(S)-PFI-2 (hydrochloride)
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产品名称:
(S)-PFI-2 (hydrochloride)
产品型号:
GOY-Y3537
产品展商:
谷研
产品文档:
无相关文档
发布时间:2023-05-08
简单介绍
(S)-PFI-2 (hydrochloride)≤0.5mg/ml in ethanol;2mg/ml in DMSO;5mg/ml in dimethyl formamide
(S)-PFI-2 (hydrochloride)
的详细介绍
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性能参数
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产品名称
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(S)-PFI-2 (hydrochloride)
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规格
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1mg 5mg 10mg
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货号
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GOY-Y3537
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含量
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>98.00%
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CAS
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1627607-88-8
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别名
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(+)-PFI-2
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化学名
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8-fluoro-1,2,3,4-tetrahydro-N-[(1S)-2-oxo-2-(1-pyrrolidinyl)-1-[[3-(trifluoromethyl)phenyl]methyl]ethyl]-6-isoquinolinesulfonamide, monohydrochloride
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分子式
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C23H25F4N3O3S ? HCl
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分子量
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分子量 536.0
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溶解度
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≤0.5mg/ml in ethanol;2mg/ml in DMSO;5mg/ml in dimethyl formamide
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储存条件
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Store at -20°C
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General tips
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用途
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仅供科研
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价格
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电询
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详细内容
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(S)-PFI-2 (hydrochloride) is the inactive enantiomer of (R)-PFI-2 and may serve as a negative control. (R)-PFI-2 is a cell-permeable and potent SET7/9 inhibitor with IC50 value of 2 nM [1].
Protein methyltransferases involve in the epigenetic regulation of gene transcription, silencing, chromatin structure establishment, maintenance, DNA repair, and replication. SET domain containing (lysine methyltransferase) 7 (SETD7) (SET9; SET7/9, KMT7) is a protein lysine methyltransferases and is originally characterized as a monomethyltransferase of lysine 4 on histone H3 (H3K4me1). SET7/9 has very broad target specificity that methylates histone H3, tumor suppressor p53 and transcription factor TAF10 [1][2][3].
(S)-PFI-2 (hydrochloride), the inactive enantiomer of (R)-PFI-2, was 500-fold less potent with IC50 value of 1 μM and used as a negative control in chemical biology experiments. (R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase with IC50 value of 2 nM. In high-density MCF7 cells, (R)-PFI-2 dose-dependently increased nuclear YAP and enhanced expression of the YAP target genes AREG and CYR61, whereas (S)-PFI-2 had no effect [1].
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