Signaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S1233 2-Methoxyestradiol (2-MeOE2) <1 mg/mL 60 mg/mL <1 mg/mL
S7309 BAY 87-2243 <1 mg/mL 33 mg/mL 8 mg/mL
S7946 KC7F2 <1 mg/mL 100 mg/mL <1 mg/mL
S7958 Lificiguat(YC-1) <1 mg/mL 60 mg/mL 60 mg/mL
S8441 LW 6 <1 mg/mL 13 mg/mL 1 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
S1007 Roxadustat (FG-4592) <1 mg/mL 70 mg/mL <1 mg/mL
S2919 IOX2 <1 mg/mL 7 mg/mL <1 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
S8443 MK-8617 <1 mg/mL 20 mg/mL 1 mg/mL
S7483 DMOG 35 mg/mL 35 mg/mL 35 mg/mL

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations

2-Methoxyestradiol (2-MeOE2)

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


BAY 87-2243

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



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



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


LW 6

LW6 is a hypoxia-inducible factor 1(HIF) inhibitor which potently inhibits HIF-1α accumulation by degrading HIF-1α without affecting the HIF-1a mRNA levels during hypoxia. LW6 inhibits HIF and MDH2 expression with IC50 values of 4.4 and 6.3 μM, respectively.



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.


PX-478 2HCl

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


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.



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.


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.



FG-2216 is a potent, and orally active HIF prolyl 4-hydroxylase inhibitor with IC50 of 3.9 μM for PHD2. Phase 2.


Daprodustat (GSK1278863)

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



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.



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