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说明： BET bromodomain inhibitor
化学名： 2-Methoxy-N-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzenesulfonamide
纯度： ≥98% (HPLC)
生物活性 for PFI 1
PFI 1 is a potent BET bromodomain inhibitor; exhibits inhibitory activity at bromodomain-containing protein (BRD) 2 and BRD4 (IC50 values are 98 and 220 nM respectively). Induces apoptosis and G1 cell cycle arrest in BET inhibitor-sensitive cell lines (MV4;11). Also downregulates Aurora B expression in MV4;11 cells. Cell permeable.
许可信息
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the PFI 1 probe summary on the SGC website.
External Portal Information for PFI 1
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of PFI 1 is reviewed on the chemical probes website.
化合物库 for PFI 1
PFI 1 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for PFI 1
| 分子量 | 347.39 |
| 公式 | C16H17N3O4S |
| 储存 | Store at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1403764-72-6 |
| PubChem ID | 71271629 |
| InChI Key | TXZPMHLMPKIUGK-UHFFFAOYSA-N |
| Smiles | O=C2NC1=CC=C(NS(C3=CC=CC=C3OC)(=O)=O)C=C1CN2C |
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 1
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 17.37 | 50 |
制备储备液 for PFI 1
以下数据基于产品分子量 347.39。 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 |
|---|---|---|---|
| 0.5 mM | 5.76 mL | 28.79 mL | 57.57 mL |
| 2.5 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.58 mL | 2.88 mL | 5.76 mL |
| 25 mM | 0.12 mL | 0.58 mL | 1.15 mL |
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产品说明书 for PFI 1
参考文献 for PFI 1
参考文献是支持产品生物活性的出版物。
Fish et al (2012) Identification of a chemical probe for bromo and extra c-terminal bromodomain inhibition through optimization of a fragment-derived hit. J.Med.Chem. 55 9831 PMID: 23095041
Picaud et al (2013) PFI-1 - a highly selective protein interaction inhibitor targeting BET bromodomains. Cancer Res. 73 3336 PMID: 23576556
If you know of a relevant reference for PFI 1, please let us know.
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关键词: PFI 1, PFI 1 supplier, PFI1, bet, bromodomain, brd4, brd2, inhibitors, inhibits, epigenetics, atypical, kinases, bromodomain-containing, 2, 4, sgc, Bromodomains, 4445, Tocris Bioscience
4 篇 PFI 1 的引用文献
引用文献是使用了 Tocris 产品的出版物。 PFI 1 的部分引用包括：
Fernando et al (2023) Epigenetic inactivation of the 5-methylcytosine RNA methyltransferase NSUN7 is associated with clinical outcome and therapeutic vulnerability in liver cancer. Mol Cancer 22 83 PMID: 37173708
Clifford et al (2015) CXCL8 histone H3 acetylation is dysfunctional in airway smooth muscle in asthma: regulation by BET. Am J Physiol Lung Cell Mol Physiol 308 L962 PMID: 25713319
Fish et al (2012) Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit. J Med Chem 55 9831 PMID: 23095041
Christopher J et al (2022) Pharmacologic Targeting of TFIIH Suppresses KRAS-Mutant Pancreatic Ductal Adenocarcinoma and Synergizes with TRAIL. Cancer Res 82 3375-3393 PMID: 35819261
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PFI 1 的评论
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