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Technical Data
| Formula | C19H19N3O2 |
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| Molecular Weight | 321.37 | CAS No. | 1819363-80-8 | |
| Solubility (25°C)* | In vitro | DMSO | 64 mg/mL (199.14 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | PFI-3 is a selective chemical probe for SMARCA bromodomains, including SMARCA2, SMARCA4 and PB1(5) bromodomains. | ||||||||
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| In vitro | PFI-3 shows a significant selectivity for PB1(5) and SMARCA2/4 over 36 other tested kinases[1]. PFI-3 is a potent and cell active protein interaction inhibitor that selectively binds to essential BAF bromodomains. PFI-3 is screened in a commercial screening panel comprising 102 cellular receptors as well as 30 enzyme assays, revealing only interactions against four GPCRs with micromolar affinity and no significant additional interactions outside the BRD family, confirming its excellent broader pharmacological selectivity. Stability measurements confirmed that PFI-3 has a half-life in aqueous solutions exceeding 7 days at 37°C. In long-term experiments, PFI-3 significantly altered gene expression programs that are important for differentiation of stem cells. PFI-3 mimics the effect of Brg1 deletion, resulting in an increase of the repressive H3K27me3 mark at the TSSs and Stat3 binding sites of these genes[2]. PFI-3 has a half-life of >250 h in PBS, pH 7.4, at 20 °C[3]. |
Protocol (from reference)
| Cell Assay: |
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References
Customer Product Validation
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Data from [Data independently produced by , , Exp Cell Res, 2018, 364(2):191-197]
Selleck's PFI-3 has been cited by 13 publications
| RNF138 inhibits late inflammatory gene transcription through degradation of SMARCC1 of the SWI/SNF complex [ Cell Rep, 2023, 42(2):112097] | PubMed: 36800290 |
| Brahma-related gene 1 acts as a profibrotic mediator and targeting it by micheliolide ameliorates peritoneal fibrosis [ J Transl Med, 2023, 21(1):639] | PubMed: 37726857 |
| Brahma-related gene 1 acts as a profibrotic mediator and targeting it by micheliolide ameliorates peritoneal fibrosis [ J Transl Med, 2023, 21(1):639] | PubMed: 37726857 |
| Actionable Cytopathogenic Host Responses of Human Alveolar Type 2 Cells to SARS-CoV-2 [ Mol Cell, 2020, 80(6):1104-1122.e9] | PubMed: 33259812 |
| Dual roles of chromatin remodeling protein BRG1 in angiotensin II-induced endothelial-mesenchymal transition [ Cell Death Dis, 2020, 11(7):549] | PubMed: 32683412 |
| BRG1 Stimulates Endothelial Derived Alarmin MRP8 to Promote Macrophage Infiltration in an Animal Model of Cardiac Hypertrophy [ Front Cell Dev Biol, 2020, 8:569] | PubMed: 32733885 |
| Chemical Genetics Screen Identifies Epigenetic Mechanisms Involved in Dopaminergic and Noradrenergic Neurogenesis in Zebrafish. [ Front Genet, 2020, 11:80] | PubMed: 32158467 |
| The maternal to zygotic transition regulates genome-wide heterochromatin establishment in the zebrafish embryo [ Nat Commun, 2019, 10(1):1551] | PubMed: 30948728 |
| Dynamic reversal of random X-Chromosome inactivation during iPSC reprogramming. [ Genome Res, 2019, 29(10):1659-1672] | PubMed: 31515287 |
| Targeting CDK9 Reactivates Epigenetically Silenced Genes in Cancer [Zhang H, et al. Cell, 2018, 175(5):1244-1258] | PubMed: 30454645 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.