T025

SKU: orb1708431

Description

T025 is a potent pan-CLK inhibitor exhibiting low nanomolar affinity for CLK1-4. It demonstrates anti-proliferative activity in various cancer cell lines and is a useful research tool for investigating MYC-driven pathologies, including in studies of hematological and solid tumor models.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 2407433-00-3
• MW: 382.42
• Purity: 99.20% (May vary between batches)
• Formula: C₂₁H₁₈N₈
• SMILES: CNc1nc(NCc2ncccn2)c2c(c[nH]c2n1)-c1ccc2ncccc2c1
• Target: CDK,Apoptosis,DYRK
• Solubility: DMSO:10 mg/mL (26.15 mM)

Bioactivity

• Target IC50:
  CLK4:0.61 nM (kd)|CLK2:0.096 nM (kd)|DYRK1A:0.074 nM (Kd)|DYRK1B:1.5 nM (Kd)|DYRK2:32 nM (Kd)|CLK1:4.8 nM (kd)|CLK3:6.5 nM (kd)
• In Vivo:
  In Balb/c nude mice, gavage administration of T025 (50 mg/kg) suppresses tumor growth and < 10% nadir body weight loss. Gavage administration of T025 (50 mg/kg) inhibits the CLK-dependent phosphorylation and decreases the RPS6KB1 exon 7 and BCLAF1 exon 11 percentage splice-in values.
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• In Vitro:
  In MDA-MB-468 cells, T025 (1-1000 nM) dose-dependently suppresses cell growth and reduces pCLK2 and CLK2 phosphorylation levels.

Storage & Handling

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

Alternative Names

CLK3, CLK1, CLK2, CLK4, T025, T-025, T 025

Compound Identifiers

PubChem CID

133082038