产品描述: PFI-4 (compound 11) is a potent and highly selective BRPF1 Bromodomain (BRPF1B) inhibitor, with an IC50 of 172 nM. PFI-4 can be used to explore the functional mechanisms of the HBO1/BRPF1 complex and to study bone loss and osteolytic malignant bone lesions |
靶点:
IC50: 3.517 μM (BRPF2), >10 μM (BRD4 (1)), 0.172 μM (BRPF1B), >10 μM (TRIM24);EpigeneticReaderDomain |
体外研究:
PFI-4 (1.25 µM; 7 or 11 days) inhibits differentiation of human osteoclasts. Cell Viability Assay Cell Line: Osteoclasts Concentration: 1.25 µM Incubation Time: 7 or 11 days Result: Significantly reduces MMP9 secretion in osteoclasts. |
参考文献:
1. Meier JC, et al. Selective Targeting of Bromodomains of the Bromodomain-PHD Fingers Family Impairs Osteoclast Differentiation. ACS Chem Biol. 2017 Oct 20;12(10):2619-2630. 2. Demont EH, et al. 1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain. (2014) ACS Med Chem Lett. 5(11):1190-1195. |
溶解性:
soluble in DMSO |
保存条件:
-20℃ |
配置溶液浓度参考:
|
1mg |
5mg |
10mg |
1 mM |
2.629 ml |
13.143 ml |
26.285 ml |
5 mM |
0.526 ml |
2.629 ml |
5.257 ml |
10 mM |
0.263 ml |
1.314 ml |
2.629 ml |
50 mM |
0.053 ml |
0.263 ml |
0.526 ml |
|
注意: |
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