产品描述: | I-BRD9 is a selective cellular chemical probe of bromodomain-containing protein 9 (BRD9) with pIC50 value of 7.3 μM. I-BRD9 has high selectivity for bromodomain and extra terminal domain (BET) family and highly homologous bromodomain-containing protein 7 (BRD7). I-BRD9 can be used to identify genes regulated by BRD9 in Kasumi-1 cells involved in oncology and immune response pathways |
靶点: |
Epigenetic Reader Domain;EpigeneticReaderDomain |
体外研究: |
I-BRD9 (10 μM, 6 h) has a regulation role in cancer and immunology pathways. I-BRD9 (10 μM) has high BRD9 affinity and excellent broader bromodomain selectivity. I-BRD9 (10 μM) has affinity for BRD9 (TR-FRET), BRD4 BD1 (TR-FRET) and BRD9 NanoBRET with pIC50 values of 7.3 μM, 5.3 μM and 6.8 μM. I-BRD9 (10 μM) has high aqueous solubility (CLND) with 359 μM. I-BRD9 (10 μM) displays >625 fold selectivity in binding with endogenous BRD9 against BET family member BRD3 in HUT-78 cell lysate. RT-PCR Cell Line: Kasumi-1 cells Concentration: 10 μM Incubation Time: 6 h Result: Showed 4 genes (CLEC1, 62 DUSP6, 63 FES64 and SAMSN165) that were strongly down-regulated and not by I-BET151. |
参考文献: |
1. Natalie H Theodoulou, et al. Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition. J Med Chem |
溶解性: |
soluble in DMSO |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.01 ml |
10.049 ml |
20.098 ml |
5 mM |
0.402 ml |
2.01 ml |
4.02 ml |
10 mM |
0.201 ml |
1.005 ml |
2.01 ml |
50 mM |
0.04 ml |
0.201 ml |
0.402 ml |
|
注意: |
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