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IMR-1

Cat. No. M8679
IMR-1 Structure
Size Price Availability Quantity
5mg USD 58  USD58 In stock
10mg USD 95  USD95 In stock
25mg USD 220  USD220 In stock
50mg USD 380  USD380 In stock
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Quality Control & Documentation
Biological Activity

IMR-1 is a first-in-class, cell-permeable inhibitor of the Notch transcription activation complex, with an IC50 of 26 μM. IMR-1 prevents Maml1 from recruiting to the Notch ternary complex (NTC) in chromatin, inhibits transcription of Notch target genes, and has antitumor activity.

Chemical Information
Molecular Weight 353.41
Formula C15H15NO5S2
CAS Number 310456-65-6
Solubility (25°C) DMSO 90 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Enjun Zhu, et al. The association between myocardial scar and the response of moderate ischemic mitral regurgitation to isolated coronary artery bypass grafting

[2] Fatma Nasser, et al. Dual targeting of Notch and Wnt/β-catenin pathways: Potential approach in triple-negative breast cancer treatment

[3] Tessa S Stewart, et al. Population risk factors for late-stage presentation of cervical cancer in sub-Saharan Africa

[4] Soo Lim, et al. Attenuation of carotid neointimal formation after direct delivery of a recombinant adenovirus expressing glucagon-like peptide-1 in diabetic rats

[5] Luisana Astudillo, et al. The Small Molecule IMR-1 Inhibits the Notch Transcriptional Activation Complex to Suppress Tumorigenesis

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Keywords: IMR-1 supplier, Notch, inhibitors, activators


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