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C7280948

Cat. No. M3783
C7280948 Structure
Size Price Availability Quantity
5mg USD 45  USD45 In stock
10mg USD 80  USD80 In stock
50mg USD 250  USD250 In stock
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Quality Control & Documentation
Biological Activity

C7280948 is a sulfone inhibitor of PRMT1 (IC50 values 12.75 μM and 26.7 μM, respectively, methylated substrates for oligopeptides containing human histone H4 and non-histone Npl3 1-21 amino acids). PRMT inhibitors are a potential compound and interesting tool for cell biology. C7280948 is an effective tool for studying the epigenetic effects of PRMT1. PRMT1 is also involved in activation of estrogen and androgen receptors. PRMT1 is an essential component of the oncogenic transformation induced by the mixed line leukemia (MLL) complex, and thus may represent a new research direction in hormone-dependent cancers.

Chemical Information
Molecular Weight 276.35
Formula C14H16N2O2S
CAS Number 587850-67-7
Solubility (25°C) DMSO 35 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] Bissinger EM, et al. Bioorg Med Chem. Acyl derivatives of p-aminosulfonamides and dapsone as new inhibitors of the arginine methyltransferase hPRMT1.

[2] Heinke R, et al. ChemMedChem. Virtual screening and biological characterization of novel histone arginine methyltransferase PRMT1 inhibitors.

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  Catalog
Abmole Inhibitor Catalog




Keywords: C7280948 supplier, PRMTs, inhibitors, activators


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