应用
PFI-1 has been used as a bromodomain inhibitor in breast cancer cell line MCF7 dechorionated zebrafish embryos. It has also been used in human peripheral blood mononuclear cells (PBMCs), to inhibit the release of interleukin-6 in lipopolysaccharide (LPS) challenge assay.
生化/生理作用
PFI-1 is a quinazolinone inhibits androgen receptor (AR) mediated signaling in prostate cancer cells. It elicits minimum toxicity and is effective for anti-HIV-latency therapy. In leukemia cells, PFI-1 inhibits Aurora B kinase and promotes caspase-dependent apoptosis.
The human BET family, which includes BRD2, BRD3, BRD4 and BRDT, play a role in regulation of gene transcription. PFI-1 is a selective BET bromodomain inhibitor with activity at BRD2 (IC50 = 98 nM) and BRD4 (IC50 = 220 nM). For full characterization details, please visit the PFI-1 probe summary on the Structural Genomics Consortium (SGC) website.
To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
特点和优势
PFI-1 is an epigenetic chemical probe available through a partnership with the Structural Genomics Consortium (SGC). To learn more and view other SGC epigenetic probes, visit sigma.com/SGC.
This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
其他说明
PFI-1 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the PFI-1 probe summary on the Chemical Probes Portal website.
相关产品
产品编号
说明
价格
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Design and chemoproteomic functional characterization of a chemical probe targeted to bromodomains of BET family proteins
Wu J, et al.
MedChemComm, 5(12), 1871-1878 (2014)
Justin Hall et al.
Biochemical and biophysical research communications, 527(1), 250-256 (2020-05-25)
DNA-encoded libraries (DELs) can contain billions of unique chemical species; selecting against such large inputs, it is typical to find more candidate binders than is reasonable to pursue for follow-up synthesis and testing. Given this wealth of choices, common practice
A Chemical Screen Identifies Compounds Limiting the Toxicity of C9ORF72 Dipeptide Repeats
Corman A, et al.
Cell Chemical Biology, 26(2), 235-243 (2019)
Estrogen-dependent control and cell-to-cell variability of transcriptional bursting
Fritzsch C, et al.
Molecular Systems Biology, 14(2) (2018)
Panpan Lu et al.
Scientific reports, 7(1), 16646-16646 (2017-12-02)
Persistent latent reservoir in resting CD4+ T cells is a major obstacle in curing HIV-1 infection. Effective strategies for eradication of the HIV-1 reservoir are urgently needed. We report here for the first time that two BET inhibitors, RVX-208, which
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We offer a variety of small molecule research tools, such as transcription factor modulators, inhibitors of chromatin modifying enzymes, and agonists/antagonists for target identification and validation in gene regulation research; a selection of these research tools is shown below.
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