cancer. Anticancer Res. 2017 May;37(5):2425-2436.
[2] Hodge CD, Edwards RA, Markin CJ, et al. Covalent Inhibition of Ubc13 Affects Ubiquitin Signaling and Reveals Active Site Elements Important for Targeting. ACS Chem Biol. 2015 Jul 17;10(7):1718-28.
[3] Zhang K, Zhao Y, Chen X, et al. p53 promote oxidative stress, neuroinflammation and behavioral disorders via DDIT4-NF-κB signaling pathway. Redox Biol. 2025 Oct;86:103836.
[4] Cao DY, Zhang ZH, Li RZ, et al. A small molecule inhibitor of caspase-1 inhibits NLRP3 inflammasome activation and pyroptosis to alleviate gouty inflammation. Immunol Lett. 2022 Apr;244:28-39.
[5] Pulvino M, Liang Y, Oleksyn D, 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.
[6] 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(2):e1079.
[7] Dikshit A, Jin YJ, Degan S, et al. UBE2N Promotes Melanoma Growth via MEK/FRA1/SOX10 Signaling. Cancer Res. 2018 Nov 15;78(22):6462-6472.
[8] Pontrelli P, Conserva F, Menghini R, et al. Inhibition of Lysine 63 Ubiquitination Prevents the Progression of Renal Fibrosis in Diabetic DBA/2J Mice. Int J Mol Sci. 2021 May 14;22(10):5194.
NSC697923是一种有效的、细胞可渗透的UBE2N（泛素结合酶E2 N，Ubc13）抑制剂。NSC697923通过促进p53的核输入，或激活JNK介导的凋亡途径诱发细胞死亡。NSC697923可用于神经母细胞瘤和弥漫性大B细胞淋巴瘤（DLBCL）的相关研究[1-4]。
在体外，NSC697923（0.5-2μM）处理ABC-DLBCL细胞、GCB-DLBCL细胞及原代DLBCL细胞24小时。NSC697923显著抑制细胞增殖和存活，同时诱导细胞凋亡[5]。NSC697923（0.1-0.5μM）处理神经母细胞瘤细胞系（包括SH-SY5Y、IMR32、SK-N-AS、LA-N-6等）24小时。NSC697923显著诱导细胞凋亡，同时抑制细胞增殖和克隆形成[6]。
在体内，NSC697923（5mg/kg）每隔一天腹腔注射于携带A375异种移植瘤的NSG SCID小鼠18天。NSC697923显著减少了皮下肿瘤生长[7]。NSC697923（3mg/kg；每周三次）联合Ramipril（2mg/kg；每周三次）腹腔注射于STZ诱导的糖尿病DBA/2J小鼠6周。NSC697923显著减少了K63泛素化蛋白的积累、肾纤维化和肾小球硬化[8]。
| Cell experiment [1]: | |
Cell lines | A panel of neuroblastoma cell lines (including SH-SY5Y, IMR32, SK-N-AS, LA-N-6, NGP, NB19, CHLA-255) |
Preparation Method | Cells were treated with NSC697923 (0.1-0.5μM) for 24 hours. |
Reaction Conditions | 0.1-0.5μM; 24h |
Applications | NSC697923 significantly induced apoptosis, inhibited cell proliferation and colony formation, promoted nuclear translocation of p53 in p53 wild-type cells, and activated JNK-mediated apoptotic pathway in p53 mutant cells. |
| Animal experiment [2]: | |
Animal models | NSG SCID mice |
Preparation Method | Mice were injected subcutaneously with 150,000 A375 cells in both flanks. Mice were treated every other day for a total of 18 days with either solvent (0.5% DMSO and 30% Corn oil) or 5mg/kg NSC697923. |
Dosage form | 5mg/kg; i.p.; every other day for 18 days |
Applications | NSC697923 treatment significantly reduced subcutaneous tumor growth, decreased total K63-Ub, reduced the number of Ki-67-positive proliferative cells, increased the number of cleaved caspase 3-positive apoptotic cells, decreased the expression of SOX10, Nestin and ABCB5, and increased the expression of p16. |
References: | |
| 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.7417 mL | 18.7084 mL | 37.4167 mL |
| 5 mM | 748.3 μL | 3.7417 mL | 7.4833 mL |
| 10 mM | 374.2 μL | 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。
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet