SGC SMARCA-BRDVIII

Catalog # Availability Size / Price Qty
7460/10
7460/50
SGC SMARCA-BRDVIII | CAS No. 1997319-84-2 | Bromodomain Inhibitors
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Description: Potent and selective SMARCA2/4 and PB1(bromo 5)-selective SWI/SNF bromodomain inhibitor

Chemical Name: 1,1-Dimethylethyl 4-[3-amino-6-(2-hydroxyphenyl)-4-pyridazinyl]-1-piperazinecarboxylate bromodomains

Purity: ≥98%

Product Details
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Biological Activity

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).

External Portal Information

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.

Technical Data

M.Wt:
371.44
Formula:
C19H25N5O3
Solubility:
Soluble to 100 mM in DMSO and to 10 mM in ethanol
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
1997319-84-2

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.

Additional Information

Licensing Caveats:
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.

Background References

  1. BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design.
    Farnaby et al.
    Nat.Chem.Biol., 2019;15:672

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