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10058-F4
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
10058-F4图片
CAS NO:403811-55-2
规格:98%
分子量:249.35
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍
C-Myc-Max dimerization inhibitor
CAS:403811-55-2
分子式:C12H11NOS2
分子量:249.35
纯度:98%
存储:Store at -20°C

Background:

10058-F4 is a novel small-molecule inhibitor of c-Myc. 10058-F4 prevented the binding of c-Myc/Max dimers to its DNA targets, inhibited leukemic proliferation, and induced apoptosis through mitochondrial pathway, such as downregulation of Bcl-2, upregulation of Bax and release of cytoplasmic cytochrome C. [1]


10058-F4 blocks the C-MYC/Max heterodimerization which is required for c-Myc activity as a transcription factor. 10058-F4 efficiently inhibits the induction of PGC-1β mRNA by both HRG and IGF-1 and also abolishes the induction of PGC-1β protein levels by HRG and IGF-1, confirming that the induction of PGC-1b protein by these growth factors is a transcriptional event requiring C-MYC activity.[2] 10058-F4 acts not only to block c-Myc function through the mechanism of c-Myc/Max heterodimer dissociation, but it also resulted in decreased c-Myc mRNA levels (65%, n = 3) in lymphoma cells.[3]


参考文献:
[1] Huang MJ, Cheng YC, Liu CR, Lin SF, Liu H. E. A small-molecule c-Myc inhibitor, 10058-F4, induces cell-cycle arrest, apoptosis, and myeloid differentiation of human acute myeloid leukemia. Experimental Hematology. 2006; 34: 1480–1489.
[2] Ching-yi Chang, Dmitri Kazmin, Jeff?S. Jasper, Rebecca Kunder, William?J. Zuercher, Donald?P. McDonnell. The Metabolic Regulator ERRα, a Downstream Target of HER2/IGF-1R, as a Therapeutic Target in Breast Cancer. Cancer Cell. 18 October 2011. 20(4): 500-510.
[3] Ilsa Gomez-Curet, R. Serene Perkins, Ryan Bennett, Katherine L. Feidler, Stephen P. Dunn, Leslie J. Krueger. c-Myc inhibition negatively impacts lymphoma growth. Journal of Pediatric Surgery. January 2006. 41(1): 207-211.