| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
IMR-1 targets the Notch transcriptional activation complex by disrupting the recruitment of Mastermind-like 1 (Mam1) to chromatin. Unlike gamma-secretase inhibitors, which block Notch receptor cleavage, IMR-1 acts downstream by inhibiting the formation of the active transcriptional complex. This mechanism attenuates the transcription of Notch target genes.
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| ln Vitro |
In vitro, IMR-1 is a Notch inhibitor with an IC50 of 6 μmol/L. It disrupts the recruitment of Mam1 to the Notch transcriptional activation complex, thereby inhibiting Notch target gene transcription. This activity makes it a valuable tool for studying Notch signaling and its role in cancer and other diseases.
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| ln Vivo |
In basal cell xenograft models, IMR-1 (ip; 15 mg/kg; for 28 days) suppresses Notch and stimulates tumor growth [1].
In vivo, IMR-1 has been studied for its potential to inhibit Notch signaling and its effects on tumor growth. By targeting the transcriptional activation process, it offers a novel approach to inhibiting the Notch pathway. Its activity has been evaluated in various preclinical models. |
| Enzyme Assay |
In vitro assays for IMR-1 typically measure its ability to inhibit Notch target gene transcription. Cells are treated with the compound, and the expression of Notch target genes is measured using qRT-PCR or reporter gene assays. The compound's ability to disrupt Mam1 recruitment to chromatin can be assessed using chromatin immunoprecipitation (ChIP) assays.
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| Cell Assay |
Cell-based assays for IMR-1 involve treating cells with the compound and measuring its effects on Notch signaling, cell proliferation, and apoptosis. The compound's ability to inhibit Notch target gene expression and its effects on cell viability are assessed. These studies help elucidate its mechanism of action and its potential as an anticancer agent.
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| Animal Protocol |
Animal/Disease Models: Adenocarcinoma nude mouse transplanted tumor [1]
Doses: 15mg/kg Route of Administration: IP; lasted for 28 days Experimental Results: Prevented tumor formation. In vivo animal studies for IMR-1 typically involve administration to mouse models of cancer. The compound's effects on tumor growth, Notch target gene expression, and survival are assessed. These studies help evaluate its therapeutic potential and its efficacy as a Notch inhibitor. |
| ADME/Pharmacokinetics |
IMR-1 has a molecular weight of 353.41 g/mol and a molecular formula of C15H15NO5S2. It has a purity of ≥98%. For storage, the powder should be kept at -20°C for up to 3 years; in solution, it can be stored at -80°C for 2 years.
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| Toxicity/Toxicokinetics |
The toxicological profile of IMR-1 has not been extensively characterized. As a research compound, it should be handled with appropriate safety precautions. Its use is limited to research applications.
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| References | |
| Additional Infomation |
IMR-1 is a research compound with no approved human therapeutic use. It is a novel Notch inhibitor that targets the transcriptional activation process by disrupting Mam1 recruitment to chromatin. It is a valuable tool for studying Notch signaling and its role in cancer and other diseases, and it offers a new approach to inhibiting the Notch pathway.
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| Molecular Formula |
C15H15NO5S2
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|---|---|
| Molecular Weight |
353.407
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| Exact Mass |
353.039
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| CAS # |
310456-65-6
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| Related CAS # |
IMR-1A;331862-41-0
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| PubChem CID |
1246059
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.641
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| LogP |
1.38
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
23
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| Complexity |
508
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCOC(=O)COC1=C(C=C(C=C1)/C=C/2\C(=O)NC(=S)S2)OC
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| InChi Key |
QHPJWPQRZMBKTG-KPKJPENVSA-N
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| 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+
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| Chemical Name |
(E)-Ethyl 2-(2-methoxy-4-((4-oxo-2-thioxothiazolidin-5-ylidene)methyl)phenoxy)acetate
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| Synonyms |
IMR-1 IMR 1 IMR1. Inhibitor of Mastermind Recruitment-1.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~282.96 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.07 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (7.07 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.07 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8296 mL | 14.1479 mL | 28.2957 mL | |
| 5 mM | 0.5659 mL | 2.8296 mL | 5.6591 mL | |
| 10 mM | 0.2830 mL | 1.4148 mL | 2.8296 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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