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说明： Potent and selective pan-BD2 inhibitor; orally bioavailable
别名： GSK046
化学名： 4-(Acetylamino)-3-fluoro-N-(trans-4-hydroxycyclohexyl)-5-[(1S)-1-phenylethoxy]benzamide
纯度： ≥98% (HPLC)
生物活性 for iBET-BD2
iBET-BD2 is a potent and selective pan-BD2 inhibitor (IC50 values are 49, 98, 214 and 264 nM for BRD4BD2, BRD3BD2, BRDTBD2 and BRD2BD2, respectively). iBET-BD2 is selective for BD2 over BD1 (IC50 values are 10965, 36317, 70558, and >50119 µM for BRD2BD1, BRD3BD1, BRD4BD1, and BRDTBD1, respectively) in a time-resolved FRET (TR-FRET) assay. iBET-BD2 (1 μM) inhibits IFN-γ-induced protein expression of MHC class I in K562 cells. iBET-BD2 reduces the production of anti-KLH IgM antibodies in mice immunized with keyhole limpet hemocyanin (KLH). iBET-BD2 exhibits immunomodulatory activity. iBET-BD2 is orally bioavailable.
许可信息
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the iBET-BD2 probe summary on the SGC website.
化合物库 for iBET-BD2
iBET-BD2 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 iBET-BD2
| 分子量 | 414.48 |
| 公式 | C23H27FN2O4 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 2474876-09-8 |
| PubChem ID | 146018690 |
| InChI Key | FRBRZGLUFOZRGD-JVPBZIDWSA-N |
| Smiles | C[C@@H](C1=CC=CC=C1)OC2=C(C(F)=CC(C(N[C@H]3CC[C@@H](CC3)O)=O)=C2)NC(C)=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.
溶解性数据 for iBET-BD2
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 41.45 | 100 | |
| ethanol | 41.45 | 100 |
制备储备液 for iBET-BD2
以下数据基于产品分子量 414.48。 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 | 2.41 mL | 12.06 mL | 24.13 mL |
| 5 mM | 0.48 mL | 2.41 mL | 4.83 mL |
| 10 mM | 0.24 mL | 1.21 mL | 2.41 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
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产品说明书 for iBET-BD2
参考文献 for iBET-BD2
参考文献是支持产品生物活性的出版物。
Gilan et al (2020) Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation. Science 368 387 PMID: 32193360
Preston et al (2020) Design and synthesis of a highly selective and in vivo-capable inhibitor of the second bromodomain of the bromodomain and extra terminal domain family of proteins. J.Med.Chem. 63 9070 PMID: 32691591
If you know of a relevant reference for iBET-BD2, please let us know.
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关键词: iBET-BD2, iBET-BD2 supplier, GSK046, GSK-046, GSK, 046, iBET, BD2, iBETBD2, pan-BD2, selective, inhibitors, inhibits, SGC, Bromodomains, 7458, Tocris Bioscience
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引用文献是使用了 Tocris 产品的出版物。
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该领域的文献
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。
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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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