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IMR-1 Notch pathway inhibitor

Catalog No.B6110
Size Price Stock Qty
5mg
$80.00
In stock
25mg
$280.00
In stock
100mg
$630.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Chemical structure

IMR-1

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Chemical Properties

Cas No. 310456-65-6 SDF Download SDF
Chemical Name (E)-ethyl 2-(2-methoxy-4-((4-oxo-2-thioxothiazolidin-5-ylidene)methyl)phenoxy)acetate
Canonical SMILES CCOC(COC1=C(OC)C=C(/C([H])=C(S2)\C(NC2=S)=O)C=C1)=O
Formula C15H15NO5S2 M.Wt 353.41
Solubility ≥35.3mg/mL in DMSO Storage Store at -20°C
Physical Appearance A solid Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

IC50: 26 μmol/L

IMR-1 is a inhibitor of Notch pathway.

Aberrant Notch activity has been reported to play a important role in the initiation and maintenance of the neoplastic phenotype and in various cancer stem cells, which alludes to its additional involvement in metastasis and resistance.

In vitro: In order to determine the effect of IMR-1 on the assembly of the Notch ternary complex (NTC) in cells, Notch-dependent cell lines OE33 and 786-0 were treated with IMR-1 or DAPT. Results showed that treatment of OE33 and 786-0 with IMR-1 could decrease the occupancy of Maml1 on the HES1 promoter but, in contrast to DAPT, IMR-1 treatment could not affect the occupancy of Notch1 on the HES1 promoter. In addition, western blot analyses indicated that IMR-1 treatment did not change the cellular levels of NICD [1].

In vivo: Animal study showed that treatment of mice with 15 mg/kg IMR-1 could readily block tumor establishment. Moreover, IMR-1 treatment at 15 mg/kg caused no observable adverse effects on the animal. In two independent PDX models, IMR-1 could significantly abrogate the tumor growth to a similar level achieved with DAPT treatment, without any significant weight loss or other visible signs of adverse effects in the treated mice [1].

Clinical trial: Up to now, IMR-1 is still in the preclinical development stage.

Reference:
[1] Astudillo L,Da Silva TG,Wang Z,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.