An inhibitor of Maml1 recruitment to chromatin; binds to the intracellular domain of Notch (KD = 11 µM) and prevents transcription of Notch target genes by inhibiting the recruitment of Maml1 to chromatin; inhibits colony formation in Notch-dependent cell lines but not Notch-independent cell lines at 15 and 45 µM; decreases the expression of Notch target genes and reduces tumor growth in a patient-derived esophageal adenocarcinoma mouse xenograft model at 15 mg/kg

IMR-1 – 5 mg

Brand:
Cayman
CAS:
310456-65-6
Storage:
-20
UN-No:
Non-Hazardous - /

IMR-1 is an inhibitor of mastermind-like 1 (Maml1) recruitment to chromatin.{35889} It binds to the intracellular domain of Notch (KD = 11 µM) and prevents transcription of Notch target genes by inhibiting the recruitment of Maml1, but not Notch1, to chromatin. It inhibits colony formation in the Notch-dependent cell lines SUM149, SUM159, and HT-1080, but not the Notch-independent cell lines T47D, MCF-7, and H23 when used at concentrations of 15 and 45 µM. IMR-1 (15 mg/kg) decreases the expression of the Notch target genes HES1, HEYL, and NOTCH3 and reduces tumor growth in a patient-derived esophageal adenocarcinoma mouse xenograft model.  

 

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Description

An inhibitor of Maml1 recruitment to chromatin; binds to the intracellular domain of Notch (KD = 11 µM) and prevents transcription of Notch target genes by inhibiting the recruitment of Maml1 to chromatin; inhibits colony formation in Notch-dependent cell lines but not Notch-independent cell lines at 15 and 45 µM; decreases the expression of Notch target genes and reduces tumor growth in a patient-derived esophageal adenocarcinoma mouse xenograft model at 15 mg/kg

Formal name: 2-[2-methoxy-4-[(4-oxo-2-thioxo-5-thiazolidinylidene)methyl]phenoxy]-acetic acid, ethyl ester

Synonyms:  Inhibitor of Mastermind Recruitment-1

Molecular weight: 353.4

CAS: 310456-65-6

Purity: ≥95% (mixture of isomers)

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Cell Signaling|Notch Signaling||Research Area|Cancer|Transcription Factors||Research Area|Cell Biology|Cell Signaling|Notch Signaling

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