PFI3
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Cat.No：IP3040 Solarbio
CAS：1819363-80-8
Storage：Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Solid
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> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Epigenetics > PFI3
Product Information
| CAS | 1819363-80-8 |
| Name | PFI3 |
| Molecular Formula | C19H19N3O2 |
| Molecular Weight | 321.37 |
| Solubility | Soluble in DMSO ≥5mg/mL(Need ultrasonic) |
| Purity | ≥98% |
| Appearance | Solid |
| Storage | Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD28100807 |
| SMILES | OC1=C(C(/C=C/N2[C@H](C3)CN(C4=NC=CC=C4)[C@H]3C2)=O)C=CC=C1 |
| Target Point | Epigenetic Reader Domain（SMARCA2/4） |
| Passage | Epigenetics |
| Background | PFI-3 is a potent and selective SMARCA2/4 bromodomain inhibitor. |
| Biological Activity | PFI-3是高效选择性，可渗透细胞的SMARCA2/4溴结构域抑制剂，Kd值为89 nM。[1-3] |
| IC50 | Kd: 89nM(SMARCA2/4)[1] |
| In Vitro | PFI-3是一种有效的细胞渗透性探针，能够从染色质中置换异位表达的GFP标记的SMARCA2-溴结构域。 PFI-3与SMARCA2和SMARCA4溴结构域(BROMOScan Kd在55和110nM之间)紧密结合，与通过等温滴定量热法测量的结合常数(Kd = 89nM)一致。 PFI-3不能模拟SMARCA2敲低对肺癌的生长抑制作用[1]。将胚胎干细胞暴露于PFI-3导致干燥剥夺并解除对谱系规格的控制。此外，在PFI-3存在下滋养层干细胞的分化显著增强[2]。 PFI-3与某些家族VIII溴结构域结合，同时显示出显著的，更广泛的溴结构域家族选择性。 PFI-3对VIII家族的高度特异性是通过酚类头部基团的新溴结构域结合模式实现的，该模式导致水分子的异常位移，这些水分子通常由迄今为止报道的大多数其他溴结构域抑制剂保留[3]。 |
| Kinase Experiment | 为了确定PFI-3是否嵌入DNA，使用DNA解旋测定法评估化合物。在小麦胚芽拓扑异构酶I存在下，将PFI-3(1，5或10μM)，顺铂或多柔比星与超螺旋pBR322一起在37℃温育30分钟。在存在或不存在酶的情况下用DMSO孵育的DNA作为对照。用丁醇和氯仿/异戊醇24：1萃取后，将DNA在1％(w / v)琼脂糖凝胶中用1-kb DNA梯度在80V下运行4小时。然后用SYBR Safe染色凝胶。紫外线可视化前30分钟[2]。 |
| Data Literature Source | [1]. Vangamudi B，et al. The SMARCA2/4 ATPase Domain Surpasses the Bromodomain as a Drug Target in SWI/SNF-Mutant Cancers: Insights from cDNA Rescue and PFI-3 Inhibitor Studies. Cancer Res. 2015 Sep 15;75(18):3865-78. [2]. Fedorov O，et al. Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance. Sci Adv. 2015 Nov 13;1(10):e1500723. [3]. Gerstenberger BS，et al. Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit. J Med Chem. 2016 May 26;59(10):4800-11 |
| Unit | Bottle |
| Specification | 2mg 5mg 10mg |
PFI-3是高效，选择性的 SMARCA2/4 溴结构域抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
Note：
1. The products are all for scientific research use only. Do not use it for medical, clinical diagnosis or treatment, food and cosmetics, etc. Do not store them in ordinary residential areas.
2. For your safety and health, please wear laboratory clothes, disposable gloves and masks.
3. The experimental results may be affected by many factors, after-sale service is limited to the product itself and does not involve other compensation.
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