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Postion:Product Catalog >Biochemical Engineering>Inhibitors>Epigenetics>Epigenetic Reader Domain inhibitors>PFI-1
PFI-1
  • PFI-1

PFI-1 NEW

Price $43 $70 $123
Package 5mg 10mg 25mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-16

Product Details

Product Name: PFI-1 CAS No.: 1403764-72-6
Purity: 98.59% Supply Ability: 10g
Release date: 2024/11/16

Product Introduction

Bioactivity

名稱PFI-1
描述PFI-1 (PF-6405761), a specific BET (bromodomain-containing protein) inhibitor for BRD4, is with the IC50 of 0.22 μM in a cell-free assay.
細(xì)胞實(shí)驗(yàn)To determine dose response, cells are aliquoted into 96-well plate at 5 × 103 cells per well in triplicates. PFI-1 is added by 2- or 4-fold serial dilutions. Cell number is measured 5 days after plating using the CellTiter-Glo Kit and normalized to corresponding vehicle-treated groups. IC50 values are calculated by the GraphPad Prism 5 software using the 4-parameter logistic nonlinear regression model. To calculate the relative growth of cells, averaged cell titers of each group on day 1 are assigned a value of 1. All subsequent cell titer values are normalized accordingly. (Only for Reference)
體外活性In rats, PFI-1, administered intravenously at a dose of 1 mg/kg, exhibits a distribution volume of 1 L/kg and a plasma clearance rate of 18 mL/kg per minute, with a half-life of 1 hour. Orally administered PFI-1 at a dose of 2 mg/kg demonstrates a low efficacy of 32%. When PFI-1 is administered subcutaneously to mice at a 2 mg/kg dose, the peak concentration (Cmax) reaches 58 ng/mL, the time to peak concentration (Tmax) is 1 hour, and the half-life is approximately 2 hours.
體內(nèi)活性In human monocytes stimulated by lipopolysaccharides, PFI-1 (EC50=1.89 μM) suppresses the production of IL-6. It also inhibits cell proliferation in three NET cell lines (pancreatic NET-derived Bon-1 and lung NET-derived H727 and H720). In T4302 CD133+ cells, PFI-1 induces a dose-dependent decrease in cell viability. PFI-1 (KD=49 μM) binds to the cAMP response element-binding protein.
存儲(chǔ)條件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度DMSO : 40 mg/mL (115.14 mM)
關(guān)鍵字Inhibitor | PFI-1 | inhibit | PF 6405761 | Apoptosis | Autophagy | PF6405761 | Epigenetic Reader Domain
相關(guān)產(chǎn)品Stavudine | 5-Fluorouracil | Sodium 4-phenylbutyrate | L-Ascorbic acid | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Tributyrin | Curcumin | Paeonol | Naringin | Gefitinib
相關(guān)庫(kù)高選擇性抑制劑庫(kù) | 細(xì)胞凋亡化合物庫(kù) | 組蛋白修飾化合物庫(kù) | 經(jīng)典已知活性庫(kù) | 表觀遺傳庫(kù) | 激酶抑制劑庫(kù) | 抑制劑庫(kù) | NO PAINS 化合物庫(kù) | 抗衰老化合物庫(kù) | 已知活性化合物庫(kù)

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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