| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
|
Purity: ≥98%
PFI-3 (PFI3) is a potent, selective, acetyl-lysine-competitive, and cell-permeable inhibitor of SMARCA bromodomains (SMARCA2/4 and PB1(5)) with antineoplastic activity. It inhibits SMARCA2/4 bromodomains with Kd values of 55 and 110 nM, respectively.
| ln Vitro |
PFI-3 is a potent, cell-permeable probe capable of displacing ectopically produced, GFP-tagged SMARCA2-bromodomain from chromatin. PFI-3 binds aggressively to both SMARCA2 and SMARCA4 bromodomains (BROMOScan Kd's between 55 and 110 nM) comparable with the binding constant (Kd=89 nM) observed by isothermal titration calorimetry. PFI-3 does not phenocopy the growth inhibitory effects of SMARCA2 knockdown in lung cancer[1]. Exposure of embryonic stem cells to PFI-3 leads to deprivation of stemness and deregulates lineage specification. Furthermore, differentiation of trophoblast stem cells in the presence of PFI-3 is considerably enhanced[2]. PFI-3 binds to some family VIII bromodomains while demonstrating significant, broader bromodomain family selectivity. The remarkable specificity of PFI-3 for family VIII is accomplished through a new bromodomain binding method of a phenolic headgroup that results to the unusual displacement of water molecules that are normally maintained by most other bromodomain inhibitors described to date[3].
|
||
|---|---|---|---|
| ln Vivo |
|
||
| Animal Protocol |
|
||
| 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.
[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 |
| Molecular Formula |
C19H19N3O2
|
|
|---|---|---|
| Molecular Weight |
321.37
|
|
| CAS # |
1819363-80-8
|
|
| Related CAS # |
|
|
| SMILES |
OC1=C(C(/C=C/N2[ C@H](C3)CN(C4=NC=CC=C4)[ C@H]3C2)=O)C=CC=C1
|
|
| Synonyms |
|
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|---|
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Pharmacological inhibition of SMARCA2/4 bromodomain in lung cancer. Cancer Res. 2015 Sep 15; 75(18): 3865–3878. |
Pharmacological inhibition of SMARCA2/4 bromodomain in lung cancer. Cancer Res. 2015 Sep 15; 75(18): 3865–3878. |
PFI-3 is a potent, selective and cell permeable bromodomain inhibitor of SMARCA2/4. Cancer Res. 2015 Sep 15; 75(18): 3865–3878. |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
