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PFI-2
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图片
CAS NO:1627676-59-8
规格:98%
分子量:499.52
包装与价格:
包装价格(元)
5mg电议
25mg电议
50mg电议

产品介绍
SETD7 methyltransferase inhibitor
CAS:1627676-59-8
分子式:C23H25F4N3O3S
分子量:499.52
纯度:98%
存储:Store at -20°C

Background:

PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase with IC50 value of 2.0 nM [1].


SET domain containing (lysine methyltransferase) 7 (SETD7) is a protein lysine methyltransferase that acts as monomethyltransferase of lysine 4 on histone H3 (H3K4) and regulates DNA methyltransferase 1 (DNMT1) [1].


PFI-2 is a potent and selective SETD7 methyltransferase inhibitor. (R)-PFI-2 inhibited human SETD7 methyltransferase activity with IC50 value of 2.0 nM. However, (S)-PFI-2 was 500-fold less active with IC50 value of only 1.0 μM. (R)-PFI-2 potently inhibited SETD7 with Morrison Kiapp value of 0.33 nM. (R)-PFI-2 occupied the peptide binding groove and effectively inhibited the binding of SETD7 substrates. In the presence of 20 μM SAM, (R)-PFI-2 bound to SETD7 with KD value of 4.2 nM in a SAM-dependent way. In HEK293 cells, (R)-PFI-2 (10 μM) bound to and stabilized SETD7. In Setd7+/+ murine embryonic fibroblasts (MEFs), (R)-PFI-2 increased nuclear localization of Yes-associated protein (YAP) and the expression of YAP target genes Ctgf, Gli2 and Cdc20 [1].


Reference:
[1].  Barsyte-Lovejoy D, Li F, Oudhoff MJ, et al. (R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells. Proc Natl Acad Sci U S A, 2014, 111(35): 12853-12858.