HIF

Sigaling Pathway Map

Research Area

Inhibitory Selectivity

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Notes:
2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations
S1007

Roxadustat (FG-4592)

Roxadustat (FG-4592) is an HIF α prolyl hydroxylase inhibitor in a cell-free assay, stabilizes HIF-2 and induces EPO production. Phase 3.

S1233

2-Methoxyestradiol (2-MeOE2)

2-Methoxyestradiol (2-MeOE2) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. Phase 2.

S2919

IOX2

IOX2 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.

S7309

BAY 87-2243

BAY 87-2243 is a potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor. Phase 1.

S7946

KC7F2

KC7F2 is a selective HIF-1α transcription inhibitor with IC50 of 20 μM in a cell-based assay.

S7939New

Chetomin

Chetomin is an inhibitor of HIF-1 by weaken transcription of HIF-1,disrupting the binding of HIF-1α and HIF-2α to p300 at low nanomolar concentrations.

S8171New

Daprodustat (GSK1278863)

Daprodustat (GSK1278863) is an orally administered hypoxia-inducible factor-prolyl hydroxylase (HIF-PH) inhibitor. Phase 2.

S8138New

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.

S7979New

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.

S7612

PX-478 2HCl

PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. Phase 1.

Catalog No. Information Product Use Citations Product Validations
S1007

Roxadustat (FG-4592)

Roxadustat (FG-4592) is an HIF α prolyl hydroxylase inhibitor in a cell-free assay, stabilizes HIF-2 and induces EPO production. Phase 3.

S1233

2-Methoxyestradiol (2-MeOE2)

2-Methoxyestradiol (2-MeOE2) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. Phase 2.

S2919

IOX2

IOX2 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.

S7309

BAY 87-2243

BAY 87-2243 is a potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor. Phase 1.

S7946

KC7F2

KC7F2 is a selective HIF-1α transcription inhibitor with IC50 of 20 μM in a cell-based assay.

S7939New

Chetomin

Chetomin is an inhibitor of HIF-1 by weaken transcription of HIF-1,disrupting the binding of HIF-1α and HIF-2α to p300 at low nanomolar concentrations.

S8171New

Daprodustat (GSK1278863)

Daprodustat (GSK1278863) is an orally administered hypoxia-inducible factor-prolyl hydroxylase (HIF-PH) inhibitor. Phase 2.

S8138New

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.

S7979New

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.

S7612

PX-478 2HCl

PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. Phase 1.

Tags: HIF pathway | HIF cancer | hypoxia-inducible factor cancer | HIF-1 cancer | HIF activation | HIF-1 pathway | hypoxia-inducible factor pathway | HIF-1 activation | HIF-1α pathway | HIF inhibitor review