PFI-3 - Epigenetic Reader Domain 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPFI-3Cat. No.: HY-12409CAS No.: 1819363-80-8分式: CHNO分量: 321.37作靶点: Epigenetic Reader Domain作通路: Epigenetics储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 125 mg/mL (388.96 mM; Need ultraso

2、nic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.1117 mL 15.5584 mL 31.1168 mL5 mM 0.6223 mL 3.1117 mL 6.2234 mL10 mM 0.3112 mL 1.5558 mL 3.1117 mL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，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；

3、以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.25 mg/mL (7.00 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.25 mg/mL (7.00 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.25 mg/mL (7.00 mM); Cle

4、ar solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 PFI-3效，选择性，可渗透细胞的 SMARCA2/4 溴结构域抑制剂，Kd 值为89 nM。IC50 & Target Kd: 89 nM (SMARCA2/4) 1体外研究 PFI-3 is a potent, cell-permeable probe capable of displacing ectopically expressed, GFP-tagged SMARCA2-bromodomain from chromat

5、in. PFI-3 binds avidly to both SMARCA2 and SMARCA4 bromodomains(BROMOScan Kds between 55 and 110 nM) consistent with the binding constant (Kd=89 nM) measured byisothermal titration calorimetry. PFI-3 does not phenocopy the growth inhibitory effects of SMARCA2knockdown in lung cancer 1. Exposure of e

6、mbryonic stem cells to PFI-3 leads to deprivation of stemnessand deregulates lineage specification. Furthermore, differentiation of trophoblast stem cells in the presenceof PFI-3 is markedly enhanced 2. PFI-3 binds to certain family VIII bromodomains while displayingsignificant, broader bromodomain

7、family selectivity. The high specificity of PFI-3 for family VIII is achievedthrough a novel bromodomain binding mode of a phenolic headgroup that leads to the unusual displacementof water molecules that are generally retained by most other bromodomain inhibitors reported to date 3.PROTOCOLKinase As

8、say 2 To establish whether PFI-3 intercalates DNA, the compound is assessed using a DNA unwinding assay. PFI-3 (1, 5, or 10 M), cisplatin, or doxorubicin is incubated with supercoiled pBR322, in the presence of wheatgerm topoisomerase I, for 30 min at 37C. DNA incubated with DMSO in the presence or

9、absence of theenzyme is run as control. After extraction by butanol and chloroform/isoamyl alcohol 24:1, the DNA is run in a1% (w/v) agarose gel with a 1-kb DNA ladder for 4 hours at 80 V. The gel is then stained with SYBR Safe for30 min before ultraviolet visualization 2.MCE has not independently c

10、onfirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Patent. US20180263995A1.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Vangamudi B, et al. The SMARCA2/4 ATPase Domain Surpasses the Bromodomain as a Drug Target in SWI/SNF-Mutant Cancers:Insights

11、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 MedChem. 2016 May 26;59(10):4800-11.McePdfHeight2/2 Master of Small Molecules 您边的抑制剂师www.MedChemECaution: Product