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Submit ReviewOF 1 is a selective BRPF1B and BRPF2 bromodomain inhibitor (Kd values are 100 and 500 nM respectively). Exhibits 39-fold selectivity for BRPF1B and BRPF2 over BRD4. Accelerates FRAP recovery at 5 μM in a BRPF2 FRAP assay. Inhibits RANKL-induced differentiation of primary murine bone marrow cells and human primary monocytes into osteoclasts.
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the OF 1 probe summary on the SGC website.
OF 1 is also offered as part of the Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
M. Wt | 440.31 |
Formula | C17H18BrN3O4S |
Storage | Store at +4°C |
Purity | ≥98% (HPLC) |
CAS Number | 919973-83-4 |
PubChem ID | 35397514 |
InChI Key | YUNQZQREIHWDQT-UHFFFAOYSA-N |
Smiles | CN1C2=C(C=C(OC)C(NS(C3=C(C)C=C(Br)C=C3)(=O)=O)=C2)N(C)C1=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
References are publications that support the biological activity of the product.
Meier et al (2017) Selective targeting of bromodomains of the bromodomain-PHD fingers family impairs osteoclast differentiation. ACS Chem.Biol. 12 2619 PMID: 28849908
Keywords: OF 1, OF 1 supplier, OF1, selective, BRPF1B, BRPF2, bromodomain, inhibitors, inhibits, epigenetics, Bromodomains, 5289, Tocris Bioscience
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
Rheumatoid arthritis (RA) is a chronic destructive inflammatory autoimmune disease that results from a breakdown in immune tolerance, for reasons that are as yet unknown. This poster summarizes the pathology of RA and the inflammatory processes involved, as well as describing some of the epigenetic modifications associated with the disease and the potential for targeting these changes in the discovery of new treatments.