PFI-2盐酸盐
货号：
IP3070
品牌：
Jinpan
暂无详情
产品简介
| 有效期 | 2年 |
| MDL | MFCD28133380 |
| 英文名称 | (R)-PFI-2 Hydrochloride |
| CAS | 1627607-87-7 |
| 分子式 | C23H25F4N3O3S·HCl |
| 分子量 | 535.98 |
| 储存条件 | 2-8℃ |
| 纯度 | ≥98% |
| 外观（性状） | White to off-white solid |
| 单位 | 瓶 |
| 生物活性 | PFI-2 hydrochloride is a a first-in-class, potent, highly selective, and cell-active inhibitor of the methyltransferase activity of SETD7 with IC50 of 2 nM, 500 fold active than (S)-PFI-2. IC50 value: 2 nM [1] |
| In Vitro | SETD7 (R)-PFI-2 is highly selective (>1,000-fold) for SETD7, over a panel of 18 other human protein methyltransferases and DNMT1, and was shown to be inactive against 134 additional ion channel, GPCR, and enzyme targets (<35% inhibition at 10 μM). (R)-PFI-2 binds to SETD7 only in the presence of SAM. PFI-766, a biotinylated variant of (R)-PFI-2 that retains the ability to bind and inhibit SETD7 (IC50 110 ± 26 nM in our in vitro enzymatic assay). [1] |
| SMILES | O=S(C1=CC2=C(CNCC2)C(F)=C1)(N[C@H](CC3=CC=CC(C(F)(F)F)=C3)C(N4CCCC4)=O)=O.[H]Cl |
| 靶点 | SETD7 |
| 数据来源文献 | [1]. 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. |
| 规格 | 5mg 10mg |
PFI-2是一种强效的，有选择性和细胞活性的lysine methyltransferase SETD7抑制剂。