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NSC697923

Katalog-Nr.GC11932

NSC697923 ist ein potenter UBE2N-Hemmer (Ubiquitin-konjugierendes Enzym E2 N, Ubc13). NSC697923 induziert den Zelltod des Neuroblastoms (NB), indem es den Kernimport von p53 in p53-Wildtyp-NB-Zellen fÖrdert. NSC697923 induziert auch den Zelltod in p53-mutierten NB-Zellen durch Aktivierung des JNK-vermittelten apoptotischen Signalwegs. NSC697923 hemmt DNA-SchÄden und die NF-κB-SignalÜbertragung. Antitumor-AktivitÄt.

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NSC697923 Chemische Struktur

Cas No.: 343351-67-7

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Sample solution is provided at 25 µL, 10mM.

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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.

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