PFI-2 HCl

製品コードS7294 バッチS729401

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C23H25F4N3O3S.HCl
分子量 535.98 CAS No. 1627607-87-7
Solubility (25°C)* 体外 DMSO 99 mg/mL (184.7 mM)
Ethanol 66 mg/mL warmed with 50ºC water bath (123.13 mM)
Water 4 mg/mL warmed with 50ºC water bath (7.46 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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生物活性

製品説明 PFI-2 is a potent, selective, and cell-active lysine methyltransferase SETD7 inhibitor with Ki (app) and IC50 of 0.33 nM and 2 nM, 1000-fold selectivity over other methyltransferases and other non-epigenetic targets.
in vitro (R)-PFI-2 shows 500-fold more inhibitory activity against human SETD7 than its enantiomer, (S)-PFI-2. In a cellular environment, through direct interactions with SETD7, affects Yes-Associated protein localization and phenocopies Setd7 genetic deletion on Hippo pathway signaling. [1]

プロトコル(参考用のみ)

キナーゼアッセイ IC50 and Morrison Ki determination
The reaction mixtures containing 2 nM SETD7, 2μM biotinylated peptide H3 (1-25) and 2 μM SAM in 20 mM Tris, pH 8, 5 mM DTT and 0.01% Triton X-100 are incubated for 1 hour at 23℃. Compound concentration is varied from 0.3 nM to 5μM (IC50 determination) and 0.04 to 125 nM (Ki determination). All reactions (in 10 μM) started by adding 3H-SAM and stopped by addition of 10 μM of 7.5 M guanidine hydrochloride. 60μM of buffer (20 mM Tris, pH 8) is added, mixed and transferred to a 384-well FlashPlate. The reaction mixtures in Flash plate are incubated for 1 hour and the CPM counts are measured using Topcount plate reader. The CPM counts in the absence of compound for each data set are defined as 100% activity. In the absence of the enzyme, the CPM counts in each data set are defined as background (0%). The data points are fitted to Morrison equation using GraphPad Prism 6. The IC50 values are determined using GraphPad Prism 6 with Sigmoidal 4PL equation.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

H4K20me1 plays a dual role in transcriptional regulation of regeneration and axis patterning in Hydra [ Life Sci Alliance, 2023, 6(5)e202201619] PubMed: 36944423
BRD4770 functions as a novel ferroptosis inhibitor to protect against aortic dissection [ Pharmacol Res, 2022, 177:106122] PubMed: 35149187
Recapitulating early human development with 8C-like cells [ Cell Rep, 2022, 39(12):110994] PubMed: 35732112
SETD7 mediates spinal microgliosis and neuropathic pain in a rat model of peripheral nerve injury. [ Brain Behav Immun, 2019, 82:382-395] PubMed: 31505256
Epigenetic Reprogramming with Antisense Oligonucleotides Enhances the Effectiveness of Androgen Receptor Inhibition in Castration-Resistant Prostate Cancer [ Cancer Res, 2018, 78(20):5731-5740] PubMed: 30135193
[ Cell Death Dis, 2018, ] PubMed: 29988031

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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