IMR-1, Notch transcriptional activation inhibitor

Product Details

Formal Name: 2-[2-Methoxy-4-[(4-oxo-2-thioxo-5-thiazolidinylidene)methyl]phenoxy]-acetic acid ethyl ester

Molecular Formula: C₁₅H₁₅NO₅S₂

Formula Weight: 353.41

CAS Number: 310456-65-6

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 45 mg/ml) or in Ethanol (up to 9 mg/ml with warming)

Storage: -20°C

Stability: ≥ 2 years.

Applications

Notch transcriptional activation inhibitor

Functions

Inhibitor of Mastermind Recruitment-1 (IMR-1) disrupts the recruitment of Mastermind-like 1 to the Notch transcriptional activation complex (NTC) on chromatin, which attenuates Notch target gene transcription. IC50=26 µM (in vitro assay).  IMR-1 inhibits the growth of Notch-dependent cell lines and attenuates the growth of patient-derived tumor xenografts. The ethylester is hydrolyzed by intracellular esterases which produces the free acid compound (IMR-1A), IC50=0.5 µM (in vitro assay). Binding of IMR-1 to NTC is non-covalent and reversible.

Application Procedures

First dissolved in DMSO (up to 45 mg/ml) or in Ethanol (up to 9 mg/ml with warming), then diluted to aqueous buffer. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month.

Research use only.

Documents

• Datasheet (PDF)
• MSDS (PDF)