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(R)-PFI 2 hydrochloride

Cat. No. 4892 4 篇引用文献 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Potent and selective SETD7 inhibitor
化学名： 8-Fluoro-1,2,3,4-tetrahydro-N-[(1R)-2-oxo-2-(1-pyrrolidinyl)-1-[[3-(trifluoromethyl)phenyl]methyl]ethyl]-6-isoquinolinesulfonamide hydrochloride
纯度： ≥97% (HPLC)
说明书
引用文献 (4)
评论
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for (R)-PFI 2 hydrochloride

(R)-PFI 2 hydrochloride is a potent and selective SETD7 histone lysine methyltransferase inhibitor (IC50 = 2 nM). Exhibits >1000-fold selectivity over DNMT1 and a panel of 18 other methyltransferases. Inhibits YAP nuclear translocation and function following activation of the Hippo signaling pathway in MCF7 cells.

Negative Control also available.

许可信息

This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the (R)-PFI 2 probe summary on the SGC website.

External Portal Information for (R)-PFI 2 hydrochloride

Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of (R)-PFI 2 is reviewed on the chemical probes website.

技术数据 for (R)-PFI 2 hydrochloride

分子量 535.98
公式 C23H25F4N3O3S.HCl
储存 Store at -20°C
纯度 ≥97% (HPLC)
CAS Number 1627607-87-7
PubChem ID 78243738
InChI Key ZADKZNVAJGEFLC-ZMBIFBSDSA-N
Smiles O=C(N4CCCC4)[C@@H](CC3=CC=CC(C(F)(F)F)=C3)NS(C2=CC1=C(C(F)=C2)CNCC1)(=O)=O.Cl

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 (R)-PFI 2 hydrochloride

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 53.6 100
ethanol 10.72 20 超声处理

制备储备液 for (R)-PFI 2 hydrochloride

以下数据基于产品分子量 535.98。 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.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 1.87 mL 9.33 mL 18.66 mL
5 mM 0.37 mL 1.87 mL 3.73 mL
10 mM 0.19 mL 0.93 mL 1.87 mL
50 mM 0.04 mL 0.19 mL 0.37 mL

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产品说明书 for (R)-PFI 2 hydrochloride

分析证书/产品说明书
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化学品安全技术说明书

参考文献 for (R)-PFI 2 hydrochloride

参考文献是支持产品生物活性的出版物。

Barsyte-Lovejoy et al (2014) (R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells. Proc.Natl.Acad.Sci.U S A 111 12853 PMID: 25136132

Scheer et al (2019) A chemical biology toolbox to study protein methyltransferases and epigenetic signaling. Nat.Commun. 10 19 PMID: 30604761

If you know of a relevant reference for (R)-PFI 2 hydrochloride, please let us know.

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关键词: (R)-PFI 2 hydrochloride, (R)-PFI 2 hydrochloride supplier, (R)-PFI2, HCl, potent, selective, inhibitors, inhibits, SETD7, lysine, histone, methyltransferase, epigenetics, Hippo, YAP, sgc, Lysine, Methyltransferases, Other, Hippo/Yap, signaling, 4892, Tocris Bioscience

4 篇 (R)-PFI 2 hydrochloride 的引用文献

引用文献是使用了 Tocris 产品的出版物。 (R)-PFI 2 hydrochloride 的部分引用包括：

Liu et al (2015) Repression of hypoxia-inducible factor α signaling by Set7-mediated methylation. J Neuroinflammation 43 5081 PMID: 25897119

Jing et al (2016) Miniaturization of High-Throughput Epigenetic Methyltransferase Assays with Acoustic Liquid Handling. J Lab Autom 21 208-16 PMID: 26450876

Tristan A et al (2021) Genetically variant human pluripotent stem cells selectively eliminate wild-type counterparts through YAP-mediated cell competition. Dev Cell 56 2455-2470.e10 PMID: 34407428

Judson et al (2018) Inhibition of methyltransferase Setd7 allows in vitro expansion of myogenic stem cells with improved therapetic potential. Cell Stem Cell 22 177 PMID: 29395054

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