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PFI-2 HCl

(CAS No:1627676-59-8)
PFI-2 is a potent, selective, and cell-active lysine methyltransferase SETD7 inhibitor with Ki (app) and IC50 of 0.33 nM and 2 nM, 1000-fold selectivity over other methyltransferases and other non-epigenetic targets.
CAS No:1627676-59-8
Molecular Weight(MW):499.52
Purity:99.00%
Specification:500MG;1G;5G;10G;50G;100G
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QC Documents
 COA  MSDS  HPLC  NMR
ChemicalInfomation
CAS No: 1627676-59-8
Molecular formula(MF) C23H25F4N3O3S
Molecular Weight(MW): 499.52
Alias
Solubility
In vitro DMSO 99 mg/mL (198.19 mM)
Ethanol 66 mg/mL warmed (132.12 mM)
Water 4 mg/mL warmed (8.0 mM)
In vivo
Biological Activity
Description PFI-2 is a potent, selective, and cell-active lysine methyltransferase SETD7 inhibitor with Ki (app) and IC50 of 0.33 nM and 2 nM, 1000-fold selectivity over other methyltransferases and other non-epigenetic targets.
Targets
SETD7 [1] SETD7 [1]
0.33 nM(Ki) 2 nM
In vitro

(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. [1]