IMR-1

IMR-1 is a novel class of Notch inhibitors targeting the transcriptional activation with an IC50 of 26 μM. IMR-1 prevents the recruitment of Mastermind-like 1 (Maml1) to the Notch Ternary Complex (NTC) on chromatin, inhibits Notch target gene transcription and dramatically inhibits tumor growth.

Product information

CAS Number: 310456-65-6

Molecular Weight: 353.41

Formula: C15H15NO5S2

Chemical Name: ethyl 2-(2-methoxy-4-{[(5E)-4-oxo-2-sulfanylidene-1, 3-thiazolidin-5-ylidene]methyl}phenoxy)acetate

Smiles: COC1=CC(/C=C2/SC(=S)NC/2=O)=CC=C1OCC(=O)OCC

InChiKey: QHPJWPQRZMBKTG-KPKJPENVSA-N

InChi: 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+

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : ≥ 100 mg/mL (282.96 mM)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vivo:

IMR-1 (i.p.; 15mg/kg; for 28 days) inhibits Notch-dependent tumor growth in patient-derived xenograft models.

References:

1. Astudillo L et al. The Small Molecule IMR-1 Inhibits the Notch Transcriptional Activation Complex to Suppress Tumorigenesis. Cancer Res. 2016 Jun 15;76(12):3593-603.

Products are for research use only. Not for human use.