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PFI-2 HCl

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Chemical Structure| 1627607-87-7 同义名 : (R)-PFI-2 hydrochloride;(R)-PFI-2 (hydrochloride);(-)-PFI-2;PFI-2 hydrochloride
CAS号 : 1627607-87-7
货号 : A382439
分子式 : C23H26ClF4N3O3S
纯度 : 99%+
分子量 : 535.982
MDL号 : MFCD28133380
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(55.97 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 5.5 mg/mL(10.26 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • Histone Methyltransferase

    SETD7, Ki:0.33 nM

    SETD7, IC50:2 nM
描述 PFI-2 ((R)-PFI-2 hydrochloride) hydrochloride serves as a highly potent and specific inhibitor of the SET domain-containing lysine methyltransferase 7 (SETD7), with (R)-PFI-2 exhibiting an IC50 value of 2.0 nM, indicating strong inhibitory efficacy, while (S)-PFI-2 displays an IC50 value of 1.0 μM. This compound is utilized in the study of chronic kidney disease and the inflammatory responses that contribute to the development of renal fibrosis.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.87mL

0.37mL

0.19mL

9.33mL

1.87mL

0.93mL

18.66mL

3.73mL

1.87mL
参考文献

[1]Yuzhen Niu, et al. Revealing inhibition difference between PFI-2 enantiomers against SETD7 by molecular dynamics simulations, binding free energy calculations and unbinding pathway analysis. Sci Rep. 2017 Apr 18;7:46547.

[2]Benquan Liu, et al. Pharmacological inhibition of SETD7 by PFI-2 attenuates renal fibrosis following folic acid and obstruction injury. Eur J Pharmacol. 2021 Jun 15;901:174097.