>>Signaling Pathways>> Chromatin/Epigenetics>> Histone Methyltransferase>>PFI-2

PFI-2 (Synonyms: (R)-PFI-2)

Catalog No.GC17956

PFI-2((R)-PFI-2 염산염) 염산염은 라이신 메틸트랜스퍼라제 7(SETD7) 억제제를 포함하는 강력하고 선택적인 SET 도메인입니다.

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PFI-2 Chemical Structure

Cas No.: 1627676-59-8

Size 가격 재고 수량
10mM (in 1mL DMSO)
US$97.00
재고 있음
5mg
US$54.00
재고 있음
25mg
US$182.00
재고 있음
50mg
US$320.00
재고 있음

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Sample solution is provided at 25 µL, 10mM.

Description Protocol Chemical Properties Product Documents Related Products

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.

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