SMER 3 是选择性的Skp1-Cullin-F-box (SCF)Met30泛素连接酶抑制剂。SMER 3 通过抑制 SCFMet30来增强 Rapamycin 的生长抑制作用。
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SMER 3 is an inhibitor of the Skp1-Cullin-F-box (SCF)(Met30) ubiquitin ligase, a member of the SCF E3-ligase family, which regulates diverse cellular processes including transcription, cell-cycle control and immune response.
体外活性
SMER 3 and rapidly increased PFKFB3 protein levels. Accordingly, ubiquitin-bound PFKFB3 was lower in E2- or G1-treated HUVECs. Both agents increased deubiquitinase USP19 levels through GPER signaling[1].
体内活性
SMER 3 diminishes binding of the F-box subunit Met30 to the SCF core complex in vivo and show evidence for SMER 3 directly binding to Met30[2].
Cas No.
67200-34-4
分子式
C11H4N4O2
分子量
224.18
别名
SMER 3
储存和溶解度
DMSO:8 mg/mL (35.69 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years