SGC SMARCA-BRDVIII

Name: SGC SMARCA-BRDVIII
Brand: Tocris Bioscience
SKU: 7460

Tocris Bioscience, part of Bio-Techne | Catalog # 7460

COA / SDS

Potent and selective SMARCA2/4 and PB1(bromo 5)-selective SWI/SNF bromodomain inhibitor

Key Product Details

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% (HPLC)
Molecular Weight:	371.44

View Full Technical Details for SGC SMARCA-BRDVIII

Technical Data
Citations

Biological Activity for SGC SMARCA-BRDVIII

SGC-SMARCA-BRDVIII is a selective and high affinity SMARCA2/4 and PB1(bromo 5)-selective SWI/SNF bromodomains inhibitor (K_d(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).

Licensing Information

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.

Compound Libraries for SGC SMARCA-BRDVIII

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.

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 for SGC SMARCA-BRDVIII

M. Wt	371.44
Formula	C₁₉H₂₅N₅O₃
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	1997319-84-2
PubChem ID	137045929
InChi Key	AQTNUGRRZDRZIA-UHFFFAOYSA-N
Smiles	CC(C)(OC(N1CCN(C2=C(N=NC(C3=C(C=CC=C3)O)=C2)N)CC1)=O)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 for SGC SMARCA-BRDVIII

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	37.14	100
	ethanol	3.71	10

Preparing Stock Solutions for SGC SMARCA-BRDVIII

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

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Reconstitution Calculator

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References for SGC SMARCA-BRDVIII

References are publications that support the biological activity of the product.

Farnaby BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design. Nat.Chem.Biol. 2019 PMID: 31178587
Wanior Pan-SMARCA/PB1 bromodomain inhibitors and their role in regulating adipogenesis. J.Med.Chem. 2020 PMID: 33216538