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leading to the inhibition of the JAK/STAT (signal transducer and activator of transcription) signaling including activation of STAT3
InChi: InChI=1S/C16H14N2O3S/c1-11-15(12-7-9-14(10-8-12)22(17
InChiKey: AKIIPHDGVCFVCC-UHFFFAOYSA-N
3-a]pyrrolo[3
10(4):1072-81
TG003 oripenem monohydrate leading to the inhibition ofTG003 is a potent, ATP competitive inhibitor of Clk family kinases (IC50 values are 20, 200 and 15 nM for mClk1, 2 and 4 respectively and >10 M for mClk3). . TG003 inhibited SF2 ASF dependent splicing of beta globin pre mRNA in vitro by suppression of Clk mediated phosphorylation. TG003 also suppressed serine arginine rich protein phosphorylation, dissociation of nuclear speckles, and Clk1 Sty dependent alternative splicing in mammalian cells.
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