product name
Rac1抑制剂, Rac1 Inhibitor, CAS 1177865-17-6, is a cell-permeable, reversible inhibitor of Rac1 GDP/GTP exchange. Interferes with the interaction between Rac1 and Rac-specific GEFs Trio and Tiam1 (IC₅₀ ~50 µM).
质量水平
检测方案
≥93% (HPLC)
形式
lyophilized
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
desiccated (hygroscopic)
protect from light
溶解性
water: 5 mg/mL
运输
ambient
储存温度
2-8°C
InChI
1S/C24H35N7.3ClH/c1-6-31(7-2)12-8-9-16(3)27-24-28-18(5)14-23(30-24)29-19-10-11-22-20(15-19)21(25)13-17(4)26-22;;;/h10-11,13-16H,6-9,12H2,1-5H3,(H2,25,26)(H2,27,28,29,30);3*1H
InChI key
CPUHORIUXPQCHW-UHFFFAOYSA-N
一般描述
一种细胞渗透性嘧啶化合物，通过干扰Rac1和Rac特异性GEF（鸟嘌呤核苷酸交换因子）Trio和Tiam1（IC50 ~50 µM）之间的相互作用，特异性和可逆地抑制Rac1 GDP/GTP交换活性。显示有效抑制NIH3T3和PC-3细胞中Rac1介导的细胞功能（有效剂量~50至100 μM）。对Cdc42或RhoA激活无影响，且不影响Rac1与BcrGAP或PAK1的相互作用。减少TRAP诱导和胶原刺激的血小板聚集（IC50分别为50 mM和64 mM）。
生化/生理作用
主要靶标
Rac1
Rac1
产物不与ATP竞争。
可逆性：是
细胞可渗透性：是
靶标IC50：针对Rac1 GDP/GTP交换活性约为50µM；针对TRAP诱导和胶原蛋白刺激的血小板聚集为50 mM和64 mM
包装
用惰性气体包装
警告
毒性：致癌/致畸（D）
重悬
复溶后，等分并冷冻保存（-20°C）。贮备溶液在-20°C下可稳定保存至多3个月。
其他说明
Dwivedi, S., et al. 2010.J. Translational Med.8, 128.
Desire, L., et al. 2005.J. Biol. Chem.280, 37516.
Gao, Y., et al. 2004.Proc.Natl.Acad.Sci. USA101, 7618.
Desire, L., et al. 2005.J. Biol. Chem.280, 37516.
Gao, Y., et al. 2004.Proc.Natl.Acad.Sci. USA101, 7618.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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