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Submit ReviewT3 CLK
Description: Potent and selective pan-CLK inhibitor; also inhibits DYRK1A/B
Chemical Name: 4-[1,1-Dimethyl-2-(4-methyl-1-piperazinyl)-2-oxoethyl]-N-[6-(4-pyridinyl)imidazo[1,2-a]pyridin-2-yl]benzamide
Purity: ≥98% (HPLC)
Biological Activity for T3 CLK
T3 CLK is a potent and selective pan CDC-like kinase (CLK) inhibitor (IC50 values are 0.67 nM, 15 nM, and 110 nM for CLK1, CLK2, and CLK3 protein kinases, respectively). T3 CLK also inhibits DYRK1A/B (IC50 values are 230 nM and 260 nM for DYRK1B and DYRK1A, respectively in cellular assays). Exhibits dose-dependent alternative splicing effects in HCT116 colorectal cancer cells. T3 CLK is cell permeable, stable and non-toxic.
Licensing Information
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the T3 CLK probe summary on the SGC website.
Technical Data for T3 CLK
| M. Wt | 482.58 |
| Formula | C28H30N6O2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 2109805-56-1 |
| PubChem ID | 132585205 |
| InChI Key | IEFFSHLHNYVSEF-UHFFFAOYSA-N |
| Smiles | O=C(NC=1N=C2C=CC(=CN2C1)C=3C=CN=CC3)C4=CC=C(C=C4)C(C(=O)N5CCN(C)CC5)(C)C |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for T3 CLK
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 24.13 | 50 with gentle warming | |
| ethanol | 4.83 | 10 with gentle warming |
Preparing Stock Solutions for T3 CLK
The following data is based on the product molecular weight 482.58. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 4.14 mL | 20.72 mL | 41.44 mL |
| 2.5 mM | 0.83 mL | 4.14 mL | 8.29 mL |
| 5 mM | 0.41 mL | 2.07 mL | 4.14 mL |
| 25 mM | 0.08 mL | 0.41 mL | 0.83 mL |
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Product Datasheets for T3 CLK
References for T3 CLK
References are publications that support the biological activity of the product.
Funnell et al (2017) CLK-dependent exon recognition and conjoined gene formation revealed with a novel small molecule inhibitor. Nat.Commun. 8 7 PMID: 28232751
If you know of a relevant reference for T3 CLK, please let us know.
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Keywords: T3 CLK, T3 CLK supplier, T3CLK, inhibitors, inhibits, Cdc2-like, kinase, Clk, kinases, DYRK, DYRK1A, DYRK1B, potent, selective, permeable, colorectal, cancer, CLK, (Cdc2-like, kinases), 7570, Tocris Bioscience
Citations for T3 CLK
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