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TG003

Catalog No.S7320

For research use only.

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.

CAS No. 300801-52-9

Selleck's TG003 has been cited by 5 Publications

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CDK Signaling Pathway Map

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	NV;EWWhGTnWwY4Tpc44h[XO\|YYm=				MYHNc4R2dGG2aX;uJI9nKEOuaz;zeJkheHKnLX3SUmEhe3CuaXPpcochcW5iaIXtZY4hW1SRIHPlcIx{KGG\|c3Xzd4VlKGG\|IHPvcoNmdnS{YYTpc44hemWzdXny[YQhfG9iaX7jdoVie2ViaX6gcYF1fXKnIFPsb\|IhdVKQQTDs[ZZmdCCkeTDSWE1RS1JiYX7hcJl{cXNuIFXDOVA:Pi54IN88US=>	MX[yOVIzOTZ2OR?=

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Assay

Methods	Test Index	PMID

Western blot	CLK1 / SRPK1	27397683
Immunofluorescence	tubulin / emerin	27015110

In vivo

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

Protocol (from reference)

Kinase Assay: ^[1]	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]	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.
Animal Research: ^[1]	Animal Models: Xenopus laevis embryos Dosages: ~10 μM Administration: --

References	[1] Muraki M, et al. J Biol Chem. 2004, 279(23), 24246-24254. [2] Brown GT, et al. J Immunol. 2011, 186(9), 5489-5496. [3] Li P, et al. PLoS One. 2013, 8(1), e53268.

References

Solubility (25°C)

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

Chemical Information

Molecular Weight	249.33
Formula	C₁₃H₁₅NO₂S
CAS No.	300801-52-9
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CCN1C2=C(C=CC(=C2)OC)SC1=CC(=O)C

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In vivo Formulation Calculator (Clear solution)

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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