| S2919 |
IOX2 |
IOX2 (JICL38) is a potent inhibitor of HIF-1α prolyl hydroxylase-2 (PHD2) with IC50 of 21 nM in a cell-free assay, >100-fold selectivity over JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH. |
Selective |
PHD2, IC50: 21 nM |
| S6490 |
Vadadustat |
Vadadustat (AKB-6548, B-506, PG-1016548) is a novel, titratable, oral HIF-PH inhibitor. |
Selective |
PH2, IC50: 0.029 μM |
| S9656 |
Enarodustat (JTZ-951) |
Enarodustat (JTZ-951) is a potent and orally active HIF prolyl hydroxylase inhibitor with IC50 of 0.22 μM for PHD2 and EC50 of 5.7 μM for EPO release from Hep3B cells. Enarodustat has the potential for the treatment of renal anemia. |
Selective |
PHD2, IC50: 0.22 μM |
| s7979 |
FG-2216 |
FG-2216 is a potent, and orally active HIF prolyl 4-hydroxylase inhibitor with IC50 of 3.9 μM for PHD2. Phase 2.
|
Selective |
PHD2, IC50: 3.9 μM |
| S8443 |
MK-8617 |
MK-8617 is an orally active pan-inhibitor of Hypoxia-inducible factor prolyl hydroxylase 1−3 (HIF PHD1−3), inhibiting PHD1, 2, 3 with IC50s of 1.0, 1.0 and 14 nM, respectively. |
Pan |
PHD2, IC50: 1 nM |
| S6684 |
IOX4 |
IOX4 is a potent and selective HIF prolyl-hydroxylase 2 (PHD2) inhibitor with IC50 of 1.6 nM. IOX4 induces HIFα in various mouse tissues and human cell lines. |
Pan |
PHD2, IC50: 1.6 nM |
| S0729 |
TP0463518 |
TP0463518 is a potent hypoxia-inducible factor prolyl hydroxylases (PHDs) inhibitor with Ki of 5.3 nM for human PHD2. TP0463518 inhibits human PHD1, human PHD3 and monkey PHD2 with IC50 of 18 nM, 63 nM and 22 nM, respectively. |
Pan |
hPHD2, Ki: 5.3 nM; monkey PHD2, IC50: 22 nM |
| S8138 |
Molidustat (BAY 85-3934) |
Molidustat (BAY 85-3934) is a potent hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor with IC50 of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD, respectively. Phase 2. |
Pan |
PHD2, IC50: 280 nM |
