High affinity BRPF inhibitor (Kd values are 40, 210 and 943 nM for BRPF1B, 2 and 3, respectively). Also exhibits modest activity at BRD9 (Kd = 1130 nM). Exhibits selectivity for BRPF over 44 other bromodomains. Orally bioavailable.
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. NI 42 is listed on the Chemical Probes website.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 353.39. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.5 mM||5.66 mL||28.3 mL||56.59 mL|
|2.5 mM||1.13 mL||5.66 mL||11.32 mL|
|5 mM||0.57 mL||2.83 mL||5.66 mL|
|25 mM||0.11 mL||0.57 mL||1.13 mL|
References are publications that support the biological activity of the product.
Igoe et al (2017) Design of a biased potent small molecule inhibitor of the bromodomain and PHD finger-containing (BRPF) proteins suitable for cellular and in vivo studies. J.Med.Chem PMID: 28068087
If you know of a relevant reference for NI 42, please let us know.
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Keywords: NI 42, NI 42 supplier, NI42, Bromodomains, PHD, fingers, BRPF, inhibitors, inhibits, orally, available, 5786, Tocris Bioscience
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Literature in this Area
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Epigenetics Scientific Review
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.
Epigenetics Research Bulletin
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:
- DNA Methyltransferases
- Histone Deacetylases
- Histone Demethylases
- Histone Methyltransferases
Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.