TG003

For research use only. Not for use in humans.

Catalog No.S7320

2 publications

Molecular Weight(MW): 249.33

TG003 is a potent and ATP-competitive Cdc2-like kinase (Clk) inhibitor with IC50 of 20 nM, 200 nM, and 15 nM for Clk1, Clk2, and Clk4, respectively. No inhibitory effect on Clk3, SRPK1, SRPK2, or PKC.

Selleck's TG003 has been cited by 2 publications

Purity & Quality Control

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Biological Activity

Description

Targets

mCLK4 ^[1] (Cell-free assay)	mCLK1 ^[1] (Cell-free assay)	mCLK2 ^[1] (Cell-free assay)
15 nM	20 nM	200 nM

In vitro

TG003 inhibits SF2/ASF-dependent splicing of human β-globin in vitro by suppression of Clk1/Sty-mediated phosphorylation. TG003 inhibits Clk1/Sty kinase activity in mammalian cells, while has no toxic effect on growth of HeLa and COS-7 cells at 10 μM concentration. ^[1] TG003 blocks IL-1β RNA production by platelets by inhibiting splicing of IL-1β heteronuclear RNA. ^[2] During 3T3-L1 adipocyte differentiation, TG003 also blocks alternative splicing of PKCβII and expression of PPARγ1 and PPARγ2. ^[3]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
human STO cells	NXu3OVd[TnWwY4Tpc44h[XO\|YYm=				NXLGU4ZKVW:mdXzheIlwdiCxZjDDcIswe3S7IIDy[U1uWk6DIIPwcIlkcW6pIHnuJIh2dWGwIGPUU{Bk\WyuczDhd5Nme3OnZDDhd{Bkd26lZX70doF1cW:wIILldZVqemWmIITvJIlv[3KnYYPlJIlvKG2jdIXy[UBEdGt{IH3SUmEhdGW4ZXygZpkhWlRvUFPSJIFv[Wy7c3nzMEBGSzVyPU[uOkDPxE1?	MorUNlUzOjF4NEm=

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	CLK1 / SRPK1 ; PubMed: 27397683 Mol Cell Single turnover curves for SRSF1 phosphorylation using SRPK1, CLK1 and the SRPK1-CLK1 complex with and without TG003.	27397683
Immunofluorescence	tubulin / emerin ; PubMed: 27015110 eLife Immunofluorescence microscopy of A549 cells depleted of CLK1 by shRNA (top row), cells treated with 10 µM TG003 for 12 hr (middle row), and a control treatment with DMSO (bottom row); green: tubulin, red: emerin (nuclear envelope), and blue: DAPI. Scale bar 10 µm.	27015110

In vivo

TG003 (10 μM) rescues the embryonic defects induced by excessive Clk activity in Xenopus. ^[1]

Protocol

Kinase Assay: ^[1]	- Collapse In Vitro Kinase Assay : Kinase activity of Clks and SRPKs is assayed in a reaction mixture, containing 200 mM Tris-HCl (pH 7.5), 12.5 mM MgCl₂, 8 mM dithiothreitol, 4 mM EGTA, 1–20 μM ATP, 1 μCi of [γ-³²P]ATP, 1 μg of synthetic peptide of SF2/ASF RS domain (NH2-RSPSYGRSRSRSRSRSRSRSRSNSRSRSY-OH), and 0.1–1 μg of purified kinases in a final volume of 40 μL. cAMP-dependent protein kinase activity is assayed in a reaction mixture containing 80 mM Tris-HCl (pH 7.5), 12.5 mM MgCl₂, 8 mM dithiothreitol, 4 mM EGTA, 10 μM ATP, 1 μCi of [γ-³²P]ATP, 5 μg of histone H1, and 1 μg of catalytic subunit of rat cAMP-dependent protein kinase purified. Protein kinase C activity is assayed in a reaction mixture containing 200 mM Tris-HCl (pH 7.5), 12.5 mM MgCl₂, 1 mM CaCl₂, 80 μg/mL phosphatidylserine, 8 μg/mL diolein, 10 μM ATP, 1 μCi of [γ-³²P]ATP, 5 μg of histone H1, and 2 μL of partially purified rat protein kinase C. The final concentration of Me₂SO is adjusted to 1% regardless of inhibitor concentration. The reaction mixture is incubated at 30 or 25 °C for mammalian or Xenopus recombinant proteins, respectively, for 10 min, and a half-portion is spotted on P81 phosphocellulose membrane. The kinase assay conditions, including the incubation period and concentration of kinases and substrates, are optimized to maintain the linearity during incubation. The membrane is washed with 5% phosphoric acid solution (SF2/ASF RS domain) or 5% trichloroacetic solution (histone H1) at least over 15 min. The radioactivity is measured using a liquid scintillation counter. The net radioactivity is deduced by subtracting the background count from the reaction mixture without kinase, and the data are expressed as the percentage to the control sample containing the solvent.
Cell Research: ^[1]	- Collapse Cell lines: HeLa cells and COS-7 cells Concentrations: ~10 μM Incubation Time: 3 days Method: 2 × 10⁵ HeLa cells or 1.5 × 10⁵ COS-7 cells resuspended in 2 mL of medium are plated on 6-well dishes, and 2 μL of 10 mM TG003 dissolved in Me₂SO (final concentration at 10 μM), or 2 μL of Me₂SO, is added to some wells. Cells are trypsinized, and the density is counted every 24 h for 3 days. Cells are then fixed with 1 mL of ice-cold 70% ethanol, washed with PBS, incubated in 1 ml of PBS containing 1 μg/mL DNase-free RNase A and 50 μg/mL propidium iodide for 20 min at 37 °C, and proceeded to cell cycle analysis by FACSCalibur. (Only for Reference)
Animal Research: ^[1]	- Collapse Animal Models: Xenopus laevis embryos Formulation: DMSO Dosages: ~10 μM Administration: -- (Only for Reference)

References

Solubility (25°C)

In vitro	DMSO	6 mg/mL warmed (24.06 mM)
	Water	Insoluble
	Ethanol	Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download TG003 SDF

Molecular Weight	249.33
Formula	C₁₃H₁₅NO₂S
CAS No.	300801-52-9
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	N/A
Smiles	CCN1\C(SC2=C1C=C(OC)C=C2)=C\C(C)=O

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TG003