Y16 is a specific inhibitor of Leukemia-associated Rho guanine nucleotide exchange factor (LARG) with a K d value of 76 nM. Y16 is active in blocking the interaction of LARG and related G-protein-coupled Rho GEFs with RhoA. Y16 shows no detectable effect on other diffuse B-cell lymphoma (Dbl) family Rho GEFs, Rho effectors, or a RhoGAP.
性状
Solid
IC50 & Target[1][2]
Kd: 76 nM (LARG)
体外研究(In Vitro)
Y16 (10-30 μΜ; 24 hours; NIH 3T3 cells) could inhibit RhoA-GTP formation induced by serum dose dependently and is specific for RhoA.Y16 (10-30 μΜ; 24 hours; NIH 3T3 cells) efficiently inhibits serum or SDF-1α-induced phospho-MLC and phospho-FAK formation, which are downstream of RhoA. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 25 mg/mL (65.03 mM; Need ultrasonic)配制储备液