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Submit ReviewLP 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.
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.
LP 99 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
M. Wt | 516.05 |
Formula | C26H30ClN3O4S |
Storage | Store at -20°C |
Purity | ≥98% (HPLC) |
CAS Number | 1808951-93-0 |
PubChem ID | 91827372 |
InChI Key | LVDRREOUMKACNJ-BKMJKUGQSA-N |
Smiles | CC(C(C=CC(N1[C@@H]([C@H](CCC1=O)NS(=O)(CC(C)C)=O)C2=CC=C(C=C2)Cl)=C3)=C3N4C)=CC4=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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 51.6 | 100 | |
ethanol | 51.6 | 100 |
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 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.
Keywords: LP 99, LP 99 supplier, LP99, selective, BRD7, BRD9, bromodomain, inhibitors, inhibits, Bromodomains, 5496, 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.
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