| 货号 | 17257-50mg |
| 描述 | VER-155008 is an adenosine-derived inhibitor of heat shock protein 70 (Hsp70; IC50 = 0.5 µM) that is selective over Hsp90.1 It targets the nucleotide-binding domain (NBD) of Hsp70 and similarly binds the NBDs of Hsp70 cognates Hsc70 (Ki = 10 µM) and glucose-regulated protein 78 (Grp78; KD = 80 nM).2,3 VER-155008 inhibits the proliferation of human breast and colon cancer cell lines, inducing apoptosis or caspase-independent cell death.4 It induces the proteasome-dependent degradation of Hsp90 client proteins and potentiates the apoptotic activity of Hsp90 inhibitors.1,4 VER-15508 also triggers paraptosis in anaplastic thyroid carcinoma cells.5 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Williamson, D.S.,Borgognoni, J.,Clay, A., et al. Novel adenosine-derived inhibitors of 70 kDa heat shock protein, discovered through structure-based design. Journal of Medicinal Chemistry 52(6), 1510-1513 (2009). 2.Schlecht, R.,Scholz, S.R.,Dahmen, H., et al. Functional analysis of Hsp70 inhibitors. PLoS One 8(11), (2013). 3.Macias, A.T.,Williamson, D.S.,Allen, N., et al. Adenosine-derived inhibitors of 78 kDa glucose regulated protein (Grp78) ATPase: insights into isoform selectivity. Journal of Medicinal Chemistry 54(12), 4034-4041 (2011). 4.Massey, A.J.,Williamson, D.S.,Browne, H., et al. A novel, small molecule inhibitor of Hsc70/Hsp70 potentiates Hsp90 inhibitor induced apoptosis in HCT116 colon carcinoma cells. Cancer Chemotherapy and Pharmacology 66(3), 535-545 (2015). 5.Kim, S.H.,Kang, J.G.,Kim, C.S., et al. The hsp70 inhibitor VER155008 induces paraptosis requiring de novo protein synthesis in anaplastic thyroid carcinoma cells. Biochemica et Biophysica Acta 454, 36-41 (2014). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 556.4 |
| 分子式 | C25H23Cl2N7O4 |
| CAS号 | 1134156-31-2 |
| 稳定性 | ≥ 2 years |
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