(S)-PFI-2 (hydrochloride)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
(S)-PFI-2 (hydrochloride) is the inactive enantiomer of (R)-PFI-2 and may serve as a negative control. (R)-PFI-2 is a cell-permeable and potent SET7/9 inhibitor with IC50 value of 2 nM [1].
Protein methyltransferases involve in the epigenetic regulation of gene transcription, silencing, chromatin structure establishment, maintenance, DNA repair, and replication. SET domain containing (lysine methyltransferase) 7 (SETD7) (SET9; SET7/9, KMT7) is a protein lysine methyltransferases and is originally characterized as a monomethyltransferase of lysine 4 on histone H3 (H3K4me1). SET7/9 has very broad target specificity that methylates histone H3, tumor suppressor p53 and transcription factor TAF10 [1][2][3].
(S)-PFI-2 (hydrochloride), the inactive enantiomer of (R)-PFI-2, was 500-fold less potent with IC50 value of 1 μM and used as a negative control in chemical biology experiments. (R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase with IC50 value of 2 nM. In high-density MCF7 cells, (R)-PFI-2 dose-dependently increased nuclear YAP and enhanced expression of the YAP target genes AREG and CYR61, whereas (S)-PFI-2 had no effect [1].
References:
[1]. Barsyte-Lovejoy D, Li F, Oudhoff MJ, et al. (R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells. Proc Natl Acad Sci U S A. 2014 Sep 2;111(35):12853-8.
[2]. Kurash JK, Lei H, Shen Q, et al. Methylation of p53 by Set7/9 mediates p53 acetylation and activity in vivo. Mol Cell. 2008 Feb 15;29(3):392-400.
[3]. Couture JF, Collazo E, Hauk G, et al. Structural basis for the methylation site specificity of SET7/9. Nat Struct Mol Biol. 2006 Feb;13(2):140-6.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 536 |
Cas No. | 1627607-88-8 |
Formula | C23H25F4N3O3S·HCl |
Synonyms | (+)-PFI-2 |
Solubility | ≤0.5mg/ml in ethanol;2mg/ml in DMSO;5mg/ml in dimethyl formamide |
Chemical Name | 8-fluoro-1,2,3,4-tetrahydro-N-[(1S)-2-oxo-2-(1-pyrrolidinyl)-1-[[3-(trifluoromethyl)phenyl]methyl]ethyl]-6-isoquinolinesulfonamide, monohydrochloride |
SDF | Download SDF |
Canonical SMILES | O=S(C1=CC(CCNC2)=C2C(F)=C1)(N[C@@H](CC3=CC(C(F)(F)F)=CC=C3)C(N4CCCC4)=O)=O.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |