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Submit ReviewSGC SMARCA-BRDVIII
说明： Potent and selective SMARCA2/4 and PB1(bromo 5)-selective SWI/SNF bromodomain inhibitor
化学名： 1,1-Dimethylethyl 4-[3-amino-6-(2-hydroxyphenyl)-4-pyridazinyl]-1-piperazinecarboxylate bromodomains
纯度： ≥98% (HPLC)
生物活性 for SGC SMARCA-BRDVIII
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).
许可信息
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.
External Portal Information for SGC SMARCA-BRDVIII
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.
化合物库 for SGC SMARCA-BRDVIII
SGC SMARCA-BRDVIII is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。
技术数据 for SGC SMARCA-BRDVIII
| 分子量 | 371.44 |
| 公式 | C19H25N5O3 |
| 储存 | Store at -20°C |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for SGC SMARCA-BRDVIII
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 37.14 | 100 | |
| ethanol | 3.71 | 10 |
制备储备液 for SGC SMARCA-BRDVIII
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for SGC SMARCA-BRDVIII
参考文献 for SGC SMARCA-BRDVIII
参考文献是支持产品生物活性的出版物。
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.
按产品操作查看相关产品
关键词: 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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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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