CW069
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.
CW069是一种选择性HSET变构抑制剂,IC50值为75 μM[1].
HEST是一种负端微管(MT)动力蛋白,在人类和小鼠中分别由KIFC1和Kifc5a编码.HSET在功能性有丝分裂纺锤体的装配中起着重要的作用[1].
CW069是一种选择性HSET变构抑制剂.与KSP相比,CW069对HSET具有显著的选择性.在HSET结合的计算模型中,CW069的羧酸基与HSET中Arg521的胍基之间形成最有利的氢键.另外,CW069裸露的苯基与Arg521的侧链之间形成阳离子-π相互作用.Arg521是CW069选择性的关键.CW069的对映异构体与HSET结合更弱,是由于配体的羧酸基与HSET的Arg521之间的相互作用较弱.在N1E-115肿瘤细胞中,由于缺乏中心体集群,CW069显著地增加多极纺锤体的形成.在MDA-MB-231和BT549乳腺癌细胞中,CW069显著地增加多极纺锤体.在N1E-115细胞中,CW069(200 μM)诱导多极后期形成和细胞凋亡[1].
参考文献:
[1]. Watts CA, Richards FM, Bender A, et al. Design, synthesis, and biological evaluation of an allosteric inhibitor of HSET that targets cancer cells with supernumerary centrosomes. Chem Biol, 2013, 20(11): 1399-1410.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 500.33 |
Cas No. | 1594094-64-0 |
Formula | C23H21IN2O3 |
Solubility | ≥50 mg/mL in DMSO; ≥9 mg/mL in EtOH; ≥7.1 mg/mL in H2O |
Chemical Name | 2-[[(2S)-2-(benzylamino)-3-phenylpropanoyl]amino]-5-iodobenzoic acid |
SDF | Download SDF |
Canonical SMILES | C1=CC=C(C=C1)CC(C(=O)NC2=C(C=C(C=C2)I)C(=O)O)NCC3=CC=CC=C3 |
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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