PFI-2 hydrochloride
CAS No. | 1627607-87-7 | Cat. No. | BCP19500 |
Name | PFI-2 hydrochloride | ||
Synonyms | PFI 2 hydrochloride;PFI2 hydrochloride; | ||
Formula | C23H26ClF4N3O3S | M. Wt | 535.98 |
Description | (R)-PFI-2 is highly selective (>1,000-fold) for SETD7, over a panel of 18 other human protein methyltransferases and DNMT1, and was shown to be inactive against 134 additional ion channel, GPCR, and enzyme targets (<35% inhibition at 10 μM). (R)-PFI-2 binds to SETD7 only in the presence of SAM. PFI-766, a biotinylated variant of (R)-PFI-2 that retains the ability to bind and inhibit SETD7 (IC50 110 ± 26 nM in our in vitro enzymatic assay). PFI-766 engagement of endogenous SETD7 was also confirmed by mass spectrometry that supported the high specificity of the compound for endogenous SETD7. | ||
Pathways | Epigenetics | ||
Targets | Histone Methyltransferase |
Structure
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