IMR-1

An inhibitor of Maml1 recruitment to chromatin

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5mg

￥600.00

480.00

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25mg

￥2025.00

1620.00

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100mg

￥4650.00

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货号: ajci9724
CAS: 310456-65-6
别名: [2-甲氧基-4-[(4-氧代-2-硫代-5-噻唑烷亚基)甲基]苯氧基]乙酸乙酯
分子式: C15H15NO5S2
分子量: 353.41
纯度: >98%
溶解度: ≥ 35.3mg/mL in DMSO
储存: Store at -20°C
库存: 现货

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.