TG003, Clk family kinase inhibitor (TBI1292)

Description

Product Details

Formal Name: (Z)-1-(3-Ethyl-5-methoxy-2,3-dihydrobenzothiazol-2-ylidene)propan-2-one

Molecular Formula: C₁₃H₁₅NO₂S

Formula Weight: 249.33

CAS Number: 719277-26-6

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 20 mg/ml) or in Ethanol (up to 15 mg/ml).

Storage: -20°C

Stability: ≥ 2 years.

Applications

Clk family kinase inhibitor

Functions

Potent, ATP-competitive inhibitor of Clk-family kinases (IC50s = 15, 20 and 200 nM for mClk4, 1 and 2 respectively and >10 μM for mClk3). Also inhibits DYRK1A/B (IC50s = 24 and 34 nM respectively). Suppresses serine/arginine-rich protein phosphorylation, dissociation of nuclear speckles and Clk1/Sty-dependent alternative splicing in mammalian cells1. Affects the regulation of alternative splicing by phosphorylation of SR protein both in vitro and in vivo. Promotes skipping of exon 31 in the endogenous dystrophin gene. Increases levels of Clk1/4 mature mRNAs by promoting splicing of the intron-retaining RNAs.

Application Procedures

First dissolved in DMSO (up to 20 mg/ml) or in Ethanol (up to 15 mg/ml), then diluted to aqueous buffer. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months.