KD 5170
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.
KD 5170是去乙酰化酶(HADC)的新型抑制剂,IC50值为0.045 μM[1]。
去乙酰化酶(HADC)可以除去组蛋白中ε-N-乙酰赖氨酸上的乙酰基,使组蛋白更紧密地包裹住DNA,阻止转录。
KD 5170是HADC的抑制剂,抑制重组HDAC酶,对HADC1、HADC2、HADC 3、HDAC4和HDAC6的IC50分别为0.020、2.0、0.075、0.026和0.014 μM。在HeLa细胞中,KD5170以浓度依赖性方式引起组蛋白超乙酰化,EC50为25 nM。在HCT-116细胞中,KD 5170诱导p21WAF1的表达以及组蛋白H3和α-微管蛋白乙酰化[1,2]。在HL-60白血病细胞和HCT-116结直肠癌细胞中,KD5170以浓度依赖性方式引发细胞死亡[1]。
在HCT-116肿瘤异种移植小鼠中,KD 5170显著抑制其肿瘤生长[1]。在H929肿瘤异种移植小鼠中,KD 5170减小肿瘤体积,显著延长至终点的平均时间。在KD 5170处理的小鼠脾和肿瘤组织中,组蛋白乙酰化增加[3]。
参考文献:
[1]. Hassig CA, Symons KT, Guo X, et al. KD5170, a novel mercaptoketone-based histone deacetylase inhibitor that exhibits broad spectrum antitumor activity in vitro and in vivo. Mol Cancer Ther, 2008, 7(5): 1054-1065.
[2]. Payne JE, Bonnefous C, Hassig CA, et al. Identification of KD5170: a novel mercaptoketone-based histone deacetylase inhibitor. Bioorg Med Chem Lett, 2008, 18(23): 6093-6096.
[3]. Feng R, Ma H, Hassig CA, et al. KD5170, a novel mercaptoketone-based histone deacetylase inhibitor, exerts antimyeloma effects by DNA damage and mitochondrial signaling. Mol Cancer Ther, 2008, 7(6): 1494-1505.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 451.56 |
Cas No. | 940943-37-3 |
Formula | C20H25N3O5S2 |
Solubility | ≥21.2 mg/mL in DMSO with gentle warming; insoluble in H2O; insoluble in EtOH |
Chemical Name | S-(2-(6-(4-(3-(dimethylamino)propoxy)phenylsulfonamido)pyridin-3-yl)-2-oxoethyl) ethanethioate |
SDF | Download SDF |
Canonical SMILES | CN(C)CCCOC1=CC=C(S(NC2=CC=C(C(CSC(C)=O)=O)C=N2)(=O)=O)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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