A 205804
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.
A 205804是E-选择素和ICAM-1的高效选择性抑制剂,IC50值分别为20 nM和25 nM[1].
E选择素是一种细胞粘附分子,在炎症过程中募集白细胞至损伤部位中发挥重要作用.ICAM-1(胞内粘附分子1)是LFA-1的配体,参与白细胞结合内皮细胞的过程.有报道称E-选择素和ICAM-1的异常表达与多种癌症相关[2].
A205804是E-选择素和ICAM-1而非VCAM-1的选择性抑制剂.在原代脐静脉内皮细胞(HUVECs)中,A205804处理通过抑制E-选择素和ICAM-1的表达而减少细胞迁移[3].在使用全细胞高通量试验的人血管内皮细胞中,低浓度A205804能够高效选择性抑制E-选择素和ICAM-1[1].而且,人脐静脉内皮细胞(HUVECs)的实验表明A205804通过易位到细胞核,非共价结合分子量超过650KDa的大分子,从而抑制E-选择素和ICAM-1表达[4].
参考文献：
[1]. Stewart, A.O., et al., Discovery of inhibitors of cell adhesion molecule expression in human endothelial cells. 1. Selective inhibition of ICAM-1 and E-selectin expression. J Med Chem, 2001. 44(6): p. 988-1002.
[2]. Chang, C.Z., et al., Valproic acid attenuates intercellular adhesion molecule-1 and E-selectin through a chemokine ligand 5 dependent mechanism and subarachnoid hemorrhage induced vasospasm in a rat model. J Inflamm (Lond), 2015. 12: p. 27.
[3]. Zhu, G.D., et al., Selective inhibition of ICAM-1 and E-selectin expression in human endothelial cells. 2. Aryl modifications of 4-(aryloxy)thieno[2,3-c]pyridines with fine-tuning at C-2 carbamides. J Med Chem, 2001. 44(21): p. 3469-87.
[4]. Zhu, G.D., et al., Synthesis and mode of action of (125)I- and (3)H-labeled thieno[2,3-c]pyridine antagonists of cell adhesion molecule expression. J Org Chem, 2002. 67(3): p. 943-8.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 300.39 |
| Cas No. | 251992-66-2 |
| Formula | C15H12N2OS2 |
| Solubility | ≥30 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
| Chemical Name | 4-(4-methylphenyl)sulfanylthieno[2,3-c]pyridine-2-carboxamide |
| SDF | Download SDF |
| Canonical SMILES | CC1=CC=C(C=C1)SC2=C3C=C(SC3=CN=C2)C(=O)N |
| 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。 |
| Description | A 205804是E-选择素和ICAM-1表达的高效选择性抑制剂,IC50值分别为20 nM和25 nM. | |||||
| 靶点 | E-selectin | ICAM-1 | ||||
| IC50 | 20 nM | 25 nM | ||||
质量控制和MSDS
- 批次:
化学结构
