HIF

Sigaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S1007 Roxadustat (FG-4592) <1 mg/mL 70 mg/mL <1 mg/mL
S1233 2-Methoxyestradiol (2-MeOE2) <1 mg/mL 60 mg/mL <1 mg/mL
S2919 IOX2 <1 mg/mL 7 mg/mL <1 mg/mL
S7309 BAY 87-2243 <1 mg/mL <1 mg/mL 8 mg/mL
S7946 KC7F2 <1 mg/mL 100 mg/mL <1 mg/mL
S8443 MK-8617 <1 mg/mL 20 mg/mL 1 mg/mL
S7958 Lificiguat(YC-1) <1 mg/mL 60 mg/mL 60 mg/mL
S8138 Molidustat (BAY 85-3934) <1 mg/mL 3 mg/mL <1 mg/mL
S7979 FG-2216 <1 mg/mL 56 mg/mL <1 mg/mL
S8171 Daprodustat (GSK1278863) <1 mg/mL 10 mg/mL <1 mg/mL
S7483 DMOG 35 mg/mL 35 mg/mL 35 mg/mL
S7939 Chetomin <1 mg/mL 100 mg/mL 10 mg/mL
S7612 PX-478 2HCl 78 mg/mL 78 mg/mL 78 mg/mL

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.

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.

S7958New

Lificiguat(YC-1)

YC-1 is an nitric oxide (NO)-independent activator of soluble guanylyl cyclase(sGC) and an inhibitor of Hypoxia-inducible factor-1alpha (HIF-1alpha).

S7939

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.

S7612

PX-478 2HCl

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

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.

S8443New

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.

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.

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.

S8171

Daprodustat (GSK1278863)

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

S7483

DMOG

DMOG is an antagonist of α-ketoglutarate cofactor and inhibitor for HIF prolylhydroxylase.

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.

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.

S7958New

Lificiguat(YC-1)

YC-1 is an nitric oxide (NO)-independent activator of soluble guanylyl cyclase(sGC) and an inhibitor of Hypoxia-inducible factor-1alpha (HIF-1alpha).

S7939

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.

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
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.

2015, 10.1007/s00204-015-1549-y

2015, 46:192-203

2015, 14(1):63-72

S8443New

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.

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.

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.

S8171

Daprodustat (GSK1278863)

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

S7483

DMOG

DMOG is an antagonist of α-ketoglutarate cofactor and inhibitor for HIF prolylhydroxylase.

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