Senexin B
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.
Senexin B是高效的、选择性的和可口服的CDK8/CDK19抑制剂，IC50值范围为24-50 nM[1]。
CDK8是周期蛋白依赖性激酶8，与之密切相关的亚型是CDK19，是一种致癌转录调节激酶。CDK8在多能干细胞的表型中发挥重要作用。此外，CDK8是多个转录程序的调节剂，参与致癌，已被确定为黑色素瘤和结肠癌的致癌基因[1]。
Senexin B是高效的、选择性的和可口服的CDK8/CDK19抑制剂。 Senexin B对CDK8和CDK19表现出选择性，Kd值分别为140 nM和80 nM。1 mM的Senexin B完全溶解在20％的丙二醇中，在水中的溶解度为50 mM。在体外和体内实验中，低纳摩尔范围的Senexin B以ATP竞争性的方式抑制CDK8/19的活性[2]。在HT1080细胞中，Senexin B抑制IPTG诱导性p21诱导的CMV-GFP表达[1]。
在8周龄的CB-17 SCID小鼠中，腹膜内注射40 mg/kg的Senexin B或对照试剂5天，然后皮下注射1×106的人类A549肺癌细胞系，Senexin B显著减缓肿瘤的生长。在脂肪垫原位注射MDA-MB-468三阴性乳腺癌（TNBC）细胞的雌性裸鼠中，每天使用25 mg/kg的Senexin B (i.p.)预处理5天，强效且持续的抑制肿瘤生长[1]。
参考文献：
1. Cdk8/cdk19 selective inhibitors and their use in anti-metastatic and chemopreventative methods for cancer. Publication number: WO2013116786 A1.
2. Donald C. Porter, Mengqian Chen, Jiaxin Liang, et al. Abstract PR08: Targeting tumor microenvironment with selective small-molecule inhibitors of CDK8/19.
- 1. Vanessa Maria Knab, Dagmar Gotthardt, et al. "Triple-negative breast cancer cells rely on kinase-independent functions of CDK8 to evade NK-cell-mediated tumor surveillance." Cell Death Dis. 2021 Oct 23;12(11):991. PMID:34689158
- 2. Menzl I, Zhang T, et al. "A kinase-independent role for CDK8 in BCR-ABL1(+) leukemia." Nat Commun. 2019 Oct 18;10(1):4741. PMID:31628323
| Storage | Store at -20°C |
| M.Wt | 450.53 |
| Cas No. | 1449228-40-3 |
| Formula | C27H26N6O |
| Solubility | ≥22.55 mg/mL in DMSO with gentle warming; insoluble in H2O; insoluble in EtOH |
| Chemical Name | 4-((2-(6-(4-methylpiperazine-1-carbonyl)naphthalen-2-yl)ethyl)amino)quinazoline-6-carbonitrile |
| SDF | Download SDF |
| Canonical SMILES | CN(CC1)CCN1C(C2=CC3=CC=C(C=C3C=C2)CCNC4=C(C=C(C#N)C=C5)C5=NC=N4)=O |
| 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
相关生物数据
相关生物数据
