HIF

PHD-1-IN-1 is an orally active and potent HIF prolylhydroxylase domain-1 (PHD-1) inhibitor with an IC50 of 0.034 μM.

M1001 is a weak hypoxia-inducible factor-2α (HIF-2α) agonist. M1001 can bind to the HIF-2α PAS-B domain, with a Kd of 667 nM. M1001 can be used in chronic kidney disease research.

M1002 is a hypoxia-inducible factor-2 (HIF-2) agonist, and can enhance the expression of HIF-2 target genes. M1002 shows synergy with prolyl-hydroxylase domain (PHD) inhibitors.

(S,R,S)-AHPC-C5-COOH (VH032-C5-COOH) is a synthesized?E3 ligase ligand-linker conjugate, contains the VH032 VHL-based ligand and a linker to form PROTACs. VH-032 is a selective and potent inhibitor of VHL/HIF-1α interaction with a Kd of 185 nM, has the potential for the study of anemia and ischemic diseases.

PT2399 is a potent and selective HIF-2α antagonist, which directly binds to HIF-2α PAS B domain with an IC50 of 6 nM. PT2399 displays potent antitumor activity in vivo.

HIF1-IN-3 (compound F4) is a potent HIF1 inhibitor with an EC50 value of 0.9 μM. HIF1-IN-3 can be used for researching anticancer.

HIF-1α-IN-2 is an effective HIF-1α inhibitor with anticancer potencies (IC50s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively). HIF-1α-IN-2 suppresses HIF-1α expression by blocking transcription and protein translation.

Deferoxamine (Deferoxamine B) is an iron chelator (binding Fe(III) and many other metal cations), widely used to reduce the accumulation and deposition of iron in tissues.

HIF-2α-IN-8 is an effective orally active inhibitor of HIF2α with IC50 values of 9, 37, and 246 nM for HIF2α SPA, HIF2α iScript, and HIF2α HRE RGA respectively. It has anti-tumor activity.

HIF-2α agonist 2 (compound 10) is a HIF-2α activator with an EC50 value of 1.68 μM at a dose of 20 μM. HIF-2α agonist 2 has no cytotoxicity on 786-O-HRE-Luc cells. It can be used for oxygen metabolism research.

HIF-IN-1 (Compound 3c) is a hypoxia-inducible factor (HIF-1) inhibitor. HIF-IN-1 inhibits the aggregation of HIF-1α protein without affecting the level of HIF-1α mRNA. HIF-IN-1 has no significant cytotoxicity.

Moracin P is a 2-arylbenzofuran isolated from Mori Cortex Radicis. It exhibits strong in vitro inhibitory activity against hypoxia-inducible factor (HIF-1). Moracin P reduces the production of reactive oxygen species (ROS) induced by oxygen-glucose deprivation (OGD). Moracin P has neuroprotective and anti-inflammatory effects.

(Rac)-Arnebin 1 is the racemic form of β,β-Dimethylacrylalkannin and/or β,β-Dimethylacrylshikonin. These compounds are naphthoquinones isolated from plants in the Lithospermum genus, with β,β-Dimethylacrylshikonin exhibiting anti-tumor activity.

Steppogenin is an effective inhibitor of HIF-1α and DLL4, with IC50 values of 0.56 and 8.46 μM, respectively. Steppogenin can be used for research on angiogenesis-related diseases such as solid tumors.

BNS is a cell penetrant, potent and selective PHD2 (prolyl-hydroxylase 2) inhibitor.

HIF-1α-IN-2 drochloride is an effective HIF-1α inhibitor with anticancer potencies (IC50s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively).

PRLX-93936 didrochloride (Compound 16) is a HIF-1α inhibitor with anticancer activity.

HIF-1/2α-IN-2 is an inhibitor of HIF-1/2α.

HIF-1α-IN-4 is a HIF-1α inhibitor with an IC50 value of 24 nM (in HEK293T cell).

HIF-1α-IN-5 is a HIF-1α inhibitor with an IC50 value of 24 nM (in HEK293T cell).

VHL-IN-1 (compound 30) is a ubiquitin E3 ligase von Hippel-Lindau (VHL) inhibitor (dissociation constant Kd=37 nM) that stabilizes and induces HIF-1α transcriptional activity.

IOX5 is a selective prolyl droxylases (PHD) inhibitor.

AFP464 (didrochloride) (NSC710464 (didrochloride)) is the drochloride form of AFP464 and is a potent HIF-1α inhibitor with an IC50 value of 0.25 μM.