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SGC-SMARCA-BRDVIII is a selective and high affinity SMARCA2/4 and PB1(bromo 5)-selective SWI/SNF bromodomains inhibitor (Kd(ITC) values are 35, 36 and 13 nM, respectively). SGC-SMARCA-BRDVIII exhibits selectivity over 25 other bromodomain families and shows no off-target activity on 85 protein kinases screened using temperature-shift binding assays. SGC-SMARCA-BRDVIII suppresses formation of 3T3-L1 mouse fibroblasts into adipocytes (EC50 <1.0 μM).
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the SGC SMARCA-BRDVIII 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 SGC-SMARCA-BRDVIII is reviewed on the chemical probes website.
SGC SMARCA-BRDVIII is also offered as part of the Tocriscreen 2.0 Max and 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 371.44. 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||2.69 mL||13.46 mL||26.92 mL|
|5 mM||0.54 mL||2.69 mL||5.38 mL|
|10 mM||0.27 mL||1.35 mL||2.69 mL|
|50 mM||0.05 mL||0.27 mL||0.54 mL|
References are publications that support the biological activity of the product.
Wanior et al (2020) Pan-SMARCA/PB1 bromodomain inhibitors and their role in regulating adipogenesis. J.Med.Chem. 63 14680 PMID: 33216538
Farnaby et al (2019) BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design. Nat.Chem.Biol. 15 672 PMID: 31178587
If you know of a relevant reference for SGC SMARCA-BRDVIII, please let us know.
Keywords: SGC SMARCA-BRDVIII, SGC SMARCA-BRDVIII supplier, SGC-SMARCA-BRDVIII, selective, high, affinity, SMARCA2, SMARCA4, PBI, bromo, 5, bromodomains, Bromodomains, Other, ATPases, 7460, 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!
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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.
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