Bobcat339 is a novel cytosine-based TET enzyme inhibitor with IC50s of 33 and 73 uM for TET1/2, it does not inhibit the DNA methyltransferase DNMT3a. Bobcat339 (10 μM in 1% DMSO) treated 24 hrs significantly reduces global 5hmC levels by inhibiting TET enzyme function in HT-22 cells.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
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Vitamin D2 is a selective inhibitor of mammalian DNA polymerase A (pol A) with IC50 of 123 mM.
SGI-1027 is a DNMT inhibitor with IC50 of 6, 8, 7.5 μM for DNMT1, DNMT3A, and DNMT3B
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