S-Trityl-L-cysteine 是别构驱动蛋白Eg5的选择性抑制剂。rityl-L-cysteine抑制基础 ATPase 活性的IC50为 1 μM,抑制微管激活的 ATPase 活性的IC50为 140 nM。S-Trityl-L-cysteine 显示出抗肿瘤活性。
In vitro, S-trityl-L-Cysteine targets the catalytic domain of Eg5 and inhibits Eg5 basal and microtubule-activated ATPase activity as well as mant-ADP release. S-trityl-L-Cysteine is a tight binding inhibitor (estimation of K(i,app)<150 nm at 300 mm NaCl and 600 nm at 25 mm KCl). S-trityl-L-Cysteine binds more tightly than monastrol because it has both an approximately 8-fold faster association rate and approximately 4-fold slower release rate (6.1/microM/s and 3.6/s for S-trityl-L-Cysteine versus 0.78 /microM/s and 15/s for monastrol). S-trityl-L-Cysteine inhibits Eg5-driven microtubule sliding velocity in a reversible fashion with an IC50 of 500 nm[2].
产品描述
S-trityl-L-Cysteine is a potent inhibitor of human mitotic kinesin Eg5
体外活性
In vitro, S-trityl-L-Cysteine targets the catalytic domain of Eg5 and inhibits Eg5 basal and microtubule-activated ATPase activity as well as mant-ADP release. S-trityl-L-Cysteine is a tight binding inhibitor (estimation of K(i,app)<150 nm at 300 mm nacl and 600 25 kcl). s-trityl-l-cysteine binds more tightly than monastrol because it has both an approximately 8-fold faster association rate 4-fold slower release (6.1 microm s 3.6 for versus 0.78 >
Cas No.
2799-07-7
分子式
C22H21NO2S
分子量
363.47
储存和溶解度
DMSO:Slightly soluble
Methanol:1 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years