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[Effect of ADAM10 Inhibitor GI254023X on Proliferation and Apoptosis of Multiple Myeloma H929 Cells and Its Possible Mechanisms]

Li-Li Chen, Guo-Qin Fan, Zhi-Yao Zhang, Bing-Yun Zhang, Zhi-Ling Yan, Hu-Jun Li, Jian-Ping Luo, Chong Chen, Yao Yao, Kai-Lin Xu, Zhen-Yu Li

Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2015 Dec;23(6):1628-32.

PMID: 26708884

Abstract:

Objective:
To investigate the effect of ADAM10 inhibitor GI254023X on the proliferation and apoptosis of multiple myeloma H929 cell line and its mechanisms.
Methods:
H929 cells were treated with different concentrations of GI254023X, the proliferation-inhibitive curve was assayed and plotted by CCK-8 method, the cell viability and apoptosis were detected by flow cytometry with Annexin V/7-AAD double staining. The cleavage of Notch1 protein (cleaved notch1) was determined by Western blot. The transcripts of Notch1 target gene Hes-1 were detected by real-time PCR.
Results:
The GI254023X inhibited the proliferation of H929 cells in the time- and dose- dependent manners. As compared with the control group, the apoptosis of cells increased along with enhancement of GI254023X concentration; The expression of cleaved Notch1 was down-regulated after the treatment with GI254023X. The levels of Hes-1 mRNA transcripts in H929 cells was reduced in GI254023X treated group.
Conclusion:
GI254023X can remarkably inhibit the proliferation and induce the apoptosis of H929 cells. Its mechanism may be associated with inbihition of Notch1 activation.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP260264935 GI254023X GI254023X 260264-93-5 Price
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