PFI-2 hydrochloride 是一种有效的、高度选择性的、具有细胞活性的 SETD7 甲基转移酶抑制剂，IC50值为2nM，活性是 (S)-PFI-2 的 500 倍。

PFI-2 hydrochloride is a potent, highly selective, and cell-active inhibitor of the methyltransferase activity of SETD7 (IC50: 2 nM), 500 fold active than (S)-PFI-2.

(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).

1627607-87-7

C23H26ClF4N3O3S

535.98

(R)-PFI-2 hydrochloride;PFI-2 HCl

DMSO:50 mg/mL
Ethanol:10 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years