COA | MSDS | HPLC | NMR |
CAS No: | 1627676-59-8 |
Molecular formula(MF) | C23H25F4N3O3S |
Molecular Weight(MW): | 499.52 |
Alias |
In vitro | DMSO | 99 mg/mL (198.19 mM) |
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Ethanol | 66 mg/mL warmed (132.12 mM) | |
Water | 4 mg/mL warmed (8.0 mM) | |
In vivo |
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. | ||||
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Targets |
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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] |