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You are here:Home-Inhibitors & Agonists-Nuclear Receptor/Transcription Factor-HIF/HIF Prolyl-hydroxylase

Request The Product List ofHIF/HIF Prolyl-hydroxylase HIF/HIF Prolyl-hydroxylase

HIFs (Hypoxia-inducible factors) are transcription factors that respond to changes in available oxygen in the cellular environment, to be specific, to decreases in oxygen, or hypoxia. The HIF signaling cascade mediates the effects of hypoxia, the state of low oxygen concentration, on the cell. Hypoxia often keeps cells from differentiating. However, hypoxia promotes the formation of blood vessels, and is important for the formation of a vascular system in embryos, and cancer tumors. The hypoxia in wounds also promotes the migration of keratinocytes and the restoration of the epithelium. In general, HIFs are vital to development. In mammals, deletion of the HIF-1 genes results in perinatal death. HIF-1 has been shown to be vital to chondrocyte survival, allowing the cells to adapt to low-oxygen conditions within the growth plates of bones. HIF plays a central role in the regulation of human metabolism. Recently, several drugs that act as selective HIF prolyl-hydroxylase inhibitors have been developed.

Cat. No. Product Name CAS No. Information
H9569

Izilendustat hydrochloride

1303513-80-5

Izilendustat hydrochloride is a potent inhibitor of prolyl hydroxylase which can stabilize hypoxia inducible factor- 1 alpha (HIF- lα) and hypoxia inducible factor-2 (HIF-2);Izilendustat has the potential for researching diseases that relate to the body’s inmmune response like colitis and other inflammatory bowel diseases

H9568

Izilendustat

1303512-02-8

Izilendustat is a potent inhibitor of prolyl hydroxylase which can stabilize hypoxia inducible factor- 1 alpha (HIF- lα) and hypoxia inducible factor-2 (HIF-2);Izilendustat has the potential for researching diseases that relate to the body’s inmmune response like colitis and other inflammatory bowel diseases

H9522

BPC 157

137525-51-0

BPC 157 is a stable gastric pentadecapeptide and a partial sequence of the human gastric juice protein BPC;BPC 157 is an anti-ulcer peptidergic agent with no reported toxicity. BPC 157 links inflammatory bowel disease and multiple sclerosis.

H8930

Belzutifan

1672668-24-4

PT2977 (MK-6482) is an orally active and selective HIF-2α inhibitor with an IC50 of 9 nM. PT2977, as a second-generation HIF-2α inhibitor, increases potency and improves pharmacokinetic profile. PT2977 is a potential treatment for clear cell renal cell carcinoma (ccRCC).

H5818

Vadadustat

1000025-07-9

Vadadustat (PG-1016548, AKB-6548)?is a novel, potent, orally active HIF-PH inhibitor in development for the treatment of anemia in both nondialysis-dependent (NDD) and dialysis-dependent CKD; induces endogenous erythropoietin synthesis and enhances iron mobilization.

H5817

TP-0463518

1558021-37-6

TP-0463518 is a novel, highly potent HIF prolyl hydroxylase (PHD) inhibitor with IC50 of 13 nM and 18 nM for human and rat PHD2, respectively; demonstrates to promote the production of erythropoietin (EPO) following oral administration in mice and rats, shows potential for treatment of renal anemia.

H5816

THS-044

62054-67-5

THS-044 is a low micromolar HIF2α PAS-B binding compound (Kd=2 uM); modulates the affinity of the HIF2α:ARNT PAS-B heterodimer in vitro.

H5815

SYP-5

1384268-04-5

A novel potent HIF-1 inhibitor that inhibits hypoxia-induced upregulation of HIF-1, suppresses tumor cells invasion and angiogenesis; down-regulates VEGF and MMP-2, suppresses angiogenesis induced by hypoxia and VEGF in vitro; inhibits tumor cell migration and invasion by suppressing PI3K/AKT- and MAPK/ERK-dependent HIF-1 pathway.

H5814

Roxadustat

808118-40-3

Roxadustat (FG4592, FG-4592) is a potent, orally available HIF prolyl hydroxylase (HIF-PHD) with IC50 of 591.4 nM; FG-4592 stimulates erythropoiesis, regulates iron metabolism, and reduces hepcidin, demonstrates potential for treatment of anemia.

H5813

PX-478

685898-44-6

A potent, selective inhibitor of HIF-1α and HIF-1 transcription factor activity; inhibits the hypoxia-induced increase in HIF-1α protein in PC-3, MCF-7, HT-29 and Panc-1 with IC50 of 3.9, 4.0, 19.4 and 10.1 nM, respectively; suppresses HIF-1α levels in HT-29 human colon cancer xenografts and inhibits the expression of HIF-1 target genes including VEGFR and the glucose transporter-1.

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