IOX2 is a potent inhibitor of HIF-1α prolyl hydroxylase-2 (PHD2) with IC50 of 21 nM, >100-fold selectivity over JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH.
|Source||Sci Rep (2017). Figure 5. IOX2|
|Cell Lines||Primary articular chondrocytes|
|Incubation Time||72 hours|
|Results||We found that expression of proliferation markers, p57 and cyclin D1, were both reduced by 28%|
|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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
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PT2385 is an orally active, selective inhibitor of hypoxia inducible factor (HIF)-2alpha, with a Ki value of less than 50 nM.
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Daprodustat (GSK1278863) is a novel, orally active HIF-prolyl hydroxylase inhibitor.
BIQ (FG-2216) is an orally available and potent inhibitor of prolyl-hydroxylase (PHD) with IC50 of 3.9 uM for PDH2 enzyme.
Oltipraz is a potent Nrf2 activator and a potent inducer of Phase II detoxification enzymes, most notably glutathione-S-transferase (GST). Phase 3.
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