An inhibitor of Maml1 recruitment to chromatin
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Active Metabolite(s)
37432IMR-1A
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IMR-1

Item No. 27920

Technical Information
Formal Name
2-[2-methoxy-4-[(4-oxo-2-thioxo-5-thiazolidinylidene)methyl]phenoxy]-acetic acid, ethyl ester
CAS Number
310456-65-6
Synonyms
  • Inhibitor of Mastermind Recruitment-1
Molecular Formula
C15H15NO5S2
Formula Weight
Purity
≥95% (mixture of isomers)
Formulation
A crystalline solid
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:4): 0.20 mg/mlDMSO: 25 mg/ml
λmax
260, 287, 392 nm
SMILES
COC1=C(OCC(OCC)=O)C=CC(/C=C2C(NC(S\2)=S)=O)=C1
InChi Code
InChI=1S/C15H15NO5S2/c1-3-20-13(17)8-21-10-5-4-9(6-11(10)19-2)7-12-14(18)16-15(22)23-12/h4-7H,3,8H2,1-2H3,(H,16,18,22)/b12-7+
InChi Key
QHPJWPQRZMBKTG-KPKJPENVSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    IMR-1 is an inhibitor of mastermind-like 1 (Maml1) recruitment to chromatin.1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Astudillo, L., Da Silva, T.G., Wang, Z., et alThe small molecule IMR-1 inhibits the Notch transcriptional activation complex to suppress tumorigenesis. Cancer Res. 76(12), 3593-3603 (2016).