TG003 Chemical Properties

Melting point:

132-132.5 °C

Boiling point:

386.0±42.0 °C(Predicted)

Density 

1.237±0.06 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

DMSO: 33 mg/mL

form 

solid

pka

-1.54±0.20(Predicted)

color 

pale yellow

Stability:

Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months.

Safety Information

Hazard Codes 

Xi

Risk Statements 

36/37/38

Safety Statements 

26-36

WGK Germany 

3

MSDS

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TG003 Usage And Synthesis

Description

TG003 (719277-26-6) is a potent, ATP-competitive inhibitor of Clk-family kinases (IC50‘s = 15, 20 and 200 nM for mClk4, 1 and 2 respectively and >10 μM for mClk3).1?Also inhibits DYRK1A/B (IC50‘s = 24 and 34 nM respectively).2 Suppresses serine/arginine-rich protein phosphorylation, dissociation of nuclear speckles and Clk1/Sty-dependent alternative splicing in mammalian cells.1?TG003 affects the regulation of alternative splicing by phosphorylation of SR protein both in vitro and in vivo. Promotes skipping of exon 31 in the endogenous dystrophin gene.3 TG003 increases levels of Clk1/4 mature mRNAs by promoting splicing of the intron-retaining RNAs.4

Uses

TG 003 is a potent, ATP-competitive inhibitor of Clk-family kinases.

in vivo

IC 50

CLK1: 20 nM (IC₅₀); CLK2: 200 nM (IC₅₀); CLK4: 15 nM (IC₅₀)

storage

Store at +4°C

References

[1] MICHIKO MURAKI. Manipulation of alternative splicing by a newly developed inhibitor of Clks.[J]. The Journal of Biological Chemistry, 2004: 24246-24254. DOI:10.1074/jbc.m314298200
[2] ALICIA FOUCOURT. Design and synthesis of thiazolo[5,4-f]quinazolines as DYRK1A inhibitors, part II.[J]. Molecules, 2014, 19 10: 15411-15439. DOI:10.3390/molecules191015411
[3] ATSUSHI NISHIDA. Chemical treatment enhances skipping of a mutated exon in the dystrophin gene.[J]. Nature Communications, 2011: 308. DOI:10.1038/ncomms1306
[4] KENSUKE NINOMIYA  Masatoshi H  Naoyuki Kataoka. Stress-responsive maturation of Clk1/4 pre-mRNAs promotes phosphorylation of SR splicing factor.[J]. Journal of Cell Biology, 2011, 195 1: 27-40. DOI:10.1083/jcb.201107093

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