TG003

SKU: orb1689653

Description

TG003 is a small molecule inhibitor of Clk1 and Clk4 kinases. It demonstrates anti-proliferative and pro-apoptotic effects in cancer cell studies and is also a valuable research tool for investigating splicing-related diseases such as Duchenne muscular dystrophy in cellular models.

Research Area

Cell Biology

Key Properties

• CAS Number: 719277-26-6
• MW: 249.33
• Purity: >98%
• Formula: C₁₃H₁₅NO₂S
• SMILES: C(C)N\1C=2C(S/C1=C\C(C)=O)=CC=C(OC)C2
• Target: Kinase
• Solubility: Soluble in DMSO (up to 20 mg/ml) or in Ethanol (up to 15 mg/ml).

Bioactivity

• Target IC50:
  CLK1/Sty:15–20 nM|CLK2:200 nM|CLK4:15–20 nM
• In Vivo:
  Intrathecal injection of either TG003 (1-100 pM) or IC261 (0.1-1 nM) dose-dependently reduces mechanical allodynia and thermal hyperalgesia induced by carrageenan or CFA.
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• In Vitro:
  The small drug TG003 increases endogenous expression of p53β and p53γ protein isoforms by modulation of TP53 intron 9 alternative splicing. TG003 exhibits the most potent effect on Clk1/Sty and Clk4 (IC50, 15–20 nM) with lesser effect on Clk2 (IC50=200 nM). TG003 inhibits SF2/ASF-dependent splicing of β-globin pre-mRNA in vitro by suppression of Clk-mediated phosphorylation.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Clk1, Clk4, TG 003

Compound Identifiers

PubChem CID

1893668