|A 205804 E-selectin/ICAM-1 expression inhibitor|
Sample solution is provided at 25 µL, 10mM.
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|Description||A-205804 is a potent and selective inhibitor of E-selectin and ICAM-1 expression with IC50 values of 20 nM and 25 nM, respectively.|
|IC50||20 nM||25 nM|
|Cas No.||251992-66-2||SDF||Download SDF|
|Solubility||≥30mg/mL in DMSO||Storage||Store at -20°C|
|Physical Appearance||A solid||Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
A-205804 is a potent and selective inhibitor of E-selectin and ICAM-1 with IC50 value of 20 nM and 25 nM, respectively .
E-selectin is a cell adhesion molecule and plays an important role in recruiting leukocytes to injury site during inflammation process. ICAM-1 (intracellular adhesion molecule 1) is a ligand for LFA-1 and involves in leukocytes binding to endothelial cells process. It has been reported that abnormal expression of E-selectin and ICAM-1 are correlated with a variety of cancers .
A-205804 is a selective E-selectin and ICAM-1 inhibitor over VCAM-1. When tested with primary HUVECs cells, A-205804 treatment reduced cell migration ability by inhibiting the expression of E-selectin and ICAM-1 . In human vascular endothelial cells using whole-cell high-throughput assay, it was shown that A-205804 exhibited potent and selective inhibition to E-selectin and ICAM-1 with low concentrations . Further, it was revealed that A-205804 inhibited E-selectin and ICAM-1 expressions by translocating to cell nucleus and noncovalently associated with macromolecules of molecular weight greater than 650 kDa when tested with human umbilical vein endothelial cells (HUVECs) .
. 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.
. 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.
. 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.
. 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.