PFI-3

製品コードS7315 バッチS731501

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₉H₁₉N₃O₂
	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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	PFI-3 is a selective chemical probe for SMARCA bromodomains, including SMARCA2, SMARCA4 and PB1(5) bromodomains.
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].

製品説明

PFI-3 is a selective chemical probe for SMARCA bromodomains, including SMARCA2, SMARCA4 and PB1(5) bromodomains.

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].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	trophoblast stem cells
	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.

参考

[4] Vangamudi B, et al. Cancer Res. 2015, 75(18):3865-78.

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カスタマーフィードバック

: Data from [Data independently produced by , , Exp Cell Res, 2018, 364(2):191-197]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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

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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。

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