PFI-2

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Danger

• 危険有害性情報

  H315：皮膚刺激

  H318：重篤な眼の損傷

  H411：長期的影響により水生生物に毒性

• 注意書き

  P264：取扱い後は皮膚をよく洗うこと。

  P264：取扱い後は手や顔をよく洗うこと。

  P270：この製品を使用する時に、飲食または喫煙をしないこ と。

  P273：環境への放出を避けること。

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。

  P332+P313：皮膚刺激が生じた場合：医師の診断/手当てを受けるこ と。

  P391：漏出物を回収すること。

  P501：内容物/容器を．．．に廃棄すること。

PFI-2 化学特性,用途語,生産方法

• 使用

  PFI-2 is a potent and selective lysine methyltransferase SETD7 inhibitor which is a crucial factor in many disease related pathways.

• 酵素阻害剤

  This SETD7 inhibitor (FW = 499.52 g/mol; CAS 1627676-59-8; IUPAC: 8- fluoro-1,2,3,4-tetrahydro-N-[(1R)-2-oxo-2-(1-pyrrolidinyl)-1-[[3- (trifluoromethyl)phenyl]methyl]ethyl]-6-isoquinolinesulfonamide, targets the SET domain containing lysine methyltransferase, or SETD7 (Ki = 0.33 nM; IC50 = 2 nM), showing 1000-times selectivity versus other methyltransferases and other non-epigenetic targets. (R)-PFI-2 exhibits an unusual cofactor-dependent and substrate-competitive inhibitory mechanism by occupying the substrate peptide binding groove of SETD7, including the catalytic lysine-binding channel, and by making direct contact with the donor methyl group of the cofactor, S-adenosylmethionine. In murine embryonic fibroblasts, (R)-PFI-2 treatment phenocopies the effects of Setd7 deficiency on Hippo pathway signaling, via modulation of the transcriptional coactivator Yes-associated protein (YAP) and regulation of YAP target genes. In confluent MCF7 cells, (R)-PFI-2 rapidly alters YAP localization, suggesting continuous and dynamic regulation of YAP by the methyltransferase activity of SETD7.

PFI-2 生産企業

Global(48)Suppliers

PFI-2 スペクトルデータ(¹HNMR)

1627676-59-8, PFI-2 キーワード