PFI 3 |
| Catalog No.GC14361 |
inhibitor of polybromo 1 and SMARCA4
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1819363-80-8
Sample solution is provided at 25 µL, 10mM.
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PFI 3 is a potent and selective inhibitor of polybromo 1 and SMARCA4 with Kd values of 48 and 89 nM, respectively [1].
Transcription activator BRG1 (SMARCA4) is a member of the SWI/SNF family and regulates transcription. Protein polybromo-1 (PB1, PBRM1) is a BRG1-associated factor and tumor suppressor.
PFI 3 is a potent and selective inhibitor of polybromo 1 and SMARCA4. PFI 3 bound to SMARCA2 and SMARCA4 bromodomains with Kd values of 55 and 110 nM, respectively. PFI-3 (2 μM) inhibited PBRM1 by 70%. In cell-based chromatin binding assays, PFI-3 replaced GFP-tagged SMARCA2 bromodomain in a dose-dependent way with IC50 value of 5.78 μM. PFI-3 was a cell-permeable probe suitable for studying SMARCA2/4 bromodomains. In the SMARCA4-deficient A549, H1299, H157 cell lines, PFI-3 had no anti-proliferative effects and was unable to replace SMARCA2 from chromatin. In THP-1 and MV4-11 leukemic cells, PFI 3 did not induce anti-cancer phenotype [1].
Reference:
[1]. Vangamudi B, Paul TA, Shah PK, 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, pii: canres.3798.2015.
Kinase experiment: | To establish whether PFI-3 intercalates DNA, the compound is assessed using a DNA unwinding assay. PFI-3 (1, 5, or 10 μM), cisplatin, or doxorubicin is incubated with supercoiled pBR322, in the presence of wheat germ topoisomerase I, for 30 min at 37°C. DNA incubated with DMSO in the presence or absence of the enzyme is run as control. After extraction by butanol and chloroform/isoamyl alcohol 24:1, the DNA is run in a 1% (w/v) agarose gel with a 1-kb DNA ladder for 4 hours at 80 V. The gel is then stained with SYBR Safe for 30 min before ultraviolet visualization[2]. |
References: [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. | |
| Cas No. | 1819363-80-8 | SDF | |
| Canonical SMILES | O=C(C1=CC=CC=C1O)/C=C/N(C2)[C@@H]3C[C@H]2N(C4=NC=CC=C4)C3 | ||
| Formula | C19H19N3O2 | M.Wt | 321.37 |
| Solubility | ≥ 15.15mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.1117 mL | 15.5584 mL | 31.1168 mL |
| 5 mM | 0.6223 mL | 3.1117 mL | 6.2234 mL |
| 10 mM | 0.3112 mL | 1.5558 mL | 3.1117 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 1 reference(s) in Google Scholar.)
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