(S)-PFI-2 (hydrochloride)
(Synonyms: (+)-PFI-2) 目录号 : GC13634
Negative control of (R)-PFI 2
Cas No.:1627607-88-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
(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].
References:
[1]. Barsyte-Lovejoy D, Li F, Oudhoff MJ, 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.
[2]. Kurash JK, Lei H, Shen Q, et al. Methylation of p53 by Set7/9 mediates p53 acetylation and activity in vivo. Mol Cell. 2008 Feb 15;29(3):392-400.
[3]. Couture JF, Collazo E, Hauk G, et al. Structural basis for the methylation site specificity of SET7/9. Nat Struct Mol Biol. 2006 Feb;13(2):140-6.
| Cas No. | 1627607-88-8 | SDF | |
| 别名 | (+)-PFI-2 | ||
| 化学名 | 8-fluoro-1,2,3,4-tetrahydro-N-[(1S)-2-oxo-2-(1-pyrrolidinyl)-1-[[3-(trifluoromethyl)phenyl]methyl]ethyl]-6-isoquinolinesulfonamide, monohydrochloride | ||
| Canonical SMILES | O=S(C1=CC(CCNC2)=C2C(F)=C1)(N[C@@H](CC3=CC(C(F)(F)F)=CC=C3)C(N4CCCC4)=O)=O.Cl | ||
| 分子式 | C23H25F4N3O3S • HCl | 分子量 | 536.0 |
| 溶解度 | ≤0.5mg/ml in ethanol;2mg/ml in DMSO;5mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8657 mL | 9.3284 mL | 18.6567 mL |
| 5 mM | 0.3731 mL | 1.8657 mL | 3.7313 mL |
| 10 mM | 0.1866 mL | 0.9328 mL | 1.8657 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。