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IMR-1 | Notch transcriptional activation inhibitor

Inhibitor of Mastermind Recruitment-1 (IMR-1, 310456-65-6) disrupts the recruitment of Mastermind-like 1 to the Notch transcriptional activation complex (NTC) on chromatin, which attenuates Notch target gene transcription1. IC50=26 mM (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 mM (in vitro assay). Binding of IMR-1 to NTC is non-covalent and reversible.1

References/Citations
1) Austudilo et al. (2016), The Small Molecule IMR-1 Inhibits the Notch Transcriptional Activation Complex to Suppress Tumorigenesis; Cancer Res., 76 3593

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Catalog#  10-3601-0005

$60.00
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CAS:
310456-65-6
Catalog Number:
10-3601
Activity:
Notch transcriptional activation inhibitor
Chemical Name:
2-[2-Methoxy-4-[(4-oxo-2-thioxo-5-thiazolidinylidene)methyl]phenoxy]-acetic acid ethyl ester
Molecular Weight:
353.41
Molecular Formula:
C15H15NO5S2
Solubility:
Soluble in DMSO (up to 45 mg/ml) or in Ethanol (up to 9 mg/ml with warming).
Physical Properties:
Yellow solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20° (des.)
Stability:
Stable for 2 years as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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