- FLI-06
- Z-Ile-Leu-aldehyde
| IMR-1Notch pathway inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
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- Purity = 99.05%
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- NMR (Nuclear Magnetic Resonance)
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Chemical structure
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| 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. | ||
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.
