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Submit ReviewPFI 3
说明： Potent and selective SMARCA2/4 and polybromo 1 inhibitor
化学名： (2E)-1-(2-Hydroxyphenyl)-3-[(1R,4R)-5-(pyridin-2-yl)-2,5-diazabicyclo[2.2.1]heptan-2-yl]prop-2-en-1-one
纯度： ≥98% (HPLC)
生物活性 for PFI 3
PFI 3 is a potent and selective polybromo 1 (PBRM1) and SMARCA4 inhibitor (Kd values are 48 and 89 nM respectively) that also inhibits SMARCA2. This compoud displays 30-fold selectivity over other sub-family branches. PFI 3 accelerates FRAP recovery in cells at a concentration of 1 μM.
许可信息
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the PFI 3 probe summary on the SGC website.
External Portal Information for PFI 3
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of PFI 3 is reviewed on the chemical probes website.
化合物库 for PFI 3
PFI 3 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。
技术数据 for PFI 3
| 分子量 | 321.37 |
| 公式 | C19H19N3O2 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1819363-80-8 |
| PubChem ID | 78243717 |
| InChI Key | INAICWLVUAKEPB-QSTFCLMHSA-N |
| Smiles | O=C(C3=C(O)C=CC=C3)/C=C/N1[C@H](C4)CN(C2=NC=CC=C2)[C@H]4C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for PFI 3
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 32.14 | 100 | |
| ethanol | 1.61 | 5 温和加热 |
制备储备液 for PFI 3
以下数据基于产品分子量 321.37。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.11 mL | 15.56 mL | 31.12 mL |
| 5 mM | 0.62 mL | 3.11 mL | 6.22 mL |
| 10 mM | 0.31 mL | 1.56 mL | 3.11 mL |
| 50 mM | 0.06 mL | 0.31 mL | 0.62 mL |
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产品说明书 for PFI 3
参考文献 for PFI 3
参考文献是支持产品生物活性的出版物。
Vangamudi et al (2015) The SMARCA2/4 ATPase domain surpasses the bromodomain as a drug target in SWI/SNF mutant cancers: Insights from cDNA rescue and PFI-3 inhibitor studies Cancer Res. 75 3865 PMID: 26139243
Gerstenberger et al (2016) Identification of a chemical probe for family VIII bromodomains through optimization of a fragment hit. J.Med.Chem. 59 4800 PMID: 27115555
If you know of a relevant reference for PFI 3, please let us know.
按产品操作查看相关产品
关键词: PFI 3, PFI 3 supplier, PFI3, potent, selective, SMARCA4, PolyBromo, 1, inhibitors, inhibits, SMARCA2, epigenetics, PB1, PBRM1, Bromodomains, Other, ATPases, 5072, Tocris Bioscience
2 篇 PFI 3 的引用文献
引用文献是使用了 Tocris 产品的出版物。 PFI 3 的部分引用包括：
Yi et al (2021) Neuronal activity-induced BRG1 phosphorylation regulates enhancer activation. Cell Rep 36 109357 PMID: 34260936
Jongbum et al (2020) Cytotoxic activity of bromodomain inhibitor NVS-CECR2-1 on human cancer cells. Sci Rep 10 16330 PMID: 33004947
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
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