CPI-637
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CBP/EP300和BRD4,IC50分别为0.03和11.0 μM。
CPI-637是CBP/EP300 bromodomain抑制剂。
据报道,在涉及多种疾病途径的含bromodomain的蛋白质中,环AMP应答元件结合蛋白(CBP)和300kDa的腺病毒E1A结合蛋白(EP300)是高度同源的含bromodomain转录共激活因子对,并且由于参与多种疾病状态而作为潜在的药物靶点。
体外:先前的研究发现,CPI-637对EP300强效,其相反对映体显示超过200倍的效力损失。此外,CPI-637的生化效力很好地转化到含有CBP BRET的细胞中,EC50为0.3μM,并且CPI-637的选择性比BET bromodomain家族高700倍以上。此外,CPI-637也对其他bromodomain具有高度选择性,仅针对BRD9表现出显著的生物化学活性。此外,在细胞测定中发现CPI-637能够抑制MYC的表达,EC50为0.60 μM。[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,CPI-637仍处于临床前研究阶段。
参考文献:
[1] Taylor, A. M. et al. Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637). ACS medicinal chemistry letters 7, 531-536, doi:10.1021/acsmedchemlett.6b00075 (2016).
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 386.45 |
Cas No. | 1884712-47-3 |
Formula | C22H22N6O |
Solubility | insoluble in EtOH; insoluble in H2O; ≥19.3 mg/mL in DMSO with gentle warming |
Chemical Name | (S)-4-methyl-6-(1-methyl-3-(1-methyl-1H-pyrazol-4-yl)-1H-indazol-5-yl)-4,5-dihydro-1H-benzo[b][1,4]diazepin-2(3H)-one |
SDF | Download SDF |
Canonical SMILES | O=C1NC2=CC=CC(C3=CC4=C(N(C)N=C4C5=CN(C)N=C5)C=C3)=C2N[C@@H](C)C1 |
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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