"目录号: HY-15338
TG003是高效的Clk1/Sty抑制剂，抑制Clk1 和Clk4的IC50值分别为20和15 nM。
相关产品
LY2835219-Palbociclib-THZ1-Dinaciclib-LEE011-Roscovitine-Ro-3306-Flavopiridol-THZ2-1-NM-PP1-BIO-AZD-5438-BS-181-SNS-032-LY2857785-
生物活性
Description
TG003 is a potent inhibitor ofClk1/Sty; inhibits Clk1 and Clk4 withIC50values of 20 and 15 nM, respectively.
IC50& Target
IC50: 20 nM (Clk1), 200 nM (Clk2), >10 μM (Clk3), 15 nM (Clk4)[1]
In Vitro
TG003, shows the most potent effect on Clk1/Sty and Clk4 (IC50, 15–20 nM) and lesser on Clk2 (200 nM). TG003 inhibits SF2/ASF-dependent splicing of β-globin pre-mRNAin vitroby suppression of Clk-mediated phosphorylation. It suppresses serine/arginine-rich protein phosphorylation, dissociation of nuclear speckles, and Clk1/Sty-dependent alternative splicing in mammalian cells[1]. The small drug TG003 increases endogenous expression of p53β and p53γ protein isoforms by modulation of TP53 intron 9 alternative splicing[2].
In Vivo
Intrathecal injection of either TG003 (1-100 pM) or IC261 (0.1-1 nM) dose-dependently decreases mechanical allodynia and thermal hyperalgesia induced by carrageenan or CFA[3].
References
