TG003
Based on 9 publication(s) in Google Scholar
TG003 is a potent inhibitor of Clk1/Sty; inhibits Clk1 and Clk4 with IC50 values of 20 and 15 nM, respectively.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.57%
- No. CAS: 719277-26-6
- Fòrmula: C13H15NO2S
- Peso molecular:249.33
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) TG003
More- Sci Adv. 2025 Nov 28;11(48):eadz2345. [Abstract]
- Cell Chem Biol. 2025 Jul 17;32(7):908-925.e9. [Abstract]
- Cancer Immunol Res. 2026 May 4;14(5):875-891. [Abstract]
- Int J Mol Sci. 2023 Apr 4;24(7):6733. [Abstract]
- Cancers (Basel). 2023 Apr 13;15(8):2271. [Abstract]
- Mol Oncol. 2025 Oct 17. [Abstract]
- Glycobiology. 2024 Dec 10;34(12):cwae081. [Abstract]
- SSRN. 2026 May 27.
- bioRxiv. 2024 Aug 16:2024.08.15.608201. [Abstract]
Actividad biológica
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CLK1 20 nM (IC50) |
CLK2 200 nM (IC50) |
CLK4 15 nM (IC50) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 719277-26-6
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Appearance Solid
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Peso molecular 249.33
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Fòrmula C13H15NO2S
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Color White to yellow
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SMILES
CC(/C=C1SC2=CC=C(C=C2N\1CC)OC)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (9)
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Journal Impact Factor
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Most Recent
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Sci Adv
FeaSion decodes the regulatory landscape and functional diversity of RNA polymerase II CTD phosphorylation. [Abstract]2025 Nov 28;11(48):eadz2345. PMID: 41313762 -
Cell Chem Biol
2025 Jul 17;32(7):908-925.e9. PMID: 40553690 -
Cancer Immunol Res
CLK1 Promotes Myeloid-Derived Suppressor Cell Trafficking and Reprograms the Tumor Microenvironment by Activating Hippo/YAP Signaling in Colorectal Cancer. [Abstract]2026 May 4;14(5):875-891. PMID: 41686262 -
Int J Mol Sci
2023 Apr 4;24(7):6733. PMID: 37047705 -
Cancers (Basel)
SRSF5 Regulates the Expression of BQ323636.1 to Modulate Tamoxifen Resistance in ER-Positive Breast Cancer. [Abstract]2023 Apr 13;15(8):2271. PMID: 37190199 -
Mol Oncol
CDK11 inhibition induces cytoplasmic p21WAF1 splice variant by p53 stabilisation and SF3B1 inactivation. [Abstract]2025 Oct 17. PMID: 41105927 -
Glycobiology
Compromised CDK12 activity causes dependency on the high activity of O-GlcNAc transferase. [Abstract]2024 Dec 10;34(12):cwae081. PMID: 39361894 -
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bioRxiv
2024 Aug 16:2024.08.15.608201. PMID: 39211199
Solvente y solubilidad
DMSO : 125 mg/mL (501.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (8.34 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (8.34 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Muraki M, et al. Manipulation of alternative splicing by a newly developed inhibitor of Clks. J Biol Chem. 2004 Jun 4;279(23):24246-54. [Content Brief]
[2]. Marcel V, et al. Modulation of p53β and p53γ expression by regulating the alternative splicing of TP53 gene modifies cellular response. Cell Death Differ. 2014 Sep;21(9):1377-87. [Content Brief]
[3]. Kurihara T, et al. Alleviation of behavioral hypersensitivity in mouse models of inflammatory pain with two structurally different casein kinase 1 (CK1) inhibitors. Mol Pain. 2014 Mar 10;10:17. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.0107 mL | 20.0537 mL | 40.1075 mL | 100.2687 mL |
| 5 mM | 0.8021 mL | 4.0107 mL | 8.0215 mL | 20.0537 mL | |
| 10 mM | 0.4011 mL | 2.0054 mL | 4.0107 mL | 10.0269 mL | |
| 15 mM | 0.2674 mL | 1.3369 mL | 2.6738 mL | 6.6846 mL | |
| 20 mM | 0.2005 mL | 1.0027 mL | 2.0054 mL | 5.0134 mL | |
| 25 mM | 0.1604 mL | 0.8021 mL | 1.6043 mL | 4.0107 mL | |
| 30 mM | 0.1337 mL | 0.6685 mL | 1.3369 mL | 3.3423 mL | |
| 40 mM | 0.1003 mL | 0.5013 mL | 1.0027 mL | 2.5067 mL | |
| 50 mM | 0.0802 mL | 0.4011 mL | 0.8021 mL | 2.0054 mL | |
| 60 mM | 0.0668 mL | 0.3342 mL | 0.6685 mL | 1.6711 mL | |
| 80 mM | 0.0501 mL | 0.2507 mL | 0.5013 mL | 1.2534 mL | |
| 100 mM | 0.0401 mL | 0.2005 mL | 0.4011 mL | 1.0027 mL |
TG003 Related Classifications
HY-15338 Related Classifications
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