1. Cell Cycle/DNA Damage
  2. CDK
  3. TG003

TG003 

Cat. No.: HY-15338 Purity: 98.77%
Handling Instructions

TG003 is a potent inhibitor of Clk1/Sty; inhibits Clk1 and Clk4 with IC50 values of 20 and 15 nM, respectively.

For research use only. We do not sell to patients.

TG003 Chemical Structure

TG003 Chemical Structure

CAS No. : 719277-26-6

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 198 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 540 In-stock
Estimated Time of Arrival: December 31
100 mg USD 660 In-stock
Estimated Time of Arrival: December 31
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500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

TG003 is a potent inhibitor of Clk1/Sty; inhibits Clk1 and Clk4 with IC50 values of 20 and 15 nM, respectively[1].

IC50 & Target[1]

CLK1

20 nM (IC50)

CLK2

200 nM (IC50)

Clk4

15 nM (IC50)

In Vitro

TG003, shows the most potent effect on Clk1/Sty and Clk4 (IC50, 15–20 nM) and lesser on Clk2 (200 nM). TG003 inhibits SF2/ASF-dependent splicing of β-globin pre-mRNA in vitro by suppression of Clk-mediated phosphorylation. It suppresses serine/arginine-rich protein phosphorylation, dissociation of nuclear speckles, and Clk1/Sty-dependent alternative splicing in mammalian cells[1]. The small drug TG003 increases endogenous expression of p53β and p53γ protein isoforms by modulation of TP53 intron 9 alternative splicing[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Intrathecal injection of either TG003 (1-100 pM) or IC261 (0.1-1 nM) dose-dependently decreases mechanical allodynia and thermal hyperalgesia induced by carrageenan or CFA[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

249.33

Formula

C₁₃H₁₅NO₂S

CAS No.

719277-26-6

SMILES

CC(/C=C1SC2=CC=C(C=C2N\1CC)OC)=O.[Z]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 31 mg/mL (124.33 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.0107 mL 20.0537 mL 40.1075 mL
5 mM 0.8021 mL 4.0107 mL 8.0215 mL
10 mM 0.4011 mL 2.0054 mL 4.0107 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (10.03 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (10.03 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (10.03 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[1]

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 and 0.1-1 μg of purified kinases in a final volume of 40 μL. 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 or 5% trichloroacetic solution at least over 15 min. The radioactivity is measured using a liquid scintillation counter[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

2×105 HeLa cells or 1.5×105 COS-7 cells re-suspended 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 mM), 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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 98.77%

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Keywords:

TG003TG 003TG-003CDKCyclin dependent kinasebreastcancerWilm'stumormutationsplicesiteInhibitorinhibitorinhibit

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