(S)-PFI-2 hydrochloride 

(S)-PFI-2 hydrochloride is an inhibitor of lysine methyltransferase SETD7 and is approximately 500-fold more active than its enantiomer (R)-PFI-2. (R)-PFI-2 is a cofactor-dependent and substrate-competitive inhibitor. (R)-PFI-2 can occupy the substrate peptide binding groove of SETD7 (including the catalytic lysine binding channel) and interact with the cofactor The donor methyl group is in direct contact. However, (S)-PFI-2 was not observed to have the same interaction as (R)-PFI-2^[1][2].

Lysine methyltransferase SETD7^[1][2]

(S)-PFI-2 hydrochloride (10 μM; 2 h) 不能导致 MCF7 细胞中核 YAP 呈剂量依赖性增加，或者使 YAP 靶基因 AREG 和 CYR61 的表达增强；而 (R)-PFI-2 可以增加 YAP、AREG 和 CYR61 的表达^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

535.98

C₂₃H₂₆ClF₄N₃O₃S

1627607-88-8

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Niu Y, et al. Revealing inhibition difference between PFI-2 enantiomers against SETD7 by molecular dynamics simulations, binding free energy calculations and unbinding pathway analysis. Sci Rep. 2017 Apr 18;7:46547.  [Content Brief]

  [2]. Barsyte-Lovejoy D, 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 Sep 2;111(35):12853-8.  [Content Brief]