PFI-2
(Synonyms:PFI-2 抑制剂;8-氟-1,2,3,4-四氢-N-[(1R)-2-氧代-2-(1-吡咯烷基)-1-[[3-(三氟甲基)苯基]甲基]乙基]-6-异喹啉磺酰胺;PFI-2 盐酸盐)
目录号 : KG10472
CAS No. : 1627676-59-8
纯度 : 98%
PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase with IC50 value of 2.0 nM .
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) .
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 .
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分子式 |
C23H25F4N3O3S
|
分子量 |
499.52
|
CAS号 |
1627676-59-8
|
中文名称 |
PFI-2
|
储存方式 |
Store at -20°C
|