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- 文献和实验
- 技术资料
- 保存条件:
-20°C, stored under nitrogen
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
1936421-41-8
- 规格:
10 mM * 1 mL/5 mg/10 mg/25 mg/50 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥1112.0 |
|---|---|---|---|
| 规格: | 5 mg | 产品价格: | ¥990.0 |
| 规格: | 10 mg | 产品价格: | ¥1585.0 |
| 规格: | 25 mg | 产品价格: | ¥2395.0 |
| 规格: | 50 mg | 产品价格: | ¥4050.0 |
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GNE-049
CAS No. : 1936421-41-8
MCE 国际站:GNE-049
产品活性:GNE-049 是一种高效的选择性 CBP 抑制剂,在 TR-FRET 实验中 IC50 为 1.1 nM。GNE-049 还抑制 BRET 和 BRD4(1),IC50 分别为 12 nM 和 4200 nM。
研究领域:Epigenetics
作用靶点:Epigenetic Reader Domain | Histone Acetyltransferase
In Vitro: GNE-049 is selected for further profiling as it has the best balance of liver microsomes (LM) stability, selectivity, and cellular potency GNE-049 has excellent potency in the BRET cellular assay and, in an orthogonal measure of the target engagement, GNE-049 is shown to inhibit the expression of MYC (MV4-11 cell line) with an EC50 of 14 nM.
In Vivo: GNE-049 demonstrates acceptable PK in mouse, rat, dog, and monkey. Determination of potency versus a selection of bromodomains revealed that GNE-049 is selective for CBP/P300 and, importantly, quite selective (3820-fold) over BRD4(1). GNE-049 is further evaluated in a rat single dose (30-250 mg/kg QD) toxicokinetic study. Adverse central nervous system (CNS)-related signs (e.g., marked hyperactivity and vocalization) are observed in several of the rats at the 250 mg/kg dose level. Furthermore, at the 250 mg/kg dose level, the ratio of the unbound drug concentration in brain to unbound drug concentration in plasma (Kp,uu) 3 h post dose is determined to be 0.43, indicating that GNE-049 is penetrating into the CNS and potentially resulting in the observed toxicity.
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文献和实验滑膜组织凝胶图谱的平均蛋白质点数分别为1 070±41、1 049±22、1 079±44和1 088±39。在4个组均有表达差异的蛋白质点中随机取20个点进行肽质指纹图分析,鉴定了部分与细胞代谢、信号转导及结构相关的差异表达蛋白质。结论:建立了分辨率较高且重复性较好的正常大鼠与CIA大鼠不同时间点滑膜组织的双向凝胶电泳图谱,鉴定了一些与CIA大鼠滑膜病变相关的差异表达蛋白质,为识别RA病变相关蛋白质及推断RA病变过程奠定基础。
【共享】Methods in molecular biology 下载
and Applications http://rapidshare.com/files/10750768/015-PCR_Protocols__1st_Edition.pdf http://ec1.images-amazon.com/images/I/41SCA8GTPXL.jpg Vol 16 Enzymes of Molecular Biology http://rapidshare.com/files/9844513/016-Enzymes_of_molecular_biology__1993_MMB
785.2 H2 O [ml] 948.35 895 840.65 784.6 727.15 668.2 607.55 545.7 %(w/w) 9.379 17.988 25.940 33.350 40.295 46.846 53.070 58.998 H2 O %(w/w) 90.621 82.012 74.060 66.650 59.705 53.154 46.930 41.002 p (g
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