(E/Z)-TG003

SKU: orb1307181

Description

TG003 is a potent, ATP-competitive inhibitor of Cdc2-like kinases (Clks). This small molecule is a valuable research tool for studying alternative splicing regulation in vitro and has been used in cellular models to investigate its effects on kinase-dependent processes.

Research Area

Cell Biology

Key Properties

• CAS Number: 300801-52-9
• MW: 249.33
• Purity: 98.73%
• Formula: C₁₃H₁₅NO₂S
• SMILES: O=C(C=C1SC2=CC=C(OC)C=C2N1CC)C
• Target: Bcl-2 Family,CDK
• Solubility: DMSO:6 mg/mL (24.06 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  CLK1 (mouse):20 nM|CLK2 (mouse):200 nM|CLK4 (mouse):15 nM
• In Vivo:
  TG003 inhibits the splicing of heteronuclear RNA of IL-1β, thereby blocking the production of IL-1β RNA in platelets. During the differentiation process of 3T3-L1 adipocytes, TG003 also obstructs the alternative splicing of PKCβII and the expression of PPARγ1 and PPARγ2. Furthermore, it inhibits the in vitro SF2/ASF-dependent splicing of human β-globin by suppressing the phosphorylation mediated by Clk1/Sty. TG003 inhibits the kinase activity of Clk1/Sty in mammalian cells without exhibiting toxic effects on the growth of HeLa and COS-7 cells at a concentration of 10 μM.
• In Vitro:
  At a concentration of 10 μM, TG003 is capable of ameliorating embryonic defects in Xenopus laevis induced by excessive Clk activity within the organism.
• Cell Research:
  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)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Cyclin dependent kinase, CDK, breast, (E/Z)-TG 003, (E/Z)TG003, (E/Z)-TG003, (E/Z)-TG-003, (E/Z) TG003, cancer, Inhibitor, mCLK1, mCLK2, mCLK4, inhibit, mutation, tumor, Wilm's, site, TG 003, TG003, TG-003, splice

Compound Identifiers

PubChem CID

647991