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NI 57 is a potent and selective BRPF bromodomain inhibitor (Kd values are 31, 108 and 408 nM, for BRPF1B, 2 and 3, respectively, which exhibits >32-fold selectivity for BRPFs over BRD9 and other non-Class IV bromodomains. NI 57 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 NI 57 probe summary on the SGC website.
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of NI 57 is reviewed on the chemical probes website.
NI 57 is also offered as part of the Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 383.42. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.61 mL||13.04 mL||26.08 mL|
|5 mM||0.52 mL||2.61 mL||5.22 mL|
|10 mM||0.26 mL||1.3 mL||2.61 mL|
|50 mM||0.05 mL||0.26 mL||0.52 mL|
References are publications that support the biological activity of the product.
Igoe et al (2017) Design of a chemical probe for the bromodomain and plant homeodomain finger-containing (BRPF) family of proteins. J.Med.Chem. 60 6998 PMID: 28714688
Meier et al (2017) Selective targeting of bromodomains of the bromodomain-PHD fingers family impairs osteoclast differentiation. ACS Chem.Biol. 12 2619 PMID: 28849908
If you know of a relevant reference for NI 57, please let us know.
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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.
Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:
Adapted from the 2015 Cancer Product Guide Edition 3, 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.