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NAcM-OPT

Cat. No. M20714
NAcM-OPT Structure
Size Price Availability Quantity
5mg USD 35  USD35 In stock
10mg USD 60  USD60 In stock
50mg USD 210  USD210 In stock
100mg USD 330  USD330 In stock
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Quality Control & Documentation
Biological Activity

NAcM-OPT is a specific, reversible and orally bioavailable inhibitor of cullin neddylation 1 (DCN1) that targets N-Acetyl-UBE2M (E2 conjugating enzyme, UBC12) interaction with DCN1 with IC50 of 79 nM.

Chemical Information
Molecular Weight 434.4
Formula C23H29Cl2N3O
CAS Number 2089293-61-6
Solubility (25°C) DMSO 87 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] Jared T Hammill, et al. J Med Chem. Discovery of an Orally Bioavailable Inhibitor of Defective in Cullin Neddylation 1 (DCN1)-Mediated Cullin Neddylation

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Keywords: NAcM-OPT supplier, E1/E2/E3 Enzyme, inhibitors, activators


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