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Biological Activity for LP 99
LP 99 is a selective BRD7 and BRD9 inhibitor (Kd values are 99 and 909 nM, respectively) that exhibits selectivity for BRD7/9 over a panel of 48 bromodomains (at 10 μM). LP 99 inhibits interactions with histones H3.3 and H4 at low micromolar concentrations, and decreases the level of IL-6 secreted from LPS-stimulated THP-1 cells, in vitro. A negative control for LP 99, ent-LP 99 (Cat.No. 5497), is also available.
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the LP 99 probe summary on the SGC website.
External Portal Information for LP 99
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of LP 99 is reviewed on the chemical probes website.
Compound Libraries for LP 99
Technical Data for LP 99
|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.
Solubility Data for LP 99
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for LP 99
The following data is based on the product molecular weight 516.05. 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||1.94 mL||9.69 mL||19.38 mL|
|5 mM||0.39 mL||1.94 mL||3.88 mL|
|10 mM||0.19 mL||0.97 mL||1.94 mL|
|50 mM||0.04 mL||0.19 mL||0.39 mL|
References for LP 99
References are publications that support the biological activity of the product.
Clark et al (2015) LP99: discovery and synthesis of the first selective BRD7/9 bromodomain inhibitor. Angew.Chem.Int.Ed.Engl. 54 6217 PMID: 25864491
If you know of a relevant reference for LP 99, please let us know.
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Keywords: LP 99, LP 99 supplier, LP99, selective, BRD7, BRD9, bromodomain, inhibitors, inhibits, Bromodomains, 5496, Tocris Bioscience
Citations for LP 99
Citations are publications that use Tocris products.
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Reviews for LP 99
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Literature in this Area
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.
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
Epigenetics in Cancer Poster
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 Poster
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.