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Y16
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Y16图片
CAS NO:429653-73-6
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议

产品介绍
Y16是G蛋白欧联RhoGEFs抑制剂,能协同并增强Rhosin对RhoA的抑制活性。
Cas No.429653-73-6
Canonical SMILESO=C(N1)/C(C(N1C2=CC=CC=C2)=O)=C\C3=CC(OCC4=CC(C)=CC=C4)=CC=C3
分子式C24H20N2O3
分子量384.43
溶解度DMSO : 25 mg/mL (65.03 mM);Water :< 0.1 mg/mL (insoluble)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Y16 is an inhibitor of G-protein-coupled Rho GEFs; works synergistically with Rhosin/G04 in inhibiting LARG-RhoA interaction, RhoA activation, and RhoA-mediated signaling functions.IC50 value: Target: RhoA inhibitorY16 binds to this catalytic fragment of LARG with a Kd of ~76 ± 8 nM. Y16 was able to inhibit the GDP dissociation from RhoA catalyzed by LARG dose dependently without affecting the GEF reactions of Rac1 and Cdc42 catalyzed by TrioN and Intersectin, respectively. The N983A mutant lost the binding ability to Y16 with a Kd >500 μM, whereas the K979A and E982A mutants showed a reduced affinity with Kd values of 0.47 and 2.1 μM, respectively. At 2.5 μM each, Rhosin and Y16 inhibited ~50% RhoA-GTP content, and at 5 μM each ~80% RhoA-GTP stimulated by serum, which were much more potent than the effect of Rhosin/G04 or Y16 acting alone (~80% inhibition at 30 μM). Even under a higher concentration of Y16 and Rhosin/G04 combination (50 μM each) when endogenous RhoA-GTP content was effectively suppressed, no effect on Rac1-GTP or Cdc42-GTP content in cells was observed. Although Rhosin/G04 or Y16 administration alone caused ~50% inhibition of RhoA activity at 10 μM, combined Rhosin/G04 and Y16 reached 70% inhibition of RhoA-GTP or the downstream p-MLC when each was at 2.5 μM.

[1]. Shang X, et al. Small-molecule inhibitors targeting G-protein-coupled Rho guanine nucleotide exchange factors. Proc Natl Acad Sci U S A. 2013 Feb 19;110(8):3155-60.