CPI-455 HCl
![mRNA synthesis](/media/diy/images/page/figure1-mrna.png)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
![Tyramine Signal Amplification (TSA)](/media/diy/images/page/figure2-01.png)
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
![screening library](/media/diy/images/page/figure3-01.png)
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
![Cell Counting Kit-8 (CCK-8)](/media/diy/images/page/CCK-8.jpg)
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
![SYBR Safe DNA Gel Stain](/media/diy/images/page/SYBR Safe DNA Gel Stain.png)
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
![Inhibitor Cocktails](/media/diy/images/page/Inhibitor Cocktails.jpg)
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50为10 nM。
CPI-455是一种KDM5抑制剂。
KDM5组蛋白去甲基化酶家族催化组蛋白H3赖氨酸4(H3K4)的去甲基化,并且为耐药存留癌细胞(DTP)存活所需。
体外:先前的研究发现,在酶测定中,CPI-455可以强效抑制全长KDM5A,半数最大抑制浓度为10±1 nM。CPI-455抑制KDM5A、KDM5B和KDM5C水平相似,但对KDM4C和KDM7B表现出显著较弱的效力(分别为约200和770倍),并且对KDM2B、KDM3B或KDM6A未表现出可检测的抑制。此外,研究发现CPI-455介导的KDM5抑制导致HeLa细胞中全局H3K4me3剂量依赖性的增加,并且CPI-455的去除导致HeLa细胞中H3K4me3增加的快速逆转。此外,CPI-455可以延迟重H3K4me3的出现,这与KDM5酶对H3K4me3转化的作用一致,然而,H3K4me2的转化仅仅稍微改变。恰如所料,CPI-455可以影响H3K4单甲基化的转化[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-455仍处于临床前研究阶段。
参考文献:
[1] Vinogradova M, et al. An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells. Nat Chem Biol. 2016 Jul;12(7):531-8.
Storage | Store at -20°C |
M.Wt | 314.77 |
Cas No. | 2095432-28-1 |
Formula | C16H15ClN4O |
Solubility | ≥31.5 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
Chemical Name | 6-isopropyl-7-oxo-5-phenyl-4,7-dihydropyrazolo[1,5-a]pyrimidine-3-carbonitrile hydrochloride |
SDF | Download SDF |
Canonical SMILES | N#CC1=C(NC(C2=CC=CC=C2)=C(C(C)C)C3=O)N3N=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
- 批次:
化学结构
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