TG003 (300801-52-9) Description
TG003 is potent, specific, reversible, and ATP-competitive inhibitor of Cdc2-like kinase (Clk). Ki = 10 nM for mClk1/Sty; IC50 = 15 nM, 20 nM, 200 nM, and > 10 mM for mClk4, mClk1, mClk2, and mClk3, respectively.
TG003 regulates alternative splicing and reduces the phosphorylation of SF2/ASF1.
TG003 has been used to develop assays for screening substances that affect mRNA splicing
Cdc2-like kinase (Clk), among a number of other kinases, phosphorylates serine/arginine-rich proteins which play a role in alternative splicing of pre-mRNA. The Clk family consists of four members, which include Clk1/Sty and Clk2-4. TG003 is a novel benzothiazole compound that demonstrates potent inhibition of Clk1/Sty and Clk4 with IC50 values of 20 and 15 nM, respectively.1 TG003 exhibits considerably weaker inhibition of Clk2 and Clk3 (IC50 = 200 nM and >10 μM, respectively).1 Through suppression of Clk-mediated phosphorylation, TG003 inhibits SF2/ASF-dependent splicing of β-globin pre-mRNA at 1 μM in vitro.1 At 10 μM, TG003 rescues the embryonic defects induced by excessive Clk activity in Xenopus.
TG003 (300801-52-9) Specifications
|Synonyms||TG003; 300801-52-9; TG 003; Cdc2-Like Kinase Inhibitor, TG003; TG-003
|Drug Class||Cdc2-Like Kinase Inhibitor;Clk inhibitor|
|Molecular Weight||249.328 g/mol|
|Monoisotopic Mass||249.082 g/mol|
|Form||white solid powder|
|Color||white to beige|
|Solubility||Soluble in DMSO, not in water|
|Storage Temp.||0 – 4 C for short term (days to weeks), or -20 C for long term (months).|
|Shelf life||>2 years if stored properly|
|Handling||Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).|
|Application||TG003 has been used to develop assays for screening substances that affect mRNA splicing|