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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-PFI-2 hydrochloride
PFI-2 hydrochloride

Chemical Structure : PFI-2 hydrochloride

CAS No.: 1627607-87-7

PFI-2 hydrochloride ((R)-PFI-2 hydrochloride)

货号: PC-45489Not For Human Use, Lab Use Only.

PFI-2 ((R)-PFI-2) hydrochloride is a first-in-class, potent and selective inhibitor of SETD7 methyltransferase with Ki app/IC50 of 0.33/2 nM, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

PFI-2 ((R)-PFI-2) hydrochloride is a first-in-class, potent and selective inhibitor of SETD7 methyltransferase with Ki app/IC50 of 0.33/2 nM, respectively.
PFI-2 shows high selectivity (>1,000-fold) for SETD7 over 18 other methyltransferases and DNMT1, 500-fold more active than enantiomer (S)-PFI-2.
PFI-2 increases YAP nuclear localization, regulates YAP target genes, and phenocopys the effects of Setd7 deficiency on Hippo pathway signaling in murine embryonic fibroblasts.

物理化学性质&存储条件

分子量 535.9825
分子式 C23H26ClF4N3O3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: ≥ 32 mg/mL

Chemical Name/SMILES

6-Isoquinolinesulfonamide, 8-fluoro-1,2,3,4-tetrahydro-N-[(1R)-2-oxo-2-(1-pyrrolidinyl)-1-[[3-(trifluoromethyl)phenyl]methyl]ethyl]-, hydrochloride (1:1)

参考文献

1. Barsyte-Lovejoy D, et al. Proc Natl Acad Sci U S A. 2014 Sep 2;111(35):12853-8.

2. Niu Y, et al. Sci Rep. 2017 Apr 18;7:46547.

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