S88629 |
PBIT |
源叶(MedMol) | ≥98%(HPLC) |
- 产品描述: PBIT is a specific inhibitor of the Jumonji AT-rich Interactive Domain 1 (JARID1) enzymes. PBIT inhibits JARID1B (KDM5B or PLU1) histone demethylase with an IC50 of about 3 μM . PBIT also inhibits JARID1A and JARID1C with IC50s of 6 μM and 4.9 μM, respectively
- 靶点: IC50: 3 μM (JARID1B), 6 μM (JARID1A), 4.9 μM (JARID1C);HistoneDemethylase; HistoneMethyltransferase
- 体外研究:
PBIT inhibits proliferation of cells expressing higher levels of JARID1B. PBIT (1-10 μM for UACC-812 cells, 2.5-10μM for MCF7 and MCF10A cells; 72 hours) inhibits cell proliferation in a JARID1B level-dependent manner. Cell Proliferation Assay Cell Line: Human breast cancer cell lines (UACC-812 and MCF7) and human mammary epithelial cells (MCF10A) Concentration: 1, 3, and 10 μM for UACC-812 cells; 2.5, 5, and 10 μM for MCF7 and MCF10A cells Incubation Time: 72 hours Result: Inhibited cell proliferation in a JARID1B level-dependent manner. 10 μM killed most of the UACC-812 cells, but showed minimal toxicity to MCF7 cells and MCF10A cells.
- 参考文献:
1. Sayegh J, et al. Identification of small molecule inhibitors of Jumonji AT-rich interactive domain 1B (JARID1B) histone demethylase by a sensitive high throughput screen. J Biol Chem. 2013 Mar 29;288(13):9408-17.
- 溶解性: Soluble in DMSO
- 保存条件: -20°C
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 4.144 ml 20.72 ml 41.44 ml 5 mM 0.829 ml 4.144 ml 8.288 ml 10 mM 0.414 ml 2.072 ml 4.144 ml 50 mM 0.083 ml 0.414 ml 0.829 ml
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