PF-CBP1 hydrochloride
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
作用于CREBBP和p300 bromodomain,IC50分别为125和363 nM。
PPF-CBP1 hydrochloride是CBP / p300 bromodomain抑制剂。
据报道,Bromodomains通过识别乙酰赖氨酸修饰参与转录调节。然而,尽管疏水口袋使得bromodomain成为有吸引力的靶点,仍然缺乏选择性bromodomain调节剂。
体外:PF-CBP1 hydrochloride显著降低BRD4效力,而保留CBP亲和力。为了评价在基因转录期间化合物相关的细胞毒性,用LPS刺激原代巨噬细胞并进一步分析以确定细胞活力。结果表明,即使在高达30 mM的高浓度下,PF-CBP1和阴性对照ISOX-INACT也不引起细胞毒性。此外,10 mM的PF-CBP1 hydrochloride能够适度降低LPS诱导的IL-6和IFN-b表达,并且在3 mM的PF-CBP1下观察到IL-1b表达降低。此外,用PF-CBP1 hydrochloride、载体或阴性对照ISOX-INACT处理大鼠原代皮质神经元,结果显示在1h时,RGS4表达与载体相比没有变化。然而,与载体相比,10倍IC50剂量PF-CBP1 hydrochloride的处理可以在24h时显著降低RGS4的mRNA水平[1]。
体内:迄今为止,尚无动物体内数据报道。
临床试验:到目前为止,PF-CBP1仍处于临床前研究阶段。
参考文献:
[1] Chekler EL, et al. Transcriptional Profiling of a Selective CREB Binding Protein Bromodomain Inhibitor Highlights Therapeutic Opportunities. Chem Biol. 2015 Dec 17;22(12):1588-96.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 525.08 |
Cas No. | 2070014-93-4 |
Formula | C29H37ClN4O3 |
Solubility | ≥52.5 mg/mL in DMSO; insoluble in H2O; ≥40.6 mg/mL in EtOH |
Chemical Name | 4-(2-(5-(3,5-dimethylisoxazol-4-yl)-2-(4-propoxyphenethyl)-1H-benzo[d]imidazol-1-yl)ethyl)morpholine hydrochloride |
SDF | Download SDF |
Canonical SMILES | CCCOC1=CC=C(CCC2=NC3=CC(C4=C(C)ON=C4C)=CC=C3N2CCN5CCOCC5)C=C1.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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