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PFI-2 HCl
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PFI-2 HCl图片
CAS NO:1627607-87-7
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)535.98
FormulaC23H25F4N3O3S. HCl
CAS No.1627607-87-7
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 32 mg/mL
Water: NA
Ethanol: NA
Other info

Chemical Name: (R)-8-fluoro-N-(1-oxo-1-(pyrrolidin-1-yl)-3-(3-(trifluoromethyl)phenyl)propan-2-yl)-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide hydrochloride

InChi Key: ZADKZNVAJGEFLC-ZMBIFBSDSA-N

InChi Code: InChI=1S/C23H25F4N3O3S.ClH/c24-20-13-18(12-16-6-7-28-14-19(16)20)34(32,33)29-21(22(31)30-8-1-2-9-30)11-15-4-3-5-17(10-15)23(25,26)27;/h3-5,10,12-13,21,28-29H,1-2,6-9,11,14H2;1H/t21-;/m1./s1

SMILES Code: O=S(C1=CC2=C(CNCC2)C(F)=C1)(N[C@H](CC3=CC=CC(C(F)(F)F)=C3)C(N4CCCC4)=O)=O.[H]Cl

Synonyms

PFI-2; PFI2; PFI 2; PFI-2 hydrochloride

实验参考方法
In Vitro

In vitro activity: (R)-PFI-2 shows 500-fold more inhibitory activity against human SETD7 than its enantiomer, (S)-PFI-2. In a cellular environment, through direct interactions with SETD7, affects Yes-Associated protein localization and phenocopies Setd7 genetic deletion on Hippo pathway signaling.


Kinase Assay: The reaction mixtures containing 2 nM SETD7, 2 uM biotinylated peptide H3 (1-25) and 2 uM SAM in 20 mM Tris, pH 8, 5 mM DTT and 0.01% Triton X-100 were incubated for 1 hour at 23°C. Compound concentration was varied from 0.3 nM to 5 uM. All reactions (in 10 ul) started by adding 3H-SAM and stopped by addition of 10 ul of 7.5 M guanidine hydrochloride. 60 ul of buffer (20 mM Tris, pH 8) was added, mixed and transferred to a 384-well FlashPlate (Cat. # SMP410A001PK; Perkin Elmer; www.perkinelmer.com). The reaction mixtures in Flash plate were incubated for 1 hour and the CPM counts were measured using Topcount plate reader ((Perkin Elmer, www.perkinelmer.com). The CPM counts in the absence of compound for each data set were defined as 100% activity. In the absence of the enzyme, the CPM counts in each data set were defined as background (0%). The IC50 values were determined using GraphPad Prism 6 with Sigmoidal 4PL equation. Cell assay [1] Compound stability was checked in the media with and without cell. Samples were analyzed using Waters Synapt G2 S Quadruple Time-of-flight (Q-Tof) hybrid mass spectrometer (MS) system coupled with second generation ACQUITY ultra-performance liquid chromatography (UPLC-II). Chromatographic separations were carried out on an ACQUITY UPLC BEH C18 (2.1 X 50 mm, 1.7 um) column. The mobile phase was 0.1% formic acid in water (solvent A) and 0.1% formic acid in acetonitrile (solvent B). Compound concentrations were measured as relative peak areas at various time points.

In Vivo
Animal model
Formulation & Dosage
References

Proc Natl Acad Sci U S A. 2014 Sep 2;111(35):12853-8.