JNJ-42041935 (HIF-PHD Inhibitor II) is a potent (pKi = 7.3-7.9), 2-oxoglutarate competitive, reversible, and selective inhibitor of PHD enzymes.

JNJ-42041935是对PHD2181–417效果较强的抑制剂，具有7.0±0.03的pIC50值。此外，JNJ-42041935还能抑制全长PHD1、PHD2和PHD3酶，它们的pKi值分别为7.91±0.04、7.29±0.05和7.65±0.09 [1]。

JNJ-42041935被用于比较针对PHD的选择性抑制与间歇性高剂量（50 μg/kg i.p.）外源性红细胞生成素受体激动剂在大鼠炎症诱导的贫血模型中的效果。JNJ-42041935（100 μmol/kg，每天一次，连续14天）在逆转炎症诱导的贫血中表现出有效性，而红细胞生成素无效。连续5天口服JNJ-42041935（100 μmol/kg）可使网织红细胞数量增加2倍，血红蛋白增加2.3 g/dl，以及血细胞比容增加9%。在口服300 μmol/kg JNJ-42041935两小时后，相对于鼠标荧光素酶处理的对照组，腹膜区域的生物发光增加了2.2 ± 0.3倍[1]。

The potency of JNJ-42041935 for inhibition of the structurally related enzyme FIH is assessed by methods similar to those described for PHD2. In brief, activity of FIH is determined using purified glutathione transferase-tagged full-length FIH amino acids 1 to 350 and a synthetic HIF-1α peptide corresponding to residues Asp788 to Leu822. Compounds are preincubated with 17.1 nM FIH for 30 min, followed by a 10-min incubation with 1 μM [2-14C]2-oxoglutarate, in the presence of 10 μM FeNH4SO4 in reaction buffer. The selectivity of JNJ-42041935 for inhibition of a range of other targets available for testing in commercial assays is also assessed at concentrations of 1 and 10 μM[1].