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Submit ReviewBAY 299 is a potent and selective BRD1 and TAF1 inhibitor (IC50 values are 6-67 and 8-13 nM, respectively). Displays selectivity over other bromodomains (>30-fold over other members of the BRPF family; BRD9 and ATAD2; >300-fold over BRD4). Displays BRD1 and TAF1 inhibition in a NanoBRET cell assay. Inhibits binding of BRD1 and TAF1 to histone H4 (IC50 values are 575 nM and 0.9 μM, respectively) and histone H3.3 (IC50 values are 825 nM and 1.4 μM, respectively).
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the BAY 299 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 BAY 299 is reviewed on the Chemical Probes website.
BAY 299 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。
分子量 | 429.47 |
公式 | C25H23N3O4 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 2080306-23-4 |
PubChem ID | 122705990 |
InChI Key | OFWWWKWUCDUISA-UHFFFAOYSA-N |
Smiles | OCCCC1=CC=C(C(N2C3=C(C)C=C(N(C)C(N4C)=O)C4=C3)=O)C5=C1C=CC=C5C2=O |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 42.95 | 100 |
以下数据基于产品分子量 429.47。 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 | 2.33 mL | 11.64 mL | 23.28 mL |
5 mM | 0.47 mL | 2.33 mL | 4.66 mL |
10 mM | 0.23 mL | 1.16 mL | 2.33 mL |
50 mM | 0.05 mL | 0.23 mL | 0.47 mL |
参考文献是支持产品生物活性的出版物。
Klein et al (2014) Crosstalk between epigenetic readers regulates the MOZ/MORF HAT complexes. Epigenetics 9 186 PMID: 24169304
Bouche et al (2017) Benzoisoquinolinediones as potent and selective inhibitors of BRPF2 and TAF1/TAF1L bromodomains. J.Med.Chem. 60 4002 PMID: 28402630
If you know of a relevant reference for BAY 299, please let us know.
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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!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
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.
Rheumatoid arthritis (RA) is a chronic destructive inflammatory autoimmune disease that results from a breakdown in immune tolerance, for reasons that are as yet unknown. This poster summarizes the pathology of RA and the inflammatory processes involved, as well as describing some of the epigenetic modifications associated with the disease and the potential for targeting these changes in the discovery of new treatments.