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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C19H19N3O2 |
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分子量 | 321.37 | CAS No. | 1819363-80-8 | |
Solubility (25°C)* | 体外 | DMSO | 64 mg/mL (199.14 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | PFI-3 is a selective chemical probe for SMARCA bromodomains, including SMARCA2, SMARCA4 and PB1(5) bromodomains. |
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in vitro | PFI-3 shows a significant selectivity for PB1(5) and SMARCA2/4 over 36 other tested kinases[1]. PFI-3 is a potent and cell active protein interaction inhibitor that selectively binds to essential BAF bromodomains. PFI-3 is screened in a commercial screening panel comprising 102 cellular receptors as well as 30 enzyme assays, revealing only interactions against four GPCRs with micromolar affinity and no significant additional interactions outside the BRD family, confirming its excellent broader pharmacological selectivity. Stability measurements confirmed that PFI-3 has a half-life in aqueous solutions exceeding 7 days at 37°C. In long-term experiments, PFI-3 significantly altered gene expression programs that are important for differentiation of stem cells. PFI-3 mimics the effect of Brg1 deletion, resulting in an increase of the repressive H3K27me3 mark at the TSSs and Stat3 binding sites of these genes[2]. PFI-3 has a half-life of >250 h in PBS, pH 7.4, at 20 °C[3]. |
細胞アッセイ | 細胞株 | trophoblast stem cells |
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濃度 | 2 μM | |
反応時間 | 24 h | |
実験の流れ | TSC are cultured in stemness or differentiation conditions and treated with 2 μM PFI-3 or 10 μM control compound or indicated concentrations for 24 hours or during the entire differentiation induction (4 days), respectively. In case of the differentiation samples, the PFI-3 or control compound exposure started 1 day before the induction of differentiation. RNA was isolated as for the ESC samples. |
Data from [Data independently produced by , , Exp Cell Res, 2018, 364(2):191-197]
RNF138 inhibits late inflammatory gene transcription through degradation of SMARCC1 of the SWI/SNF complex [ Cell Rep, 2023, 42(2):112097] | PubMed: 36800290 |
Brahma-related gene 1 acts as a profibrotic mediator and targeting it by micheliolide ameliorates peritoneal fibrosis [ J Transl Med, 2023, 21(1):639] | PubMed: 37726857 |
Brahma-related gene 1 acts as a profibrotic mediator and targeting it by micheliolide ameliorates peritoneal fibrosis [ J Transl Med, 2023, 21(1):639] | PubMed: 37726857 |
Actionable Cytopathogenic Host Responses of Human Alveolar Type 2 Cells to SARS-CoV-2 [ Mol Cell, 2020, 80(6):1104-1122.e9] | PubMed: 33259812 |
Dual roles of chromatin remodeling protein BRG1 in angiotensin II-induced endothelial-mesenchymal transition [ Cell Death Dis, 2020, 11(7):549] | PubMed: 32683412 |
BRG1 Stimulates Endothelial Derived Alarmin MRP8 to Promote Macrophage Infiltration in an Animal Model of Cardiac Hypertrophy [ Front Cell Dev Biol, 2020, 8:569] | PubMed: 32733885 |
Chemical Genetics Screen Identifies Epigenetic Mechanisms Involved in Dopaminergic and Noradrenergic Neurogenesis in Zebrafish. [ Front Genet, 2020, 11:80] | PubMed: 32158467 |
The maternal to zygotic transition regulates genome-wide heterochromatin establishment in the zebrafish embryo [ Nat Commun, 2019, 10(1):1551] | PubMed: 30948728 |
Dynamic reversal of random X-Chromosome inactivation during iPSC reprogramming. [ Genome Res, 2019, 29(10):1659-1672] | PubMed: 31515287 |
Targeting CDK9 Reactivates Epigenetically Silenced Genes in Cancer [Zhang H, et al. Cell, 2018, 175(5):1244-1258] | PubMed: 30454645 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。